Pharmaceutical Dosage Form Lab prep 6-18

PHARMACEUTICAL DOSAGE FORMS LAB REVIEWER #6 GLYCERIN SUPPOSITORIES CATEGORY: suppository SYNONYM: glycerina

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Estrogenic substances (dienestrol) – used to restore the vaginal mucosa to its normal state.

Vaginal tablets (vaginal inserts) manufacture, more stable, and less messy.  

Anti-infective w/ homonal substances

LABEL: red label

Tablet lubricant – Magnesium stearate

CONTAINER: suppository bottle

Disintegrating agent - startch

Suppository - solid dosage form intended for insertion into the body orifices where they melt, soften, dissolvem and exert localizied or systemic effect.

Use: anti-fungal

5 TYPES OF SUPPOSITORIES 1. rectal - cylindrical or bullet shape - 32 mm (1 ½ inch) - 2g adult; 1g children Use: glyercin – laxative effect Sodium stearate – (Soap); solidifying agent 

  2. urethral shaped.

Cathartic – acts directly on colonic mucosa to produce normal peristalsis. Not appreciably affects the motility of small intestine Relieve pruritus ani – pain associated w/ hemorrhoids constipation (bougies or inserts) – slender, pencil

easier to

Anti-infective Contraceptive (w/ spermicide) 4. otic (aural) – pencil-shaped 5. nasal (burginarium) – pencil-shaped CRITERIA FOR SUPPOSITORIES 1. melts at body temperature 2. firm at room temperature 3. yields at clear melt 4. inert and compatible with other agent 5. wetting and emulsifying 6. acid value ( supp. Compression device -> apply pressure -> cool 3. fusion method -

melting of all ingredients pour directly to mold freeze wrap in Aluminum foil

#8 WHITE OINTMENT SYNONYM: salve, chrisma, unguentum album, unguentum simplex USE: protective, emollient, lubricant CONTAINER: 15 g ointment jar Ointment – semisolid preparation intended for external application to skin and mucous membrane. 2 TYPES OF OINTMENT:

#7 COLD CREAM CATEGORY: cream SYNONYM: petrolatum rose water ointment USES: emollient, cleansing cream, ointment base

1. medicated- w/ active ingredient 2. non-medicated- ointment bases. Serves as vehicles for application of medicinal substances 

CONTAINER: 15 g ointment jar Creams –semisolid preparations containing one or more medicinal agents dissolves or dispersed in either o/w or w/o emulsion or in another type of water-washable base.   

Easily spread and remove than ointment Lighter, less viscous Impart pseudo-plastic flow when applied

2 TYPES OF CREAMS 1. oil-in-water – vanishing cream (galen’s cerate) Example: cream

shaving cream, hand cream, foundation

2. water-in-oil- imparts oily feeling on skin Example: cold cream (petrolatum rose water ointment), emollient cream

Medicaments are reduced to impalpable powder before incorporation into a base to reduce grittiness and form a very smooth nucleus for a smooth homogeous ointment.

METHODS OF PREPARATION 1. fusion 2. mechanical incorporation – performed by trituration in a mortar or on a slab with spatula is a process known as levigation. 

Unguator

4 TYPES OF OINTMENT BASES 1. oleaginous bases – aka hydrocarbon bases     

Have emollient effect after application Water insoluble Non-washable Cannot absorb water Oily, occlusive, lack cosmetic appeal

Examples: a. Petrolatum, USP – good base for insoluble ingredients ex. vaseline b. White petrolatum, USP – yellow wax is decolorized ex. White vaseline

- yellow waxpurified wax obtained from honeycomb of the bee Apis mellifera d. white ointment USP - white wax (bleached and purified yellow wax) e. Lanolin derivatives e. Synthetic esters – constituents of oleaginous butyl

2. Absorption Bases     

Water insoluble Non-washable Can absorb water Anhydrous Oily, occlusive, lacks cosmetic appeal

Examples: a. Hydrophilic petrolatum – w/o emulsifier b. Aquaphor – has the capacity to absorb up to 3x its weight in water c. Aquabase – d. Wool fat (anhydrous lanolin) – from wool of sheep (Ovis aries)  

Higher percentage of cholesterol Ability to absorb twice its weight

3. Water-Removable bases – o/w emulsions; aka emulsion bases. 2 types: a. Water in oil  

water insoluble non-washable

can absorb water contains water

Examples:    

cold cream (petrolatum rose water ointment) Lanolin (hydrous wool fat) Hydrophilic ointment Vanishing creams

b. Oil in water

c. Yellow Ointment, USP – aka simple ointment;

- glyceryl monostearate, stearate, isopropyl lanolate , stearyl alcohol

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water insoluble water washable can absorb water contains water

Examples:      

Hydrophilic ointment Velvachol Unibase Acid mantle Dermabase Vanicream

Humectants – hydrating agent   

Glycerin Propylene glycol Sorbitol 70%

4. Water Soluble bases     

Water soluble Water washable Can absorb water Anhydrous or hydrous All water soluble, no oil phase

Examples: polyethylene glycol ointment Veegum Methods of Preparation: 1. Fusion – heating all ingredients. Let cool and congeal. 2. Mechanical incorporation - performed by trituration in a mortar or on a slab with spatula is a process knwon as levigation. COMPEDIAL REQUIREMENTS FOR OINTMENTS: 1. Microbial content – test for absence of Staphyloccocus aureus and Pseudomonas aeruginosa.

