solubility enhancement strategies

• What is the pharmaceutical problem posed by poor solubility?

  It leads to low and variable absorption
• What percentage of marketed drugs have low aqueous solubility?

  40%
• What is a common issue in pharmaceutical drug development?

  High lipophilicity
• What is the absorption characteristic of Piroxicam?

  Low variable
• What are Brick Dust and Grease Balls in terms of solubility?

  Brick Dust is poorly soluble; Grease Balls are soluble
• What are the strategies to enhance solubility?

  • Manipulation of pH
  • Salt formation
  • Crystal engineering
  • Particle engineering
  • Co-solvency
  • Solid dispersions
  • Surfactant solubilisation
  • Prodrug
  • Drug derivation
  • Lipid-based formulations
  • Inclusion complexes
  • Emerging strategies
• How does adjusting solution pH affect drug solubility?

  It increases the proportion of ionised form
• What percentage of drugs are weak bases?

  75%
• What is the role of pharmaceutical salts in solubility?

  They dissociate in water to alter pH
• Why are different salt forms not considered equivalent by regulatory agencies?

  They have different physicochemical properties
• How does salt formation affect drug solubility?

  It can increase or decrease solubility
• What is the common counterion for oral delivery with the highest percentage?

  Sodium
• What is the common ion effect?

  It suppresses drug solubility through ions
• What are the side effects of ferrous salts?

  Constipation, heartburn, abdominal pain, nausea
• What are the advantages and disadvantages of salt formation?

  Advantages:

  • Altered solubility and dissolution
  • Controlled release
  • Improved stability
  • Enhanced permeability
  • Improved organoleptic properties

  
  

  Disadvantages:

  • Only ionisable drugs
  • Decreased % active
  • Salt corrosion
  • Additional processing step
• What is crystal engineering?

  Design and control of molecular packing in crystals
• What type of forces are involved in bonding within a crystal?

  Van der Waals forces, hydrogen bonding, ionic interactions
• How does polymorph selection influence drug properties?

  It affects dissolution, solubility, and absorption
• What are co-crystals?

  Mixed crystals of two or more molecular species
• What is the role of co-solvents in drug formulation?

  They increase solubility of poorly soluble substances
• What is a common co-solvent used in parenteral delivery?

  Propylene glycol
• What is a significant risk of cosolvent-based formulations?

  Drug precipitation during administration
• What are surfactants?

  Ampiphilic substances with hydrophilic and hydrophobic parts
• How do surfactants enhance solubility?

  By reducing interfacial tension between phases
• What role do hydrophobic interactions play in drug-receptor interactions?

  They mediate many receptor interactions
• What are the implications of high lipophilicity in drug development?

  It complicates drug formulation and absorption
• What is the significance of particle engineering in solubility enhancement?

  It helps overcome solubility limitations
• What are the potential side effects of ferrous sulphate?

  Constipation, heartburn, abdominal pain, nausea
• Why is it important to understand the physical properties of pharmaceutical salts?

  They influence solubility and drug formulation
• What is a risk associated with parenteral products?

  Increased risk of mechanical and chemical irritation
• What serious systemic effect can occur from parenteral products?

  Pulmonary embolism
• What is a common cosolvent used in oral delivery?

  Propylene glycol
• What is the formulation type for Emtricitabine?

  Liquid dosage form
• What is the molecular weight of ethanol?

  46 Da
• What is the LogP value of propylene glycol?

  -1.1
• What is a potential side effect of using cosolvents orally?

  Pharmacological side effects
• What can happen if cosolvent-based formulations are diluted too quickly?

  Drug precipitation may occur
• What do micelles do in drug solubilisation?

  They allow water-insoluble substances to dissolve
• What is the role of Cremophor® EL in parenteral formulations?

  It acts as a surfactant
• Why are non-ionic surfactants preferred in parenteral formulations?

  They are less likely to cause hypersensitivity reactions