Abstract
Mercaptopurine is a purine antagonist, belonging to the class of antimetabolites. Its oral absorption is erratic and variable throughout GIT, with bioavailability of 5-37% and belongs to Biopharmaceutical Classification System (BCS) class IV. The focus of the present study was to improve solubility of mercaptopurine and to release the drug uniformly throughout the GIT by formulating into a novel in situ gel tablet. By in vitro swelling studies, xanthan gum was selected as the best gelling polymer and the tablets were prepared by direct compression. Sodium chloride was used as a release modifier to improve the release of drug from the tablet. A 32 full factorial design was applied to optimize the percentage of xanthan gum and sodium chloride to get desired swelling index and release profile. Tablets were evaluated for weight variation, hardness, friability, disintegration time, drug content, in vitro swelling studies and in vitro dissolution studies. The best optimized formulation showed good swelling index and extended the release up to 12 h, where as conventional tablet released the drug within 45 min. The results indicate that mercaptopurine loaded in situ gel tablet could be effective in sustaining drug release for a prolonged period of time throughout the GIT, which can possibly improve the oral bioavailability.
Highlights
Mercaptopurine (6-MP) is a highly insoluble purine antagonist and belongs to the class of antimetabolites and is well known for its antitumor activity. It belongs to Biopharmaceutical Classification System (BCS) class IV
The optimized formulation was prepared to study the effect of tablet shape and compression force on invitro release and swelling index
The powder blend was compressed on Rimek MINI PRESS-II SF (Karnavati) using oval punch size of 9.4 x 5.6 mm under different compression forces at 2000 kg (2 kg/cm2), 3000 kg (3 kg/cm2), 4000 kg (4 kg/cm2) and 5000 kg (5 kg/cm2)
Summary
Mercaptopurine (6-MP) is a highly insoluble purine antagonist and belongs to the class of antimetabolites and is well known for its antitumor activity. It belongs to BCS class IV (poor solubility and poor permeability). By formulating into sustained release (SR) dosage form the above potential problems associated with drug can be overcome (Singh et al, 2012). The most commonly used method for fabricating drugs in a SR formulation is by incorporating them into a matrix containing a hydrophilic rate-controlling polymer. Matrix systems are widely used in oral controlled drug delivery because of their simplicity in manufacturing processes, level of reproducibility, stability of the raw materials and dosage form (Gennaro, 2000)
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