Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability.
Influence of Solid Drug Delivery System Formulation on Poorly Water-Soluble Drug Dissolution and Permeability.
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DOI：
10.3390/molecules200814684
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发表时间：
2015-08-13
期刊：
影响因子：
--
通讯作者：
Ibrić S
中科院分区：
文献类型：
--
作者：
Krstić M;Popović M;Dobričić V;Ibrić S
大多数药物的溶出度较低，这是其吸收的限制步骤。在本手稿中，评估了固体分散体（SD）、固体自微乳化药物递送系统（S-SMEDDS）和固体自纳米乳化药物递送系统（S-SNEDDS）作为提高卡马西平溶出度的潜在制剂策略。使用PAMPA试验评估溶出速率增加对卡马西平渗透性的影响。在S-SMEDDS和S-SNEDDS配方中，液体SMEDDS/SNEDDS和固体载体(Neusilin® UFL2)的比例是变化的，而卡马西平含量是恒定的。在 SD 配方中，卡马西平和 Neusilin® UFL2 的比例是不同的。对卡马西平最佳溶出度的制剂（SD_1:6、SMEDDS_1:1、SNEDDS_1:6）进行相互比较，通过 DSC、PXRD 和 FT-IR 分析对这些制剂进行表征，并进行 PAMPA 测试。与纯卡马西平和速释卡马西平片剂相比，所有制剂的溶出度均显着增加。制剂S-SMEDDS_1:1显示出最快的卡马西平释放速率和渗透性。 DSC、PXRD 和 FT-IR 分析证实，在 S-SMEDDS 和 S-SNEDDS 中，卡马西平仍保持多晶型物 III 型，并且在 SD 制剂中转变成无定形状态。与纯卡马西平相比，所有制剂均显示卡马西平的渗透性增加。
The majority of drugs have a low dissolution rate, which is a limiting step for their absorption. In this manuscript, solid dispersions (SD), solid self-microemulsifying drug delivery systems (S-SMEDDS) and solid self-nanoemulsifying drug delivery systems (S-SNEDDS) were evaluated as potential formulation strategies to increase the dissolution rate of carbamazepine. Influence of increased dissolution rate on permeability of carbamazepine was evaluated using PAMPA test. In S-SMEDDS and S-SNEDDS formulations, the ratio of liquid SMEDDS/SNEDDS and solid carrier (Neusilin® UFL2) was varied, and carbamazepine content was constant. In SD formulations, the ratio of carbamazepine and Neusilin® UFL2, was varied. Formulations that showed the best dissolution rate of carbamazepine (SD_1:6, SMEDDS_1:1, SNEDDS_1:6) were mutually compared, characterization of these formulations was performed by DSC, PXRD and FT-IR analyses, and a PAMPA test was done. All formulations have shown a significant increase in dissolution rate compared to pure carbamazepine and immediate-release carbamazepine tablets. Formulation S-SMEDDS_1:1 showed the fastest release rate and permeability of carbamazepine. DSC, PXRD and FT-IR analyses confirmed that in S-SMEDDS and S-SNEDDS carbamazepine remained in polymorph form III, and that it was converted to an amorphous state in SD formulations. All formulations showed increased permeability of carbamazepine, compared to pure carbamazepine.
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影响因子：
3.3
作者：
Shakeel, Faiyaz;Baboota, Sanjula;Shafiq, Sheikh
通讯作者：
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影响因子：
5.8
作者：
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影响因子：
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作者：
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通讯作者：
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DOI：
10.1016/s0731-7085(00)00262-4
发表时间：
2000-08-01
影响因子：
3.4
作者：
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通讯作者：
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影响因子：
3.7
作者：
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通讯作者：
Kalinoski, Andrea L.