ease of admin (for pediatric patients and others with difficulty swallowing)
ease of dosage adjustment (use oral syringe or other acceptable measuring device)
optimum bioavailability (dissolution step is bypassed, usually fastest and greatest extent of absorption)
inc feasibility with bulk powders
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Non-medicated or flavored syrups
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concen, aqueous vehicle containing a sugar or sugar-substitute
vehicles for medicated substances to be added during compounding
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Fluid Extract
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liquid prep of a vegetable drug which contains alcohol as a preservative, solvent, or both
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Medicated syrups
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syrup containing one or more therapeutci agents
water-soluble drug substances that are stable in aqueous solns can be formulated as medicated syrups
always check compatibility (esp if syrup contains other flavorants/colorants)
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Aromatic Water
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aqueous solution of a volatile/aromatic substance
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Tincture
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alcoholic or hydro-alcoholic soln prepared from vegetable material or a chem substance
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Solubility can be inc by
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chemical mod (use salt form to inc polarity)
co-solvency: inc hydrophobic characteristics of solvent in an aqueous soln through addition of a non-polar substance
use of a surfactant, which has hydrophillic-lipophillic character forming micelles of colloidal dimension - allows water and oil-soluble active agents to be formulated in a single phase
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Co-solvents
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decrease polarity
increase solubility of non-polar drugs
inc drug stability
little or no toxicity
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Non-medicated Elixirs
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sweetened, hydroalcoholic vehicles that can contain alcohol-soluble flavoring oils
Elixirs are less sweet and less viscous than syrups and, as a result, they are less effective at masking unpleasant tastes
lower sugar content
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Preservatives
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antimicrobials
antioxidants
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Advantages of Elixirs
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they can effectively dissolve both water-soluble and alcohol-soluble components
can be prepared by simple solution
many elixirs are self-preserving due to their ethyl alcohol content (>15%)
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Rate of solution can be inc by
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inc temp - rate of solution usually increase, and once the temp is returned to normal, solubility is unchanged
inc agitation - shake or stir the soln more vigorously so that contact btwn the solute and fresh solvent is inc
reduced particle size - use communition in a mortar and pestle to inc surface area of the solid to be dissolved
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Propylene glycol
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solvent
like glycerin: viscous, miscible with water and alcohol and an effective wetting agent
used as a glycerin substitue
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Antimicrobial preservatives
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benzoic acid (0.1-0.2%), sodium benzoate (0.1-0.2%), and combinations of methyl-, ethyl-, and propylparabens (0.1% total)
can be used to preserve the free water portions of syrups
ethyl alcohol is not present in concentrations high enough for preservation (15-20%)
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Glycerin
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solvent
also known as glycerol
Glycerin, USP is miscible with both water and ethyl alcohol
usually slowly soluble due to high viscosity (unless heated)
glycerin is viscous, sweet, and an effective wetting agent for some extemporaneously compounded preparations
has some preservative qualities
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Medicated Elixirs
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elixirs containing one or more therapeutic agents
water-soluble and alcohol-soluble drug substances that are stable in hydroalcoholic solutions can be formulated as medicated elixirs
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Spirit
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alcoholic or hydro-alcoholic soln of a volatile substance
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Oral Solutions
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solutions are liquid preparations that contain one or more chem substances dissolved in a suitable solvent or mixture of mutually miscible solvents
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Pharmaceutical ingredients
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excipients
are employed in oral solutions for color, sweetness, flavor, and as buffers and preservatives
solubility and stability data for the drug substance and pharmaceutical ingredients in the solvent of solvents are esp important for formulation or oral solutions
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For elixir preparation
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add water solution to alcoholic solution to prevent separation
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Sucrose Syrups
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Syrup, NF contains eighty-five percent sucrose, also known as simple sugar
most syrups contain sucrose as the sweetener because it gives both a sweet taste and high viscosity
Syrup, NF does not require a preservative because it is so concentrated that there is not enough "free water" available to support microbial growth
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Powders or granules for oral solution
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unstable drug substances may be formulated as powders or granules for reconstitution
inc shelf-life
usually stable for 7-14 days once reconstituted
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Disadvantages of Solutions
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not all drugs are stable in solution
not all drugs are soluble in a solvent fit for human consumption
subject to compliance, or patients admin, errors
bad taste
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Syrups usually contain
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purified water, sugar or sugar substitiute, antimicrobial preservatives, flavorants and colorants
may also contain other solvents (alcohol), stabilizers, and/or thickeners
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Ethyl Alcohol
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solvent
also known as ethanol
Alcohol, USP is between 94.9 and 96%
Dehydrated Alcohol, USP contains not less than 99.5% of ethanol
Diluted alcohol, NF is made from equal volumes of Alcohol, USP and Purified Water, USP
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Elixir
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sweetnened hydro-alcoholic solution
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Syrups
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aqueous solution containing high concen of sugar
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Buffers
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adjust pH for optimum stability or for inc solubility
dec irritation
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Water
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solvents
Purified Water, USP is most often used pharmaceutical solvent
Purified water must not contain more than 0.001% of dissolved and un-dissolved solids
ordinary drinking water (tap) not acceptable for manufacture or compounding of pharmaceutical preparations
most commonly available as distilled water
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Non-sucrose syrups
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in addition to sucrose, other sugars such as dextrose (glucose) or sugar substitutes such as sorbitol, glycerin, or propylene glycol may be used
thickening agents (methylcellulose) may be added to artificially sweetened vehicles to increase viscosity for use in diabetic patients