传统表面活性剂和基于分子描述符的模型作为药物在禁食状态下模拟肠液溶解度的替代品

IF 1 4区 医学 Q4 PHARMACOLOGY & PHARMACY Dissolution Technologies Pub Date : 2021-01-01 DOI:10.14227/dt280321p32
Nahal Rahimi Ardabili, A. Shayanfar
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引用次数: 0

摘要

生物相关介质,如禁食状态模拟肠液(FaSSIF),常用于预测口服固体制剂在胃肠道中的体内行为。本研究使用传统表面活性剂(Tween 80和十二烷基硫酸钠)和基于结构参数(即分子描述符)的模型来评估三种难溶性药物的溶解度评估中FaSSIF的可能替代品。测定恩诺沙星、拉莫三嗪和苯巴比妥在磷酸缓冲液(PBS, pH 6.5)和FaSSIF中的溶解度。计算药物的分子描述符,并生成基于逻辑回归的数学模型来估计FaSSIF与PBS的增溶作用。结果表明,恩诺沙星、拉莫三嗪和苯巴比妥在Tween 80 (0.1% w/v)中的溶解度与它们在FaSSIF中的溶解度相似,所建模型计算的增溶比准确率为80%。综上所述,低浓度(即0.05%)的Tween 80是一种合适的低成本替代FaSSIF,所建立的模型可用于评估FaSSIF中增溶的可能性。
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Conventional Surfactants and a Model Based on Molecular Descriptors as Alternatives to the Drug Solubility in Fasted State Simulated Intestinal Fluid
Biorelevant media, such as fasted state simulated intestinal fluid (FaSSIF), are often used to forecast in vivo behavior of oral solid formulations in the gastrointestinal tract. This study uses conventional surfactants (Tween 80 and sodium lauryl sulfate) and a model based on structural parameters (i.e., molecular descriptors) to evaluate possible alternatives to FaSSIF for solubility evaluation of three poorly soluble drugs. The solubility of enrofloxacin, lamotrigine, and phenobarbital was determined in phosphate buffer solution (PBS, pH 6.5) and FaSSIF. The molecular descriptors of drugs were computed, and a mathematical model based on logistic regression was generated to estimate solubilization in FaSSIF compared with PBS. The results demonstrated that solubility of enrofloxacin, lamotrigine, and phenobarbital in Tween 80 (0.1% w/v) was similar to their solubility in FaSSIF, and the proposed model calculated the solubilization ratio with 80% accuracy. In conclusion, Tween 80 in low concentration (i.e., 0.05%) is an appropriate low-cost alternative to FaSSIF, and the proposed model can be used to evaluate the possibility of solubilization in FaSSIF.
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来源期刊
Dissolution Technologies
Dissolution Technologies 医学-药学
CiteScore
1.20
自引率
33.30%
发文量
14
审稿时长
3 months
期刊介绍: Dissolution Technologies is a peer reviewed quarterly publication reporting ongoing, useful information on dissolution testing of pharmaceuticals. It provides an international forum for dissolution analysts to receive and exchange information on various dissolution topics. Dissolution Technologies welcomes submissions related to dissolution, in vitro release, and disintegration testing. These topics should be the major focus of the article. Do not submit articles where the focus is formulation development with dissolution testing as one of many tests.
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