Topical Dermatologic Products 18 สค 2015

7/25/2019 Topical Dermatologic Products 18 2015

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(Semisolid dosage forms for skin) 1

(Semisolid dosage forms for skin)

..

0702 362 21 2557

1.

2.

3.

4.

5.

6.

1.

2.

3.

4.

1.


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2. (Multiple choice)

1.

2.

Microsoft PowerPoint

1.

2. (Creams)

(emulsifying agents)

w/o creams

o/w creams

o/w w/o creams

1

1 o/w w/o creams

o/w creams w/o creams

oleaginous


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ointment

(

)

o/w creams

oleaginous

ointment

oleaginous ointment

(occlusive effect)

occlusive effect o/w

creams oleaginous

ointment

-

2.1

2.1.1

2.1.2

petrolatum lanolin occlusive effect fatty alcohols

esters 2

2 ( Khar et al., 2013)

Hydrocarbons

Mineral oil (liquid

paraffin)

5-10

Petrolatum

1-2

Polyethylene waxes -


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Microcrystalline

waxes

-

Esters

Vegetable oil

-

Animal fats -

Lanolin -

Isopropyl myristate

Fatty alcohols

Cetyl alcohol 45-52oC

Stearyl alcohol 59-

60oC

hydrocarbons auxiliary

emulsifying agents 10-20 cetyl

alcohol stearyl alcohol cetostearyl alcohol

Fatty acids Stearic acid

69-70oC

1-2

Triethanolamine

Ethers Polyoxypropylene

Mixed Plant waxes


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Animal waxes e.g.

Beeswax

w/o creams

petrolatum lanolin

fatty alcohols esters

fatty alcohols

2.1.3

2 1) Primary emulsifying agents true emulsifying agents

triethanolamine stearate, polysorbate sorbitan

esters

2) Auxilliary emulsifying agents emulsion stabilizers Primary

emulsifying agents auxiliary emulsifying agents

alkyl sulfonate, cetomacrogol polyethylene glycol stearate

1)

(1) (anionic surfactants)

. (Soap) lauric

acid, myristic acid palmitic acid

+1 o/w

creams +1

w/o creams

2


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) Alkaline soap

alkaline soap sodium oleate, potassium laurate sodium stearate

(pH )

(incompatibility)

sodium stearate

oleic acid

) Amine soap

(triethanolamine) stearic acid oleic acid 1:5 triethanolamine vegetable oil triethanolamine 2-4

triethanolamine triethanolamine

triethanolamine

triethanolamine in situsoap

(pH 7.5-8.0)

alkaline soap

in

situsoap

70oC isopropanalamine triethanolamine

triethanolamine stearate o/w creams

Rx Barrier creamsHard paraffin 25 g

Soft paraffin 12 g

Liquid paraffin 3 g

Stearic acid 1.8 g

Triethanolamine 0.7 g

Cetostearyl alcohol 5 g

Chlorocresol 0.2 g


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Purified water qs to 100 g

. Alkyl sulfate

(H2SO4) alkyl sulfate sodium lauryl sulfate, sodium dodecyl benzene sulfate

sodium cetostearyl sulfate o/w creams (pH 7)

pH crystal violet, antazoline hydrochloride

salicylic acid hydrolysis

Sodium lauryl sulfate 0.1-0.5

Alkyl sulfate Rx Emulsifying wax, BP

Sodium lauryl sulfate 10 g


Purified water 4 mL

. Akyl sulfonate dioctyl sodium sulfosuccinate

o/w wetting agents auxiliary emulsifying agents primary emulsifying agents

(2) (cationic surfactants)

o/w creams

(antiseptic creams)

pH 3-5 carboxymethylcellulose tragacanth

cetrimide, distearyl dimethyl ammonium chloride, cetyl pyrinium chloride,

benzalkonium chloride cetyl trimethyl ammonium chloride

Rx Cetrimide cream, BP

Cetrimide 5 g


Liquid paraffin 500 g


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(3) (Amphoteric surfactants)

pH pH

pH

betaines, sulfobetaines, 1,2-

diacyl-L-phosphotidylcholine (lecithin) lauryl sulfobetaine (lauryl sultaine)

(4) (nonionic surfactants)

hydrophilic part alcohol (-OH) ethylene oxide (-OCH2CH2-) lipophilicpart fatty acid, fatty alcohol hydrocarbon HLB

(hydrophilic-lipophilic balance) HLB

o/w creams HLB w/o creams

pH

. Polyalkoxyethers (Polyoxyethylene glycol ethers) Polyoxyethylene

glycol fatty alcohol cetyl alcohol cetostearyl alcohol

parabens

cetomacrogol (Polyoxyethylene glycol monocetyl ether 1000)

fatty alcohol

Rx Cetomacrogol emulsifying wax, BP

Cetomacrogol 1000 200 g


Polyoxyethylene lauryl ether Brij

. Polyalkoxyesters (Polyoxyethylene glycol esters) polyoxyethylene

glycol o/w creams fatty alcohol


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polyoxyl 40 stearate 40 oxyethylene,

