Abstract

DESIGN AND DEVELOPMENT OF ORAL DOSAGE FORM FOR COLON SPECIFIC DRUG RELEASE OF INDOMETHACINE

Kondapuram Parameshwar*, Sajal Kumar Jha and Monica Diyya

ABSTRACT

Rheumatoid arthritis are severe in early morning hours, so an attempt has been made to overcome the problem by delaying drug release by colon targeting to maintain peak plasma concentrations in early morning hours. Indomethacin, a non-steroidal anti- inflammatory drug effectively used for treatment of inflammation and pain caused by rheumatoid arthritis, was selected as a model drug. Indomethacin has a plasma half life of 4.5hr. Its administration rate is frequent due to its short half life. The aim of this study was to develop a pulsincap containing Indomethacin microsponges to relieve pain and inflammation caused by rheumatoid arthritis in early morning hours by colon targeting and also to reduce the gastric irritation. Development of calibration curves, Preparation of indomethacin microsponges, Determination of drug content & encapsulation efficiency, Fourier transform infra red spectroscopy Development of pulsincap dosage forms Five batches of microsponge formulations containing different ratios of Indomethacin and ethyl cellulose [F1(1:1), F2(1.5:1), F3(2:1), F4(1:1.5) and F5(1:2)] were prepared and parameters like practical yield, percentage of drug content and percentage of encapsulation efficiency of microsponges were evaluated. 8%w/v Ethyl cellulose solution was ideal for coating of body of the pulsincap, as the percentage change of weight was minimum. The prepared gelatin hydrogel plugs were full and half coated with different concentrations of enteric polymers. Half enteric (10% CAP, 10% HPMCP, and 10% EUDRAGIT L-100) coated hydrogel plugs were selected for development of pulsincap in respect to its maximum swelling ratio shown in pH 6.8 compared to the full enteric coated hydrogel plugs. In-vitro release studies were carried out for formulated pulsincaps. The release studies indicate that all the dosage forms released the drug uniformly with out any significant difference. The drug release from the pulsincap dosage forms was started after 6hrs lag time. It has been concluded from the above investigation that pulsincap dosage form of Indomethacin could delay the release up to 6hrs and further exhibited controlled release of the drug for 18hrs.Hence it is suitable for the treatment of pain and inflammation caused by Rheumatoid arthritis in early morning hours.

Keywords: colon targeting, microsponges, ethyl cellulose, pulsincap dosage forms, hydrogel plugs.