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Role of Polyethylene Glycol and Silica for Dissolution Enhancement of cefuroxime axetil: In-Vitro Performance Evaluation and Characterization

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Pharmacology & Pharmacy 2023年第5期14卷 156-175页

作者： Mst. Boby Aktar Bithy Milon Kumar Ghosh Ashim Kumar Md. Rafiqul Islam Khan Mir Imam Ibne Wahed Ranjan Kumar Barman Laboratory of Pharmaceutics Department of Pharmacy Faculty of Science University of Rajshahi Rajshahi Bangladesh Department of Pharmacy Faculty of Biological Sciences Islamic University Kushtia Bangladesh

cefuroxime axetil (CA) a widely used cephalosporin antibiotic displays low aqueous solubility and high membrane penetrability. This results in its solubility driven variable and/or low oral bioavailability and therapeutic efficacy as a major drawback. Thus, most of the goal of our study was to increase the solubility as well as dissolution rate of CA using the simple and cost-effective solid dispersion (SD) method. At first, the SD formulations of CA were prepared at various weight ratios of Carplex-67 and PEG-4000 by solvent evaporation technique. These new formulations were then subjected to an in-vitro drug release performance study and tested for physicochemical characterization to distinguish the thermal behavior, crystallinity, interactions phenomena, and surface morphology. Among the formulated cefuroxime axetil Solid Dispersion (CSD), CSD-8 which contained CA, Carplex-67, and PEG-4000 at the weight ratio 1:3:2, respectively showed the most significant (p in-vitro dissolution in water, Gastric Simulated Fluid (GSF), and Intestinal Simulated Fluid (ISF). This study also showed a significant (p < 0.001) increase in drug release compared to the marketed product. Therefore, it is supposed to be a promising alternative to conventional antimicrobial therapy.

关键词： Carplex-67 cefuroxime axetil Improved Dissolution PEG-4000 Solid Dispersion Solvent Evaporation

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Development and evaluation of taste-masked dry suspension of cefuroxime axetil for enhancement of oral bioavailability

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Asian Journal of Pharmaceutical Sciences 2013年第5期8卷 287-294页

作者： Yuqian Du Yinglei Zhai Juhong Zhang Chunnuan Wu Cong Luo Jin Sun Zhonggui He School of Pharmacy Shenyang Pharmaceutical UniversityNo.103Wenhua RoadShenyang 110016China School of Medical Devices Shenyang Pharmaceutical UniversityNo.103Wenhua RoadShenyang 110016China Institute of Biopharmaceuticals of Shandong No.989Xinluo StreetJinan 250000China

cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated *** work was to mask the bitter taste of CA and enhance its oral *** suspensions were prepared by means of wet granulation method and solid dispersion ***,suspending agents and other compositions involved in the formulation were *** differential scanning calorimetry(DSC)analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier,which contributed to an improvement of the dissolution *** evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above.A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations,i.e.,two self-made dry suspensions and the commercial *** a better release characteristic and a satisfying taste masking ability,the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle *** values of Cmax and AUC0e12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension,*** obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.

关键词： cefuroxime axetil Taste masking Dry suspension Solid dispersion Bioavailability

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cefuroxime axetil单剂量治疗单纯性尿道感染

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国外医药(抗生素分册) 1991年第2期 154-155页

作者：刘屏

尿道感染最常见的病原菌是大肠杆菌,近年来,产酶菌株增加,医院内50%的菌株对羟氨苄青霉素和氨苄青霉素耐药。同样磺胺/甲氧苄氨嘧啶耐药性也增加。cefuroximeaxetil是一种新的cefuroxime的酯,口服后,可迅速从胃肠道吸收,血清和尿液中均... 详细信息

尿道感染最常见的病原菌是大肠杆菌,近年来,产酶菌株增加,医院内50%的菌株对羟氨苄青霉素和氨苄青霉素耐药。同样磺胺/甲氧苄氨嘧啶耐药性也增加。cefuroximeaxetil是一种新的cefuroxime的酯,口服后,可迅速从胃肠道吸收,血清和尿液中均可达到较高的浓度。cefuroxime对酶的稳定性可以用于治疗尿道感染。本研究报告使用cefuroxime axetif单剂量治疗妇女单纯性

关键词：尿道感染 cefuroxime axetil 单纯性单剂量

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Accelerated Aqueous Solubility and Antibacterial Activity of cefuroxime axetil Using Microcrystalline Cellulose as Carrier

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Pharmacology & Pharmacy 2020年第8期11卷 159-173页

作者： Moushumi Tabassoom Salam Ashim Kumar Akito Hata Hiromu Kondo Md. Abdus Salam Mir Imam Ibne Wahed Md. Rafiqul Islam Khan Ranjan Kumar Barman Laboratory of Pharmaceutics Department of Pharmacy Faculty of Science University of Rajshahi Rajshahi Bangladesh Laboratory of Pharmaceutical Engineering & Drug Delivery Science School of Pharmaceutical Science University of Shizuoka Shizuoka Japan Department of Basic Medical Sciences Faculty of Medicine International Islamic University Malaysia Kuantan Malaysia

This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a β-lactamase-stable broad spectrum second generation cephalosporin through solid dispersion (SD) technique. For this purpose, CA loaded SDs (CSDs) were prepared by solvent evaporation method using different concentrations of microcrystalline cellulose (MCC) as carrier. The CSDs were characterized by in-vitro dissolution study, thermal analysis (DSC), crystallinity (PXRD), interactions (FTIR) and morphology (SEM). Among the formulations, CSD-2 showed the highest dissolution rate which was 2.59-fold higher than pure CA with a drug-carrier (CA: MCC) ratio of 1:3. Enhanced dissolution rate was attributed to conversion of drug from crystalline to amorphous state during preparation of SDs, which was validated by DSC, PXRD, FTIR and SEM analyses. Antibacterial activity of CSD-2 against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) showed 1.94- and 6.75-fold higher relative zone of inhibition (RZOI), respectively than pure CA. CSD-2 has been found to be the most effective optimized formulation in terms of both enhanced dissolution rate and antibacterial activity. Thus, it can be an effective alternative to conventional dosage forms of CA. However, further investigations are needed to validate its pharmacokinetic properties, in-vivo antibacterial efficacy and safety before recommending as a novel

关键词： cefuroxime axetil Dispersion Solubility Antibacterial Activity

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口服cefuroxime axetil与氨苄青霉素治疗急性无并发症淋病的疗效比较

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国外医学.皮肤病学分册 1988年第3期14卷 170-170页

作者：林跃

一些研究表明头孢氨呋肟(cefuroxime, CXM)治疗产与不产β-内酰胺酶的淋球菌引起的淋病均有效.cefuroxime axetil是CXM酯的药物前体,口服后该酯在肠粘膜水解,吸收良好,外周循环中仅可测得CXM. CXM的抗淋球菌活性及其药物前体的药动学性... 详细信息

一些研究表明头孢氨呋肟(cefuroxime, CXM)治疗产与不产β-内酰胺酶的淋球菌引起的淋病均有效.cefuroxime axetil是CXM酯的药物前体,口服后该酯在肠粘膜水解,吸收良好,外周循环中仅可测得CXM. CXM的抗淋球菌活性及其药物前体的药动学性质表明cefuroxime axetil

关键词：淋球菌淋病奈瑟氏球菌疗效比较并发症并发病疾病淋病性病 cefuroxime axetil

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