Department of Pharmacy, Abasyn University, Peshawar, Pakistan.
Department of Pharmacy, Kohat University of Science and Technology (KUST), Kohat, Pakistan.
PLoS One. 2021 Aug 2;16(8):e0249075. doi: 10.1371/journal.pone.0249075. eCollection 2021.
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.
液固体制剂是一种新型剂型，将液体药物（液体药物、非挥发性溶剂/溶剂系统中的药物溶液/分散体）转化为干燥、自由流动的粉末并进行压缩。研究目的是阐明载体材料对氯吡格雷从液固体制剂中释放特性的影响。使用微晶纤维素、玉米淀粉、聚乙烯吡咯烷酮和羟丙基甲基纤维素作为载体材料，在三个浓度（40、30 和 20%，w/w）下开发了不同的液固体制剂配方。液体载体是根据氯吡格雷的溶解度选择的。胶体二氧化硅用作包衣材料，载体与包衣材料的比例保持在 10。采用直接压片技术制备由微晶纤维素（稀释剂）、麦芽糖糊精-80（稀释剂）、普鲁兰（崩解剂）和硬脂酸镁（润滑剂）组成的对照制剂，并用于比较。所有配方均在压缩前后进行评估。酸溶解度曲线显示在 HCl 缓冲液 pH2 中具有更高的溶解度（296.89±3.49μg/mL）。选择丙二醇和水（2:1，v/v）的混合物作为液体载体。药物含量在规定量的 99-101%范围内。所有配方均表现出更好的机械强度，其脆碎度在官方限度内（<1%）。微晶纤维素和玉米淀粉导致药物更快释放，而聚乙烯吡咯烷酮和 HPMC 通过凝胶形成导致药物持续释放。结果表明，通过适当选择载体材料可以实现氯吡格雷的快速释放和持续释放。
