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    Endang diyah ikasari

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    Sel-sel yang cepat mengadakan proliferasi terdiri 5 lapisan yang berbeda, dari dalam ke

    luar:1. stratum germinativum (basal)

    2. stratum spinosum (prickle)3. stratum granulosum (granular)4. stratum lucidum (lucid)5. stratum korneum

    Selain stratum korneum, lapisan-lapisanmempunyai sel-sel yang hidup

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    Transdermal drug delivery is an approachused to deliver drugs through the skin for

    therapeutic use as an alternative to oral,intravascular, subcutaneous, andtransmucosal routes.

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    1. Local application formulations, e.g.,transdermal gels

    2. Penetration enhancers

    3. Drug carriers, e.g., liposomes and nanoparticles

    4. Transdermal patches

    5. Transdermal electrotransport

    6. Use of physical modalities to facilitatetransdermal drug transport

    7. Minimally invasive methods of transdermal drugdelivery, e.g., needle-free

    8. Injections

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    a. Transdermal delivery system (patch) is easyto use

    b. Used for lipid soluble drugs with low doseand low MW

    Kerugian :

    a. Some irritation by patch or drug

    b. Permeability of skin variable withcondition, anatomic site, age, and gender

    c. Expensive

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    Type Examples Mechanism of actionSynthetic surfactants Laureth-9 membrane interaction

    sodium lauryl sulphate extraction of membrane proteinspolysorbate 20 and 80 and lipidsPEG-8 laurate solubilization of peptidessorbitan laurateglyceryl monolauratesaponins (e.g., Quillaja saponins)

    Bile salts sodium deoxycholate denaturation of proteinssodium glycocholate decrease of mucus viscositysodium fusidate decrease of peptidase activitysodium taurodihydrofusidate solubilization of peptides

    formation of reversed micellesFatty acids and derivatives oleic acid fosfolipid acylchain disruption

    caprylic acidlauric acidPalmitoylcarnitine

    Chelators Na2EDTA Ca2complexation (influencing tight junctions)citric acidSalicylates

    Inclusion complexes cyclodextrins and derivatives increasing peptide stabilityincreasing solubilityenzyme inhibition

    Other agents Azone lipid structure disruption

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    Transdermal scopolamin (prevent travel-

    related motion sickness)

    Transdermal nitroglycerin (prophylactictreatment of angina)

    Transdermal clonidin (for hypertensi)

    Transdermal estradiol

    Transdermal testosterone

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    Drugs have been administered nasally forseveral years both for topical and systemiceffect.

    Topical administration includes agents for thetreatment of nasal congestion,rhinitis,sinusitis, and related allergic and otherchronic conditions.

    Various medications include corticosteroids,antihistaminics, anticholinergics, andvasoconstrictors.

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    1.High permeability of the nasal mucosa, compared with

    the epidermis or the gastrointestinal mucosa2. Highly vascularized subepithelial tissue

    3. Rapid absorption, usually within half an hour

    4. Avoidance of first pass effect that occurs after absorption

    of drugs from the gastrointestinal tract5. Avoidance of the effects of gastric stasis and vomiting,

    for example, in migraine patients

    6. Ease of administration by the patients, who are usually

    familiar with nasal drops and sprays7. Higher bioavailability of the drugs than in the case of

    gastrointestinal route or pulmonary route

    8. Most feasible route for the delivery of peptides

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    1. Diseases conditions of the nose may result in impaired

    absorption.

    2. Dose is limited because of relatively small area available

    for absorption.

    3. Time available for absorption is limited.

    4. Little is known of the effect of common cold on transnasal

    drug delivery, and it is likely that instilling a drug into a

    blocked nose or a nose with surplus of watery rhinorrhea

    may expel the medication from the nose.

    5. The nasal route of delivery is not applicable to all drugs.

    Polar drugs and some macromolecules are not absorbed in

    sufficient concentration because of poor membrane

    permeability, rapid clearance, and enzymatic degradation

    into the nasal cavity.

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    Factors that inf luence drug del ivery to colorectal area:

    1. The rate of absorption of drugs from the colon isinfluenced by the rate of blood flow to and from theabsorptive epithelium.