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Addition of preservatives such as methyparaben, propylparaben,phenols, benzoic acid, sorbic acid, and quarternary ammonium salts

2. Minimum fill – to ensure proper contents compared with labeled amount. - 30% max (overage) - 10% minimum 3. Packaging, storing, and labeling Packaging – jar: glass, plastics ( DO NOT POUR WHILE HOT)

#11 CINNAMON WATER SYNONYM: cassia oil, cassio nare USE: flavored vehicle for internal aqueous solution, carminative

- dispensing jars: plastic

DESCRIPTION OF FINAL PRODUCT: solution

- tubes: plasitc, tin, aluminum

CONTAINER: 30 ml narrow amber bottle

Labeling – protect w/ tape - Dual labels Storage – store in a cool place 4. Sterility test and metal particles content for ophthalmic ointment 5. non-gritty – non sand-like feeling to be achieved by heavy trituration. SELECTION OF APPROPRIATE BASE:       

Active ingredient: precipitated sulfur – make a smoother ointment than any other sulfur. Provides greater reactive surfaces.

Topical or percutaneous drug absorption Release rate Occlusion Stability of the drug Effect of drug on ointment base Easy removable Characteristics of surface for application

clear, saturated

#12 CONCENTRATED PEPPERMINT WATER SYNONYM: Aqua Mint USE: flavoring vehicle, carminative CONTAINER: 30 ml narrow amber bottle DESCRIPTION OF FINAL PRODUCT: clear, saturated solution 

Computed by alligation alternate (x method)

Aromatic water- clear, aqueous soution saturated with volatile oils or other aromatic or volatile substances. 

Should be free from empyreumatic (smole-like) and other foreign odor.

METHODS OF PREPARATION

#9 ZINC OXIDE OINTMENT

1. distillation - most satisfactory methos of preparation but the slowest and most expensive of the 2 methods.

SYNONYM: Zinc oxide unguentum

Example: Strong Rose Water

USE: Tx and Prevention for diaper rash (protectant)

Cohobation – process of repeatedly using the distillate to distille with fresh portions of flowers/ plant materials to minimize loss of water soluble components.

CONTAINER: 10 g ointment jar Active ingredient: ZnO #10 SULFUR OINTMENT SYNONYM: Unguentum sulfuris, Unguentum de Azufre USE: Tx for scabies, ketolytic, acne vulgaris

Example: Orange or Rose flowers 2. Solution 2a. Direct solution method - prepared by repeatedly shaking and set aside or 12 hours, filtered through wetted filter paper and qs ad. Example: cinnamon water

2b. Alternate solution method – prepared by incorporating the volatile oil with talc or siliceous earth or pulped filter paper, agitate for 10 mins, filtered and qs ad. Example: concentrated peppermint water Dispersing agent - ↑ surface of volatile substances ensuring more rapid saturation of water and forms an efficient filter aid for a clearer solution.

#15 MAGNESIUM CITRATE ORAL SOLUTION SYNONYM: Milk of Magnesia, Ascapate of Magnesia USE: saline cathartic DESCRIPTION OF FINAL PRODUCT: colorless to slightly yellow clear effervescent liquid having a sweet, aciduloud taste and a lemon flavor.

#13 CALCIUM HYDROXIDE TOPICAL SOLUTION

REMARKS:

CATEGORY: astringent

NOTE: CaOH is more soluble in cold water

DESCRIPTION OF FINAL PRODUCT: clear, colorless solution

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SYNONYM: hydrated lime, lime water, liqoud calcis

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Ca(OH)2 + CO2 → CaCO3 + H2O CONTAINER: 30 ml narrow mouth flint bottle REMARKS: 

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Should be stored in well-filled, tightly stoppered containers to determine the absorption of CO2 and should be kept in the cool place to avoid degradation. Best accomplished by the use of a siphon with care not to entrain the residue. Prepared by simple solution

Is has tendency to deposit a crystalline solid upon standing Official MgCo3 – a basic hydrated MgCO3, or a normal hydrated MgCO3

STORAGE: cool place preferably a ref keepping the cork or rubber liner moist and swollen maintaining airtight seal between cap and bottle. CONTAINER: 120 ml wide mouth flint bottle Solutions – liquid preparations that contain one or more chemical substances dissolves in a suitable solvent or mixture of mutually miscible substances. 

