利用糖基载体的固体分散技术提高辛伐他汀的溶解度和生物利用度

Q2 Pharmacology, Toxicology and Pharmaceutics
Venkata Naga JYOTHI NAKKA, Kumar Shiva Gubbiyappa, Nagesh Nagaraju
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引用次数: 0

摘要

研究目的研究旨在通过使用乳糖、木糖醇、山梨醇和 Soluplus 等各种糖载体进行固体分散(SD),提高水溶性差的药物辛伐他汀(SMV)的溶解度和生物利用度:首先,测定药物的容积密度、卡尔指数、豪斯纳比率、休止角,分析药物在 0.1 N HCl、6.8pH、7.2pH 磷酸盐缓冲液、甲醇和乙醇等不同溶剂中的溶解度,并进行制剂前研究。通过溶剂蒸发和熔融,以不同的载体浓度(1:0.5、1:1、1:1.5、1:2 和 1:3)制成 SMV 固体分散体(SD s)。对每种配方的各种理化参数进行了测试:结果:所有制剂的各种理化指标均在药典允许范围内。傅立叶变换红外光谱等制剂前研究表明,药物与辅料之间不存在相互作用。与其他溶剂相比,0.1N HCl 显示 SMV 的溶解度更高。对 SDs 进行了产量、夹带和体外药物释放研究评估。结果表明,回收率为 88% 至 100.68%,捕获效率为 92% 至 101%。含有山梨醇的 SD 释放了 74-98% 的药物,使用山梨醇的配方释放了 80-99% 的药物,使用木糖醇作为载体的配方释放了 83-99% 的药物。在超过 60 分钟的时间里,包括乳果糖在内的制剂可释放 91-100% 的辛伐他汀剂量:结论:含乳果糖的SMV SD表现出卓越的释放特性,并选择了药物与载体比例为1:1.5的优化配方。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
ENHANCEMENT OF DISSOLUTION AND BIOAVAILABILITY OF SIMVASTATIN BY SOLID DISPERSION TECHNIQUE USING SUGAR-BASED CARRIERS
Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus. Methods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysis in various solvents like 0.1 N HCl, 6.8pH, 7.2pH phosphate buffers, methanol, and ethanol and preformulation studies. via various carrier concentrations (1:0.5, 1:1, 1:1.5, 1:2, and 1:3), SMV solid dispersions (SD s) were made by solvent evaporation and fusion. The various physiochemical parameters of each formulation were tested. Results: For various physicochemical criteria, all of the formulations were found to be within the allowed pharmacopoeial limits. Preformulation studies such as FT-IR demonstrated the lack of interactions between drugs and excipients. In comparison to the other solvents, 0.1N HCl showed SMV to be more soluble. The SDs underwent yield, entrapment, and in vitro drug release study evaluations. 88 to 100.68% recovery rates and 92 to 101% capture efficiency were observed. While SDs containing Sorbitol released 74-98% of the medicine, formulations utilizing Sorbitol demonstrated 80-99% drug release, and formulations using xylitol as a carrier released 83-99% of the drug. For more than 60 min, the formulation, including lactulose, delivered 91-100% of the Simvastatin dose. Conclusion: Lactulose-containing SMV SDs demonstrated superior release characteristics, and an optimized formulation with a 1:1.5 drug-to-carrier ratio has been chosen.
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来源期刊
International Journal of Applied Pharmaceutics
International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.40
自引率
0.00%
发文量
219
期刊介绍: International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.
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