控释乐卡地平片:湿法制粒的制剂与评估研究

Sujana A, Durga Prasad K, Sarada Mrinalini Talluri
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引用次数: 0

摘要

乐卡地平能阻止细胞外钙进入血管和心肌细胞,防止心肌平滑肌因细胞内钙减少而收缩。这将导致冠状动脉和全身动脉扩张,从而降低血压。本研究旨在利用 HPMC K 100M、海藻酸钠和瓜尔豆胶等聚合物,开发和评估用于口服的勒卡尼平控释片剂。将乐卡地平、聚合物和稀释剂过筛并混合 10 分钟。用异丙醇制成颗粒,在 60°C 下干燥一小时,然后过筛。用胶体二氧化硅(Aerosil-200)和硬脂酸镁润滑颗粒,混合 5 分钟,然后用旋转机压缩(平均重量:500 毫克;硬度:5-6 千克/平方厘米)。所有配方的体积密度和敲击密度几乎相同。可压缩指数和豪斯纳比率介于 0.18 至 1.09-1.21 之间,表明具有良好的流动性。片剂厚度为 5.82 至 5.91 毫米,硬度为 5.9 至 6.3 千克/平方厘米,易碎性小于 1.0 %W/W。药物含量在 98-102% 之间。从溶解数据来看,控释顺序为 F9 > F7 > F8,表明 HPMC 和两种天然聚合物的组合具有最佳释放效果。
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Controlled Release Lercanidipine Tablets: A Study on Formulation and Evaluation by Wet Granulation
Lercanidipine blocks the entry of extracellular calcium into vascular and cardiac muscle cells, preventing myocardial smooth muscle contraction due to decreased intracellular calcium. This results in the dilation of coronary and systemic arteries, reducing blood pressure. This study aimed to develop and evaluate lercanidipine controlled-release tablets for oral administration using polymers like HPMC K 100M, sodium alginate, and guar gum. Lercanidipine, polymers, and diluents were sieved and mixed for 10 minutes. Granules were formed using isopropyl alcohol, dried at 60°C for one hour, and sieved. The granules were lubricated with colloidal silicon dioxide (Aerosil-200) and magnesium stearate, blended for 5 minutes, and compressed using a rotary machine (average weight: 500 mg; hardness: 5-6 kg/cm²). Bulk and tapped densities were nearly identical for all formulations. Compressibility index and Hausner ratio ranged from ?18 to 1.09-1.21, indicating good flow properties. Tablet thickness ranged from 5.82 to 5.91 mm, hardness from 5.9 to 6.3 kg/cm², and friability was less than 1.0 %W/W. Drug content was between 98-102%. The controlled-release order from dissolution data was F9 > F7 > F8, showing optimal release with a combination of HPMC and two natural polymers.
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