Term
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Definition
suppositories are solid dosage forms intended for insretion into body orifices |
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Term
what are the different sites of insertion for suppositories |
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Definition
vagina, rectum, and urethra (vagina and rectum are the most common) |
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Term
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Definition
- has similar advantages as TDDS (skips hepatic first pass metabolism) - good dosage forms for treating pts. with vomiting - more drugs can be made into suppositories than can be made into TDDS - suppositories have a faster rate of onset than TDDS - local effects |
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Term
shapes of rectal suppositories |
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Definition
- usually tapered at one or both ends - inserted with fingers |
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Term
adult rectal suppositories |
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Definition
- about 2 grams - cocoa butter or theobroma oil (bases - synonyms of eachother) |
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Term
child rectal suppositories |
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Definition
- cocoa butter or theobroma oil (bases - synonyms of eachother) - half the weight of adult suppositories |
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Term
shapes, weight, and content of vaginal suppositories |
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Definition
- globular or oviform - 5 grams - cocoa butter is the base - "pessaries" |
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Term
most common urethral suppository |
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Definition
- medicated urethral system for erection (MUSE) |
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Term
another term used to describe urethral suppositories |
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Definition
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Term
physiologic factors affecting drug absorption from rectal suppositories |
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Definition
- colonic content - pH and lack of buffering capacity of the rectal fluids |
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Term
physicochemical factors of the drug and suppository base |
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Definition
- lipid-water solubility - particle size - nature of the base |
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Term
when systemic effects are desired, can greater absorption be aquired when the rectum is empty or distended with fecal matter? |
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Definition
- empty rectum because drug has greater opportunity to make contact with absorbing surfaces |
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Term
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Definition
- empties rectum so that suppository can be administered |
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Term
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Definition
- ability of drug buffer to resist change in pH |
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Term
relationship between rectal fluids and buffer capacity |
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Definition
- rectal fluids have no buffer capacity therefore rectal fluids do not react with weak acid or weak base of drug - without using another form for the suppository (i.e. ionic) the suppository is immiscible with body gluid and fails to release fat soluble drug readily into the rectum |
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Term
how do you incorporate fat soluble drugs in cocoa butter |
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Definition
- use ionic form therefore it is more soluble in aqueous solution and increases bioavailability |
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Term
between hydrophilic and lipophilic forms of the drug, which two has more tendency to escape out of the fatty suppository base? |
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Definition
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Term
between hydrophilic and lipophilic forms of a drug, which of the two has more tendency to escape out of the fatty suppository base? |
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Definition
- both - lipophilic escapes out readily because it has no affinity for water - hydrophilic escapes out because the base dissolves in aqueous fluids |
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Term
relationship bt particle size and suppositories |
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Definition
- the smaller the particle size, the more readily the dissolution of the particle and the greater the chance for rapid absorption |
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Term
essential features of the base for suppositories |
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Definition
- must be capable of melting, softening, or dissolving in order to release drug for absorption - should not interact with the drug to inhibit its release - should not irritate the mucous membrane |
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Term
3 categories of suppositories |
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Definition
- fatty or oleaginous bases - water-soluble or water-miscible bases - miscellaneous bases |
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Term
fatty or oleaginous bases |
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Definition
- most frequently employed suppository base (cocoa butter) |
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Term
under what conditions should cocoa butter be prepared for suppository bases |
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Definition
- melts bt 30-36 degrees (just below body temp) - should not be hastily or carelessly melted |
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Term
What happens if you overheat cocoa butter for a suppository base? |
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Definition
- the suppository formed will melt below 30 degrees - cocoa butter exists in two forms (alpha and beta) - want the beta form which has a melting point bt 30-35 degrees (ideal) - melting point for alpha form is below 30 degrees therefore it will not solidify at room temperature - alpha can convert back to beta form but it takes several days |
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Term
2 main members of water-soluble and water-miscible bases |
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Definition
- glycerinated gelatin - PEG's |
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Term
glycerinated gelatin as a water-soluble base |
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Definition
- slower to soften and mix with the fluids and therefore provides a slower release - tendency to absorb moisture as a result of hygroscopic nature of glycerin |
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Term
what must you do to the suppository when it has a glycerinated gelatin base before insertion? |
