Upload
rajesh-kumar
View
22
Download
0
Embed Size (px)
DESCRIPTION
Art
Citation preview
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
1/82
Chapter No. 1 - General Introduction
Sem. 1 Second Professional
Abdul Aleem Awan
Lecturer
Pharmacy Department
Hazara University.
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
2/82
Pharmacognosy
Pharmacognosy is a branch of pharmacy which deals with
the basic resources of medicines from nature (plant &
animal) and their uses as medicaments from ancient time
to present day.
Pharmacognosy is derived from two Greek words,
Pharmakon&Gnosis Pharmakon meansdrug.
Gnosis meansknowledge.
In brief, Pharmacognosy meansknowledge of drugs.
It is a study of drugs that originate in theplant & animal
kingdoms.
2
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
3/82
At present pharmacognosy involves not only the crude
drugs but also their natural derivatives (pure compounds
or constituents).
Digitalis leafand its isolated glycoside,digitoxin;Rauwolfia
rootand its purified alkaloid,reserpine; andthyroid gland
with its extracted hormone,thyroxine, are all part of the
subject matter of pharmacognosy.
Pharmacognosy
Pharmacognosymay be defined as an important branch
of Pharmacy which deals with the study of structural,
physical, chemical, biochemical and sensory characters ofnatural drugs of plant and animal origin. It also includes
a study of their history, distribution, cultivation,
collection, identification, preparation, evaluation,
preservation, use and commerce.
3
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
4/82
Pharmacognosy -History
The first or beginning of pre-history on use of
medicinal plants or herbs or animals, and the placewhere and how used were not well known, and those
information were unwritten for a long time. As a
result, the pre-history on herbs was almost lost.
However, some information was recorded by oral
transmission from generation to generation.
Pre-history:
History of pharmacognosy is actually the history of
medicine that is medicinal plants.
4
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
5/82
Pharmacognosy -History
The written history has originated which was based on
region, religion and culture etc.
The written history was divided into the following:
1. The western medicine
2. The Unani (Islam)
3. The Ayurveda (Indian)4. The orient
5. The Greek History
6. The African System
Written History:
5
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
6/82
Pharmacognosy -History
This is originated inMesopotamia and Egypt.Mesopotamiaisconsidered as the first origin of human civilization. The
Sumerians (peoples of ancient Mesopotamia) developed
cuneiform tablet of herbal medicines. Those tablets are
preserved in British museum.
In Egypt,information had been written on paper Papyrus
ebers(1600BC). It consisted of 800 prescriptions, mentioning
700 drugs.
The first pharmacopoeia named London Pharmacopoeia was
published in 1618 and then British Pharmacopoeia was
published in 1864.
1. The western medicine:
6
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
7/82
This herbal system was developed byArabian Muslim
Ibn Sina(980 1037 AD). He was a prince and ruler.
He was a very brilliant pharmacist and physician who
wrote a book Kitab-Al-Shifa, means Book of
Healing.
The book was written on Arabic language. This is a
great contribution of Ibn Sina towards medical and
pharmaceutical sciences.
Pharmacognosy -History
2. The Unani (Islam)
7
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
8/82
Ayurveda is the term for traditional medicine of ancient
India.
The word Ayur means Life and veda means The
study of that isStudy of Life.
The Ayurvedic writings were divided into three systems:
1) Charaka Samhita, 2) Sushruta Samhita and 3)
Astanga samhita.
The oldest writing was Charaka Samhita (six to seven
century before Christ).
The book describes uses of many metallic drugs eg.,
iron, mercury, sulphur, copper etc with herbs.
Pharmacognosy -History
3. The Ayurveda (Indian, 2500-600 BC):
8
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
9/82
This is originated from Chinese, Japanese and
Tibetiansetc. The orient herbalism was very old
(142 220 BC) and called Kampo. The writtendocuments were made by the King Shen Nung
(2700 BC) and Shang (1766 1122 BC) etc.
Shen Nunginvestigated medicinal value of severalherbs and written a book Pen T-Saoor native
herbal.
Pharmacognosy -History
4. The orient (2700 BC):
9
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
10/82
Hippocrates (Father of Medicine, 460-370 BC):
He was the first natural doctor who utilized simple remedies such as
vinegar, honey, herbs etc in healing. He is also known to have collected
and identified a number of medicinal plants.
Aristotle (384-322 BC):
He gave the philosophy of medicine. He listed more than 500 plants of
medicinal importance.
Theophrastus (371-287 BC):
gave scientific basis of use of plants as medicine.
Galen (131-200 AD):
a Greek pharmacist-physician. He developed the methods of preparing
and compounding medicines by mechanical means. He was the
originator of the formulae for a cold cream.
Pharmacognosy -History5. The Greek History:
Some of the early naturalists, scientists and physicians who contributed enormously tothe development of human knowledge about medicinal plants include following:
10
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
11/82
They keep information in their groups or tribes.
The information transmitted from one generation
to another.
These regions are richest sources of medicinal
plants and needs to explore for new drug
discovery.
Pharmacognosy -History
6. The African System (Tropical Africa, North
and South America):
11
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
12/82
Scope of Pharmacognosy
1. Primary source of medicines(from ancient time to
present day), for example hyoscine, morphine,
ergotamine, ouabain etc.
2. Providing Template/guide for the discovery of new
drugs, for example Pathidine (analgesic drug)
designed from morphine.
Pharmacognosy deals primarily with information on
thesourcesandconstituentsof natural drugs.