Macrogol stearate 2000 Myrj

. Polysorbate sorbitol ethylene oxide

Polysorbate Tween oxyethylene Polysorbate 20, 40 60 o/w creams

pH

parabens polysorbate paraben paraben

benzyl alcohol ( 2

) brobopol ( 0.2-0.4 ) sorbic acid ( 0.2 ) chlorocresol

( 0.1 ) polysorbate sorbitan ester HLB

. Polalkoxyamide fatty amides ethylene oxide

PEG-8 tallow amide Ethmoid

. Fatty acid ester of polyhydric alcohol polyols

o/w

creams hydrolysis

) Glycerol Glycol esters polyethylene glycol stearate

(stiffening agents) glyceryl monostearate auxiliary

emulsifying agents glyceryl monooleate, diethylene

glycol,monostearate propylene glycol monooleate primary emulsifying

agents ) Sorbitan esters sorbitol sorbitan

esters Span lauric acid, oleic acid, palmitic acid

stearic acid Span w/o creams

pH

Polysorbate Tween o/w w/o creams HLB

. Fatty alcohols auxiliary emulsifying agents

(emollients) w/o creams


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cetyl alcohol, stearyl alcohol, Cremophor A6 Cremophor A25

Cremophor ethoxylated saturated fatty alcohol HLB 15-17

2)

- beeswax w/o creams white wax

beeswax auxiliary emulsifying agents

- wool fat anhydrous lanolin

w/o creams (emollient) auxiliary emulsifying agents

primary emulsifying agents

wool fat

ethylene oxide

polyoxyethylene lanolin derivatives

(emollients) o/w creams- wool alcohol

w/o creams wool fat (hydrous ointment)

wool fat

2.1.4

1) (humectants) (moisturizers)

5

- glycerin 10


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- propylene glycol

- polyethylene glycol 200-600 (PEG)

glycerin glycerin

- sorbitol glycerin 3

2) (thickening agents)

o/w creams o/w creams

colloidal suspension

methylcellulose, carboxy methylcellulose, hydroxyethylcellulose, sodium carboxy methylcellulose carbopol carbopol

0.1-0.3

3) (antioxidants)

- Tocopherol acetate vitamin E

- Butylated hydroxytoluene (BHT) 10 ppm

- Butylated hydroxyanisole (BHA) 0.02

fixed oils 0.1 essential

oils

- Ascorbic acid, isoascorbic acid, ascorbylpalmitate


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- Propyl, octyl, dodecyl esters of gallic acid 0.001

fixed oils 0.1

essential oils

- Sodium metabisulfite, sodium sulfite, sodium bisulfite, sodium thiosulfate- Chelating agents EDTA

- Thioglycerol

- Cystein hydrochloride

4) (preservatives) pH

log P log P

-p-Hydroxy benzoates (parabens)

pH

propylene glycol Polysorbate methyl paraben, propyl paraben butyl paraben

0.01-0.50 methyl paraben propyl paraben

methyl paraben 0.18 propyl paraben 0.02

- Alcohols ethanol 70 , isopropyl alcohol,

chlorobutanol, p-chlorophenyl propanediol (bronopol) 0.01-0.20

benzyl alcohol 2-3 ethanol isopropyl alcohol

- Acids benzoic acid, sorbic acid propionic acid

0.1-0.2

- Mercurials phenyl mercuric acetate

borate

thimerosol 0.1-0.2


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3 HLB (: Ansels Pharmaceutical dosage

forms and drug delivery systems, 2011)

HLB 1-3

3-6 w/o

7-9 (wetting agents)

8-16 o/w

13-15 (detergents)

15-18 (solubilizing agents)

4 HLB (: The HLB system

a time-saving guide to emulsifier selection, 1984)

HLB

1-4

3-6

6-8

8-10

10-13

>13


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5 HLB (: Ansels Pharmaceutical dosage forms and

drug delivery systems, 2011)

HLB HLBEthylene glycol distearate 1.5 Triton X-45 10.4

Sorbitan tristearate (Span65) 2.1 Methylcellulose 10.5

Propylene glycol monostearate 3.4 Polyoxyethylene monostearate (Myrj

45)

11.1

Triton X-15 3.6 Triethanolamine oleate 12.0

Sorbitan monooleate (Span80) 4.3 Tragacanth 13.2

Sorbitan monostearate (Span60) 4.7 Triton X-100 13.5

Diethylene glycol monolaurate 6.1 Polysorbate 60 (Tween60) 14.9

Sorbitan monopalmitate (Span40) 6.7 Polysorbate 80 (Tween80) 15.0

Sucrose dioleate 7.1 Polysorbate 20 (Tween20) 16.7

Acacia 8.0 Plurinic F 68 17.0

Amercol L-101 8.0 Sodium oleate 18.0

Polyoxyethylene lauryl ether (Brij

30)

