Formulation optimization and evaluation of aceclofenac sustained release dosage form based on Kollidon sustained release

Abstract

S ustained release aceclofenac matrix tablets constituting Kollidon sustained release (KSR) (polyvinyl acetate and povidone-based matrix retarding polymer) were developed in this study in an attempt to design a dosage form that manifests desirable release profile and thorough adherence to official monographs. Nine matrix tablet formulations were prepared by dry blending and direct compression method by varying the proportion of KSR and compression load with fixed percentage of aceclofenac. Among this, by comparing response variables of the prepared formulations with that of the marketed product, two formulations (KSR5 and KSR7) were chosen as the optimized formulations. The formulation showed close resemblance to commercial products and compliance with United States Pharmacopoeia USP specification. The exponential model was applied to characterize the drug release behavior from polymeric systems. It was found that non-Fickian release is predominant in tablets containing KSR with a trend toward zero-order kinetics. The study also involves in vivo evaluation of the optimized formulations to find out relevant pharmacokinetic parameters. Correlation of in vitro drug release with that of amount of drug absorbed in vivo has also been performed.

Quantitative Characterization of Sustained Release Tablets With Diclofenac Sodium by Means of Near-Infrared Spectroscopy and Chemometry

“…Few papers described IR, NIR and Raman spectroscopic methods for quantification of diclofenac in pharmaceuticals [38,39,62]. Kollidon ® SR is widely used for the manufacturing of sustained release matrix preparation of tablets and granules [12], due to its excellent properties (flowability, compressibility, dissolution profile of matrix tablets based on Kollidon ® SR, independent from pH of media) [25,37,42,48,49,51,56]. NIR is a powerful tool of Process Analytical Technology (PAT) used for easy and rapid pharmaceutical processes monitoring [18-20, 23, 30] and non-destructive chemical and physical characterization of pharmaceutical finished products [58,59,61] and intermediate products [46,55,60].…”

“…In the same time, at industrial scale manufacturing, the reproducible drug release profile from sustained release matrix tablets is related with the possibility to prepare tablets with same composition (constant ratio between APImatrix forming polymerfiller). This is a challenge in condition when the powder have segregation tendency [42,48,49,51,56].…”