12
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
13/82
Terms & Phrase
used inPharmacognosy
13
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
14/82
Standard dictionaries definedrug as an original, simple
medicinal substance, organic or inorganic, used by itself
or as an ingredient in medicine.
According to WHOs definition any substance used in
a pharmaceutical product that is intended to modify or
explore physiological systems or pathological states for
the benefit of the recipient.
DrugTerminology
Pharmaceutical product/Medicine means a dosage form
(tablet/capsule/syrup/Inj - IV/IM) containing one or more
drugs along with other substances included during the
manufacturing process. 14
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
15/82
Application of Drug
Prevention of a disease :for example,vaccine.
Fight against an infection:for example,antibiotics.
Temporary blocking of a normal function:for example,
general & local anesthetics
Detoxification of the body:for example,antidotes.
Diagnostic agents:for example,radioisotopes.
Correction of dysfunction:for example,cardiotonics (eg,
digoxin)for the treatment of congestive heart failure. Correction of hyperfuntion:for example,Rauwolfia root
(eg., reserpine)for the treatment of hypertension.
15
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
16/82
Crude Drug:
The term Crude, as used in relation to natural products.
A crude drug is a natural drug of plant or animal origin
which has undergone no treatment other than collection
and drying,that is, the quality or appearance of the drug
has not been advanced in value or improved in condition
by any physical or chemical treatment.
For example:Digitalis leaf, Rauwolfia root etc.
Terminology
16
T i l
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
17/82
Indigenous vs Naturalized
Indigenous :
Plants growing in theirnative countriesare said to be indigenous to
those regions.
For example:Aconite (Aconitum napellus)in the mountainous region
of Europe. It is highly poisonous used as diuretic in Homeopathypreparation
Terminology
Naturalized:
Plants are said to be naturalized when they grow in aforeign land or
in a localityother than their native homes.
For example:Datura (Datura stramonium)which was introduced into
the USA from Europe.
17
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
18/82
Official Books
It provides guideline for the manufacturing, quality control,
packaging, storage, dose regimen, indication, contraindicationetc
of different pharmaceutical products/medicine for the treatmentof diseases.
USP United States Pharmacopoeia
BP British Pharmacopoeia
NF National Formulary BNF British National Formulary
BDNF Bangladesh National Formulary
BPC British Pharmaceutical Codex
Martin Dale Extra Pharmacopoeia
Materia Medica
Physicians Index
Goodmans & Gilmanns:The Pharmacological Basis of
Therapeutics. 18
i
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
19/82
Official vs Unofficial vs Nonofficial drug
Official drug:
Any drug (crude or prepared) which is included inpharmacopoea or in national formulary or in recognized books
is called an official drug.
For example: quinine, morphine, codeine, paracetamol are
included in BP, USP, NF and so on.
Terminology
Unofficial drug:
A drug which has been recognized earlier in the pharmacopoeia
or in national formulary or in recognized books but not found
in the current issue is designated as an unofficial drug. Those
substances were excluded from the recognized books due to
their severe toxic effects on humans. For example:Sucralfate
(hyperacidity), mercurial compounds (diuretics), benzoic acid
(preservative) etc. 19
T i l
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
20/82
Official vs Unofficial vs Nonofficial drug
Nonofficial drug
Substance that has never been appeared in either of
the official books may be called nonoffical. Suchtypes of compounds may be published in current
journals having proven clinical value, but we do not
know about their side effects.
For example - Curcumine (sinusitis), etc.
Terminology
20
T i l
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
21/82
Terminology
Extractive
Thecrude mixtures of chemical constituentsthat are removed
from plants or animals by various extraction processes are
called extractives or derivatives.
Secondary metabolites
These are substances synthesized or produced asby-products
by plants during theirmetabolic activities. Apparently they
are of no primary use to plants.
They are therefore also regarded as waste products of
metabolism, which are usually accumulated in some parts of
the plant and are physiologically active on living organisms. 21
T i l
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
22/82
Monograph
The descriptive material pertaining to any drug,
therapeutic agent included in the pharmacopoeia is
known as the monograph.
The monograph of a drug includes the following
information on the drug:
official title, synonyms, definition, description,
collection or preparation, identity tests, tests for
adulterants, method of assay, storage, uses and doses.
Terminology
22
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
23/82
Monograph of
Trigonella foenum-graecum (Family: Papilionacacae)
Common name:Fenugreek (Eng.), Methi (Bengali)
Cultivation:It is cultivated in different area of Bangladesh, India, Pakistan, MiddleEast, Africa.
Description:The Latin species namefoenum-graecummeans Greek hay, which
is a dried plant's (leaves or seeds) and has a strong hay-like scent. It has a
strong, pleasant and a peculiar odor and grows best in well-drained soils witha low rainfall into brownish- yellow rhombic shape seeds.
Parts used: Ripe, dried seeds
Chemical constituents: Seeds are rich in mucilage (maily galactomannans),
fixed oil, fatty acids and protein. They also contain alkaloids, saponine,
glycosides etc.
Uses:Seeds are diuretics, astringent. They are popularly used in the treatment
of loss of appetite, weight loss, menstrual disorder. Also used in
hypertension, diabetes, etc. It lowers TG, cholesterol, LDL.