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Definition
- moisten with water prior to instertion - moistening prevents dehydrating effect and irritation of tissues |
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Term
PEG's as a water-soluble base for suppositories |
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Definition
- polymers of ethylene oxide and water (HO-(CH2-CH2-O-)n-H) - 300, 400, 600, 1000, 1450, 3350, 4600, 6000, 8000 - do not melt at body temp. but dissolve slowly in the body fluids |
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Term
what base is the most convenient in terms of storage and handling of suppositories? |
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Definition
- PEG's because it does not melt at body temp. and you do not need to refridgerate |
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Term
3 methods of preparing suppositories |
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Definition
- molding from a melt ("fusion method") - compression - hand rolling and shaping |
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Term
steps taken when molding from a melt for preparation of a suppository |
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Definition
- melting the base - incorporating any req. medicaments - pouring the melt into molds - allowing melt to cool an congeal into suppositories - removing the formed suppositories from the mold |
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Term
types of molds used when molding from a melt for preparing suppositories |
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Definition
- stainless steel - aluminum - brass - plastic - rubber molds |
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Term
is lubrication of a mold required when molding from a melt in preparing a suppository? |
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Definition
- depends on the formulation of suppository used - cocoa butter or PEG (seldom necessary because suppositories contract significantly when cooling and they separate from inert surfaces) - glycerinated gelatin (necessary; ex. mineral oil which is also used as a levigating agent) |
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Term
role of the physician in compounding of suppositories |
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Definition
- prescribes the dose for the pt. |
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Term
role of the pharmacists in compounding of suppositories |
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Definition
- determines the amt. of the base - preparation of the suppository |
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Term
2 things required when molding from a melt in preparing a suppository |
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Definition
- density calculations - mold calibrations |
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Term
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Definition
- different bases will have different densities - DO PRACTICE PROBLEMS |
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Term
calculation for density factor |
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Definition
- density factor = wt. of drug/wt. of base displaced |
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Term
steps taken when doing a mold calibration |
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Definition
- determine the vol. of each cell in the mold by pouring the base into each cell and let it solidify; remove the bases from each cell and determine the total wt.; transfer all the solidified bases into a beaker; melt to get the vol.; calculate the wt. and vol. of each cell |
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Term
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Definition
- liquid preparations that contain one or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents - mixture of one substance dissolved in another |
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Term
classifications of solutions - based on use |
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Definition
- oral - otic - opthalmic - topical |
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Term
classification of solutions - based on composition |
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Definition
- syrups - elixirs - spirits/aromatic water - tinctures/fluid extracts - injections |
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Term
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Definition
- aqueous solutions containing a sugar - can be vehicles without drug or liquid dosage forms with the drug |
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Term
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Definition
- sweetened hydroalcoholic solutions - no aromatic materials |
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Term
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Definition
- solutions of aromatic materials - spirits have a OH solvent - aromatic water has a aqueous solvent |
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Term
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Definition
- solutions prepared by extracting active constiuents from crude drugs - tinctures are when w:v is either 1:4, 1:5, or 1:10 - fluid extracts are when the w:v is 1:1 only |
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Term
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Definition
- solutions prepared to be sterile and pyrogen free and intended for parenteral administration |
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Term
how can you define high solubility |
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Definition
- highest dose strength (of drug substance) is soluble in 250mL or less of aqueous media over the pH range of 1-7.5 |
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Term
how can you define high permeability |
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Definition
- when the extent of absorption in humans is 90% or more |
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Term
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Definition
- max equilibrium amt. of solute that can dissolve per amt. of solvent |
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Term
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Definition
- kinetic phenomenon - amt. of solute dissolved per unit time |
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Term
6 techniques to improve the solubility or the dissolution rate |
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Definition
- slat form - particle size - amorphous form - temperature (increased temp. = increased solubility in liquid dosage forms) - rigorous agitation in liquid dosage forms - pH |
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Term
5 types of solvents used for liquid preparations |
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Definition
- alcohol, USP - diluted OH - rubbing OH - isopropyl rubbing OH - purified water, USP |
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Term
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Definition
- most useful solvent next to water - forms hydroalcoholic mixture with water - 94.9%-96% C2H5OH by vol. - ethyl OH, ethanol |
