Evaluation of the effect of carrier material on modification of release characteristics of poor water soluble drug from liquisolid compacts.

Liquisolid compact is a novel dosage form in which a liquid medication (liquid drug, drug solution/dispersion in non-volatile solvent/solvent system) is converted to a dry, free flowing powder and compressed. Objective of the study was to elucidate the effect of carrier material on release characteristics of clopidogrel from liquisolid compacts. Different formulations of liquisolid compacts were developed using microcrystalline cellulose, starch maize, polyvinyl pyrollidone and hydroxypropyl methylcellulose as carrier material in three concentrations (40, 30 and 20%, w/w). Liquid vehicle was selected on the basis of solubility of clopidogrel. Colloidal silicondioxide was used as coating material and ratio of carrier to coating material was kept 10. A control formulation comprised of microcrystalline cellulose (diluents), tabletose-80 (diluents), primojel (disintegrant) and magnesium stearate (lubricant) was prepared by direct compression technique and was used for comparison. All the formulations were evaluated at pre and post compression level. Acid solubility profile showed higher solubility in HCl buffer pH2 (296.89±3.49 μg/mL). Mixture of propylene glycol and water (2:1, v/v) was selected as liquid vehicle. Drug content was in the range of 99-101% of the claimed quantity. All the formulations showed better mechanical strength and their friability was within the official limits (<1%). Microcrystalline cellulose and starch maize resulted in faster drug release while polyvinyl pyrollidone and HPMC resulted in sustaining drug release by gel formation. It is concluded from results that both fast release and sustained release of clopidogrel can be achieved by proper selection of carrier material.

Déclaration de conflit d'intérêts

The authors of this study have read the journal’s policy, and the authors have the following competing interests to declare: Feorzsons Laboratories Ltd. provided material support in the form of API and facilities. The model drug clopidogrel (Mithri Laboratories Ltd. India; purity 99.81% with reference to USP standard) was obtained from Ferozsons Laboratories Ltd. Nowshera, Pakistan. Excipients used in the study, included tablettose-80 (Molkerei Meggle, Germany), microcrystalline cellulose (F.M.C International, Ireland), primojel {sodium starch glycolate} (F.M.C International, Ire Land), Colloidal silicon dioxide {Aerosil-200} (F.M.C International, Ireland), hydroxylpropyl methylcellulose (Merck KGA, Germany), polyvinyl pyrollidone (I.S.P. Technology, Texas), starch maize (I.C.I, Pakistan) and magnesium stearate (Coin Powder International Company Ltd, Taiwan) were purchased from local market of Peshawar, Pakistan. All the excipients were of pharmaceutical grade and were used as received. This does not affect our adherence to PLOS ONE policies on sharing data and materials. There are no patents, products in development or marketed products associated with this research to declare.