Dose:Daily dose, 18 g. 23
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
24/82
Fenugreek (Kasuri Methi)
Fenugreek seeds Fenugreek with flowers
Dried Fenugreek Fenugreek Powder
24
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
25/82
Pharmacognosy & Modern Medicine
Simultaneous advancement in the field of
chemistry, biochemistry, biosynthesis and
pharmacologyhas developed pharmacognosy.
Various active compounds have been isolated fromplants which are used in modern medicine.
With the advancement of synthetic organic
chemistrymost of the active constituents of plantshave been synthesized.
100s of plants are used in modern medicine in
various parts of the world. 25 25
Ph & M d M di i
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
26/82
Pharmacognosy & Modern Medicine
Important active constituents of plants used in medicine
Active constituents Plants Pharmacological activity
Morphine, Codeine,
Papaverine
Papaver somniferumL. Sedative, smooth muscle
relaxant
Quinine, Quinidine Cinchona sp. Antimalarial,
antiarrthythmic
Hyoscine, Atropine Daturasp., Parasympatholytic
Digitoxin, Digoxin Digitalis lanata Cardiotonic
Reserpine, Rescinamine Rauwolfiasp. Hypotensive,
vasodialator
Vincristine, Vinblastin Catharanthus roseus Anticancer
26
Pharmacognosy & Modern Medicine
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
27/82
Pharmacognosy & Modern Medicine
Important active constituents of plants used in medicine
Active constituents Plants Pharmacological activity
Caffeine Camellia sinenssis CNS stimulant
Cocaine Erythroxylum coca Anaesthetic
Ephedrine Ephedrasp. Sympathomimetic
Pilocarpine Pilocarpus jaborandi Parasympathomimetic
ErgometrineErgotamine
Ergotoxine
Claviceps purpurea OxytocicVasoconstrictor
Vasodialator
27
Pharmacognosy & Modern Medicine
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
28/82
Pharmacognosy & Modern Medicine
Important active constituents of plants used in medicine
Active constituents Plants Pharmacological activity
Psyllium mucilage Plantago ovata Laxative
Sennosides Cassia
angustifolia
Laxative
Theophylline Caffea arabica CNS stimulant
Diuretic
Steroid hormones Solanumsp. Anti-inflammatory,
antiarthriytic
28
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
29/82
Plants always provide novel molecular structure,
which played important role for the molecular designand development of novel potent, less toxic or
nontoxic drugs e.g. natural morphine has got
analgesic & narcotic effect but meperidine a syntheticdrug originates from morphine basic skeleton is non-
narcotic.
Plant & animal products give potential biologicaleffect without any undesirable effects.
Plant & animal products can be taken with very ease.
Application of Pharmacognosy
29
Li it ti f Ph
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
30/82
Drugs obtained from natural sources have a variety of
limitations. The majors are;
A natural compound may be highly active but usually this is
associated with high toxicity problem, ex- the toxic and
therapeutic dose of digitalis are very close which create
serious problem to use this medicine by the patient alone.
Some compounds are found in nature that give beneficial
pharmacological actions but their potencies are too low to be
employed therapeutically.
The yield of active natural products may be very low andthus the production cost of those drugs will be very high
The source of a natural drug may be very limited with
respect to geography, season and climate etc.
Limitation of Pharmacognosy
30
Sources of Medicaments
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
31/82
At present the prime source of modern or allopathic
medicines issynthesisin the laboratory by organic chemist. Only a few of compounds are isolated from plants, which
cannot be replaced by synthetic method.
For example:morphineisolated fromPapaver somniferum;
vincristin & vinblastin(anticancer drug) fromVinca rosea,
the most potent anticancer drug taxol from Texus
brevifolia;
the constituents ofdigitaliscannot be properly replaced byany synthetic drug likequinidine which is used for the
treatment of arrhythmia.
Sources of Medicaments
31
Cl ifi i f D
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
32/82
In pharmacognosy, drugs may be classified according to -
1. Their morphology
2. The taxonomy of the plants and animals from
which they are obtained3. Their therapeutic/ pharmacological application
4. Their chemical constituents or active principles.
Each of these methods of classification has
advantages and disadvantages.
Classification of Drugs
32
Classification of Drugs1 M h l i l l ifi ti
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
33/82
In this system, the drugs are grouped according to the part of the
plants, such as roots, leaves, stems, barks, flowers, seeds etc.
The drugs obtained from the direct parts of the plants are called as
organized drugs. They are made up of whole plants or any parts
derived from them.
eg.,Root Rauwolfia, aconite, ginger;Bark Cinnamon, CinchonaFruit Amla, Bahera, Capsicum,Leaf Digitalis, Senna, Tulsi, coca;
Wood Sandal wood.
The drugs which are prepared from plants by some intermediate
physical process such as incision, drying or extraction with a solventare called unorganized drugs, eg., Dried juice (Aloe juice), Dried
extract (agar), Dried latex (Opium latex), Honey, Beewax etc.
Classification of Drugs1. Morphological classification
The main drawback of morphological classification is that there is no co-
relation of chemical constituents with the therapeutic actions. 33
Classification of Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
34/82
In this system crude drugs are arranged according to the
natural groups (e.g. Families) of their source.
For example: all the drugs obtained from Solanaceae are
grouped together as Solanaceous drugs.
Tropane alkaloids are the main constituents of
Solanaceous drugs.
Classification of Drugs
2. Taxonomical classification
Family Drugs
Solanaceae Solanaceous drugs.
eg. Tropane alkaloids
Umbelliferae Umbelliferous drugs. eg.,
volatile oils 34 34
Classification of Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
35/82
In pharmacological classification the drugs are grouped
according to their therapeutic use.