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Term
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Definition
- contains not less that 99,5% C2H5OH by vol. |
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Term
Recommended OH content for OTC oral products |
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Definition
- <6yrs. = 0.5% or less - 6-12yrs. = 5% or less - >12 yrs. = 10% or less |
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Term
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Definition
- equal volumes of OH, USP and purified water, USP - final volume is less than initial because OH contracts upon mixing |
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Term
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Definition
- 70% C2H5OH - rubefacient - disinfectant - denaturant employed is formula 23-H - separation of ethyl OH becomes virtually impossible when it is added - by adding denaturant you are discouraging use of rubbing OH as beverage |
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Term
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Definition
- 70% IPA by vol. - rubefacient - disinfectant |
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Term
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Definition
- any agent that increases the redness of skin |
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Term
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Definition
- obtained by distillation, ion exchange tx, reverse osmosis, etc - should not yield more than 0.001% of residue - for aqueous dosage forms - not for parenteral administrations (including injections) |
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Term
dry mixtures for solution |
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Definition
- some medicinal agents will have insufficient stability in aq. sol'n to meet extended shelf life periods "antibiotics" - commercial manufacturers provide these products to the manufacturer in dry form "drugs to be reconstituted" |
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Term
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Definition
- concentrated aq. preparations of a sugar or sugar substitute with or without flavoring agents and medicinal substances |
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Term
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Definition
- medicated syrups - non-medicated syrups (flavored vehicles) |
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Term
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Definition
- purified water - medicinal agents - sugar (usually sucrose or sugar substitute) - antimicrobial preservatives - flavorants - colorants - may contain some other excipients |
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Term
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Definition
- sugars that are converted to glucose in the body |
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Term
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Definition
- nonglycongenetic substances (ideal for diabetic pt.) - ex: methyl cellulose or hydroxy ethylcellulose |
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Term
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Definition
- physical concealment of the taste of the drug - inherent stability - make them viscous by adding 60-80% of sugar |
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Term
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Definition
- resistant to microbial growth b/c of the unavailability of the water req. |
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Term
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Definition
- sweetened hydroalcoholic sol'n intended for oral use |
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Term
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Definition
- nonmedicated elixirs (vehicles) - medicated |
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Term
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Definition
- have less sugar than syrups - less viscous than syrups but not more susceptible to microbial - elixirs are less effective in masking the taste - elixirs are capable of dissolving both water-soluble and water-insoluble - elixirs cannot be used in kids and adults who choose to avoid OH |
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Term
2 principle methods of drug extraction |
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Definition
- maceration - percolation |
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Term
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Definition
- comminuted drug is allowed to soak in a solvent until the cellular structure is softene and penetrated by the solvent - i.e. tea bag in a cup of water - immobile |
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Term
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Definition
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Term
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Definition
- mobile (i.e. coffee maker) - drug extraction by slow passage of a suitable solvent through a column of the drug |
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Term
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Definition
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Term
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Definition
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Term
what are dispersed systems |
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Definition
- drug is undissolved or immiscible - "dispersion" |
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Term
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Definition
- drug dispersed - solute in liquid dosage |
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Term
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Definition
- solvent - dispersion medium - continuous phase |
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Term
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Definition
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Term
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Definition
- size is greater than 500 nm |
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Term
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Definition
- suspensions - emulsions - gels and magmas - aerosols |
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Term
suspensions (dispersions) |
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Definition
- coarse dispersions containing finely divided insoluble material suspended in a liquid medium (particle size usually > 0.5 micrometers) |
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Term
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Definition
- liquid drug dispersed in liquid - system consisting of at least two immiscible liquid phases - study slide |
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Term
gels and magmas (dispersions) |
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Definition
- very fine particles dispersed in liquid but liquids are made semisolid |
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Term
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Definition
- solid or liquid drug is dispersed in gaseous medium |
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Term
