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Liquid Dosage Forms: Pharmaceutical Solutions

Unit 7 Module 11: Liquid Dosage Forms (LDFs)

Introduction to Liquid Dosage Forms (LDFs)

  • LDFs are pourable pharmaceutical formulations containing active drug components and non-drug components (excipients) dissolved or suspended in a suitable solvent or solvent mixtures.

  • Purpose: Designed to provide maximum therapeutic response for populations with difficulty swallowing solid dosage forms (e.g., pediatric, geriatric patients) and/or to produce rapid therapeutic effects.

  • Preparation Methods:

    • By dissolving the active drug substance in an aqueous or non-aqueous solvent (e.g., alcohol, ether, glycerin).

    • By suspending the drug in an appropriate medium.

    • By incorporating the drug substance into an oil or water phase.

  • Classification:

    • Monophasic LDFs

    • Biphasic LDFs

Pharmaceutical Solutions

  • Definition: Liquid preparations containing one or more soluble chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents.

  • Physicochemical terms: Solutions can be prepared from any combination of solid, liquid, or gas.

  • Characteristics: Homogenous mixture where solute molecules are dispersed in a solvent.

Types of Solutions

  1. Solid Solution (solvent is solid)

    • Solid in solid: Example: Copper in gold = 12 karat yellow gold.

    • Liquid in solid: Example: Mercury dissolved in silver = amalgam.

    • Gas in solid: Example: Air dissolved in soap = floating soap.

  2. Liquid Solution (solvent is liquid)

    • Solid in liquid: Example: Salt in water.

    • Liquid in liquid: Example: Alcohol and water.

    • Gases in liquid: Example: Carbonated beverages.

  3. Gaseous Solutions (solvent is gas)

    • Solid in gas: Example: Sulfur in air.

    • Liquid in gas: Example: Water vapor in air.

    • Gas in gas: Example: Oxygenated air.

Solubility

  • Expression: Grams of solute dissolving in milliliters of solvent.

  • USP Descriptive Terms of Solubility:

    • Very soluble: Less than 1 part of solvent required for 1 part of solute.

    • Freely soluble: 1 - 10 parts of solvent required for 1 part of solute.

    • Soluble: 10 - 30 parts of solvent required for 1 part of solute.

    • Sparingly soluble: 30 - 100 parts of solvent required for 1 part of solute.

    • Slightly soluble: 100 - 1,000 parts of solvent required for 1 part of solute.

    • Very slightly soluble: 1,000 - 10,000 parts of solvent required for 1 part of solute.

    • Practically insoluble or insoluble: More than 10,000 parts of solvent required for 1 part of solute.

Factors Affecting the Rate of Solubility

  1. Particle size: Reducing particle size (comminution) increases surface area, thus increasing the rate of solution.

  2. Agitation: Increases the rate of solution by removing the concentrated solution from the solute surface, allowing less concentrated solvent to interact.

  3. Temperature: Heating a liquid increases molecular collision frequency between solvent and solute, leading to a more rapid solution.

Factors Affecting Solubility of Solute

  1. Temperature:

    • Endothermic reaction: Heat is absorbed; an increase in temperature increases solute solubility.

    • Exothermic reaction: Heat is given off; an increase in temperature decreases solute solubility. Example: Methyl cellulose and calcium salts like ext{Ca(OH)}_2 are more soluble in cold water.

  2. Molecular Structure: