Samie Muhammad, Bashir Sajid, Abbas Jabbar, Khan Samiullah, Aman Nargis, Jan Habibullah, Muhammad Naveed
COMSATS Institute of Information Technology, Department of Pharmacy, Abbottabad, Pakistan.
Sargodha University, Faculty of Pharmacy, Sargodha, Pakistan.
Turk J Pharm Sci. 2018 Dec;15(3):309-318. doi: 10.4274/tjps.29200. Epub 2018 Nov 20.
Levosulpiride is a widely used gastroprokinetic agent in the treatment of various gastric disorders; however, its short half-life and increased dosage frequency leads to non-compliance and possible adverse effects. The prime objective of the current study was to develop a sustained-release formulation of Levosulpiride incorporating bioresorbable cellulose derivatives.
Sustained-release formulations of Levosulpiride were prepared through direct compression using various cellulose derivatives such as CMC sodium, HPC, and HPMC in different polymer-to-drug weight ratios as release-modifying polymers. The powder blends and compressed tablets were then subjected to pre-compressional and post-compressional evaluation, as well as FTIR analysis. release studies were performed for all formulations of the model drug in buffer solution of pH 6.8 at a wave length of 214 nm by a UV-visible light spectrophotometer.
The FTIR results confirmed that the interaction between components was physical, and from the different kinetic models data, the release profile was best expressed by the Higuchi model because the results showed high linearity. The results also showed formulation F9 to be the ideal one among the developed formulations, exhibiting sustained- release behavior.
Levosulpiride sustained-release matrices were prepared successfully using CMC sodium, HPC, and HPMC as the release-retarding polymer/carrier.
左舒必利是一种广泛用于治疗各种胃部疾病的促胃肠动力药；然而，其半衰期短且给药频率增加会导致患者依从性差并可能产生不良反应。本研究的主要目的是开发一种包含生物可吸收纤维素衍生物的左舒必利缓释制剂。
以不同聚合物与药物重量比使用各种纤维素衍生物（如羧甲基纤维素钠、羟丙基纤维素和羟丙甲纤维素）作为释放调节聚合物，通过直接压片法制备左舒必利缓释制剂。然后对粉末混合物和压制片剂进行压前和压后评估以及傅里叶变换红外光谱分析。使用紫外可见分光光度计在波长214nm下于pH 6.8的缓冲溶液中对模型药物的所有制剂进行释放研究。
傅里叶变换红外光谱结果证实各组分之间的相互作用是物理性的，并且从不同动力学模型数据来看，释放曲线最好用 Higuchi 模型表示，因为结果显示出高线性。结果还表明制剂F9是所开发制剂中的理想制剂，表现出缓释行为。
成功地使用羧甲基纤维素钠、羟丙基纤维素和羟丙甲纤维素作为释放阻滞剂/载体制备了左舒必利缓释基质。
