The in vivo transformation and pharmacokinetic properties of a liquid crystalline drug delivery system.

The in vivo transformation and pharmacokinetic properties of a liquid crystalline drug delivery system.
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液晶药物递送系统的体内转化和药代动力学特性。

DOI:
10.1016/j.ijpharm.2017.08.098
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发表时间:
2017
影响因子:
5.8
通讯作者:
Kinam Park
Kinam Park
中科院分区:
医学2区
文献类型:
--
作者:
A. Otte;Y. M. Báez;E. A. Mun;B. Soh;Young;Kinam Park

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研究了由磷脂酰胆碱、脱水山梨醇单油酸酯和生育酚乙酸酯组成的液晶(LC)系统,以了解皮下注射后的体内转化,以及制剂的理化和药代动力学性质。利用大鼠模型监测前体LC制剂至LC基质的伪时程转化,以及含醋酸亮丙瑞林制剂的血药浓度曲线。使用了导致III相的三种制剂,证明了不同的体外释放曲线。显示最高AUC、Cmax和Tmax的制剂也显示最大的体外释放速率、最低的粘度(LC基质)和较早的体内转化(LC前体到基质)。描述了液晶系统的粘度、相变和药物释放性质之间的潜在联系。
A liquid crystalline (LC) system, composed of phosphatidylcholine, sorbitan monoleate, and tocopherol acetate, was investigated to understand thein vivotransformation after subcutaneous injection, coupled with the physicochemical and pharmacokinetic properties of the formulation. The rat model was utilized to monitor a pseudo-time course transformation from a precursor LC formulation to the LC matrix, coupled with the blood concentration profiles of the formulations containing leuprolide acetate. Three formulations that result in theHIIphase, demonstrating dissimilarin vitrorelease profiles, were used. The formulation showing the highest AUC,CmaxandTmax, also displayed the greatest release ratein vitro, the lowest viscosity (LC matrix), and an earlier transformation (LC precursor to matrix)in vivo. A potential link between viscosity, phase transformation, and drug release properties of a liquid crystalline system is described.
DOI: 10.1016/j.jconrel.2010.01.001
发表时间: 2010-04-19
影响因子: 10.8
作者:
Solorio, Luis;Babin, Brett M.;Patel, Ravi B.;Mach, Justyna;Azar, Nami;Exner, Agata A.
通讯作者: Exner, Agata A.
DOI: 10.1002/jps.24673
发表时间: 2015-12
影响因子: 3.8
作者:
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通讯作者: Exner AA
DOI: 10.1016/j.jconrel.2010.08.020
发表时间: 2010-11-01
期刊: Journal of controlled release : official journal of the Controlled Release Society
影响因子: --
作者:
Patel RB;Solorio L;Wu H;Krupka T;Exner AA
通讯作者: Exner AA
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