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Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2020-12-01 , DOI: 10.2147/dddt.s279955 Afrasim Moin 1 , Hosahalli V Gangadharappa 2 , Mohd Adnan 3 , Syed M Rizvi 1 , Syed A Ashraf 4 , Mitesh Patel 5 , Amr S Abu Lila 1, 6 , Ahmed N Allam 7
Drug Design, Development and Therapy ( IF 4.8 ) Pub Date : 2020-12-01 , DOI: 10.2147/dddt.s279955 Afrasim Moin 1 , Hosahalli V Gangadharappa 2 , Mohd Adnan 3 , Syed M Rizvi 1 , Syed A Ashraf 4 , Mitesh Patel 5 , Amr S Abu Lila 1, 6 , Ahmed N Allam 7
Affiliation
Purpose: The present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug.
Methods: Central design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out.
Results and Discussion: It was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug–polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile.
Conclusion: The results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.
Keywords: locust bean gum, karaya gum, diltiazem hydrochloride, response surface methodology, sustained release
中文翻译：
通过响应面方法调节天然聚合物基质的药物释放：体外和体内评价
目的：本工作旨在挑战天然树胶、刺梧桐树胶和刺槐豆胶作为基质形成聚合物用于配制模型药物地尔硫卓缓释片剂的功效。
方法：采用中心设计复合材料进行片剂配方的制定和优化。这两种牙龈被选为自变量。选择的相关因素是第 1 小时释放的药物量 (Y1)、12 小时后释放的药物量 (Y2)、扩散指数 (Y3) 和释放总药物一半的时间 (T 50% ) (Y4 ）。湿法制粒方法用于片剂的配制。进行了FT-IR、DSC、体外溶出度、溶胀-侵蚀研究、SEM和稳定性研究。
结果和讨论：很明显，所制备制剂的释放模式受到片剂中胶的量的显着影响。FT-IR 和 DSC 结果证实了药物-聚合物的相容性。多项式方程用于预测不同水平的独立因素对响应变量的定量影响。经ANOVA分析，考虑显着因素进行约束优化，得到优化后的公式。对响应面法生成的优化公式进行了体外和体内特性评估。优化配方和缓释上市产品在兔体内进行了研究，结果-测试表明两种制剂的药代动力学参数变化不大，证实制备的片剂具有缓释特性。
结论：结果表明刺梧桐和刺槐豆胶可有效地用于制备缓释片。
关键词：刺槐豆胶，刺梧桐胶，盐酸地尔硫卓，响应面法，缓释
更新日期：2020-12-01
Methods: Central design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out.
Results and Discussion: It was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug–polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile.
Conclusion: The results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.
Keywords: locust bean gum, karaya gum, diltiazem hydrochloride, response surface methodology, sustained release
中文翻译：
通过响应面方法调节天然聚合物基质的药物释放：体外和体内评价
目的：本工作旨在挑战天然树胶、刺梧桐树胶和刺槐豆胶作为基质形成聚合物用于配制模型药物地尔硫卓缓释片剂的功效。
方法：采用中心设计复合材料进行片剂配方的制定和优化。这两种牙龈被选为自变量。选择的相关因素是第 1 小时释放的药物量 (Y1)、12 小时后释放的药物量 (Y2)、扩散指数 (Y3) 和释放总药物一半的时间 (T 50% ) (Y4 ）。湿法制粒方法用于片剂的配制。进行了FT-IR、DSC、体外溶出度、溶胀-侵蚀研究、SEM和稳定性研究。
结果和讨论：很明显，所制备制剂的释放模式受到片剂中胶的量的显着影响。FT-IR 和 DSC 结果证实了药物-聚合物的相容性。多项式方程用于预测不同水平的独立因素对响应变量的定量影响。经ANOVA分析，考虑显着因素进行约束优化，得到优化后的公式。对响应面法生成的优化公式进行了体外和体内特性评估。优化配方和缓释上市产品在兔体内进行了研究，结果-测试表明两种制剂的药代动力学参数变化不大，证实制备的片剂具有缓释特性。
结论：结果表明刺梧桐和刺槐豆胶可有效地用于制备缓释片。
关键词：刺槐豆胶，刺梧桐胶，盐酸地尔硫卓，响应面法，缓释
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