    2. Dietary components such as complex carbohydrates trap

    molecules within polysaccharide chains.3. Lipid-soluble molecules are readily absorbed by passive

    diffusion.

    4. The rate of gastric emptying and small bowel transit

    time.5. Motility patterns of the colon determine the rate of

    transit through the colon and hence the residence time ofa drug and its absorption.

    6. Drug absorption varies according to whether the drug is

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    1. A relatively large amount of the drug can be administered.

    2. Oral delivery of drugs that are destroyed by the stomach acidand/or metabolized by pancreatic enzymes.

    3. This route is safe and convenient particularly for the infants

    and the elderly.

    4. This route is useful in the treatment of emergencies such asseizures in infants when the intravenous route is not available.

    5. The rate of drug absorption from the rectum is not influenced

    by ingestion of food or rate of gastric emptying.

    6. The effect of various adjuvants is generally more effective inthe rectum than in the upper part of the gastrointestinal tract.

    7. Drugs absorbed from the lower part of the rectum bypass the

    liver.

    8. Degradation of the drugs is much less in the rectal lumen thanin the upper gastrointestinal tract.

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    1. Some hydrophilic drugs such as antibioticsand peptide drugs are not easily absorbedfrom the rectum and absorption enhancersare required.

    2. Drugs may cause rectal irritation andsometimes proctitis with ulceration andbleeding.

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    Hormon, peptida, dan protein tidak cocokuntuk pemberian obat melalui mulut, sehingga

    kebanyakan diberikan secara parenteral.

    Keunggulan formulasi peptida dan protein antaralain : Memperbaiki stabilitas secara fisika dan kimia

    Memperpanjang waktu paro Meningkatkan laju absorpsi

    Mengurangi terjadinya metabolisme

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    Gastric retensive system Colonic delivery system

    Penambahanbahan/senyawa untukmemperlama bertahan dilambung

    Sistem bioadhesive

    Sistem sediaan floating

    Polimer yang spesifik

    pada pH usus

    Transit time di usus

    diperlama

    Polimer sensitif denganbakteri pada kolon

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    Pharmacology, particularly pharmacokinetics andpharmacodynamics, have traditionally influenced drug

    delivery formulations. Some of the newer

    developments in pharmacology and therapeutics that

    influence the development of DDSs are as follows:

    1. Pharmacogenetics

    2. Pharmacogenomics

    3. Pharmacoproteomics4. Pharmacometabolomics

    5. Chronopharmacology

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    Use of recombinant DNA technology Expansion of use of protein and peptide drugs in current

    therapeutics

    Introduction of antisense, RNA interference, and gene therapy

    Advances in cell therapy: introduction of stem cells

    Miniaturization of drug delivery: microparticles andnanoparticles

    Increasing use of bioinformatics and computer drug design

    A trend toward development of target-organ-oriented dosageforms

    Increasing emphasis on controlled-release drug delivery Use of routes of administration other than injections

    Increasing alliances between pharmaceutical companies andDDS companies

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    Mencari jurnal ilmiah internasional tahunjurnal > 2009

    Diketik dengan huruf arial ukuran 12 dikertas A4

    Masing-masing kelas dijilid jadi 1 dandikumpulkan paling lambat tanggal 11Nopember 2011

    Setiap pertemuan untuk diskusi 2 atau 3

    kelompok Setiap kelas dibagi menjadi 12 kelompok

    (2 kelompok membuat dengan materi sama)

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    Oral S terdiri dari:1. Sistem floating non effervescent

    2. Sistem floating effervescent3. Sistem osmotic pump with osmogen

    4. Sistem osmotic pump

    5. Sistem matriks larut (soluble matrix)

    6. Sistem matriks tidak larut (insoluble matrix)

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    1. Oral DDS Sistem membran reservoir2. Oral DDS Sistem mucoadhesive

    3. Oral DDS Sistem enterik

    4. Nasal DDS (Gel dosage form)5. Nasal DDS (Spray dosage form)

    6. Inhalasi DDS

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    1. Transdermal DDS2. Transdermal DDS with patch

    3. Colon targetted DDS

    4. Liposom DDS

    5. Nanopartikel DDS

    6. Buccal adhesive DDS