尖锐可乐胶基双氯芬酸钠黏附缓释片的研制及评价。

Emmanuel Adelaja Bamigbola, Anthony Amaechi Attama, Franklin Chimaobi Kenechukwu, Jude Nkemjika Oraeluno
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引用次数: 0

摘要

目的:考察尖锐可乐胶(CAG)在双氯芬酸钠黏附缓释片中的应用效果。方法:将CAG与DS分别按0.5:1、1:1、2:1、3:1的比例配制成不同批号的颗粒剂,压制成片剂,在SGF (pH 1.2)和SIF (pH 7.4)中测定黏附强度、溶胀指数和药物释放度。结果:片剂的溶胀指数和黏附强度均呈ph依赖性。pH 7.4时的溶胀指数为56±2.03 ~ 121±2.19%,黏附强度为7.25±1.45 ~ 15.43±2.71 g/cm2,明显高于pH 1.2时的p2。在pH 1.2条件下,2h (T2h)后DS的释放率不显著。然而,在pH 7.4下,所有批次的药物释放率都很显著,并且与CAG浓度有关。释药顺序为:3 g(80.44±7.75)< 2 g(86.35±5.65)< 1 g(90.08±6.14)< 0.5 g(99.70±3.90)。添加0.5 g CAG的最大释放时间为7h (T7h),其他批次为10h (T10h)。结论:CAG可用于黏附持续给药。
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Formulation and Evaluation of Cola acuminata Gum-based Mucoadhesive Sustained-release Matrix Tablets of Diclofenac Sodium.

Objective: This study aimed to evaluate Cola acuminata gum (CAG) for the formulation of mucoadhesive sustained-release matrix tablets of diclofenac sodium.

Methods: Different batches of granules containing CAG and 100 mg of DS in ratios 0.5:1, 1:1, 2:1, and 3:1 were prepared, compressed into tablets, and evaluated for mucoadhesive strength, swelling index, and drug release in SGF (pH 1.2) and SIF (pH 7.4).

Results: Swelling indices and mucoadhesive strengths of the tablets were pH-dependent. Swelling indices of 56 ± 2.03 to 121 ± 2.19% and mucoadhesive strengths of 7.25 ± 1.45 to 15.43 ± 2.71 g/cm2 obtained at pH 7.4 were significantly higher (p<0.05) than swelling indices of 25 ± 2.43 to 47 ± 3.15% and mucoadhesive strengths of 5.52 ± 0.76 to 9.22 ± 1.95 g/cm2 obtained at pH 1.2. The percentage release of DS from the matrix tablets at pH 1.2 after 2 h (T2h) was insignificant. However, the percentage of drug release at pH 7.4 was significant for all the batches and dependent on the CAG concentration. The drug release was in the order of batches containing 3 g (80.44 ± 7.75) < 2 g (86.35 ± 5.65) < 1 g (90.08 ± 6.14) < 0.5 g (99.70 ± 3.90). The time for maximum drug release was 7 h (T7h) for CAG containing 0.5 g and 10 h (T10h) for other batches.

Conclusion: This study showed that CAG could be useful for mucoadhesive sustained drug delivery.

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