Development and evaluation of film coated aceclofenac and chlorzoxazone tablet with enhanced dissolution rate

摘要

Out of many complications two major problems facing in formulation industry are poor solubility and short half-life of drugs which results into poor bioavailability after oral administration. Solid dosage forms are coated for a number of reasons, the most important of which is controlling the release profiles and bioavailability of the active ingredient. Thus the development of a significant dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Aceclofenac (Biopharmaceutical classification Class II drug) is a novel non-steroidal anti-inflammatory drugs (NSAIDs) having anti-inflammatory and analgesic properties, and is widely used in the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. The investigation revealed that there is no official dissolution medium available in the literature. The objective of present study is to formulate film coated tablet of Aceclofenac and Chlorzoxazone having short half-life by coating with hydroxyl propyl methyl cellulose (E5 LV). Then the formulated tablets were evaluated for its physicochemical properties and in vitro release studies. The incorporation of drugs into polymer matrices is considered a valid tool in order to optimize insufficient features of the drug molecule, like solubility, stability or toxic effects. In the present work, the incorporation of aceclofenac was performed in inert HPMC and there was no chemical interaction between the drug and polymers as concluded from the FTIR studies. In the present study, parameters such as solubility, medium pH, surfactant type, dissolution behavior of formulations, stability, and discriminatory effect of dissolution testing in different dissolution mediums were studied for the selection of a proper dissolution medium. The drug showed an enhanced release rate in the dissolution media containing pH 6.8 phosphate buffer, 900 ml with 0.5 % sodium lauryl sulphate at 75 rpm for 60 min and thus was chosen as the discriminating dissolution method for film coated aceclofenac formulation. It was found that greater than 80 % of the label amount is released over 60 min.