The main components in roseous liquid were analyzed qualitatively by GC-MS combination method.The results indicated that 6 organic compounds which had never been reported till now were separated from the extract of hawthorn kernel oil.

The objective of this study was to develop the dextromethorphan hydrobromide sustained-release (DMB-SR) tablets using floating technique to prolong the gastric residence time and compared their pharmacokinetic behavior with conventional sustained release tablets. DMB-SR floating tablets were prepared employing hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and hexadecanol as floating assistant agent. An orthogonal experiment design method was used to select the optimized formulation. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating characteristics, in vitro release and in vivo bioavailability. The optimized tablets were prepared with HPMC K4M 25mg, sodium bicarbonate 20mg and hexadecanol 18mg. The prepared tablets could float within 3min and maintain for more than 24h. The data of physical parameters were all lie within the limits. Drug release at 12h was more than 85%. The comparative pharmacokinetic study was performed by administration of the DMB-SR floating tablets and conventional DMB-SR tablets. The area under curve of plasma concentration–time (AUC) of floating tablets was slightly higher than that of reference tablets, Tmax was prolonged apparently. The results showed the floating tablets are a feasible approach for the sustained-release preparation of drugs, which have limited absorption sites in the stomach.

A method based on cloud point extraction was developed to determine benzoic acid in milk using high-performance liquid chromatography detection.The non-ionic surfactant Tween-20 was chosen as extraction solvent,the extraction parameters affecting extraction efficiency,such as concentrations of Tween-20 and(NH4)2SO4,equilibration temperature,equilibration time and pH were evaluated and optimized.The optimum CPE conditions were:3%(V/V)Tween-20,300g/L(NH4)2SO4,pH4,equilibration temperature 90℃ for 10min;chromatographic conditions were:mobile phase of ammonium acetate buffer-methanol 90:10(V/V),flow rate 1mL/min,the detection wave length 230nm.Under the above optimized conditions,the linearity of the calibration curve for benzoic acid was in the range of 0.2～2.0μg/mL,the limits of detection was 0.025μg/mL,the correlation coefficient was 0.9998.The recovery for the standard addition of the benzoic acid in the milk ranged from 98.90% to 100.16%,the relative standard deviations was in the range of 1.2%～2.5%.

In this study, solid lipid nanoparticles (SLNs) were successfully prepared by an ultrasonic and high-pressure homogenization method to improve the oral bioavailability of the poorly water-soluble drug cryptotanshinone (CTS). The particle size and distribution, drug loading capacity, drug entrapment efficiency, zeta potential, and long-term physical stability of the SLNs were characterized in detail. A pharmacokinetic study was conducted in rats after oral administration of CTS in different SLNs, and it was found that the relative bioavailability of CTS in the SLNs was significantly increased compared with that of a CTS-suspension. The incorporation of CTS in SLNs also markedly changes the metabolism behavior of CTS to tanshinone IIA. These results indicate that CTS absorption is enhanced significantly by employing SLN formulations, and SLNs represent a powerful approach for improving the oral absorption of poorly soluble drugs.

The object of this study was to prepare rosiglitazone maleate (RM) sustained-release floating microspheres and investigate their pharmacokinetics. RM microspheres were prepared with ethyl cellulose (EC) and octadecyl alcohol as the carrier materials by an emulsion-solvent diffusion method, and the properties of morphology in vitro floating capability, drug loading (DL), entrapment efficiency (EE), in vitro release and in vivo pharmacokinetics were investigated. The prepared microspheres had a completely spherical shape. The percentage of microspheres floating after 12 h was (91.45 +/- 1.62)%, and the DL and EE were (9.31 +/- 0.31)% and (89.55 +/- 1.65)% respectively. Pharmacokinetic studies demonstrated that the RM floating microspheres were superior to commercial tablets in terms of the decrease in peak plasma concentration and maintenance of RM concentration in plasma. The area under the curve of plasma concentration-time (AUC) of the floating microspheres was equivalent to that of reference tablets. The results showed that floating microspheres are a feasible approach for the sustained-release preparation of drugs which have limited absorption sites in the upper small intestine.

目的:制备银杏叶提取物微丸,并测定其体外释放度.方法:采用3种不同包衣材料(欧巴代Ⅱ、Eudragit L30D-55、Eu-dragit S 100)对银杏叶提取物进行包衣.采用离心造粒法制备成相应的包衣微丸;将3种包衣微丸按预设比例混合制成混合包衣微丸;采用pH梯度改变介质方式(0.1 mol·L-1盐酸、pH 5.8 PBS、pH 7.2 PBS)测定包衣微丸和混合包衣微丸的释放度.结果:3种不同包衣微丸分别在0.1 mol·L-1盐酸、pH 5.8 PBS、pH 7.2 PBS中可以迅速释放;混合包衣微丸在pH梯度改变介质中持续释放,约8 h释放完全.结论:该制备工艺可行,可为工业化生产提供理论依据.

Biomembrane-coated capillaries are prepared by coating different kinds of biomembranes including mice red cell membrane, human red cell membrane and S-180 cell membrane on the inner surface of the capillary, respectively. Effects of immobilized biomembrane amount, pH and biomembrane species on the interactions between drugs and biomembranes have been evaluated. The results showed that the chromatographic retention factor for each drug was essentially related to the amount of immobilized biomembrane, the pH and the type of biomembrane.

Objective: To develop a capillary gas chromatography method for the determination of nitrobenzene in milk slice. Method: Nitrobenzene was extracted by benzene. The analysis was performed on a SE-54 capillary column. The detector is FID. The temperature was elevated from 70-120°C,10. 00°C·min -1,120°C maintains 3min, 120°C-220°C, 20.00°C·min -1,220°C maintains 3min. The carrier gas was N 2. The flow rate was 2.0 mL·min -1. Result: Nitrobenzene was linear within the range from 0.2976 to 0. 7737μg·mL -1. The standard regression equation: Y = 30395x - 303.1, r=0.9994. The average recovery was 99.3%. Conclusion: This method has high sensitivity, good reproducibility and convenient for operation. The result is reliable and it provides nitrobenzene was accurate detected qualitatively and quantitatively by this method. Copyright CJI.

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) μg·mL-1 and(26.87±0.66)μg·mL-1 respectively;tmax were(3.67±0.52) h and(3.83±0.75) h;AUC0～24 were(181.20±5.12)μg·h·mL-1 and(187.58±5.29)μg·h·mL-1;AUC0～∞ were(184.34±5.35)、(191.19±4.87)μg·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.

目的研制氯沙坦钾氢氯噻嗪片,并对其稳定性进行考察。方法通过对处方的筛选和影响因素实验,研究各处方因素对片剂成型的影响。结果选择氯沙坦钾处方量1.6的倍微晶纤维素、预胶化淀粉为填充剂,3%聚乙烯吡咯烷酮为黏合剂,滑石粉、硬脂酸镁为混合润滑剂,低取代-羟丙基纤维素为崩解剂制备氯沙坦钾氢氯噻嗪片。经影响因素实验,在高温、高湿、强光条件下,外观性状、溶出度未发生明显变化,但有关物质、含量均略有下降,且在高湿条件下,吸湿明显,应避光、干燥保存。结论该工艺可制备出符合药品标准的稳定的制剂。