For examplecardiotonic drug include digitalis, purgative
drugs include castrol oil.
Classification of Drugs
3. Pharmacological classification
Pharmacological action Drugs
Anticancer VincaAnalgesic Opium, cannabis
Purgatives Senna, Aloe, Castrol oil, Plantago
husk
Cardiotonic Digitalis, strophanthus
Tranquillizer Rauwolfia root
Anti-inflammatory Tumeric, colchicum
The main drawback of this classification is that a drug can be placed in
various classes according to its therapeutic use. For example: Cinchona(quinine)can be grouped inantimalarial and antiarrhythmic catagories. 35
Classification of Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
36/82
The biological activity of a drug is due to the
presence of certain chemical constituents in the
drug.
Plants and animals synthesize chemical
compounds such as carbohydrates, protein, fat,
volatile oils, alkaloids, resin etc.
The chemical classification of drugs is dependent
upon the grouping of drugs with identical
chemical constituents.
Classification of Drugs
4. Chemical classification
36
Classification of Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
37/82
g
Chemical classification of drugsChemical constituents Drugs
1. Carbohydrates
a) Monosaccharidaseb) Disaccharide
c) Polysaccharide
Gum
Mucilages
Cellulose
- Dextrose, fructose, galactose-Sucrose, Lactose, Maltose
-Starch
- Acacia, Tragacanth
-Plantago seed
-Cotton
2. Glycosides
a) Cardiac
b) Anthraquinone
c) Saponins
d) Cyanophore
-Digitalis, strophanthus
- Aloe, Cascara, senna
- Arjuna
-Wild cherry bark
3. Tanins Amla, Bohera, Ashoka bark
4. Volatile oil Clove oil, rose oil, peppermint oil, tulsi etc
5. Lipids
a) Fixed oils & fats
b) Waxes
-Olive oil, castor oil, coconut oil etc
-Bees wax
37
Classification of Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
38/82
g
Chemical classification of drugsChemical constituents Drugs
6. Resins ginger, capsicum etc.
7. Alkaloids
a) Pyridine & piperidine
b) Tropane
c) Quinoline
d) Isoquinoline
e) Indole
f) Steroidal
g) Purine
a) Nicotiana, areca nut
b) Coca, Belladonna, Datura
c) Cinchona
d) Opium, Ipecac
e) Ergot, Nuxvomica, Rauwolfia, catharanthus, Physostigma
f) Kurchi
g) Tea, Coffee
8. Protein Gelatin, gluten etc
9. Vitamins Thiamine (B1), Riboflavin (B2), Ascorbic acid etc
10. Antibiotics Penicillin, streptomycin, tetracycline etc
11. Hormones Adrenaline, thyroxine etc
38
E l ti f D
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
39/82
A natural substance is considered as food if it fills stomach
in every day life without any harmful effect. A substance becomes a drug if it changes a pathological or
disease state of human/ animal to normal physiological
condition having no undesirable effect in specific dose.
A long-term studies (chemical, biological and physical etc)
are required to establish whether a substance will be
considered as drug or food or eliminate for consumption.
Those studies are referred to asevaluation.
Evaluation of drug means
Identification
Determination of quality
Determination of purity
Evaluation of Drugs
39
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
40/82
Cultivation
The identification can be established bycareful observational studyof the collected drug, and thencompared with authentic specimen
by the collector.
Therefore, for proper identification of a drug from plant or animal
sources, a collector must be educated about plant taxonomy and
very much experienced with his/her job.
Therefore, drugs from plants/animals are identified by
o A qualified, specialized & experienced person
o Comparison with the authentic sample specimen.
In every country, there is anational herbariumwhere most of plants
specimen are preserved. A number of specialists are working on
plant identification there.
Identification
40
Quality
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
41/82
Quality
The word quality refers tothe intrinsic value of the drug,i.e.,
the amount of medicinal principles or active constituents
present. These principles are classified as carbohydrate,alkaloid, glycoside, volatile oil, lipid, antibiotics and steroids etc.
A high grade of quality in a drug is of primary importance. An
effort should be made to obtain and maintain high quality.
To maintain high quality products one should do the following:
1. Select proper source (wild or cultivated)
2. Appropriate time of collection
3. Collection of required parts of plants (bark, leaf, stem, rhizome,
root)
4. Preparation of the collected drug by proper cleaning, drying.
5. Proper preservation to avoid contamination by microorganisms
and moisture, heat, air and light.41
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
42/82
Purity
The purity of drug can be achieved by
1. Proper identification
2. Quality assurance.
42
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
43/82
Evaluation Method
The evaluation of a drug involves a number ofmethods, which may be classified as follows:
1. Organoleptic
2. Microscopic
3. Biological
4. Chemical
5. Physical
43
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
44/82
1. Organoleptic evaluation of drug
Organoleptic evaluation means the study of a drug with
the help oforgans of sense. It includes any drugs macroscopic or external
appearance, color, odor, taste & sounds of its fracture
etc.
The macroscopic or external characteristic of a drug may
be divided into 7 headings -
1. Shape
2. Size3. Color
4. Internal color
5. Fracture
6. Odor
7. Taste 44
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
45/82
2. Microscopic evaluation of drug
Microscopic evaluation of drug can be done in the
laboratory by the use of microscopes and utilizes
variousmicroscopic characters of the drugs,
such astypes and arrangement of variouscells and
tissues.
