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

Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared by means of wet granulation method and solid dispersion method.Binders,suspending agents and other compositions involved in the formulation were optimized.The 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 rate.Taste 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 one.With 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 dogs.The 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,respectively.The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.

Effect of Jianpi therapy in treatment of chronic obstructive pulmonary disease:a systematic review

OBJECTIVE:To evaluate the efficacy of Jianpi therapy in Traditional Chinese Medicine (TCM) for treatment of chronic obstructive pulmonary disease (COPD) in stable phase by performing a systematic review and meta-analysis. METHODS: The literatures concerning randomized controlled trials (RCTs) and quasi-RCTs comparing TCM treatment plus Western Medicine (WM) treatment with TCM alone, orTCM treatment vs no treatment, placebo for stable phase of COPD were searched in PubMed (1990-December 2010), in English and using Chinese National Knowledge Infrastructure (CNKI, 1990-December 2010), Chinese Biomedical Database (1990-December 2010), Wangfang Database (1990-December 2010), and Weipu (VIP) Database in Chinese. The quality assessment and data extraction for RCTs were conducted by two reviewers independently. Jadad scale and allocation concealment were used to assess the quality of the included studies, and meta-analyses were conducted with the Collaboration's Revman 5.0 software. RESULTS: Seventeen RCTs or quasi-RCTs involving 1269 patients were included. The methodological quality was poor in all trials except one trial (Jadad score=4). In the meta-analysis, TCM-WM treatment was significantly superior to WM treatment in cure rate [OR=3.82, 95%CI (2.45, 5.95)], and the effective rate between TCM treatment and placebo also had significant difference [OR=4.31, 95%CI (2.35, 7.91)]. Moreover, pulmonary function of the patients in TCM-WM group and TCM group was significantly improved [forced vital capacity (FVC), P=0.01, quality of life, P<0.001]. CONCLUSION: The experience in TCM-WM treatment of COPD in stable phase was encouraging. The current evidence shows that TCM-WM treatment might be more efficient in effective rate, quaity of life, and FVC than WM treatment alone. But for forced expiratory volume in one second (FEV1) and FEV1/FVC, no matter TCM-WM treatment compared with WM treatment alone or TCM treatment compared with placebo, there was no significant difference, with no obvious adverse reactions. Due to the low methodological quality of trials included, more RCTs of high quality in large scale are required.