Interpolymer Complexation. II. Entrapment of Ibuprofen by In-Situ Complexation Between Polyvinyl Acetate Phthalate (PVAP) and Polyvinylpyrrolidone (PVP) and Development of a Chewable Tablet Formulation

Abstract

A new method involving in situ complexation between polyvinyl acetate phthalate (PVAP) and polyvinylpyrrolidone (PVP) has been developed for the entrapment of ibuprofen, a bitter tasting anti-inflammatory drug. The procedure involved dissolving ibuprofen in a thoroughly mixed aqueous alkaline solution of PVAP and PVP, and subsequently slowly adjusting the pH of the solution to 1 with dilute HCl. The yield of the entrapped product, and the percent entrapment of ibuprofen, were 85–90%, and 90–98%, respectively. The PVAP–PVP entrapped granules showed no bitter taste due to ibuprofen. The chewable tablets, prepared by mixing the granules with a cherry-flavored directly compressible tableting excipient, exhibited a release of less than 2% of ibuprofen in pH 1.2 buffer over a period of three hours. In pH 7.4, 100% of ibuprofen was released in six hours. The results presented show that in situ complexation between PVAP and PVP may be useful to produce palatable ibuprofen granules suitable for use in the development of chewable tablets.

Keywords:

• Polyvinyl acetate phthalate
• Polyvinylpyrrolidone
• Ibuprofen
• Palatable ibuprofen granules
• Polyvinyl acetate phthalate-polyvinylpyrrolidone complex