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Questions and Answers
What is a characteristic of solutions in liquid dosage forms?
What is a characteristic of solutions in liquid dosage forms?
Which of the following liquids is NOT typically classified as a monophasic liquid dosage form?
Which of the following liquids is NOT typically classified as a monophasic liquid dosage form?
Which of the following learning outcomes involves identifying inappropriate combinations during liquid dosage form preparation?
Which of the following learning outcomes involves identifying inappropriate combinations during liquid dosage form preparation?
Which factor is key in the formulation of liquid dosage forms when considering their stability?
Which factor is key in the formulation of liquid dosage forms when considering their stability?
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Which aspect of liquid dosage forms is specifically NOT concerned with the preparation of colloids?
Which aspect of liquid dosage forms is specifically NOT concerned with the preparation of colloids?
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What is a colloid primarily characterized by?
What is a colloid primarily characterized by?
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Which of the following best describes an emulsion?
Which of the following best describes an emulsion?
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What type of solution is classified as an oral solution?
What type of solution is classified as an oral solution?
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Which classification of solutions includes sweetened hydroalcoholic mixtures?
Which classification of solutions includes sweetened hydroalcoholic mixtures?
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What is a disadvantage commonly associated with solutions?
What is a disadvantage commonly associated with solutions?
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Study Notes
Liquid Dosage Forms
- Monophasic: Aqueous and non-aqueous solutions
- Polyphasic: Colloids, Suspensions, Emulsions
Pharmaceutical Solutions
- Homogenous mixtures of two or more substances
- Solute: Substance dissolved
- Solvent: Substance the solute is dissolved in
- Common example: Salt or sugar in water
Classification of Solutions
By Pharmaceutical Use (Route of Administration)
- Oral Solution: Taken through the mouth
- Otic Solution: Instilled in the ears
- Ophthalmic Solution: Instilled into the eye
- Nasal Solution: Instilled into the nose
- Topical Solution: Applied over skin surface
- Rectal and Vaginal Solutions: Enema and douche for rectal/vaginal administration
By Composition
- Syrups: Aqueous solutions with sugar
- Elixirs: Sweetened, hydroalcoholic (water & ethanol) solutions
- Spirits: Alcoholic or hydroalcoholic solutions of volatile substances
- Tinctures: Alcoholic or hydroalcoholic solutions prepared from vegetable materials or specific chemicals
By Solvent (Vehicle)
- Aqueous Solutions: Water as the solvent
- Non-Aqueous Solutions: Solvent other than water, like ether or benzene
Advantages of Solutions
- Easy to swallow for children and elderly
- Faster action compared to tablets, capsules, suspensions (Solutions > Suspensions > Capsules > Tablets)
- Uniform dose due to homogenous distribution of medication
- Dilute irritating effects of some drugs (e.g., KCl, aspirin)
Disadvantages of Solutions
- Unpleasant taste or odor difficult to mask
- Bulky to carry around
- Requires accurate measuring device for correct dosage -Poor stability for drugs in aqueous solution
- Suitable medium for microbial growth
Aqueous Solvents
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Water: Most common solvent in pharmaceuticals due to:
- Lack of toxicity
- Physiological compatibility
- Ability to dissolve a wide range of materials
Types of Water
- Tap Water: Suitable for drinking, contains dissolved & undissolved matter, including microorganisms
- Purified Water: Fewer solid impurities than tap water, suitable for pharmaceutical use
Factors Influencing Solubility & Stability in Solutions
- Chemical stability of a drug: Depends on pH, optimal solubility may not match optimal stability
- pH of Solutions: Parenteral and ophthalmic solutions need controlled pH to prevent pain and irritation
- Preservative activity: Affected by pH altering its ionization
- Concentration of co-solvents: Inclusion of alcohol or propylene glycol lowers dielectric constant of vehicle, increasing solubility of unionized drug
Methods to Improve Solubility
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Solubilization:
- Using surface active agents (SAAs) with an HLB value >15
- SAAs must be non-toxic, non-volatile, non-irritant, miscible with solvent, compatible with other ingredients, and free from disagreeable odor and taste
- Example: Polysorbates (Tweens) for fat-soluble vitamins
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Complexation:
- Interaction of poorly soluble drug with a soluble material to form a soluble complex
- “Hydrotropy”: Increase in aqueous solubility by adding additives
- Example: Iodine with 10-15% polyvinyl pyrrolidone (PVP) solution [BETADINE]
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Chemical Modification:
- Production of a water-soluble derivative of the drug
- Example: Chloramphenicol sodium succinate for parenteral administration (converted to active base)
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Particle Size Control:
- Decreasing particle size increases surface area leading to increased solubility
Non-Aqueous Solvents
- Used when drugs are poorly soluble or unstable in aqueous systems
- Depot Therapy: Intramuscular injection of solutions in oils creates a slow-release reservoir
Considerations Choosing Non-Aqueous Solvents
- Toxicity, irritancy, sensitization potential: Important for safety
- Flammability: Important for handling and storage
- Cost: A factor in manufacturing
- Stability: Ensuring the solvent doesn't degrade the drug
- Compatibility with other excipients: Ensuring the chosen solvent doesn't interfere with other components in the formulation
Some Non-Aqueous Solvents
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Alcohol, USP (Ethyl Alcohol, Ethanol):
- Widely used solvent in pharmacy
- Dissolves many organic compounds
- Together with water, forms hydroalcoholic mixtures for dissolving both alcohol-soluble and water-soluble substances
- Used for extraction of active constituents from crude drugs
- Alcohol, USP: 94.9-96.0% C2H5OH v/v
- Dehydrated Alcohol, USP: 99.5% C2H5OH v/v
Advantages of Alcohol as a Solvent
- Miscible with water
- Dissolves many water-insoluble ingredients (drugs, flavorants, antimicrobial preservatives)
- Used as a preservative alone or with parabens or benzoates
Disadvantages of Alcohol as a Solvent
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Undesired pharmacologic effects
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Potential toxic effects, particularly in oral use
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Content limit: FDA sets a maximum of 0.5% alcohol for OTC oral products intended for children under 12 years
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Diluted Alcohol: Equal volumes of alcohol and Purified Water, resulting in a final volume approximately 3% less than expected due to contraction upon mixing
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Alcohol, Rubbing: Approximately 70% ethyl alcohol by volume, with water, denaturants, color additives, perfume oils, and stabilizers
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Isopropyl Rubbing Alcohol: Approximately 70% isopropyl alcohol by volume, with water, color additives, stabilizers, and perfume oils, used for external use as rubefacient and vehicle
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Glycerin, USP (Glycerol): Clear, viscous liquid with a sweet taste, miscible with water & alcohol, comparable to alcohol as a solvent but slower due to viscosity, possesses preservative qualities
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Propylene Glycol: Viscous liquid, miscible with water and alcohol, widely used drug solubilizer in topical, oral, and injectable medications.
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Description
Test your knowledge on liquid dosage forms, including monophasic and polyphasic solutions. This quiz covers various pharmaceutical solutions based on their composition and route of administration, exploring examples and classifications in detail.