9.7 Potassium oleate 20.0

Gelatin 9.8 Sodium lauryl sulfate 40.0

2.2.1 HLB

1 HLB (required HLB)

HLB 62

3 HLB


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6 HLB (required HLB of oil phase) (: The HLB

system a time-saving guide to emulsifier selection, 1984 Aultons pharmaceutics the

design and manufacture of medicines, 2007)

HLB

w/o o/w

Stearic acid - 17

Cetyl alcohol - 15

Stearyl alcohol - 14

Lanolin, anhydrous 8 10

Cotton seed oil - 7.5

Mineral oil, light (liquid paraffin) 4 10-12

Castor oil - 14

Hard paraffin 4 10

Beeswax 5 9.5

Petrolatum 5 12

1

Rx Liquid paraffin 35%

Lanolin, anhydrous 1%

Stearyl alcohol 1 %

Cetyl alcohol 1%

Glycerin 5%

Emulsifying agents 7%Purified water qs to 100%

1) HLB

liquid paraffin, lanolin, stearyl alcohol

cetyl alcohol

1.1 = 35+1+1+1 = 38%


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Liquid paraffin (35x100)/38 = 92.11 %

Lanolin, anhydrous (1x100)/38 = 2.63%

Stearyl alcohol (1x100)/38 = 2.63%

Cetyl alcohol (1x100)/38 = 2.63%1.2 HLB HLB

6

Liquid paraffin (92.11/100) x 12 = 11.05

Lanolin, anhydrous (2.63/100) x 10 = 0.263

Stearyl alcohol (2.63/100) x 14 = 0.37

Cetyl alcohol (2.63/100) x 15 = 0.39Total = 12.073

HLB = 12.073

2)

2 HLB Span60 (HLB = 4.7) Tween40 (HLB = 15.6)

HLB = 12.073 a Span60

1-a Tween40

12.073 = (a x 4.7) + (1-a)(15.6)

12.073 = 4.7a + 15.6 15.6a

10.9a = 3.527

a = 0.324 Span60 0.324 32.4% Tween40 0.676 (1-0.324) 67.6%

HLB = 12.073

3)

7%

Span60 = (32.4/100) x 7 = 2.268 g

Tween40 = (67.6/100) x 7 = 4.732 g


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Rx Liquid paraffin 35%

Lanolin, anhydrous 1%

Stearyl alcohol 1%

Cetyl alcohol 1%Span 60 2.268%

Tween 60 4.732%

Purified water qs to 100%

2.2.2 2

1) Beaker method (conventional hot method)

(1)

(2) water bath (1)

72-75oC

75-78oC


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1beaker method

(3)

(Phase inversion) o/w creams

w/o

cream o/w

creams

(4) 40-45oC

wool fat, wool alcohol cholesterol

beaker method

water bath hot plate homogenizer

( 2)


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Toothed colloid mill (3)

jacketed (4)

2 (:http://www.alibaba.com/product-detail/Laboratory-

Homogenizer_500027937.html)

3Toothed colloid mill (: http://www.frymakoruma-us.com/products/detail/toothed-colloid-mill-type-mz)


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4 (: http://www.fong-hwang.com/category/emulsifier-homogenizer-machine.htm)

2) Incorporationmethod (non-thermal method)

slab spatula

(levigate) geometric dilution

(levigating agents) glycerin mineral

oil

(emollient)

(stiffening agents)

Beaker method


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2.3 5

2.3.1 Creaming

2.3.2 Flocculation

creaming creaming flocculation

coalescence

creaming flocculation

flocculation

2.3.3 Coalescence

auxiliary emulsifying agents

2.3.4 Sedimentation

2.3.5 Phase inversion o/w w/o w/o

o/w 2.3.6 Oswald ripening


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5 (: http://imgarcade.com/1/types-of-emulsion/)

2.4

Rx Vanishing cream

Stearic acid 15 g Stiffening agent,emulsifying agent

White wax 2 g EmollientWhite petrolatum 8 g Emollient

Triethanolamine 1.5 g Emulsifying agent

Propylene glycol 5 g Humectant

Purified water qs to 100 g Water phase

Rx Salicylic acid and sulfur cream, BP

Salicylic acid 20 g Active ingredient

Precipitated sulfur 20 g Active ingredient

Aqueous cream qs to 1000 g Base

Rx Aqueous creams, BP

Emulsifying ointment 300 g Base

Chlorocresol 1 g Active ingredient

Purified water 699 g Water phase


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Rx Mineral oil base cream

Cetyl alcohol 20 g Stiffening agent

Mineral oil 20 g Emollient

Tween 80 4.5 g Emulsifying agent, water phaseSpan 80 0.5 g Emulsifying agent, oil phase