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Definition
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Term
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Definition
- powder form and drug must be reconstituted using a suitable solvent |
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Term
why do we need suspensions |
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Definition
- some drugs are unstable in sol'n but stable when formulated as suspension - suspensions are better at masking taste - ease of swallowing - flexibility of administration of a range of doses |
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Term
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Definition
- dx/dt=d2(pi-pe)g/18n - study slides |
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Term
how do you prevent formation of cake |
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Definition
- intentional formation of a less rigid or loos aggregation of partiles - "floc" - "floccule" |
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Term
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Definition
- process of intentional formation of a less rigid or loose aggregation of the particles - dispersed particles come together but do not fuse |
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Term
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Definition
- agents used to prepare flocculated suspensions |
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Term
examples of flocculating agents |
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Definition
- clays such as diluted betonite magma |
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Term
problems with highly flocculated suspensions |
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Definition
- rapid settling - unsightly a supernatant layer - both of the above occur if large amt. of flocculating agents added |
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Term
how cam problems that occur due to highly flocculated suspensions be overcome |
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Definition
- adding suspending agents to the disperions medium - high viscosity of dispersion medium ("vehicle") - ex: acacia, methyl cellulose, carboxymethylcellulose |
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Term
what is extemporaneous compounding |
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Definition
- used in kids/adult who cannot swallow solid dosage forms |
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Term
why should you not use preservatives, colorings flavorings, or OH in extemporaneous compounding |
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Definition
- because they may have acute or long-term side effects for neonates (newborn <4wks old) |
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Term
why should you use extreme caution with benzyl OH for neonates in extemporaneous compounding |
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Definition
- because liver does not metabolize benzyl OH and benzyl OH causes gasping syndrome (condition which leads to multiple organ failure) |
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Term
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Definition
- oil in water emulsions (o/w) - water in oil emulsions (w/o) |
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Term
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Definition
- added to prepare a stable emulsion - ex: acacia, tragacanth, and gelatin |
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Term
3 most prevalent theories of emulsification |
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Definition
- surface tension theory (emulsifiying agents act to decrease interfacial tension) - oriented-wedge theory - plastic or interfacial film theory |
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Term
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Definition
- forces bt molecules of same liquid that prevent breaking down into small substances |
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Term
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Definition
- hydrophilic-lipophilic balance - emulsifying agents can be categorized by HLB - ranges from 1-40 - high HLB # = o/w - low HLB # = w/o |
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Term
tree methods used for small-scale extemporaneous preparation of emulsions |
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Definition
- continental or dry gum method - english or wet gum method - bottle or Forbes bottle method |
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Term
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Definition
- oil:water:gum - for every 4 parts oil added, 2 parts water are added and one part gym added - used in the preparation of initial or primary emulsion |
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Term
steps for dry gum emulsion preparation |
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Definition
- gum is triturated with oil until thoroughly mixed - two parts of water are added all at once - end point - creamy white and crackling sound - STUDY SLIDE |
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Term
wet gum (english) method for preparation |
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Definition
- smae proportions of oil, water, and gum except order of mixing is different (water added before oil) - mucliage prepared by triturating gum with ater - oil is added slowly in portions |
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Term
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Definition
- dispersed particles come together, fusion of particles take place and leads to the decrease in number of particles |
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Term
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Definition
- upward movement of the dispersed droplets relative to the continuous phase |
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Term
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Definition
- downward movement of the dispersed droplets relative to the continuous phase |
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Term
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Definition
- complete separation of the internal phase from the continuous phase and formation of internal phase as a separate layer |
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Term
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Definition
- an emulsion is said to be invert when it changes from an o/w to a w/o emulsion or vice versa |
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Term
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Definition
- semisolid systems consisting of either suspensions made up of small inorganic particles or large organic molecules interpenetrated by a liquid |
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Term
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Definition
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Term
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Definition
- "magma" - the gel contains small discrete particles |
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Term
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Definition
