Oral delivery of poorly water soluble drugs

Question 1

Describe the current drug methodology (based on poorly soluble active ingredients)

Answer 1

current drug methodology produce candidate drugs of increasing molecular size and lipophilicity.
1. molecular motifs often derived from molecular modelling on receptor
2. molecular motifs derived from natural compounds
3. activity screens utilising solutions diluted from DMSO (dimethyl-sulphoxide stock) which can dissolve polar and non-polar compounds.

In order to improve the pharmacokinetic profile of the lead, it is optimized and this often leads to an increased molecular weight, high Log P value, and high melting point. All of which lead to poor drug solubility and permeability
4. PK lead optimization which increases molecular weight