Propyl paraben 0.08 g Preservative

Methyl paraben 0.4 g Preservative


Rx Nonionic cream base

Cetyl alcohol 5 g Stiffening agentStearyl alcohol 5 g Stiffening agent

Glyceryl monostearate 2 g Auxilliary emulsifying agent

Petrolatum 2 g Emollient

Liquid paraffin 5 g Emollient

Cetomacrogol 1000 3 g Emulsifying agent

Glycerin 5 g HumectantPurified water qs to 100 g Water phase

Rx Zinc cream, BP

Zinc oxide 320 g Active ingredient

Calcium hydroxide 0.45 g Emulsifying agent

Oleic acid 5 mL Emulsifying agent

Arachis oil 320 g emollientWool fat 80 g Auxilliary emulsifying agent


Rx Cold cream, USP

Spermaceti 12.8 g Stiffening agent

White wax 12 g Emollient, Emulsifying agent

Liquid paraffin, light 56 g Emollient

Sodium borate 0.5 g Emulsifying agent


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cerotic acid white wax sodium

borate in situsoap

Rx Anionic cream baseStearyl alcohol 5 g Stiffening agent

Cetyl alcohol 5 g Stiffening agent

Sodium lauryl sulfate 1 g Emulsifying agent

Liquid paraffin 5 g Emollient

Glycerin 5 g Humectant

Paraben concentrate 5 g PreservativeGlyceryl monostearate 2 g Auxilliary emulsifying agent

Petrolatum 2 g Emollient



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3. (Lotions)

(Newtonian)

Non-newtonian

3

3.1

glycerin

propylene glycol Salicylic acid lotion,

betamethasone valerate lotion, Whitfields lotion Minoxidil solution

Saicylic acid lotion keratolytic agent

Rx Salicylic acid 3 g

95% ethanol 25 mL

Purified water 25 mL

Propylene glycol qs to 100 mL

Whitfields lotion Rx Benzoic acid 5 g

Salicylic acid 3 g

95% ethanol qs to 100 mL

Minoxidil solution

Rx Minoxidil 5 g

95% ethanol 30 mL


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Propylene glycol 50 mL

Isopropyl myristate 1 mL

Purified water qs to 100 mL

3.2

(suspending agents)

1)

carbomer, carboxy methylcellulose (CMC), bentonite methylcellulose

acacia tragacanth

2) (humectants)

propylene glycol, glycerin

polyethylene glycol 400

(homogenizer)

(caking)

Calamine lotion USP

Benzoyl peroxide lotion

3.3

o/w w/o emulsion Beaker method

70-73oC 73-75oC

(phase inversion)

40-45oC


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Benzoyl benzoate lot ion, USP,

Clotrimazole lotion Basic lotion

Benzoyl benzoate lotion, USP

Rx Benzyl benzoate 250 g Active ingredient ()Triethanolamine 5 g emulsifying agent

Oleaic acid 20 g emulsifying agent

Purified water qs to 1000 g water phase

oleaic acid tr iethanolamine

triethanolamineoleate o/w oleaic acid triethanolamine

benzyl benzoate 250 mL

Basic lotion (o/w lotion)

Rx Mineral oil 10 mL emollient, oil phase

Stearic acid 3 g emulsifying agent

Triethanolamine 1 mL emulsifying agent

Lanolin 1 g emollient, oil phaseColor qs color

Purified water 75 mL water phase

stearic acid triethanolamine

triethanolaminestearate o/w

Clotrimazole lotion

Rx Clotrimazole 40 g antifungalWhite petrolatum 50 g emollient, oil phase

Mineral oil 60 g emollient, oil phase

Cetyl alcohol 72 g emollient, oil phase

Cetheth-20 22.5 g emulsifying agent, oil phase

Benzyl alcohol 10 g preservative, water phase

Propylene glycol 100 g humectant, water phase

Na2HPO4 0.35 g buffer, water phase


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NaH2PO4 5 g buffer, water phase


Cetheth-20 HLB 15.7

o/w lotion Cetheth-20 (1.1 g) (160g) clotrimazole ( Cetheth-

20 clotrimazole)

25-30oC


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4. (Ointments)

(mucous membrane)

(single-phase) (base)

4.1

2

1) (Medicated ointments)

2)

(Unmedicated ointments)

4

1) (Oleaginous/hydrocarbon bases)

(vegetable oils) (silicones)

(synthetic esters) (occlusive effect)

petrolatum, white petrolatum, white ointment,

yellow ointment, beeswax, spermaceti, mineral oil, paraffin silicones -

Petrolatum, USP yellow petrolatum soft paraffin petrolatum jelly

Vaseline

petrolatum

(white petrolatum)

petrolatum

pH


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38-60oC petrolatum

6

6 petrolatum

- Yellow ointment, USP

Yellow wax 50 gPetrolatum 950 g

Yellow wax Apis mellifera petrolatum

yellow wax casserole water bath petrolatum

(congeal)

