Co-crystals: a novel approach to modify physicochemical properties of active pharmaceutical ingredients.

Abstract:

:Crystal form can be crucial to the performance of a dosage form. This is especially true for compounds that have intrinsic barriers to drug delivery, such as low aqueous solubility, slow dissolution in gastrointestinal media, low permeability and first-pass metabolism. The nature of the physical form and formulation tends to exhibit the greatest effect on bioavailability parameters of water insoluble compounds that need to be given orally in high doses. An alternative approach available for the enhancement of drug solubility, dissolution and bioavailability is through the application of crystal engineering of co-crystals. The physicochemical properties of the active pharmaceutical ingredients and the bulk material properties can be modified, whilst maintaining the intrinsic activity of the drug molecule. This article covers the advantages of co-crystals over salts, solvates (hydrates), solid dispersions and polymorphs, mechanism of formation of co-crystals, methods of preparation of co-crystals and application of co-crystals to modify physicochemical characteristics of active pharmaceutical ingredients along with the case studies. The intellectual property implications of creating co-crystals are also highly relevant.

journal_name

Indian J Pharm Sci

authors

Yadav AV,Shete AS,Dabke AP,Kulkarni PV,Sakhare SS

doi

10.4103/0250-474X.57283

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

359-70

issue

4

eissn

0250-474X

issn

1998-3743

journal_volume

71

pub_type

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