Homogenous mixture

Relative Terms of Solubility

NOTE: CaOH is more soluble in cold water

Parts of solvent required for 1 part of solute 10,000

REMARKS: 

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Iodine crystals stains hand and jewelries  1:2950  Very volatile  Very reactive to metal – use porcelain or very hard rubber spatula Addition of KI to increase solubility Prepared by simple solution

METHODS OF PREPARATION (SOLUTIONS) 1. simple solution - by dissolving solute in a suitable solvent. Example: NaCl soln, Strong Iodine solution, CaOH soln 2. solution by chemical reaction – by reacting two or more solute with each other in a suitable solvent.

Example: Aluminum subacetate soln, Magnesium citrate solution, Sulfurate lime solution 3. solution by distillation – for isolation of volatile oil 4. solution by extraction – drug or pharmaceutical necessities of vegetable or animal origin. 

DESCRIPTION OF FINAL PRODUCT: viscous, dark brown syrup with the odor and taste of cocoa CONTAINER: 15 ml amber bottle PREPAPERED BY: w/ aid of heat

Aka extractives

a. maceration – submerging solute 

SYNONYM: Cacao syrup, chocolate fllavored syrup

Best used for drugs containing little or no cellular material such as benzoin, aloe and tolu w/c dissolves almost completely in the menstruum.

Ingredients: 1. 2. 3. 4.

b. percolation – using percolator c. digestion – with the aid of gentle heat d. infusion – blanching; + hot water e. decoction – boiling for 15 mins.

#16 SIMPLE SYRUP

5. 6. 7. 8.

USE: sweetening agent, sweet vehicle and basis for many flavored and medicated syrup CONTAINER: 60 ml flint bottle Computation: → M Soln = D x V mass solvent = mass soln- mass solute vehicle (Water) - * with the mass solvent PREPARED BY: percolation REMARKS: loose cotton – permit sucrose light flow freely Tight cotton – inhibits flow of liquid Filter paper – to prevent holing of sugar

agent),

REMARKS: 

SYNONYM: syrupus, sirup, syrup DESCRIPTION OF FINAL PRODUCT: clear solution of sucrose in purified water

Cocoa powder – flavorant Sucrose – sweetening agent Liquid glucose Glycerin – humectant (hydrating preservative Sodium chloride – taste balancer Vanilin - flavorant Sodium benzoate - preservative Purified water – vehicle

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Cocoa is NMT 12% non-volatile ether soluble extractives of fats yields syrups having a minimum tendency to separate. Sodium benzoate and glycerin are preservatives added to prevent bacterial and mold growth  because of low concentration of sucrose (not self-preserving)

Syrup – concentrated aqueous solution containing sugar usually sucrose or any sugar substitute. Polyols (glycerin or sorbitol) – retart crystalliation of sucrose to increase its solubility. TYPE OF SYRUP: 1. simple syrup – clear, concentrated, sweet, aqueous, hypertonic solution with striations with concentrations of 85% w/v or 65% w/w (sp gr.: 1.313) for self preserving characteristics. 2. flavored/ non-medicated syrup - contains aromatic and pleasantly flavored substances. Example: chocolate syrup(flavorant), glycyrrhiza syrup (masks bitter taste of alkaloid)

#17 CHOCOLATE SYRUP

3. medicated syrup – with active ingredient and has therapeutic efect

USE: flavored vehicle to active medicaments or substance to improve their taste

Example: Ipecac, FeSO4

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METHODS OF PREPARATION FOR SYRUP 1. solution without aid of heat ADVANTAGE: for heat sensitive. Avoids heat induced conversions DISADVANTAGE: slowest and time consuming method

CONTAINER: 15 ml flint bottle REMARKS:  

Example: FeSO4

 2. solution with aid of heat – for heat stable only ADVANTAGE: fast DISADVANTAGE: excessive heating will cause inversion of sucrose and form caramelization    

tendency to ferment sweeter less stable prone to microbial growth

Example: acacia syrup, cocoa syrup, syrup USP 3. percolation – a percolator or a column is being used. The fluid rate of liquid(water) is controlled or adjusted to 20 drops/minute using a cotton. 

The percolator will allow the passage of water slowly through the bed of crystalline sucrose and will eventually dissolve the sugar.

Example: Tolu Balsam, Simple syrup 4. addition of sucrose to a medicated liquid – simple admixture of sugar to a prepared medicated liquid usually a fluidextract or a tincture.  

The syrup prepared through this is not self preserving. Prone to microbial growth – low concentration of sucrose.

#18 ACACIA MUCILAGE SYNONYM: Mucilage of Gum Arabic, Mucilage of Gum Acacia DESCRIPTION OF FINAL PRODUCT: adhesive liquid with brown color USE:  

Demulcent Suspending agent

thick,viscid,

Excipient in making pills and troches Emulsifying agent for cod liver oil and mineral oil emulsion

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benzoic acid – preservative must be free from molds or any other indication of decomposition it is unstable and prone to decomposition (+preservative) SHOULD NEVER BE MADE IN LARGE QUANTITIES!