- White ointment, USP

White wax 50 gWhite petrolatum 950 g

To make 1000 g

White wax yellow wax

petrolatum

white wax petrolatum casserole water bath

-

Mineral oil liquid paraffin liquid petrolatum paraffin oil

heavy mineral oil, USP

0.848-0.905 light mineral oil, NF 0.818-0.880

light mineral oil


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mineral oil

- Soft petrolatum

White petrolatum 90%Mineral oil, NF 10%

mineral oil

- Gelled petrolatum

White petrolatum 75%

Mineral oil, NF 25% mineral oil

- Paraffin hard paraffin paraffin wax

47-65oC

(stiffening agents) paraffin 7

7 paraffin

- Silicones dimethicone, methylphenylpolysiloxane cyclomethicone

mineral oil

(water repellant properties)

- mono- di- tri-glyceride

(peanut oil) (almond oil) (sesame oil)

(olive oil)


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(antioxidants) (chelating agent)

(fatty alcohol) - Beeswax Apis mellifera

white wax 62-65oC (thickening

agent) white wax 8

8 white wax

- Spermaceti 44-52oC

spermaceti 9

9 spermaceti

2) (Absorption bases)

(w/o emulsifiers) wool fat, wool alcohol, cholesterol, sorbitan ester

2


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(1) (anhydrous forms)

(w/o)

hydrophilic petrolatum, lanolin (anhydrous), simple ointment, aquabase ointment wool alcohol ointment

- Hydrophilic petrolatum, USP

Cholesterol 30 g

Stearyl alcohol 30 g

White wax 80 g

White petrolatum 860 g- Lanolin, USP (anhydrous)

wool fat

( 0.25)

30-50 36-42oC Modified lanolin, USP

lanolin (anhydrous) lanolin alcohol

lanolin 10 lanolin

10 lanolin

- Simple ointment, BP

Wool fat 50 g

Paraffin 50 g


Petrolatum 850 g


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- Aquabase ointment

Cholesterol 30 g

Cotton seed oil 30 g

White petrolatum 940 g- Wool alcohol ointment, BP

Wool alcohol 6 g

Paraffin 17 g

White petrolatum 17 g


(2) (hydrous forms) (w/o) lanolin (hydrous)

cold cream base

- Lanolin (hydrous) lanolin absorption base

Lanolin alcohol 10%

Lanolin 25%

Mineral oil, light 30%Purified water 35%

Mineral oil

(w/o) glyceryl monosterate, cholesterol, cetyl

alcohol sorbitan fatty acid

- Cold cream base

Borax 1.00%Mineral oil, light 50.00%

Synthetic beeswax flakes 13.00%

Glyceryl monostearate, pure 1.00%

Methyl paraben 0.25%

Propyl paraben 0.15%

Purified water 34.60%


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Cold cream base

3)

(Water-removable bases) (o/w) water-washable base

vanishing cream hydrophilic ointment, USP

- Vanishing cream

Stearic acid 13%

Stearyl alcohol 1%

Cetyl alcohol 1%

Glycerin 10%

Potassium hydroxide 0.9%

Methyl paraben 0.1%

Propyl paraben 0.05%

Purified water qs to 100%

- Hydrophilic ointment, USP

Sodium lauryl sulfate 10 g

Propylene glycol 120 g

Stearyl alcohol 250 g

White petrolatum 250 g

Methyl paraben 0.25 g

Propyl paraben 0.15 gPurified water 370 g

beaker method propylene glycol,

purified water, methyl paraben propyl paraben 78oC

sodium lauryl sulfate, white petrolatum stearyl alcohol

75oC


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4) (Water-soluble bases)

polyethylene glycol (PEG)

ointment, bentonite, gelatin, veegum - PEG ointment, NF

PEG 3350 400 g

PEG 400 600 g

PEG ethylene oxide

PEG 600 PEG

600-1000 PEG 1000 (wax) PEG

(w/o) paraben, phenol

polythene bake lite

PEG fatty

alcohol stearyl alcohol 5 20- bentonite, gelatin, veegum

- Universal ointment base

Veegum 10 gSodium lauryl sulfate 0.1 g

Methyl paraben 0.1 g

Glycerin 10 g

Tween 80 1 g

Purified water 78.8 g

- Bentonite ointment base

Bentonite 20 g


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Sodium lauryl sulfate 0.5 g

Glycerin 10 g

Purified water 69.5 g

4 7

7 ( Premjeet et al., 2012)

/

1. ,

PEG ointment

2.

3.

4.

5.

-

6.

7.

8.

9.

10.

