Formulation, Characterization, Optimization, and Pharmacokinetic Evaluation of Cilnidipine-Loaded Liquisolid Compacts with Improved Dissolution and Bioavailability,Journal of Pharmaceutical Innovation

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Formulation, Characterization, Optimization, and Pharmacokinetic Evaluation of Cilnidipine-Loaded Liquisolid Compacts with Improved Dissolution and Bioavailability
Journal of Pharmaceutical Innovation ( IF 2.7 ) Pub Date : 2022-05-10 , DOI: 10.1007/s12247-022-09651-z
Farhatjahan Shaikh ₁ , Deepti Jani ₁ , Meenakshi Patel ₂ , Santosh Shelke ₃ , Vandana Patel ₄ , Gajanan Shinde ₄ , Inayat Pathan ₅

Affiliation

Purpose

Cilnidipine (BCS class II drug) is a calcium channel blocker used in the treatment of hypertension. Poor water solubility, unreliable oral absorption, and poor bioavailability make it a probable candidate for designing novel drug delivery. The objective of the present investigation was to formulate, optimize, and study in vitro and in vivo performance of cilnidipine-loaded liquisolid compacts.

Methods

Solid-state characterization was performed by FTIR, DSC, SEM, and XRD. Preliminary screening was performed to select non-volatile solvent, carrier, and coating material based on flowable liquid retention potential. Liquisolid compacts were optimized using 3² factorial designs and were studied for pre- and post-compression parameters, in vitro dissolution, dissolution validation, and pharmacokinetic and stability studies, whereas bioanalysis was carried out using HPLC–MS/Ms method.

Results

In the preformulation study, Transcutol HP was selected as the non-volatile solvent, and Neusilin US2 and Cab-o-sil were selected as the carrier and coating material, respectively, exhibiting compatibility with the drug. Liquisolid compacts were found to be compressible with the selected composition. In vitro studies indicated increased dissolution behaviour, whereas in vivo studies demonstrated improved bioavailability compared to the pure drug and marketed formulation.

Conclusion

In conclusion, formulated liquisolid compacts demonstrated increased dissolution and bioavailability making the formulation suitable for oral administration.

中文翻译：

具有改善的溶解度和生物利用度的载有西尼地平的液体固体压片的配方、表征、优化和药代动力学评价

目的

Cilnidipine（BCS II 类药物）是一种钙通道阻滞剂，用于治疗高血压。水溶性差、口服吸收不可靠和生物利用度差，使其成为设计新型药物递送的可能候选者。本研究的目的是制定、优化和研究载有西尼地平的液态固体压片的体外和体内性能。

方法

通过 FTIR、DSC、SEM 和 XRD 进行固态表征。进行初步筛选以根据可流动液体保留潜力选择非挥发性溶剂、载体和涂层材料。^{使用 3 2}因子设计优化液体固体压块，并研究了压缩前和压缩后参数、体外溶出度、溶出度验证以及药代动力学和稳定性研究，而生物分析则使用 HPLC-MS/MS 方法进行。