头孢克肟与烟酰胺共晶:改善溶解度、溶出度和渗透性

IF 0.7 Q4 PHARMACOLOGY & PHARMACY INDONESIAN JOURNAL OF PHARMACY Pub Date : 2022-04-28 DOI:10.22146/ijp.2530
Abulkhair Abdullah, M. Mutmainnah, E. R. Wikantyasning
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引用次数: 2

摘要

头孢克肟是第三代头孢菌素类抗生素,其溶解度和渗透性较差。目的是比较干磨法(DG)和液助磨法(LAG)制备头孢克肟与烟酰胺共晶的方法。采用差示扫描量热法(DSC)、傅里叶变换红外(FTIR)、扫描电镜(SEM)、x射线衍射(XRD)等方法对共晶进行了表征。评价了共晶的溶解度、溶解速率和渗透速率等特性。溶度试验结果为:0.420±0.016(头孢克肟);0.675±0.016(共晶1:1 LAG);和0.632±0.016(共晶1:1 DG)。溶出度试验结果得到:186.55±4.18(头孢克肟);232.83±4.07(共晶1:1 LAG);228.82±10.07(共晶1:1 DG)。渗透性试验结果为:153.58±31.94(头孢克肟);306.22±77.81(共晶1:1 LAG);211.44±22.90(共晶1:1 DG)。DSC、FTIR、SEM、XRD等表征结果表明,用DG和LAG方法可与烟酰胺形成共晶,且其溶解度、溶出度和渗透性均增加。与共晶1:1 DG相比,共晶1:1 LAG效果更好。
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Cocrystals of Cefixime with Nicotinamide: Improved Solubility, Dissolution, and Permeability
Cefixime is a third-generation cephalosporin antibiotic with poor solubility and permeability. The aim was to compared between Dry Grinding (DG) and Liquid-Assisted Grinding (LAG) methods to formed cocrystal of cefixime with nicotinamide. Cocrystal was prepared in 1:1 molar ratio and was characterizated by differential scanning calorimetry (DSC), fourier transform infra-red (FTIR), scanning electron microscopy (SEM), x-ray diffraction (XRD) methods. Cocrystal properties such as solubility, dissolution rate, and permeation rate were evaluated. The solubility test results obtained: 0.420 ± 0.016 (cefixime); 0.675 ± 0.016 (cocrystal 1:1 LAG); and 0.632 ± 0.016 (cocrystal 1:1 DG). The dissolution test results obtained: 186.55 ± 4.18 (cefixime); 232.83 ± 4.07 (cocrystal 1:1 LAG); and 228.82 ± 10.07 (cocrystal 1:1 DG). The permeability test results obtained: 153.58 ± 31.94 (cefixime); 306.22 ± 77.81 (cocrystal 1:1 LAG); and 211.44 ± 22.90 (cocrystal 1:1 DG). Cefixime can be formed into cocrystal with nicotinamide by DG and LAG methods according to the results of characterization using DSC, FTIR, SEM, and XRD accompanied by the increasing solubility, dissolution, and permeability. Cocrystal 1:1 LAG showed better result compared to cocrystal 1:1 DG.
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来源期刊
INDONESIAN JOURNAL OF PHARMACY
INDONESIAN JOURNAL OF PHARMACY PHARMACOLOGY & PHARMACY-
CiteScore
1.20
自引率
0.00%
发文量
38
审稿时长
12 weeks
期刊介绍: The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas Gadjah Mada (UGM) Yogyakarta Indonesia in collaboration with IAI (Ikatan Apoteker Indonesia or Indonesian Pharmacist Association) and only receives manuscripts in English. Indonesian Journal of Pharmacy is Accredited by Directorate General of Higher Education. The journal includes various fields of pharmaceuticals sciences such as: -Pharmacology and Toxicology -Pharmacokinetics -Community and Clinical Pharmacy -Pharmaceutical Chemistry -Pharmaceutical Biology -Pharmaceutics -Pharmaceutical Technology -Biopharmaceutics -Pharmaceutical Microbiology and Biotechnology -Alternative medicines.
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