White ointment,

white petrolatum

Aquabase, Polysorb,

Eucerin (aquaphor)

Unibase,

Velvachol,

Dermabase

Polybase


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4.2

1)

2)

3)

4)

5)

6)

4.3

1)

2)

3)

4)

5)

6)

7)

4.4

4.4.1 (active ingredients)

4.4.2 (ointment bases)

4.4.3

(additives) 1)

Fatty acids fatty alcohol stearic acid, stearyl alcohol, cetyl alcohol

cetostearyl alcohol soft

paraffin PEG

2) (Synthesis ester of fatty acid) isopropyl

myristate (IPM), isopropyl stearate isopropyl palmitate

IPM


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isopropyl stearate IPM isopropyl palmitate

IPM

4.4.4

(antioxidants) sodium sulfate, sodium metabisulfite ascorbic acid

4.4.5 (rancids)

butylate hydroxytoluene (BHT), beta hydroxy acid (BHA), tocopherol

propylgallate

4.4.6 (chelating agents)

citric acid, maleic acid, tartaric acid disodium EDTA

4.4.7 (thickening agents)

bentonite, sodium alginate, methylcellulose,

sodium carboxymethylcellulose carbomer

4.4.8 (preservatives)

methyl paraben, propyl paraben, butyl paraben, sorbicacid, benzyl alcohol benzoic acid

4.4.9 (humectants)

2-10

glycerin,propylene glycol, sorbitol PEG

4.4.10 (buffers) -

citric acid, phosphoric acid sodium

phosphate

4.4.11 (coloring agents odoring agents)


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4.5 2

4.5.1 (Incorporation)

/

slab (11) spatula spatula

spatula

(rubber) spatula 12 13

(ointment mill)

geometric dilution

11 Slab

12 spatula


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13 spatula

(levigating agents)

mineral oil glycerin

- Compound benzoic acid ointment, BP

Benzoic acid, in fine powder 60 g

Salicylic acid, in fine powder 30 g

Emulsifying ointment, BP 910 g

To make 1000 g

Emulsifying ointment, BP

Emulsifying wax, BP 300 g

White soft paraffin 500 g


To make 1000 g


43/65


benzoic acid salicylic acid

emulsifying ointment

geometric dilution slab spatula (rubber) mineral oil

-

Zinc and castor oil ointment, BP Zinc oxide 75 g

Castor oil 500 g

Arachis oil (peanut oil) 305 g


White beeswax 100 g

castor oil, arachis oil, cetostearyl alcohol white beeswax castor oil

zinc oxide geometric dilution slab

spatula

4.5.2 (Fusion)

ointment mill

(porcelain

dish) casserole (steam jacketed kettles)

(direct heat) water bath (indirect heat)


44/65


beaker method

beeswax, paraffin, stearyl alcohol PEG

-Methyl salicylate ointment Methyl salicylate 500 g

Cajuput oil 25 g

Cineole 25 g

Purified water 45 g

Menthol 100 g

Wool fat 105 gWhite beeswax 200 g

To make 1000 g

white beeswax wool fat

menthol methyl salicylate cajuput oil cineole

-

Compound methyl salicylate ointment

Methyl salicylate 250 g

Menthol 50 g

Eucalyptus oil 50 g

Wool fat 100 g

Vaseline 80 g

Hard paraffin 100 g


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White beeswax 100 g

wool fat, vaseline, hard paraffin white beeswax

menthol methyl salicylate eucalyptus oil


46/65


5. (Pastes)

Pastes

20-50

70-80 m

5.1 2

5.1.1 Oily and fatty pastes

(oleaginous bases)

Coal tar paste, BPC

soft paraffin Compound aluminium paste, BPC liquid paraffin

white petrolatum, lanolin (anhydrous) white wax

- RxZinc oxide paste, USP


Starch 25 g Active ingredientWhite petrolatum 100 g Base

- RxZinc oxide with salicylic acid, NF

Salicylic acid, in fine powder 20 g Active ingredient

Zinc oxide paste qs to 1000 g Base


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- RxCompound Zinc oxide paste


Coal tar 60 g Active ingredient

Starch 380 g Active ingredientLanolin 50 g Base

Hard paraffin 50 g Base

White soft paraffin 400 g Base

- RxSalicylic acid paste

Salicylic acid 3.4 g Active ingredient

Glycerin 5 g HumectantZinc oxide, fine powder 25 g Active ingredient

Starch 25 g Active ingredient

White soft paraffin qs to 100 g Base

5.1.2 Water soluble gels glycerogelatins

emulsifying ointment base emulsifying wax

tragacanth, pectin, alginates, boroglycerin, methylcellulose sodium methylcellulose

Zinc and Coal tar paste, BPC emulsifying wax

Titanium dioxide paste, BPC glycerin

- RxZinc gelatin, USP (glycerogelatin bases)


Gelatin 150 g BaseGlycerin 400 g Base

Purified water 350 g Base

- Rx Magnesium sulfate paste, BP (glycerogelatin bases)

Dried MgSO4 45 g Active ingredient

Phenol 0.5 g Active ingredient

Glycerin 55 g Base


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MgSO4 150oC 1.5

glycerin 120oC 1

phenol dried MgSO4

- Rx Recorcinol and sulphor paste, BPResorcinol 50 g Active ingredient

Precipitated sulphor 50 g Active ingredient


Emulsifying ointment 500 g Base

5.2

(Incorporation)

5.2.1

5.2.2

1)

geometric dilution 1

geometric dilution

2)

lanolin (anhydrous)

