自纳米乳化给药系统增强尼莫地平溶解度的研究

S. Gande, S. Reddy, B. D. V. R. N.
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引用次数: 0

摘要

为了提高尼莫地平的生物利用度,研制了尼莫地平自纳米乳化给药系统。在尼莫地平溶解度研究的基础上,优化了Peceol、Transcutol P和peg400作为制剂油、表面活性剂和助表面活性剂,并利用化学软件构建了伪三元图。制备了15种尼莫地平SNEDDS制剂,并对其粒径、乳化时间、释药率、透过率、体外溶出度及热力学稳定性进行了分析。采用FTIR对优化后的尼莫地平SNEDDS (F13)进行了药物与辅料的配伍研究。对它们进行了zeta电位、SEM和稳定性分析。优化后的尼莫地平SNEDDS处方粒径为25.9 nm, PDI为0.382,zeta电位为-12.7 mV。尼莫地平SNEDDS的SEM研究表明其呈球形,颗粒分布均匀。F13制剂释放度(98.25±4.77%)高于纯药(38.49±3.88%)。稳定性研究表明,其药物含量、药物释放、乳化性能和外观均无变化。因此,一种潜在的尼莫地平sndds制剂具有更高的溶出率、生物利用度和溶解度。
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Enhancement of Nimodipine Solubility by Self-Nano-emulsifying Drug Delivery System
Self-nanoemulsifying drug delivery system (SNEDDS) of Nimodipine was developed with the purpose of improving the bioavailability of the drug. Based on the results of Nimodipine solubility studies Peceol, Transcutol P and PEG 400 were optimized as oil, surfactant and co-surfactant for the formulation and Pseudo ternary plots was constructed by Chemix software. Fifteen formulations of Nimodipine SNEDDS prepared and analyzed for particle size, emulsification time, percentage drug release, percentage transmittance, in vitro drug dissolution studies and thermodynamic stability. The optimized Nimodipine SNEDDS formulation (F13) subjected to drug-excipient compatibility studies by FTIR. They are analyzed for zeta potential, SEM and stability. The particle size of optimized Nimodipine SNEDDS formulation was 25.9 nm, PDI is 0.382 and zeta potential -12.7 mV that are optimal for the stability of emulsion. SEM studies of Nimodipine SNEDDS indicated spherical shape and uniform particle distribution. The drug release of formulation F13 (98.25±4.77%) was higher than pure drug (38.49±3.88%). The stability studies indicated no change in drug content, drug release, emulsifying properties and appearance. Hence a potential SNEDDS formulation of Nimodipine developed with increased dissolution rate, bioavailability and solubility.
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