Optimization of the self micro-emulsifying drug delivery system of probucol by the central composite design-response surface methodology / 复旦学报（医学版）

Objective To determine the optimized self micro-emulsifying drug delivery system (SMEDDS) formulation of probucol. Methods According to the indexes of mean particle size, zeta-potential, solubility of probucol in blank SMEDDS and the dissolution percentage in 5 minutes of the preparations, the optimized formulation was determined by the central composite design-response surface methodology. Results When the correspondent percentage of olive oil in oil phase (W/W) was 0.33, the percentage of oil phase in formulation (W/W) was 0.5, and the ratio of surfactant to co-surfactant (W/W) was 2.0, respectively. The mean particle size, zeta-potential, solubility of probucol and dissolution percentage in 5 minutes of micro-emulsion was 92.7 nm, -17.38 mV, 65.17 mg/mL and 63.46%, respectively. Conclusions The optimized formulation of the probucol SMEDDS was obtained quickly and conveniently by the central composite design-response surface methodology. The method had a reliable predictability.

Transport of aripiprazole across Caco-2 monolayer model / 药学学报

This study aimed to investigate the transport characteristics of aripiprazole.A human intestinal epithelial cell model Caco-2 cell in vitro cultured had been applied to study the transport of aripiprazole.The effects of time,concentration of donor solutions,pH,temperature and P-glycoprotein inhibitor on the transport of aripiprazole were investigated.The determination of aripiprazole was performed by HPLC.It is concluded that aripiprazole is transported through the intestinal mucosa via a passive diffusion mechanism primarily,coex- isting with a carrier-mediated transport.The transport of aripiprazole is positively correlated to transport time, concentrations.The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole.

Bioavailability and pharmacokinetics of two sustained release formulations of mizolastine in healthy volunteers / 复旦学报（医学版）

Purpose The aim of this study was to compare the pharmacokinetic(PK) profile and relative bioavailability of two sustained release tablets containing 10 mg mizolastine in healthy, young Chinese volunteers. Methods A single oral dose of mizolastine was given under fasting conditions to volunteers aged from 21 to 24 years in this open-label, randomized, crossover study. A ten-day washout period was applied between each of the two formulations. Plasma samples were obtained before dosing and at predetermined time points after dosing up to 48 hours and were analyzed for plasma concentration with a high-performance-liquid chromatography-UV method. PK parameters representing the extent and the rate of absorption of mizolastine were obtained. An analysis of variance, 90% confidence intervals, and two one-sided tests were employed for statistical analysis of relative difference between the two formulations. Results According to the pharmacokinetic and statistical analysis, parameters were not statistically different between the two formulations except the peak concentration (cmax). The point estimates of the ratios of AUC0→t, AUC0→∞ of mizolastine were (101.26 + 9.82) % and (102.52 + 8.61)% with 90% confidence intervals (CIs) of 95. 5% - 106. 5% and 97. 7% -106.9% respectively, comprised in the stipulated 80% - 125% range; for cmax values, the ratios was 82.17% - 15.32% with the 90% CIs of 71. 7% - 91.1%, fell in the recommended range of 70% -143%. Conclusions The results indicate that there is no statistically significant difference in PK parameters except cmax between the two sustained release tablets of mizolastine. The 90% CIs of AUC0→t,AUC0→∞ and cmax are within the predefined range. Thus, the two sustained release tablets of mizolastine are considered bioequivalent and generally well tolerated.

Optimization of the intranasal powders of Panax Notoginseng Saponins by the central composite design-response surface methodology / 中成药

AIM: To determine the optimized intranasal powders formulation of Panax Notoginseng Saponins(PNS). METHODS: According to the indexes of the in vitro release rate in 1h and 12h of Rb1 and Rg1, bioadhesive intensity and the ciliary toxicity in situtoad palatal mucosa of the preparations, the optimized formulation was determined by the central composite design-response surface methodology. RESULTS: When the correspondent percentage of PNS, microcrystalline cellulose (MCC) and moderate viscosity hydroxypropyl cellulose (H-HPC) was 31%, 60% and 9%, respectively, the release rate in 1h and 12h of Rb1 and Rg1 was 6.82%, 53.25% and 83.4%, 95.09%, respectively. The adhesive time was 78min, and the lasting time of ciliary movement after the rinsing of the PNS powders was 94.84% to the physiological saline group which suggested the powder was almost no toxicity. CONCLUSIONS: The optimized formulation of the PNS intranasal powder was obtained quickly and conveniently by the central composite design-response surface methodology.