(levigating

agents)

slab

spatula ointment mill

roller mill


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6. (Gels)

(small inorganic molecules)

(large organic molecules)

Thixotropic

6.1

6.1.1 2

1) Inorganic gels two-phase gels

Lyophobic solvent/medium hating

two-phase

inorganic gels aluminium hydroxide gel floccule

magma milk bentonite magma, bismuth magma magnesium magma

2) Organic gels single-phase gels

Van der Waal

boundary (dispersed

molecule) (disperse medium) Lyophlilic


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solvent/medium loving

6.1.2 2 1) (Medicated gel)

antiseptic gels NSAIDs gels

2) (Lubricant gel)

Lignocaine gel

6.1.3 2

1) (Covalent)

2) (Noncovalent)

- Physical gelatin- Coulumbic interaction

(electrostatic interaction)

- Hydrogen bonding

- Coordinate bonding

- Hydrophobic bonding

6.1.4 2 1) Hydrogels aqueous gels

2) Organogels

polyethylene glycol (low molecular weight) mineral oil metallic stearate


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6.2

6.2.1 (active ingredients)

6.2.2 (gelling agents)

(gelation gel formation) pH

gel point gelatin

30oC

pH

1) 2 polysaccharides

(1) Polysaccharides 0.5-40

- tragacanth bassarin 60-70

tragacanth 30-40

pH 4-8 tragacanth parabens parabens

parabens methyl paraben 0.22-0.26 propyl paraben 0.05

tragacanth

tragacanth ethanol,

glycerin propylene glycol tragacanth tragacanth 2-3

5

Rx Tragacanth 5 g

Alcohol 10 g

Glycerin 2 g



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- acacia tragacanth

acacia

- Alginic acid 5-10

200-300 alginic acid

alginic acid

30

- Sodium alginate alginic acid

1.5-2.0 5-10 pH 4-10 pH 3 sodium alginate

1 24

sodium alginate 1

sodium alginate

sodium alginate

calcium gluconate, calcium tartate calcium citrate sodium

alginate

(2)

- gelatin 2-15

gelatin

- pectin sodium carboxymethyl

cellulose gelatin

pectin

2)


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- Methylcellulose (MC) non-ionic cellulose 5

methylcellulose 450, 2500 4500

centistroke 20 2 MC

MC 90oC (1 3 ) MC 2 3

3-4 propylene glycol

MC MC parabens

parabens

- Carboxymethylcellulose (CMC) 4-6

pH pH = 2 pH 2-10 pH 7-9

- Sodium carboxymethylcellulose (SCMC)

SCMC 25-50 (25-50 centistroke), SCMC 400-600 (400-600

centistroke) SCMC 1500 (1500 centistroke)

methylcellulose 1.5-5

SCMC pH 1-20 pH MC

pH 5-10 NH4+

Al3+ Fe3+ SCMC

glycerin propylene glycol

SCMC

- Hydroxypropyl methylcellulose (HPMC, Hypromellose) Hypromellose 20, 50, 125, 450, 1500 4500

polyethylene glycol

2 pH 3-10 (50-90oC)

- Hydroxyethyl cellulose (HEC) non-ionic ether


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3)

(1) (ionic substances)

glycerin

triethanolamine NaOH pH 6-11 0.1-1.0

0.5-5.0 Carbomer

- Carbomer carboxy polymethylene

0.3-1.0 0.5-5.0

carbomer carbomer

benzoic acid, sodium benzoate

benzalkonium chloride carbomer carbomer 910,

carbomer 934, carbomer 940 carbomer 1342

carbomer ()

carbomer (lump) carbomer

carboxyl groups carbomer carbomer

pH 4.5-11 pH 7 carbomer

20 NaOH KOH

50 triethanolamine carbomer

EDTA

(2) (nonionic substances)


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- Povidone Polyvinyl pyrrolodone 10

4) - Veegum 10

pH 3.5

Veegum

24

- Bentonite 8-10

Veegum

- Polyvinyl alcohol

100oC

polyvinyl alcohol 2.5

polyvinyl alcohol 30,000 , 130,000

200,000 polyvinyl alcohol

6.2.3

1) (preservatives)

88 (: Premjeet et al., 2012)

Tragacanth Methyl paraben 0.2% w/v propyl paraben 0.05% w/v

Sodium alginate Methyl paraben 0.1-0.2% w/v, chlorocresol 0.1% w/v, benzoic acid 0.2% w/v

Pectin Benzoic acid 0.2% w/v, methyl paraben 0.12% w/v, chlorocresol 0.1-0.2% w/v

Methylcellulose Phenylmercuric nitrate 0.001% w/v, benzalkonium chloride solution 0.02% v/v


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SCMC, HPMC Methyl paraben 0.2% w/v propyl paraben 0.02% w/v

Carbomer Methyl paraben 0.15% w/ v propyl paraben 0.05% w/v

2) (humectants)

glycerin, propylene glycol sorbitol

3) (dispersing agents wetting agents)

