溶解
Zeta电位
溶解度
化学工程
材料科学
过饱和度
粒径
生物利用度
结晶
溶剂
埃法维伦兹
水溶液
纳米晶
降水
纳米颗粒
色谱法
化学
纳米技术
有机化学
人类免疫缺陷病毒(HIV)
药理学
气象学
病毒载量
工程类
物理
家庭医学
医学
抗逆转录病毒疗法
作者
Gabriela Julianelly Sartori,Livia Deris Prado,Helvécio Vinícius Antunes Rocha
出处
期刊:Brazilian Journal of Pharmaceutical Sciences
[SciELO]
日期:2022-01-01
卷期号:58
被引量:1
标识
DOI:10.1590/s2175-97902022e18800
摘要
Efavirenz is one of the most commonly used drugs in HIV therapy. However the low water solubility tends to result in low bioavailability. Drug nanocrystals, should enhance the dissolution and consequently bioavailability. The aim of the present study was to obtain EFV nanocrystals prepared by an antisolvent technique and to further observe possible effect, on the resulting material, due to altering crystallization parameters. A solution containing EFV and a suitable solvent was added to an aqueous solution of particle stabilizers, under high shear agitation. Experimental conditions such as solvent/antisolvent ratio; drug load; solvent supersaturation; change of stabilizer; addition of milling step and solvents of different polarities were evaluated. Suspensions were characterized by particle size and zeta potential. After freeze- dried and the resulting powder was characterized by PXRD, infrared spectroscopy and SEM. Also dissolution profiles were obtained. Many alterations were not effective for enhancing EFV dissolution; some changes did not even produced nanosuspensions while other generated a different solid phase from the polymorph of raw material. Nevertheless reducing EFV load produced enhancement on dissolution profile. The most important modification was adding a milling step after precipitation. The resulting suspension was more uniform and the powder presented grater enhancement of dissolution efficacy.
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