45
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
46/82
3. Chemical evaluation of drug
Chemical evaluation of drugs involves both
qualitative and quantitative determination of their
active principles.
In this method characteristicqualitative chemical
testsare employed to identify crude drugs and their
constituents.
46
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
47/82
4. Biological evaluation of drug
The biological evaluation of crude drugs is very useful
in determining thepharmacological activityof the drug.
Sinceliving organism or their isolated living tissuesare
used, this method is also called the biological method or
bioassay.
Many drugs, particularly the antibiotics, toxins and
toxoids and also vitaminsare assayed by this method.
47
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
48/82
5. Physical evaluation of drug
The physical evaluation of crude drugs is
accomplished by the determination of variousphysical
characteristics using various physico-chemical
techniques, for example, specific gravity(of fats and
volatile oils), melting points (of alkaloids), optical
rotation(of alkaloid and volatile oils), etc.
48
Preparation of Drugs for Commercial Market
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
49/82
Following are different steps performed for preparation of
drugs for market.
Collection
Harvesting
Drying
Garbling
Packaging, storage, and preservation
Preparation of Drugs for Commercial Market
49
1 C ll ti
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
50/82
1. Collection
Collection of drugs from cultivated plants always insures a
true natural source and a reliable product. This may, or may
not, be the case when drugs are collected from wild plants.Carelessness or ignorance on the part of the collector can
result in complete or partial substitution. This is especially
true when drugs arc difficult to collect or the natural source is
scarce.
Many drugs are collected from wild plants sometimes on a
fairly extensive scale (tragacanth, senna) when collection is the
vocation of the gatherer, and sometimes on a limited scale
when collection is an avocation (podophyllum, hydrastis).
Because drugs come from all over the world, collection areasare almost universal, and collectors may vary from
uneducated natives to highly skilled botanists.
50
1 C ll ti td
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
51/82
1. Collection contd..
Time of collecting:
The proper time of collecting is particularly important
because the nature and quantity of constituents vary greatly
in some species according to the season.
The most advantageous collection time is when the part of the
plant that constitutes the drug is highest in its content of
active principles and when the material will dry to give the
maximum quality and appearance.
51
2 Har esting
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
52/82
2. Harvesting
The mode of harvesting varies with each drug produced andwith the pharmaceutical requirements of each drug. Some
drugs may be collected by hand labor; however, when the cost
of labor is an important factor, the use of mechanical devices
is often more successful in economic production of the drug.
With some drugs, where the skillful selection of plant parts is
an important factor (digitalis), mechanical devices cannot
replace hand labor.
52
3 Drying
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
53/82
3. Drying
By drying the plant material, one removes sufficient moistureto ensure good keeping qualities and to prevent molding, the
action of enzymes, the action of bacteria, and chemicals or
other possible changes.
Drying fixes the constituents, facilitates grinding and milling,
and converts the drug into a more convenient form for
commercial handling.
Proper and successful drying involves two main principles:
Control of temperatureand
Regulation of air flow.
53
3 Drying contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
54/82
3. Drying contd..
Control of the drying operation is determined by the nature of
the material to be dried and by the desired appearance of thefinished product. The plant material can be dried either by the
sun or by the use of artificial heat.
With some natural products, such as vanilla, processes of
fermentation or sweating are necessary to bring about
changes in the constituents. Such drugs require special drying
processes, usually called"curing."
54
4 Garbling
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
55/82
4. Garbling
Garbling is the final step in the preparation of a crude drug.
Garbling consists of the removal of extraneous matter, such asother parts of the plant, dirt, and added adulterants.
This step is done to some extent during collection, but should
be carried out after the drug is dried and before the drug is
baled or packaged. Although garbling may be done by
mechanical means in some cases, it is usually a semiskilled
operation.
55
5: Packaging storage and preservation
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
56/82
5: Packaging, storage, and preservation
The packaging of drugs depends on their final disposition.
In commerce, if transportation, storage, and ultimate use for
manufacturing purposes are involved, it is customary tochoose the type of packaging that provides ample protection
to the drug and gives economy of space.
Leaf and herb material is usually baled with power balers into
a solid compact mass that is then sewn into a burlap cover.
Senna leaves from India come in bales of 400 lb; stramonium
from Argentina in bales of 700 lb.
Drugs that are likely to deteriorate from absorbed moisture
(digitalis, ergot) are packed in moisture-proof cans. Gums,
resins, and extracts are shipped in barrels, boxes, or casks.
56
5: Packaging storage and preservation contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
57/82
5: Packaging, storage, and preservation contd
Proper storage and preservation are important factors in
maintaining a high degree of quality of the drug. Hard-packed
bales, barks and resinous drugs usually reabsorb little
moisture. But leaf, herb and root drugs that are not well
packed tend to absorb amounts of moisture that reach 10, 15,
or even 30% of the weight of the drug. Excessive moisturenot
onlyincreases the weight of the drug, thus reducing the %ageof active constituents, but also favors enzymatic activity and
facilitates fungal growth.
Light adversely affects drugs that are highly colored,
rendering them unattractive and possibly causing undesirablechanges in constituents.
The oxygenof the air increases oxidation of the constituents of
drugs, especially when oxidases are present. Therefore, the
warehouse should becool,dark, andwell ventilatedwith dry
air. 57
5: Packaging storage and preservation contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
58/82
5: Packaging, storage, and preservation contd
The protection of drugs againstattacks by insectsmust not be
overlooked. The insects that infest vegetable drugs belongchiefly to the ordersLepidoptera,Coleoptera,andDiptera.