2

propylene glycol, glycerin

HLB 7-9

4) (permeation enhancers)

Stratum

corneum

Tween20, sodium lauryl sulfate, glycerin, dimethyl sulfoxide, N-methyl-2-pyrrolidone

dimethyl formamide

5) (stabilizers) (chelating agents)

EDTA

6.3

6.3.1 (gel base)

lumping

(homogenizer)

6.3.2


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-

-

-

-

glycerin, propylene glycol

6.3.3

6.4

6.4.1 (Non-homogeneous)

6.4.2

6.4.3 carbomer

6.4.4 (Lumping)


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6.4.5

Syneresis pectin, sodium alginate

6.5

-RxLubricant gel

Sodium carboxymethylcellulose 5.0 g gelling agent

Glycerin 15 g wetting agent, humectant

Methyl paraben 0.1 g preservative

Brilliant blue 0.001 g coloring agentPurified water qs to 100 g dispersing medium

-Rx Alcohol gel

Carbomer 940 0.25 g gelling agent

Ethanol 70 mL Antiseptic

Glycerin 1.0 mL wetting agent, humectant

Triethanolamine 1-2 drop pH adjustmentBrilliant blue qs coloring agent

Purified water qs to 100 mL dispersing medium

-Rx Sodium alginate gel

Sodium alginate 7 g gelling agent


Methyl paraben 0.2 g preservativeCalcium gluconate 0.05 g Viscositing agent

Purified water qs to 100 g dispersing medium

-Rx Ephedrine sulphate gel

Ephedrine sulphate 1 g active ingredient

Carbomer 934 2 g gelling agent

Triethanolamine 1.65 mL pH adjustment

Purified water qs to 100 mL dispersing medium


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-Rx Bentonite gel

Zinc oxide 10 g active ingredient

Glycerin 10 g wetting agent, humectants

Purified water qs to 100 g dispersing medium-Rx Zinc gelatin, USP

Zinc oxide 100 g active ingredient

Gelatin 150 g gelling agent

Glycerin 400 g wetting agent, humectants

Purified water 350 g dispersing medium

-Rx Flucinolone acetonide gel ( )Flucinolone acetonide 0.18 g active ingredient

Ethanol, 95% 1.82 mL cosolvent

Propylene glycol 45.45 mL wetting agent, humectants

Polyethylene glycol 400 36.36 mL wetting agent, humectants

Paraben concentrate 1.82 mL preservative

Carboxymethylcellulose 4.36 g gelling agentHot water qs to 100 mL dispersing medium


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7. (Emulsiongels)

thixotrophy

Voltaren emulgel ( 14)

Piroxicam emulsiongel

14

-RxPiroxicam emulsiongel

Piroxicam 0.5% NASIDs

Polyethylene glycol 400 19.5% cosolvent for piroxicam

Ethanol 10% cosolvent for piroxicam

Propylene glycol 10% cosolvent for piroxicam

Cream base 30%


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Cetyl alcohol 20 g stiffening agent

Mineral oil 20 g emollient

Span 80 0.5 g emulsifying agent

Tween 80 4.5 g emulsifying agentParaben concentrate 1 g preservative


Gel base 30%

Carbomer 934 1 g gelling agent


Paraben concentrate 1 g preservativeTriethanolamine qs to pH 7.0 pH adjustment

Purified water qs to 100 g dispersing medium

7.1

1)

2)

3)

4)

5) (permeation enhancer)

6)

7)

8)

7.2

1)

2) beaker method

3)

geometric dilution


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4) 3)

geometric dilution

5)


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8. (Liniments)

3

8.1

Camphor and Soap Liniments

NF

8.2 Methyl salicylate Liniment Compound methyl salicylate Liniment

8.3 (soap)

Turpine Liniment BP soft soap, camphor, turpine oil

9.

w/o

o/w


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1.

2.

3. HLB 4. Humectants

5.

6.

7.

8.

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systems. 2011. 9thed: Wolters Klumar; China.

Aulton ME. Aultons pharmaceutics the design and manufacture of medicines. 2007. 3rded:

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The HLB system. ICI Americas, Inc. 1984.

Khar RK, Vyas SP, Ahmad FJ, Jain GK. The Theory and practice of industrial pharmacy. 2013.

4thed: CBS Publishers and Distributors Pvt Ltd; India.

Mathur V, Satrawala Y, Rajput MS. Physical and chemical penetration enhancers in

transdermal drug delivery system. Asian Journal of Pharmaceutics 2010, 4: 173-183.

Pharmacopeial Forum in the United States Pharmacopeial Convention, Inc. Topical and

transdermal drug products. Vol. 35(3) [May-June 2009]

Premjeet S, Ajay B, Sunil K, Bhawana K, Sahil K, Divashish R, Sudeep B. Additives in topical

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United States Pharmacopoeia 32-National Formulary 27.2009. Pharmacopeial Convention;

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Topical Dermatologic Products 18 สค 2015