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首页> 外文期刊>International Journal of Pharmaceutical Sciences and Research >PREPARATION AND CHARACTERIZATION OF FLOATING ALGINATE BEADS OF LAFUTIDINE AS A GASTRORETENTIVE DOSAGE FORM
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PREPARATION AND CHARACTERIZATION OF FLOATING ALGINATE BEADS OF LAFUTIDINE AS A GASTRORETENTIVE DOSAGE FORM

机译:Lafutidine浮藻酸盐珠的制备与表征作为胃内剂型

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Background: Lafutidine floating beads as a gastro-retentive dosage form antagonisms of histamine H2 receptor. It is used as anti-ulcerative agent. It is effective against the oesophageal lesions induced by acid reflux through inhibition of acid secretions. Objectives: The objective of the present work was to formulate and evaluate the floating beads of Lafutidine as a model drug. The objective of this study is to develop a simple uncomplicated and easy to manufacture floating beads that are capable of delivering lafutidine at a prolonged release rate of delivery. It has a short half-life (3 h). It has a low bioavailability (60-80%). The frequent dosing, which results in unacceptable patient compliance. Methods: Lafutidine was received as a gift sample and a thorough pre-formulation study was performed on a given sample in order to estimate the physicochemical properties like solubility, melting point, partition coefficient to confirm the authenticity of sample and to confirm that there are no significant barriers to the development of dosage forms. 12 different formulation of lafutidine floating alginate beads were successfully developed using the emulsion solvent diffusion method. The beads had good yield and showed high, drug entrapment efficiency. The flow properties of microspheres were within the acceptable range and therefore would be easily filled into capsules. Release properties were satisfactory and the formulations hold promise for further development into drug delivery systems for oral administration of lafutidine. Results and Discussions: FT-IR spectra of the physical mixture showed no significant shifting of the peaks, so ingredients used in the study are suitable for the development of lafutidine floating beads formulations. The minimum cumulative percent drug release after 7 h of the Lafutidine floating beads 23.244 ± 0.82% was shown by batch AB3 and the maximum release 72.41 ± 0.09% was shown by the floating beads of batch AB4.
机译:背景:Lafutidine浮珠作为组胺H2受体的胃保留剂型拮抗作用。它用作抗溃疡性剂。通过抑制酸分泌物,对酸回流诱导的食管病变有效。目的:本作工作的目的是制定和评估Lafutidine作为模型药物的浮珠。本研究的目的是开发一种简单的简单且易于制造的浮珠,其能够以延长的释放速率递送Lafutidine。它有一个短的半衰期(3小时)。它具有低生物利用度(60-80%)。经常给药,导致不可接受的患者依从性。方法:将Lafutidine作为礼物样品接收,并在给定的样品上进行彻底的预制剂研究,以估计像溶解度,熔点,分配系数的物理化学性质,以确认样品的真实性并确认没有剂型发展的重要障碍。 12使用乳液溶剂扩散法成功开发了12种不同配方浮藻酸盐珠粒。珠子产量良好,并显示出高,药物夹带效率。微球的流动性质在可接受的范围内,因此将容易地填充到胶囊中。释放性质是令人满意的,配方占据进一步发展的承诺,以进一步发展为劳替税的口服给药。结果与讨论:物理混合物的FT-IR光谱显示出峰的显着偏移,因此该研究中使用的成分适用于Lafutidine浮珠制剂的发育。通过批量AB3示出了Lafutidine浮珠7小时后的最小累积百分比药物释放23.244±0.82%,并通过批量AB4的浮珠表示最大释放72.41±0.09%。

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