For destruction of insects and prevention of their attacks, a
number of methods have been employed.
The simplest & the most efficient method is to expose the
drug to a temperature of 65C which not only prevents insect
attacks, but also many other forms of deterioration.
For the fumigation of large lots of crude drugs, such as those
stored in warehouses and manufacturing plants, the use of
methyl bromide has met with considerable success.Small lots of drugs may readily be stored in tight, light-
resistant containers e.g. tin cans, covered metal bins, or amber
glass containers.
58
5: Packaging storage and preservation contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
59/82
5: Packaging, storage, and preservation contd
Drugs should not be stored in wooden boxes or in drawers and
never in paper bags. Not only is deterioration hastened, butodors are communicated from one drug to another, attacks by
insects are facilitated, and destruction by mice and rats may
occur.
If drugs in small quantities are stored in tight containers,
insect attack can he controlled by adding to the container a
few drops of chloroform or CCl4from time to time.
In the case of digitalis and ergot, whose low moisture contentmust be maintained at all times, the insertion of a suitable
cartridge or device containing a non-liquefying, inert,
dehydrating substance may be introduced into the tight
container. 59
5: Packaging storage and preservation contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
60/82
5: Packaging, storage, and preservation contd
Because high temperatures accelerate all chemical reactions,
including those involved in deterioration, drugs must alwaysbe stored at as low temperature as possible.
The ideal temperature is just above freezing, but since this is
impractical in most cases, the warehouse or other storage
place should be as cool as possible.
Certain drugs such as the biologics, must be stored at a
temperature between 2 and8.
60
Animal Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
61/82
Animal Drugs
Animal drugs are produced from wild or domesticated
animals. Wild animals must be hunted (whale, musk deer) orfished for (cod and halibut), and thus, in a sense, their
collection parallels the collection of vegetable drugs.
Many animal drugs, however, are produced from
domesticated animals &, therefore, correspond to the
cultivated vegetable drugs. When drugs consist of insects, the
drugs are either collected from wild insects (cantharides) or
definite attempts are made to cultivate them, i.e., to furnish
the insects with food and shelter and to maintain optimumconditions for their propagation (honeybee).
61
Animal Drugs contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
62/82
Animal Drugs contd..
Drugs such as lanolin and milk products, as well as hormones,
endocrine products, and some enzymes, are obtained fromdomesticated pigs, sheep, or cattle.
The slaughterhouse is the usual source of glandular products
and enzymes, and the larger packing establishments have
departments for the recovery and refinement of these
therapeutic agents and pharmaceuticals.
Processing and purification of the animal drugs vary with the
individual drug.
62
Adulteration of Crude Drug
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
63/82
The term'adulteration'or debasement of an article covers a
number of conditions, which may be deliberate oraccidental. Usually in crude drugs, this practice includes
substitution of the original crude drugs partially or fully
with other substances which is either free from or inferior in
therapeutic and chemical properties.
1) Inferiorityis a natural substandard condition (e.g. where a
crop is taken whose natural constituent is below the
minimum standard for that particular drug) which can beavoided by more careful selection of the plant material.
Adulteration of Crude Drug
63
Adulteration of Crude Drug contd
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
64/82
2) Spoilageis a substandard condition produced by microbial
or other pest infestation, which makes a product unfit for
consumption, which can be avoided by careful attention to
the drying, and storage conditions.
3) Deteriorationis an impairment of the quality or value of an
article due to destruction or abstraction of valuable
constituents by bad treatment or aging or to the deliberate
extraction of the constituents and the sale of the residue as
the original drugs.
4) Admixtureis the addition of one article to another through
accident, ignorance or carelessness e.g. inclusion of soil on
an underground organ or the co-collection of two similar
species.
Adulteration of Crude Drug contd..
64
Adulteration of Crude Drug contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
65/82
5) Sophistication is the deliberate addition of spurious or
inferior material with intent to defraud; such materials arecarefully produced and may appear at first sight to be
genuine e.g. powder ginger may be diluted with starch with
addition of little coloring material to give the correct shade
of yellow color.
6) Substitutionis the addition of an entirely different article in
place of that which is required e.g. supply of cheap
cottonseed oil in place of olive oil.
Adulteration of Crude Drug contd..
65
Types of Adulteration Of Crude Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
66/82
Different methods used for adulteration may be grouped as follows:
1) Substitution with inferior commercial varieties.
2) Adulteration by artificially manufactured substitutes.
3) Substitution by exhausted drugs.
4) Substitution by superficially similar but cheaper natural substances.
5) Adulteration by addition of worthless heavy materials.
6) Addition of synthetic principles.
7) Usage of vegetative matter from the same plant.
Types of Adulteration Of Crude Drugs
66
Types of Adulteration Of Crude Drugs contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
67/82
1. Substitution with Inferior Commercial Varieties
Due to morphological resemblance to the authentic drugs,
different inferior commercial varieties are used as
adulterant which may or may not have any chemical or
therapeutic potential as that original natural drug e.g.
Arabian Senna (Cassia angustifolia), dog Senna (Cassia
obovata) and avaram (Cassia auriculata)have been used to
adulterate Senna (Cassia senna); Japanese ginger (Zingiber
mioga) to adulterate medicinal ginger (Zingiber officinale).
