Case study 1 : Novel approach for development of poorly soluble drugs

• Situation : BCS Class II API (Low Solubility, High Permeability) with two known polymorphs to be developed in extended release Solid Dosage Form
• Challenges : Conventional Approach to use a combination of IR and SR granules. Use of surfactants in IR and SR, along-with coating of SR pellets with ethyl cellulose as polymers resulted in lot to lot variation in dissolution, poor polymorph stability and as also major process development issues
• Ipca Solution
  • Use of Solid Dispersion technique wherein drug precipitated along-with low viscosity HPMC. This resulted in drug available in “solution state” within polymer and improved solubility considerably in gastric fluid models
  • Use of PEG based polymers to help wetting of API (improved dissolution) as well as reduce polymorphic transitions within the product. Use of PEG based polymers hitherto not evaluated/documented for the API in consideration
• Result : Development of a stable extended release profile for the API, with a process that is inherently simpler and quicker to operate at plant