Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate.
Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate.
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用于体外测试水不溶性药物的溶出介质：表面活性剂纯度和电解质对卡马西平在十二烷基硫酸钠水溶液中体外溶出的影响。
DOI：
10.1021/js960105t
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发表时间：
1997
影响因子：
3.8
通讯作者：
Amidon,GL
中科院分区：
文献类型：
--
作者：
Crison,JR;Weiner,ND;Amidon,GL
测量了两种不同纯度（95% 和 99%）的十二烷基硫酸钠（SLS）水溶液中卡马西平的固有溶出率和溶解度，以及 95% SLS 在 0.15 M NaCl 中的溶液，以确定表面活性杂质和电解质的影响。这项工作产生了四个重要的观察结果：（1）根据 99% SLS、95% SLS 和 95% 0.15 M NaCl SLS 溶液的溶解度实验计算出的平衡系数分别为 295、265 和 233 L/mol； (2) 99% SLS 中的溶出率比 95% SLS 和 95% 0.15 M NaCl 溶液中的溶出率提高了 10%，但没有显着差异； （3）根据溶出实验估算出的载药胶束的扩散系数，99% SLS 为 8.4 × 10−7cm2/s，95% SLS 为 9.5 × 10−7cm2/s，95% 0.15 M NaCl 为 1.2 × 10−6cm2/s； (4) 99% SLS、95% SLS 和 95% SLS 与 0.15 M NaCl 的临界胶束浓度分别为 6.8、4.2 和 0.35 mM。这项研究的结果清楚地说明了胶束对杂质和电解质在尺寸和负载能力方面的敏感性，以及这些变化对溶解度和溶解速率的影响。因此，当在溶出介质中使用表面活性剂进行剂型体外测试时，必须考虑存在的杂质水平，以使结果一致且可靠。固有溶出速率、表面张力或溶解度测量可能是有用且方便的方法，可用于识别由于降解或批次间差异而导致的表面活性剂变化。
The intrinsic dissolution rate and solubility of carbamazepine was measured in aqueous solutions of sodium lauryl sulfate (SLS) prepared with two different grades of purity, 95 and 99%, and 95% SLS in 0.15 M NaCl to determine the effect of surface‐active impurities and electrolytes. Four significant observations resulted from this work: (1) the equilibrium coefficients calculated from the solubility experiments in the 99% SLS, 95% SLS, and 95% with 0.15 M NaCl SLS solutions were 295, 265, and 233 L/mol, respectively; (2) the dissolution rate enhancement in the 99% SLS was 10% greater than that in the 95% SLS and 95% with 0.15 M NaCl solutions, which were not significantly different; (3) the diffusion coefficients of the drug‐loaded micelles estimated from the dissolution experiments were 8.4 × 10−7cm2/s for the 99% SLS, 9.5 × 10−7cm2/s for the 95% SLS, and 1.2 × 10−6cm2/s for the 95% with 0.15 M NaCl; and (4) the critical micelle concentrations for the 99% SLS, 95% SLS, and 95% SLS with 0.15M NaCl were 6.8, 4.2, and 0.35 mM, respectively. The results of this study clearly illustrate the sensitivity of the micelle to impurities and electrolytes with regard to size and loading capacity and the effect these changes have on the solubility and dissolution rate. Therefore, when using surfactants in dissolution media forin vitrotesting of dosage forms, consideration must be given to the level of impurities present so that the results are consistent and reliable. Intrinsic dissolution rate, surface tension, or solubility measurements may be useful, convenient methods for identifying changes in the surfactant due to either degradation or lot‐to‐lot variability.
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相互作用的胶体对传输速率的影响。
DOI：
--
发表时间：
1964
期刊：
Journal of Pharmacy and Science
影响因子：
--
作者：
W. Higuchi
通讯作者：
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影响因子：
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作者：
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通讯作者：
W. Higuchi
表面张力和界面张力曲线的最小值
DOI：
10.1021/j150440a003
发表时间：
1945
期刊：
The Journal of Physical Chemistry
影响因子：
--
作者：
G. D. Miles
通讯作者：
G. D. Miles
影响因子：
3.8
作者：
GIBALDI, M;FELDMAN, S;WEINER, ND
通讯作者：
WEINER, ND
过量盐对表面活性剂 γ/log C 曲线中观察到的最小值的影响
DOI：
10.1021/j150572a053
发表时间：
1959
期刊：
The Journal of Physical Chemistry
影响因子：
--
作者：
S. Harrold
通讯作者：
S. Harrold