2. Adulteration by Artificially Manufactured Substitutes
To provide the general form and appearance of various
drugs, some materials are artificially manufactured and are
used as substitute of the original one, e.g. artificial invert
sugar for honey; paraffin wax after yellow coloration
substituted for bees wax. 67
Types of Adulteration Of Crude Drugs contd..
Types of Adulteration Of Crude Drugs contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
68/82
3. Substitution by Exhausted Drugs
Here the same plant material is mixed which is having no
active medicinal components as they have already been
extracted out. This practice is most common in case of
volatile oil containing materials like clove, fennel etc., where
the dried exhausted material resembles the same like
original drug (similarly with drugs likeCascara sagradaandginger). Sometimes when coloring matters have been
extracted or removed during exhaustion, the residue is re-
colored with artificial dyes as is done with saffron and red
rose petals.
68
Types of Adulteration Of Crude Drugs contd..
Types of Adulteration Of Crude Drugs contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
69/82
4. Substitution by Superficially Similar but Cheaper Natural
Substances
Usually here the adulterated product has no relation with
the genuine article, may or may not have any therapeutic
or chemical component desired, e.g. leaves of species -
Ailanthusare substituted for belladonna, senna, mint etc.;
Leaves ofPhytolaccaandScopoliafor belladona; Leaves ofXanthium for stramonium and dandelion for henbane;
Indian dill with European dill or caraway etc.
5. Adulteration by Addition of Worthless Heavy Materials
A large mass of stone mixed with Liquorice root, pieces oflimestone are found in asafoetida and lead shot has
occurred in pieces of opium etc.
69
Types of Adulteration Of Crude Drugs contd..
Types of Adulteration Of Crude Drugs contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
70/82
6. Addition of Synthetic Principles
Sometimes to fortify inferior natural products, synthetic
principles are added e.g. adding citral to oil of lemon;
benzyl benzoate to balsam of Peru etc.
7. Usage of Vegetative Matter from the Same Plant
This is done by mixing adventitious matters or naturallyoccurring with the drug in excessive amount or parts of
plant other than that which constitutes the drugs. For
example liver warts and epiphytes growing in bark portion
are mixed with Cascara or Cinchona;stems of buchu aresometimes cut into short lengths and added to the drug.
70
Types of Adulteration Of Crude Drugs contd..
Deterioration of Crude Drugs
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
71/82
Besides being adulterated by different means as discussed earlier, the
crude drugs are prone to deterioration on storage. The shelf-life of crude
drugs are influenced by many factors which include not only the quality
of storage conditions but also the stability of the secondary (2)
metabolites present therein. Several factors are to be considered for the
detrimental effects on the stored products.
Several primary environmental factors relating to storage can produce
detrimental effects on stored products e.g.
1) Light,
2) Moisture / humidity,
3) Temperature &
4) Oxygen etc.
But more deterioration usually results from a combination of these
factors, which leads to the development of living organism including
molds, mites, bacteria etc. 71
ete o at o o C ude ugs
Primary Factors for Deterioration
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
72/82
1. Light
Photo-decomposition occurs with santonin, the principal constituents of
wormseed, which on exposure to light darkens and eventually becomes
black. In general, drugs should be protected by suitable light-proof
wrapping or by the use of amber colour containers. Powdered rhubarb
stored in clear glass jars rapidly changes as the exposed surfaces
turning from yellow to more reddish colour.
For these detrimental effects, WHO has specified that medicinal plant
materials requiring protection from light should be maintained in a
light resistant container that shields the contents from the effects of
light. Alternatively, the container maybe placed inside a suitable light
resistant (opaque) covering and/or stored in a dark place.
72
Primary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
73/82
2. Moisture/Humidity
Moisture present in drugs depends largely upon the amount of moisturein the atmosphere, which is usually expressed in the terms of humidity.
When the atmosphere is completely saturated, the humidity is 100%,when half saturated it is 50% and so on. Drugs stored in non-airtightcontainers are termed air-dry and contain about 10-12% of waterdepending on the humidity of the atmosphere. This amount of water issufficient to activate the enzymes present in some dried plant materials,such as Digitalis and bring about the decomposition of the active
glycosides. Such drug should therefore be stored with a dehydratingagent or in sealed containers immediately after drying.
Squill contains a hygroscopic mucilage and the powder there from, ifexposed to the atmosphere, will pickup moisture and become a stickymass.
Therefore strict humidity control is necessary while storing; lowmoisture may be maintained, if necessary by the use of desiccant in thecontainer provided that direct contact with the product is avoided.
73
Primary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
74/82
3. Temperature
It has a marked effect which is sometime unsuspected. Many enzymatic
changes in the plant secondary metabolites proceed more rapidly at theslightly raised temperature up to about 45C. Obviously those drugs
containing volatile constituents in unprotected structures, e.g. plants
belonging to Labiatae family and the petals of rose and chamomile all
loose oil with an increase in temperature. Absorbent cotton wool
contains a small amount of fatty material which is the residualcomponent from the natural fiber. At a raised temperature these
molecules become re-oriented, spreading themselves over the surface of
the fiber to form an impervious layer. Thus cotton wool, once fully
absorbent will gradually become completely non-absorbent because of
the effect of temperature.
