Kimberley Anne See 2A-Pharmacy | A.Y. 2015-2016 Preparation 1: Divided Powders EXPERIMENT: Category: powders Category: powders Ingredients: Ingredients: Levothyroxine Na (Eltroxin) 50 mcg Lactose Synonym: Synonym: Chartulae Method of preparation: block and divide Computations:
Packaging: glassine paper & paper envelope Label: white (internal) POST-LAB: Powders -mixture of finely divided solids or chemicals in a dry form -may be used internally or externally Bulk powders -antacid, laxatives Divided powders -individual doses -dispensed in papers Types of papers used: Vegetable parchment -semi-opaque -moisture resistant -most preferred White bond paper -opaque -not moisture resistant Glassine paper -glazed; transparent -moisture resistant Waxed paper -waterproof paper -transparent Advantages: Flexibility of compounding Good chemical stability Rapid dispersion of ingredients Disadvantages:
Time consuming preparation Inaccuracy of dose Unsuitable for many unpleasant tasting, hydroscopic and deliquescent drugs Micromeritics -study of small particles Mixing -mechanical process of reducing solid particle size of solids (COMMINUTION) Different mixing techniques: Spatulation -use of spatula (on a tile/paper) -used for EUTECTIC (powders that liquefy; low melting points) MIXTURES -not applicable for large scale Trituration -mixing and reducing -use of mortar and pestle Wooden — fibrous; fibrous; comminution of o crystalline solids Glass — non-staining; non-staining; nonporous; o flavoring oils; colored substances Porcelain — commonly commonly used, grazed, less o porous Geometric Dilution -for mixing POTENT SUBSTANCES -Quinine sulfate Sifting -light blocky, dense powder -sifter is used Tumbling -mix large amount of powder -use of tumbler; 2/3 of volume Advantages Increases surface area (increase dissolution and bioavailability) Increase extraction or reactivity re activity Facilitates hot drying of masses Improves blending and mixing Uniform distribution of coloring agents Improve texture, appearance and physical stability Disadvantages Can change the polymorphic form of the active ingredients Degrades the drug Decrease bulk density
1
Kimberley Anne See 2A-Pharmacy | A.Y. 2015-2016 Decrease the particle size (cause aggregation and decrease dissolution) Increase surface area (promote air absorption and inhibits wettability) Different comminution techniques: 1. Large scale — use of mills, pulverizers 2. Small scale Trituration Pulverization by intervention — reduce particle size with aid of a volatile solvent Levigation — form a paste (use of mineral oil, glycerin) Method for determination of particle size: 1. Sieving 2. Microscopy [1/3] 3. Sedimentation rate [2/3] — use Stoke’s law 4. Light energy diffraction/light scattering 5. Laser holography 6. Cascade impaction USP Standards for Powders of Animal and Vegetable Drugs
Type of Powder
Very coarse
Sieve size all particles pass thru #20
Coarse
#20
Moderately coarse Fine
#40
Very fine
#80
#60
Sieve size % particles pass thru nmt 20% thru #60 sieve nmt 40% thru #60 sieve nmt 40% thru #80 sieve nmt 40% thru #100 sieve no limit
USP Standards for Powders of Chemicals Type of Powder
Coarse Moderately coarse Fine Very fine
Sieve size all particles pass thru #20 #40 #80 #120
Sieve size % particles pass thru nmt 60% thru #40 sieve nmt 60% thru #60 sieve no limit no limit
Preparation #2: Effervescent Granules EXPERIMENT: Category: granules Synonym: Pulvis effervescens compasitus Ingredients:
Sodium bicarbonate — effervescence (release of CO2) Citric acid — hygroscopic (pasty) Tartaric acid — loses air when exposed to water Method of preparation: wet method (classic) Packaging: 30 mL wide-mouth amber bottle Label: White (internal), unofficial Computations:
