Purpose

The goal of this study was to improve the solubility and bioavailability of poorly water-soluble atorvastatin calcium (ATC) by solid dispersion technique using natural polymer as a hydrophilic carrier. ATC is an anti-hyperlipidemic agent with low bioavailability due to its inability to dissolve in water. As a result, an effort has been undertaken to improve ATC’s oral bioavailability by making it more water-soluble using the solid dispersion approach.

Methods

Solid dispersions (SD) were prepared by using modified Samanea saman seed gum (MSSSG) as a natural hydrophilic carrier. Amongst various available methods, solvent evaporation method was selected to prepare solid dispersions. The chemical interaction between ATC and modified hydrophilic carrier was evaluated by FTIR spectroscopy.

Results

The result of the solubility study of ATC from solid dispersion found greater solubility of ATC compared to pure drug. The outcomes of an in vitro drug release study show higher cumulative drug release at 120 min, that is 96.95% of ATC from prepared solid dispersions in comparison to pure ATC, which was only 65.36%. The prepared solid dispersions were evaluated by DSC, XRD, and SEM studies. DSC and XRD study findings revealed that the crystalline drug was converted into an amorphous state. Pharmacokinetic study in rats showed approximately 1.68- and 2.3-fold increments in C_max and AUC respectively in case of solid dispersion as compared to plain ATC.

Conclusion

In conclusion, MSSSG could be a promising carrier to improve the solubility, dissolution rate, and bioavailability of poorly water-soluble ATC.

Graphical Abstract

中文翻译：

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采用改性天然聚合物作为亲水载体的固体分散技术提高难溶性阿托伐他汀钙的生物利用度

目的

本研究的目的是通过使用天然聚合物作为亲水载体的固体分散技术来提高难水溶性阿托伐他汀钙（ATC）的溶解度和生物利用度。ATC是一种抗高血脂药，由于不溶于水，生物利用度较低。因此，人们正在努力通过使用固体分散方法使其更易溶于水来提高 ATC 的口服生物利用度。

方法

采用改性萨曼种子胶（MSSSG）作为天然亲水载体制备固体分散体（SD）。在多种可用方法中，选择溶剂蒸发法制备固体分散体。通过 FTIR 光谱评估 ATC 和改性亲水载体之间的化学相互作用。

结果

固体分散体中 ATC 的溶解度研究结果发现，与纯药物相比，ATC 的溶解度更大。体外药物释放研究的结果显示，120 分钟时，制备的固体分散体的累积药物释放量更高，即 ATC 的 96.95%，而纯 ATC 仅为 65.36%。通过 DSC、XRD 和 SEM 研究对制备的固体分散体进行评估。DSC 和 XRD 研究结果表明，结晶药物已转化为无定形状态。大鼠药代动力学研究表明，与普通 ATC 相比，固体分散体的 C _max和 AUC分别增加了约 1.68 倍和 2.3 倍。

结论

总之，MSSSG 可能是一种有前途的载体，可提高难溶性 ATC 的溶解度、溶出速率和生物利用度。

图形概要