Section 1
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Sweetening Agents: sucrose
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Date created
Mar 1, 2020
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Section 1
(50 cards)
Sweetening Agents: sucrose
Advantages: Colourless, highly water soluble, stable over a wide pH range (4- 8), increase the viscosity, masks both salty and bitter taste, has soothing effect on throat
Sweetners
- Non-nutritive, synthetic sweetening agents - Saccharin sodium : 300 - 550 time as sweet as sucrose - Concentration of 0.1 to 0.2%, bitter after taste - Aspartame • Cyclamate
Factors affecting drug solubility
- Particle size - Solvents - Additives - Solvent polarity - Drug polymorphism - Temperature
Sweetening Agents: Polyhydric Alcohols
(sorbitol, mannitol and glycerol) - can be used for diabetic preparations
Solution by Chem. Rxn
Prepared by reacting two or more solutes in a suitable solvent
Improving Sol.: Physical Modifications
- size reduction - mod of crystal habit - drug dispersion in carriers
Viscosity Enhancers
Increase residence time e.g. oral gels, eye drops, on skin.
Ethanol
useful as a preservative Relatively high concentration (> 10%) to be effective
Components of Syrups
- Sugars or sugar substitutes - Antimicrobial preservatives - Flavorants - Colorants - Special solvents, stabilizers, solubilizing agents and thickeners
Prep. of Syrup: Addition of sucrose to medicated liquid
- Used for fluid extracts, tinctures,- Contain alcohol soluble agents - Syrups made in this way may develop precipitates ( alcohol and sugar ) - Not suitable when the precipitated ingredients are the valuable medicinal agents
Advantages of Solutions
-Easier to swallow - Quicker absorption than tablets and capsules - Homogenous - give uniform dose (suspension or emulsion need shaking) - Minimize irritant action of some drugs (aspirin, KCl) in GIT
The USP/NF expresses the solubility in terms of...
volume of solvent required to dissolve 1 gram of the drug at a specified temperature
Glycerin
- clear syrupy liquid with sweet taste - miscible w/ water and alcohol - excellent solvent for tannins, phenol, and boric acid - preservative qualities
Body Cavities Sol.:
Eye/ear drops, nasal sprays, enemas
Tonicity Modifiers
- Solutions for injection - Application to mucous membrane - Large-volume solutions for ophthalmic application - Dextrose and sodium chloride
Invert sugar
- more readily fermentable than sucrose - tend to darken in color - retard the oxidation of other substances - Levulose : sweeter than sucrose, so the resulting syrup is sweeter than the original syrup.
Water
- used as a vehicle and solvent for medicinal agents, flavoring agents -Microbial growth when contaminated - Favorable medium for chemical reactions
Acetone
miscible with water, alcohol, ether, chloroform and most of the volatile oils
Mouth and Throat Sol.:
Mouth washes, gargles, throat sprays
Solution by Extraction
Plant/animal products - prepared by suitable extraction process.
Colorant
Water soluble, non-reactive Correlating with flavor
Propylene Glycol, Polyethylene glycol 400
miscible with water, acetone, alcohol and other glycols
Acids
- Benzoic acid and sorbic acid - low solubility in water -only non-ionized form is effective - use restricted to preparations with a pH below 4.5
Alcohol
good solvent for many organic substances
Syrups
Concentrated aqueous preparations of a sugar or sugar-substitute with or without flavoring agents & medicinal substances
Sugar-Based Syrups
Contains sucrose / cane sugar - Glycogenetic - Sorbitol or Glycerin may be added to prevent crystallization of sucrose
Antimicrobial Preservatives
Important when concentration of sucrose in syrup is low. Amount varies with proportion of water available for microbial growth.
Preservaties should be
1. Effective against a wide spectrum of microorganisms 2. Compatible with the ingredients in the dosage form 3. Stable for its shelf life 4. Non toxic, non sensitizing 5. Free of taste and odor
Pharmaceutical Solutions
Liquid pharmaceutical formulations that contain one or more active ingredients dissolved in a suitable solvent or mixture of miscible solvents
Solution Components
-Drug - Solvents - Additives: - Solubilizing agents - Preservatives - Sweetening agents - others
Flavorant
Water soluble Volatile oils, vanilin
Additives in solutions
1. Preservatives 2. Antioxidants 3. Sweetening agents 4. Buffers 5. Tonicity modifiers 6. Viscosity enhancers 7. Flavorants & Colorant
Antioxidants
Drugs, vitamins, essential oils & fats - susceptible to oxidation propyl & octyl esters of gallic acid, tocopherols or vitamin E, sodium sulfite, ascorbic acid (vit. C)
Oral Sol.:
syrups, elixirs, drops
Simple Solution
Dissolve (by stirring or heating) - Other ingredients to stabilize or solubilize the active ingredient
Chloroform
miscible with alcohol, ether, benzene, hexane and both fixed and volatile oils
Oxidation reaction can be initiated by
1. heat 2. light: use of light- resistant container 3. heavy metals (e.g. Fe, Cu): effect minimized by using citric acid or ethylenediamine tetraacetic acid (EDTA) i.e. sequestering agent.
Characteristics of Syrups
Masks taste: - Sweetener & flavorant - Viscosity : only portion of drug in contact with taste buds - Soothing effect on irritated tissue - Antitussive syrups High proportion of sucrose - 60 to 80% - Sweetness, viscosity & stability
Prep. of Syrup: Agitation without heat
Heat sensitive components Time consuming, but avoids inversion
Improving Sol.: Chemical Modifications
Change of pH, use of buffer, complexation and salt formation.
Improving Sol.: misc.
Use of adjuvant like surfactant, use of cosolvents, solubilizers, supercritical fluid process and novel excipients
Topical sol.:
Collodions, lotions
Propylene glycol
solvent in oral solutions and topical preparations, not volatile like ethanol
Parabens
- esters (methyl, ethyl, propyl and butyl) of p-hydroxybenzoic acid - Widely used in pharmaceutical products - Effective and stable over a pH range of 3 to 8 - Frequently 2 esters are used in combination
Pharmacist's role in solution dosage form
- Extemporaneously compound a solution from bulk components - Reconstitute dry powder mixtures - Dilute concentrated solution - adult product to pediatric form - Dispense commercially prepared oral solution
Quat. Ammonium Compounds
Benzalkonium chloride - relatively low concentration 0.002 to 0.02% - Optimal activity over the pH range of 4 to 10 - Stable at most temperatures. -Incompatible with many anionic compounds due to their cationic nature
Disadvantages of Solutions
- Bulky - Need accurate spoon - Stability
3 Methods of Preparation
Simple solution Solution by Chem. rxn Solution by extraction
Prep. of Syrup: Solution w/Heat
- The sucrose is added to aqueous solution and heated until dissolved, then strained and sufficient purified water added to make the desired weight or volume - Inversion of sucrose - Excessive heating
Artificial sweeteners and non-nutritive syrups
- Formulated with artificial sweeteners and viscosity builders - Non glycogenetic - Diabetic / restricted diet patients
Section 2
(8 cards)