- gel does not appear to have discrete particles |
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Term
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Definition
- "reversible gel-sol phenonmenon" - some gels become fluid on agitation, only to resume their solid or semisolid state after remaining undisturbed for a period of time |
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Term
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Definition
- taking up of certain amt. of liquid without a measurable increase in vol. |
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Term
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Definition
- taking up of liquid by a gel with an increase in vol. |
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Term
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Definition
- when a gel stands for some time, it may shrink naturally and some of the liquid is pressed out |
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Term
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Definition
- formed when the liquid is removed from a gel and only frame work remains |
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Term
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Definition
- study of flow - addresses the viscosity and flow properties of powders, fluids, and semisolids |
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Term
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Definition
- newtonian flow - non-newtonian flow |
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Term
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Definition
- characterized by constant viscosity, regardless of shear rates applied - STUDY SLIDES |
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Term
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Definition
- fail to follow newton's eq. - plastics - pseudoplastic - dilatant |
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Term
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Definition
- higher viscosity than newtonian fluid - substances that exhibit plastic flow are called bingham bodies - plastic flow does not begin until a shearing stress corresponding to a certain yield value is exceeded - STUDY SLIDES |
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Term
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Definition
- begins when a shearing stress is applied - STUDY SLIDE |
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Term
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Definition
- exhibit an increase in resistance to flow with increasing rates of shear - STUDY SLIDE |
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Term
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Definition
- pressurized dosage forms that upon actuation emit therapeutic ingredients as a fine dispersion of a liquid or solid material in a gaseous medium |
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Term
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Definition
- rapid onset of action - avoid hepatic first pass metabolism - most of contents used are hemetic (airtight) therefore are protected from degredation by oxygen or humidity |
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Term
steps in filling aerosols |
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Definition
- determine what aerosol container will be made of - add product (drug and other excipients) - fit valve - add propellant - fit actuator |
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Term
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Definition
- dosage form that enters body other than GIT - injections - sterile (free from microorganisms) |
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Term
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Definition
- most common parental - sterile - pyrogen-free - preaparations intended to be admin. parenterally |
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Term
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Definition
- substances that induce fever |
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Term
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Definition
- rapid onset of action bc drug injected directloy into the blood - for pts. who are uncooperative or unconscious - when drugs are ineffective by other routes |
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Term
disadvantages of parentals |
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Definition
- drugs cannot be retrieved - req. trained personnel in most cases |
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Term
routes of parenteral administration |
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Definition
- intra-articular (joints) - intrasynovial (joint-fluid area) - intraspinal (spinal column) - intrathecal (spinal fluid) - intra-arterial (arteries) - intracardiac (heart) |
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Term
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Definition
- stainless-steel or AL devicesthat penetrate the skin for the purpose of admin. a parenteral product |
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Term
parts of hypodermic needles |
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Definition
- bevel (needle tips - slanting edge) - shaft or barrel (long portion of needle) - hub (connects to syringe) - needle gauge (gauge number on hub) |
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Term
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Definition
- outside diameter of the needle shaft - larger the number = smaller diameter |
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Term
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Definition
- range from 1/4 to 6 inches - choice of needle length depends on the desired penetration |
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Term
two types of hypodermic needle physical hazards |
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Definition
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Term
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Definition
- minor complication resulting from a vein injury or irritation |
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Term
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Definition
- formation of a blood clot in a vein or artery |
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Term
intravenous route of admin for parentals |
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Definition
- provides rapid action compared with other routes of admin b/c injected directly into blood and solubility, dissolution, and absorption are not factors |
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Term
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Definition
- less rapid bc drug has to absorbed into the blood from the muscle - longer lasting |
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Term
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Definition
- liquid preparations that are substances or sol'n directly injected into the human body |
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Term
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Definition
- dry solids that depend on the add'n of suitable vehicles |
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Term
