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首页> 外文期刊>European journal of pharmaceutical sciences >Exploration of supersaturable lacidipine ternary amorphous solid dispersion for enhanced dissolution and in vivo absorption
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Exploration of supersaturable lacidipine ternary amorphous solid dispersion for enhanced dissolution and in vivo absorption

机译：探索超饱和曲曲线三元无定形固体分散体，用于增强溶解和体内吸收

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摘要

Amorphous solid dispersion stands out among different formulation strategies for the improvement of dissolution rate and bioavailability via generating supersaturated drug solution, which provides a higher solubility than the crystalline counterpart, leading to a promoted intestinal absorption. Soluplus (SOL), termed as the fourth generation of solid dispersion carrier, presented a preferable effect on supersaturation maintaining and bioavailability enhancement for poorly water soluble drugs. However, some binary drug/SOL systems still suffer from insufficient dissolution and unsatisfied in vivo absorption. Thus, taking Lacidipine (LCDP) as a model drug, the aim of this study was to explore a ternary amorphous solid dispersion consisted of SOL and a surfactant to further increasing the dissolution rate and in vivo absorption. First of all, various surfactants were screened via equilibrium solubility enhancement and sodium dodecyl sulfate (SDS) was selected as the most effective candidate. Thereafter, the influence of SOL/SDS and drug/carrier weight ratio on the supersaturation maintaining was investigated. The supersaturated drug solutions were spray dried and the in vitro release, pharmacokinetic behavior as well as physical stability were investigated. It was found that although combination use of SOL and SDS did not present remarkable advantage in supersaturation maintenance in liquid state, 6-7 times higher dissolution rate under non-sink condition was noticed at SOL/SDS ratio 3: 1 after spray drying, for LCDP/SOL/SDS based formulation compared to that of the binary LCDP/SOL system, which was maintained even after 92.5% humidity and 60 degrees C accelerated stability test. Moreover, compared to the LCDP/SOL formulation, approximately 3.3 and 3.7-fold increase in C (max) and AUC(0-infinity) was achieved with LCDP/SOL/SDS based formulation. In conclusion, the presented SDS could not only be regarded as solubility enhancer but also dissolution or bioavailability promoter, highlighting its potential application in ternary supersaturable amorphous solid dispersion for further increasing the dissolution and in vivo absorption of poorly water soluble drugs.
机译：非晶固体分散在不同的配方策略中脱颖而出，通过产生超饱和药物溶液改善溶出速率和生物利用度，其提供比结晶对应物更高的溶解度，导致促进的肠道吸收。称为第四代固体分散载体的Soluplus（溶胶）呈现了对水溶性差的不饱和药物的过饱和维持和生物利用度增强的优选效果。然而，一些二元药物/溶胶系统仍然存在不足的溶解和体内吸收不满足。因此，服用LaCidipine（LCDP）作为模型药物，本研究的目的是探索由溶胶和表面活性剂组成的三元无定形固体分散体，以进一步增加溶出速率和体内吸收。首先，通过平衡溶解性筛选各种表面活性剂，并选择十二烷基硫酸钠（SDS）作为最有效的候选物。此后，研究了溶胶/ Sds和药物/载体重量比对过饱和维持的影响。将过饱和药物溶液喷雾干燥，研究体外释放，药代动力学行为以及物理稳定性。发现虽然溶胶和SDS的组合使用在液态中的过饱和维持中没有显着的优势，但在喷雾干燥后，在溶胶/ SDS比下，在溶胶/ SDS比下溶解率高的溶解速率较高6-7倍。基于LCDP /溶胶/ SDS的配方与二元LCDP /溶胶系统相比，即使在92.5％湿度和60摄氏度加速稳定性测试之后也保持了它们。另外，与LCDP /溶胶配方相比，用基于LCDP /溶胶/ SDS的制剂实现了约3.3和3.7倍的C（MAX）和AUC（0-无穷大）。总之，所呈现的SDS不仅可以被视为溶解性增强剂，还可以溶解或生物利用度启动子，突出其在三元超嘌呤无定形固体分散中的潜在应用，以进一步增加溶解和水分差的水溶性药物的体内吸收。

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  • 来源
  • 作者

    Guan Jian; Jin Liwei; Liu Qiaoyu; Xu Huan; Wu Haiyang; Zhang Xin; Mao Shirui;

  • 作者单位

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

    Shenyang Pharmaceut Univ Sch Pharm 103 Wenhua Rd Shenyang 110016 Liaoning Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    Lacidipine; Soluplus; SDS; Amorphous solid dispersion; Pharmacodynamics; Stability;

    机译：LaCidipine;soluplus;sds;无定形固体分散;药效学;稳定性;

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