RESUMEN
OBJECTIVE: To study the pharmacokinetics and bioavailability of Ibuprofen Sustained Release Tablets in healthy volunteers.METHODS: A total of 18 male healthy volunteers were randomly divided into two groups.They were assigned to receive Ibuprofen Sustained Release Tablets(trial preparation) and Ibuprofen Sustained Release Capsules(reference preparation) respectively.The concentrations of ibuprofen in plasma were determined by RP-HPLC.The main pharmacokinetic parameters were obtained using 3p97 program.RESULTS: The Cmax of the two preparations were(25.43?0.78) ?g?mL-1 and(26.87?0.66)?g?mL-1 respectively;tmax were(3.67?0.52) h and(3.83?0.75) h;AUC0～24 were(181.20?5.12)?g?h?mL-1 and(187.58?5.29)?g?h?mL-1;AUC0～∞ were(184.34?5.35)、(191.19?4.87)?g?h?mL-1;MRT were(6.51?0.73)h and(6.80?0.48) h,respectively.The relative bioavailability of the sustained-release tablets was 103.7%.CONCLUSION: The ibuprofen sustained release tablets have remarkable sustained release efficacy.
RESUMEN
OBJECTIVE:To prepare Yinxingye extract pellets and study its in vitro drug release rate.METHODS:The Yinxingye extract were coated with 3 coating materials(opadryⅡ,Eudragit L30D-55 and Eudragit S 100,respectively)to be prepared into pallets by centrifugalized palletizing method;and the 3 different coated pallets were prepared into mixed pallets in an pre-designed ratio.The in vitro release of the 3 coated pallets and the mixed-coated pallets were determined by changing the pH-gradient of media(0.1 mol?L-1 hydrochloric acid,pH 5.8 PBS,pH 7.2 PBS).RESULTS:The pallets coated with 3 different coating materials released quickly in 0.1 mol?L-1 hydrochloric acid,pH 5.8 PBS and pH 7.2 PBS,and the pellets with mixed coating materials had a sustained release until a complete release within about 8 h in pH gradient-changed media.CONCLUSION:The preparation process is feasible and provides theoretic basis for industrial production.