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Definition
- must be dissovled in emulsion mediums |
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Term
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Definition
- liquid preparation of solid suspended in a suitable liquid medium |
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Term
for injectable suspension |
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Definition
- dry powders, solids, etc. that upon add'n of suitable vehicle yields preparatio conforming in all respects to injectible suspensions |
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Term
oleaginous and suspensions relationship to injections |
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Definition
- types of injections that are restricted to types other than intravenous bc interrupts normal blood flow |
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Term
formulation of parentals for a drug unstable in sol'n |
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Definition
- prepare dry product - formulate as suspension |
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Term
formulation of parenterals if drug is unstable in water |
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Definition
- use non-aq. solvent (i.e. vegetable oils) |
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Term
formulation of parenterals if an aq. sol'n is desired |
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Definition
- use water-soluble solid form |
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Term
solvents and vehicles for injections |
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Definition
- water for injections, USP - sterile water for injection, USP - bacteriostatic water for injection, USP - sodium chloride injection, USP - bacteriostatic sodium chloride injection, USP - nonaq. vehicles |
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Term
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Definition
- purified by distillation or by reverse osmosis - presence of total solids - NMT 1mg/100mL - not req. to be sterile , it must be pyrogen free bc used for a large scale manufacture of injections |
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Term
sterile water for injection, USP |
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Definition
- designated solely for parenteral use only after add'n of drugs that req dilution or must be dissolved in an aq vehicle prior to injection - packaged in single-dose containers not larger than 1L - no antimicrobial agent |
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Term
bacterostatic water for injection, USP |
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Definition
- sterile water for injection containing one or more antimicrobial agents - flexibility for multiple dose vials - packaged in prefilled syringes or in vials containing NMT 30mL - used in parenterals that are admin in small vol. b/c do not want to admin. large amt. of antimicrobial agents into blood - USP labeling req. = NOT FOR USE IN NEONATES - limited detoxification capacity of the neonate liver for benzyl OH - benzyl Oh poisoning - gasping syndrom (multiple organ failure) |
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Term
which solvents and/or vehicles for injections are isotonic with blood |
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Definition
- sodium chloride injections - bacteriostatic sodium chloride injections |
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Term
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Definition
- used when drug has limited aq. solubility or when drugs are subject to hyrolysis - fixed vegetable oils, glycerin, PEGs, propylene glycol - oleaginous injections are mostly admin intramuscularly bc interrupt blood flow |
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Term
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Definition
- destruction of all living organisms and their spores or their complete removal from the prepation - dry heat - steam - filtration - gas - ionizing radiation |
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Term
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Definition
- usually carried out in oven - b/t 150-170 degrees C |
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Term
if chemical X melts or decomposes at 170degrees C but is un affected at 140 degrees C, what steps should be taken? |
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Definition
- decrease temp, but increase exposure time |
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Term
what is one of the important factors responsible for dug degradation |
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Definition
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|
Term
dont you tink 150 or 170 is too high for certain pharmaceutical prodcuts |
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Definition
- yes - therefore use steam because microorganisms are destroyed at much lower T |
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Term
what is the highest T steam can acieve |
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Definition
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|
Term
what if you need a T of 110 to destroy microorganism |
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Definition
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|
Term
methods of steam sterilization |
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Definition
- autoclave - employs steam under pressure in order to increase T - it sis the T, not the P, that destroys the microorganism |
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Term
sterilization by filtration |
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Definition
- physical removal of microorganism by adsorption on the filter medium - used for heat sensitive sol'ns - milipor filters (most commonly used for filtrations) |
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Term
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Definition
- exposure to ethylene oxide or propylene oxide gas |
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Term
sterilization by ionizing radiation |
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Definition
- sterilization by gamma rays and by cathode rays |
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Term
three types of properties of drug molecules |
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Definition
- additive - constitutive - colligative |
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Term
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Definition
- properties that depend on the total contribution of atoms in the molecule or on the sum of properties of the constituents in soln' |
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Term
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Definition
- properties that depend on the arrangement of atoms in a molecule |
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Term
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Definition
- properties that depend primarily on the number of particles in sol'n - lowering of v.p - increase in bp - decrease in freezing point - osmotic pressure - STUDY SLIDES |
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