74
Primary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
75/82
4. Air Oxidation
Direct oxidation of the constituents of crude drug is sometime brought
about by the oxygen of the air, e.g. Linseed oil rapidly becomeresinified as like the oil of Turpentine and oil of Lemon. Usually this
conversion is applied to the essential oil with terpenoid derivatives and
we can find the resinous deposit build-up around the stoppers used in
dispensing bottle containing this oil. Beside this, the rancidification of
fixed oils e.g. cod-liver oil, which involves the formation of unstable
peroxides, is also an oxidative process. Thus, these types of materials
require storage in a well-filled, airtight container.
75
Secondary Factors for Deterioration
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
76/82
Living organisms usually develop in stored drugs where the conditions
are satisfactory for them. From a hygienic point of view, such
contaminated material should be destroyed irrespective of whether or
not the active principles of drug have been effected. The more common
of such organisms belongs to the groups of bacteria, moulds, mites,
nematodes, worms, insects etc.
1) Bacteria and Moulds
2) Mites and Nematode Worms
3) Insects/Moths
4) Coleoptera or Beetles
76
Secondary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
77/82
1. Bacteria and Moulds
Dried herbs are particularly liable to be contaminated with the spores
of the bacteria and moulds, which are always present in the air. Under
satisfactory storage conditions their presence causes no problem, but it
is generally accepted thatthe viable count permissible for crude drugs
should be the same as that for the food stuff. The effect produced by
bacteria are not always very visible with the exception of some
chromogenic species of bacteria, e.g. Bacillus prodigious, which
produces red patches in starchy materials. However, bacterial growthis usually accompanied by the crude drug by growth of moulds whose
presence is quickly evident by the characteristic smell and by the mass
of clinging particles entrapped in the mycelial hyphae.
77
Secondary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
78/82
Dusty cotton wool, which is formed by bacterial attack causing the
trichomes to break into short length, rendered it to be very brittle. In
order to identify a particular mould or bacteria, which is proliferating
in a stored product, it is necessary to culture it on a suitable mediumwith a view to obtain fruiting bodies for examination. However, if the
drug to be examined is infested rapidly, then it may be possible to make
microscopic preparation directly from the sample. Usually the moulds
encountered with poorly stored drugs include the genera Mucor(e.g.
grey mould, M. mused), Rhizopus (e.g. black mould, R. nigricans),Penicillium(e.g. blue mould,P. glaucum),Aspergillus(e.g. green mould,
A. repens)andSaccharomyces.
78
Secondary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
79/82
2. Mites and Nematode Worms
If found in stored drugs, mites are usually present in countless numbers
upto 1.0 mm in length. Different mites found usually include
Tyroglyphces siro (Cheese mite); Aleurobius farinae (Flour mite) and
Glycyphagus spinipes (Cantharides mite). All these mites can be
examined microscopically by clearing the sample of powder containing
them with chloral hydrate reagent. The best known examples of
nematode worms are "Vinegar eel" Turbatrix aceti, Anguillula aceti,
Anguina tritici which are found in wheat flour or in the crude drugcontaining starchy materials. These worms are visible to the unaided
eye as minute threads continually curling and twisting in the medium
they inhabit.
79
3 Insects/Moths
Secondary Factors for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
80/82
3. Insects/Moths
A few species of the Lepidiptera attack the stored crude drugs and
cause damage at the larval stage, where the infestation can spread
rapidly due to the mobility of the adults. The moths involved are
unspectacular in appearance, 22-30 mm in length with off-white wings
e.g. Ephestia kuehniella (Flour moth); E. ellutella (Cocoa moth).
Besides this some other insects, cockroaches, ants and others are
sometimes found to cause deterioration to the stored products.4. Coleoptera or Beetles
These are the insects that constitute the largest order of the animal
kingdom comprising about 2,50,000, species of which about 600 have
been found to be associated with stored food product or drugs.Stegobium paniceum is one beetle, which is found in many drugs
including gentian, liquorice and rhubarb as well as leafy drugs and
seeds. Belonging to the same family isLasioderma serricorne(tobacco
or cigar beetle) which is reddish brown in colour, 2 to 2.5 mm in length
and found in many stored crude drugs including ginger and liquorice. 80
Control Measures for Deterioration
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
81/82
The container used for storage and its closure must not interact
physically or chemically with the material within in any way which
would alter its composition. A well closed container must protect the
contents from extraneous matter or from loss of the material while
handling and a tightly closed container must protect the material from
efflorescence, deliquescence or evaporation under normal condition of
handling or storage. Storage area should be kept clean and spillages not
allowed to enter cracks or in accessible crevices. Periodic spraying of thepremises with insecticides will help to prevent the spread of infestation.
The principles, which apply to the control of infestation in warehouses,
are equally applicable to small-scale storage. Good house keeping is
utmost essential. Each stock should be inspected regularly and thematerial found to be contaminated is best to be destroyed by burning. In
this respect a quick turn over to eliminate the effects of deterioration due
to both the primary and secondary factors as mentioned above are
desirable.
81
Control Measures for Deterioration contd..
5/21/2018 54928844 Ch 1 Pharma Cog Nosy Intro
82/82
Cool, dry condition is the most suitable for the retardation of living
organisms. As all leaves organisms require water for the development,
perfectly dry drugs should be immune from secondary deterioration.Sometimes the crude drugs purchased by the herbalist may already have
been sterilized, which is most commonly achieved by treatment of the
bulk consignment with ethylene oxide or methyl bromide under
controlled conditions.
Drugs so treated, should comply with an acceptable limit for toxic
residues e.g. for Senna pods 50 ppm of ethylene oxide is the limit.