Partitioning of drug model compounds between poly(lactic acid)s and supercritical CO2 using quartz crystal microbalance as an in situ detector
Partitioning of drug model compounds between poly(lactic acid)s and supercritical CO2 using quartz crystal microbalance as an in situ detector
复制标题
使用石英晶体微天平作为原位检测器在聚乳酸和超临界二氧化碳之间分配药物模型化合物
DOI：
10.1016/j.supflu.2010.04.013
复制
发表时间：
2010-08-01
影响因子：
3.9
通讯作者：
Zhang, Zhi-Bing
中科院分区：
文献类型：
--
作者：
Ma, Shao-Ling;Lu, Zhao-Wen;Zhang, Zhi-Bing
采用石英晶体微天平（QCM）作为原位检测器，研究了其在超临界co2 -药物-聚合物体系相平衡测定中的潜在应用。在313.15 K和10.0 MPa压力下，测定了CO2在聚（D， l -乳酸）（D,L-PLA）和聚（l -乳酸）（L-PLA）两种可生物降解聚合物中的溶解度。D，L-PLA由于其非晶结构表现出较好的CO2吸收能力。选取布洛芬、阿司匹林、水杨酸、萘四种水溶性较差的药物模型化合物为代表，考察PLA基质的药物摄取及超临界浸渍时的分配系数。发现药物的分配系数可高达10(3)~ 10(4)个数量级，且受药物与PLA分子间相互作用的影响较大。在8.0 ~ 10.0 MPa的超临界浸渍过程中，由于羧基和乙酰基的存在，阿司匹林的分配效果最好。药物分配还与ScCO2中的药物浓度有关，即水杨酸在7.5-8.0 MPa的ScCO2中溶解度较差，因此在PLA中几乎没有被吸收，而与L-PLA极性不同的萘具有较好的co2溶性，但其分配系数适中。(C) 2010 Elsevier B.V.版权所有
Quartz crystal microbalance (QCM) was used as an in situ detector to investigate the potential application in the phase equilibrium determination of supercritical CO2-drug-polymer systems. CO2 solubility in two biodegradable polymers, poly(D,L-lactic acid) (D,L-PLA) and poly(L-lactic acid) (L-PLA) was primarily measured at 313.15 K and pressures up to 10.0 MPa. D,L-PLA showed a better CO2 absorption ability due to its amorphous structure. Four drug model compounds of poor solubility in water, ibuprofen, aspirin, salicylic acid and naphthalene were selected as representatives for the examination of drug uptake in PLA matrices, as well as partition coefficient during supercritical impregnation. It was found that partition coefficients of drugs can reach as high as 10(3)-10(4) orders of magnitude and greatly affected by the intermolecular interactions between drugs and PLA. Aspirin exhibited the best partitioning during the supercritical impregnation at pressures of 8.0-10.0 MPa due to the existence of carboxylic acid and acetyl groups. Drug partitioning is additionally related to the drug concentration in ScCO2, i.e. salicylic acid showed little absorption in PLA according to its poor solubility in ScCO2 at 7.5-8.0 MPa, whereas the well CO2-soluble compound, naphthalene, exhibited a moderate partition coefficient although its polarity was different from L-PLA. (C) 2010 Elsevier B.V. All rights reserved.