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Formulation and Evaluation of Floating Microspheres of Acebutolol

机译:醋丁洛尔漂浮微球的制备与评价

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Oral controlled release dosage forms have been developed over the past three decades due to their considerable therapeutic advantages such as ease of administration patient compliance and flexibility in formulation. Throughout the gastrointestinal tract, these considerations have led to the development of a unique oral controlled release dosage form with Gastro retentive properties. Gastro retentive dosage forms (GRDFs) can remain in the gastric region for several hours and hence significantly prolong the gastric residence time of drugs. Prolonged gastric retention improves bioavailability, reduces drug waste, and improves solubility of drugs that are less soluble in a high pH environment. There are different types of gastro retentive dosage forms the formulation of floating microspheres is solvent diffusion evaporation technique. Acebutolol is commonly prescribed as angiotensin drug. Gastric retention time is increased because of buoyancy and site-specific delivery in stomach can be achieved. Pre formulation studies have done to formulate the floating microspheres, Acebutolol as API and three polymers were used namely Cellulose Acetate (F1), EdurgitS100 (F2), Acrycoat S100 (F3). For the above formulations all the evaluation parameters (SEM studies, buoyancy studies, the in vitro studies, Floating time) were conducted. The microspheres were placed in 6.8 pH phosphate buffer containing surfactant tween 80 to stimulate gastric condition. The drug release from floating microspheres found to be 84.22 ±0.29, 75.19 ±1.99, 67.59 ±1.97for F1, F2, and F3 respectively.
机译:在过去的三十年中,口服控释剂型由于其显着的治疗优势(如易于给药,患者顺应性和配方灵活性)而得到了发展。在整个胃肠道中,这些考虑因素导致了具有Gastro保持特性的独特口服控释剂型的开发。胃滞留剂型(GRDFs)可以在胃区域保留数小时,从而显着延长药物在胃中的停留时间。长时间的胃滞留改善了生物利用度,减少了药物浪费,并提高了在高pH环境中不易溶解的药物的溶解度。有不同类型的胃滞留剂型的浮动微球的配方是溶剂扩散蒸发技术。醋丁洛尔通常被处方为血管紧张素药物。由于浮力,胃保留时间增加,并且可以在胃中实现特定部位的递送。已经进行了配制前研究来配制漂浮的微球,使用乙酰苯丁酚作为API,并使用了三种聚合物,即醋酸纤维素(F1),EdurgitS100(F2),Acrycoat S100(F3)。对于以上配方,进行了所有评估参数(SEM研究,浮力研究,体外研究,漂浮时间)。将微球置于含有表面活性剂吐温80的6.8pH磷酸盐缓冲液中以刺激胃部状况。 F1,F2和F3的漂浮微球药物释放分别为84.22±0.29、75.19±1.99、67.59±1.97。

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