phardose lab (prep 6-10)

Preparation 6 (Glycerin Suppositories) - Suppository bottles (adult); white label Suppositories - solid dosage forms intended for insertion into body orifices where they melt, soften, dissolve and exert localized/systemic effect. Types: 1. Rectal Suppositories - cylindrical or bullet shape - 32mm (1 ½ inch) in length - weight: 2g (adult); 1g (children) 2. Urethral Suppositories - Bougies and inserts - slender or pencil shape - Male: 4g, 140mm long, 3-6mm diameter - Female: 2g, 70 mm long - Uses: dilatation of uterus, anti-infective agent & erectile dysfunction

Ideal Suppository: 1. clear melt 2. doesn’t melt at room temperature 3. inert and compatible to other substances 4. acid value of freshly prepared (pure) > Saponification – formation of esters > Fixed Oils (liquid, solid, pH) >Steric acid: stiffening agent > Above – local effect; Below – systemic effect Procedure: 1. Heat the glycerin using direct heat with constant stirring until it has reached the temp of 120 F (49C) 2. In another container, dissolve Na2CO3.H2O in H2O Add Steric Acid. Mix thoroughly until dissolved 3. Add #2 to #1 4. Continue heating until all effervescence (CO2 ^) is gone or until the liquid is clear 5. Transfer the melted suppositories in a previously chilled molder 6. Place the molder in the freezer for 10-20 min 7. Wrap the suppositories individually using aluminum foil (trapezoid shape)

3. Vaginal Suppositories - Pessaries - globular, oviform, cone-shaped - weight: 5g - Uses: anti-fungal, anti-infective, contraceptive 4. Nasal Suppositories - slender& pencil shape - Burginatium 5. Otic/Oral Suppositories - pencil shape Three Methods of preparation 1. Melting from a Melt or Fusion - (melt all ingredients > pour on molder while hot > freezer > wrap individually) - Nickel or Bronze 2. Compression (more elegant products) - small scale only - avoids sedimentation - suppository compression device (mix >scd>pressure applied>cooled>ejected) 3. Hand Rolling and shaping (ancient) Suppository Bases: 1. Tends to Melt - Cocoa Butter &Theobroma Oil (most widely used) - Theobroma Oil (polymorphic- inability to absorb in aqeoussol’n; rectal; lower melting point {chloralhydrine} - Witepsol (do not exhibit polymorphism; natural saturated fatty acid chain between C12 and C18) - Wecobee(from coconut oil) 2. Tends to be dissolved

Almazan, Jan Aira E-PH

- PEG (polyethylene glycol) – lower molecular weight > 400 – Liquid > 1000 – Semi solid > 2000 – Solid

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Preparation 7 (Cold Cream) - Red label Creams - semisolid preparation - containing one or more medicinal agents dissolved or dispersed in either an oil-in water emulsion or in another type of water-washable base - easier to spread and remove than ointment - lighter, less viscous than ointment - impart pseudo-plastic flow when applied Two types: 1 Oil-in water (O/W) - tends to vanish on skin (vanishing cream) - eg. Shaving cream , hand cram, foundation cream 2. Water-in oil (W/O) - imparts an oily feeling on skin - eg. Emollient cream, cold cream Cold Cream - petrolatum roast water ointment Galen’s cerate - vanishing cream

Procedure: 1. Melt the white wax on a water bath 2. Add white petrolatum with constant stirring 3. Pour to the ointment jar while hot. Let it congeal 4. Cover with circular glassine paper

Almond oil (better emollient property) - mineral oil (more stable cold cream)

Procedure: 1. Melt spermaceti/cetyl alcohol and white wax with mineral oil using steam bath 2. In another container, dissolve sodium borate solution to the melted wax, stirring rapidly & continuously, until a viscous white cream is formed 4. Pour to the container 5. Allow to congeal

White Ointment Uses: - emollient - protective barrier or vehicle 2 ingredients: - active ingredient and ointment base - no color, no flavorant Packaging: - tubes (plastic/aluminum/tin) - jar (plastic, aluminum) – can be clear, opal, amber, and green glass or white or green plastic ointment jars

Preparation 8 (White Ointment) - Red Label Ointment - semisolid preparation - for external application on skin and mucous membrane Methods: 1. Mechanical Incorporation - performed by trituration in a mortar / on a slab with spatula (levigation) - Medicaments are reduced to impalpable powder (trituration) before incorporation into a base to reduce grittiness, and to form a very smooth nucleus which is incorporated to the remainder of the base to obtain a smooth homogenous ointment 2. Fusion - use of heat - Heat substances with high melting point first like wax and spermaceti using water bath before adding the soft and oleaginous material

Note: > Dark Brown ointment – Oxidized - to prevent oxidation – anti-oxidant (vit C / E) >Yellow Wax and White Wax difference > Microbial Content test > Preservative Preparation 9 (Zinc Oxide Ointment) - red label Ointments - Salve or Chrisma - may be medicated or not - Unmedicated ointments (serve as vehicles for topical application of medicina substances or used as protective, emollient, or lubricant)

Four types of ointment bases 1. Oleaginous bases / Hydrocarbon bases - non-water washable; anhydrous; and insoluble in water - cannot absorb or contain water -eg. Petrolatum, synthetic ester, lanolin derivative

Characteristics of Ointment (book) 1. They should be homogenous, smooth, and free from grittiness 2. easily spreadable 3. should never be dispensed if they have the slight evidence of rancidity or mold

2. Absorption bases - non-water washable; anhydrous & insoluble can absorb water - eg. Hydrophilic petrolatum, wool fat (anhydrous lanolin)

Mechanical Incorporation - levigation - mineral oil – zinc oxide and sulfur are insoluble on water - for smooth dispersion;to prevent grittiness

3. Water-removable bases - oil-in water bases; water-washable bases - eg. Hydrophilic ointment USP, vanishing cream, galen’s cream, petrolatum rose water ointment

Ideal characteristic of ointment (maam) 1. Does not retard wound healing 2. Low 3. Pharmaceutically elegant 4. Non-dehydrating 5. Non-greasy 6. Low index irritation 7. Neutral in reaction 8. Good keeping qualities 9. Should be Bio-compatible with other ingredients

4. Water-soluble bases - water washable; greaseless - eg. Polyethylene Glycol ointment (PEG), propylene glycol, propylene glycol ethanol

Almazan, Jan Aira E-PH

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10. Washable 11. Minimum number of ingredients to b used 12. Ease in compounding

Preparation 10 (Sulfur Ointment)

Procedure: Zinc Oxide (triturate) + mineral oil >levigate +white ointment

Almazan, Jan Aira E-PH

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Sulfur > Precipitated Sulfur (is preferred because it is smoother and greater surface reaction) – treatment of scabies ***same procedure as zinc oxide