POST LAB: Granules -prepared agglomerates of small particles of powder -irregularly shaped but may be spherical -uses 4-12 sieve size range Methods of preparation: Wet method 1. Classic — moistening then passing thru sieve then oven drying 2. Fluid-bed process — Powder is placed in conical piece of equipment Dry method 1. Fusion method — passing thru roll compactor then granulating 2. Slugging — compression of powder into large slugs/tablet (8k-12k pounds_ Advantages over powders: Flow well More stable Less likely to harden upon standing Easily wetted by liquid Compressibility Preparation #4: Chocolate Base Ca Lozenges EXPERIMENT: Category: lozenges Synonym: Calx chocolate lausiae Ingredients: Calcium carbonate Corn oil Chocolate bar Method of preparation: fusion/molding method Packaging: aluminum foil, paper box
2
Kimberley Anne See 2A-Pharmacy | A.Y. 2015-2016 Label: White (internal), unofficial Computations:
POST LAB Lozenges -solid dosage form intended to slowly dissolve in the mouth -bucally or sublingually for absorption -used for local effect Types: Hard lozenges -made from syrups of sucrose and other sugars -moisture content: 0.5% to 1.5% -preparation is similar to candy making Soft lozenges -flavored fatty base [chocolate, PEG base, sugar-acacia base] Chewable gummy gel lozenges -glycerinated gummy gel base Methods of preparation: Hand-rolling -do not require special calculations and equipment -pill roller, broad bladed spatula -requires experience and special te chniques Fusion/molding method -can be used for all types of lozenges -requires heat, mold, skills and calcs -must not be used for heat sensitive drugs Preparation #5: Aspirin capsules EXPERIMENT: Category: capsules Synonym: Acetylsalicylic acid (ASA) Ingredients: Aspirin powder Method of preparation: punch method Packaging: 15 mL wide mouth amber bottle Label: White (internal), official Computations:
POST LAB Capsules -solid dosage forms in w/c medicinal agents and/or inert substances are enclosed w/in a small shell of gelatin that may be hard or soft -shells are usually made of GELATIN or STARCH Types Hard gelatin capsules -made up of gelatin, sugar, water -made opaque by adding titanium dioxide -body + cap -filled by PUNCH METHOD or FILLING MACHINES -moisture content: 13%-16% Soft gelatin capsules -made up of gelatin -more pliable due to presence of glycerin, or sorbitol (plasticizers) -active ingredient suspended in vegetable oil, water miscible glycol (PEG 400 or PEG) 000 15 gr 00 10 gr 0 7.5 gr 1 5 gr 2 4 gr 3 3 gr 4 2 gr 5 1 gr Preparation #6: Glycerin Suppositories EXPERIMENT: Category: Suppository Synonym: Suppositoria glycerin Ingredients: glycerin sodium stereate water Method of preparation: molding/fusion Packaging: suppository bottle Label: red (external), unofficial Computations:
3
Kimberley Anne See 2A-Pharmacy | A.Y. 2015-2016 Computations:
POST LAB Suppositories -solid dosage forms intended for insertion into body orifices -localized/systemic effect Types: 1. Rectal suppositories -cylindrical/bullet shaped -32 mm (1.5 in) in length -2g adult -1g children 2. Urethral suppositories [Bougies] -slender or pencil shape Male: 140 mm long; 3-6 mm in diameter; 2g Female: 70 mm long; 1g Uses: erectile dysfunction, dilation of uterus, antiinfective agent 3. Vaginal suppositories [Pessaries] -globular, oviform, cone shaped -weighs 5g Uses: anti-fungal, anti-infective, contraceptive Methods of preparation: 1. Molding from melt/fusion 2. Compression 3. Hand rolling/ shaping — easiest Bases: 1. Cocoa butter/theobroma oil -most widely used 2. Witepsol bases -fatty acid chain between C12 and C18 3. Wecobee base -derived from coconut oil 4. Glycinerated gelatin -water soluble Preparation #7: Cold cream EXPERIMENT: Category: cream Synonym: Petrolatum rose water ointment Ingredients: spermaceti white wax mineral oil sodium borate Method of preparation: fusion method
POST LAB Creams -viscous liquid or semisolid emulsions containing one or more medicinal agents -easier to spread and remove than ointment Types: Oil in water -vanishes on skin -Galen’s cerate (vanishing cream) Water in oil -imparts oily feeling on skin -emollient cream or cold cream
4
