Formulations, hemolytic and pharmacokinetic studies on saikosaponin a and saikosaponin d compound liposomes.

The aim of this study was to develop and optimise a saikosaponin a and saikosaponin d compound liposome (SSa-SSd-Lip) formulation with reduced hemolysis and enhanced bioavailability. A screening experiment was done with Plackett-Burman design, and response surface methodology of five factors (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature, pH of PBS, and ultrasound time) was employed to optimise the mean diameter, entrapment efficiency of SSa and SSd, and the reduction of hemolysis for SSa-SSd-Lip. Under the optimal process conditions (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature and pH of PBS were 26.71, 4, 50 °C and 7.4, respectively), the mean diameter, the entrapment efficiency of SSa, the entrapment efficiency of SSd and the hemolysis were 203 nm, 79.87%, 86.19%, 25.16% (SSa/SSd 12.5 mg/mL), respectively. The pharmacokinetic studies showed that the SSa-SSd-Lip had increased circulation time, decreased Cl, and increased AUC, MRT and T1/2ß (p < 0.05) for both SSa and SSd after intravenous administration in comparison with solution.

[Kinetic spectrophotometric study on hemolytic process of polysorbate 80].

To establish kinetic assay method for the analysis of hemolysis and to investigate dynamic hemolytic process of polysorbate 80. The UV-VIS spectrum of heme changes when hemoglobin is released continuously during the hemolytic process. Therefore, dynamic hemolytic curve was determined as a new way to characterize the kinetic process of interaction between polysorbate 80 and red blood cells. The effect of polysorbate 80 on blood cells could be perfectly investigated by the hemolytic dynamics. Dynamic hemolytic parameters of polysorbate 80 were calculated according to the hemolytic curves. The constants of hemolytic rate and maximum hemolytic rate of polysorbate 80 had fine linear relationships at the range of 1-20 mg x mL(-1) and 5-20 mg x mL(-1), respectively. In comparison with the present official method such as macroscopic observation and static spectrophotometric methods, kinetic spectrophotometry has the advantages of real time, on-line determination, sensitive, objective, good reproducibility and 2-dimensional information acquired. Therefore, as a biological technique, kinetic spectrophotometry could be applied to evaluate the quality of polysorbate 80 and to screen other solubilizing excipients.

[Study on selecting the suitable solubilizing excipients for Shengmai injection].

OBJECTIVE: To select the suitable solubilizing excipients for Shengmai injection by the mean of hemolysis. METHODS: The hemolysis ratio of Shengmai injection, solubilizing excipients and different proportion of them were determined by absorption spectrometry. RESULTS: In the experimental concentration, Shengmai injection itself had no hemolytic effect. Polysorbate 80, Polyethylene glycol 400, Polyethylene glycol 600, Poloxamer 188 solution had no hemolytic effect to appear, but all the experimental concentrations of Polysorbate 20 had hemolytic effect. When combining with different proportion of Polysorbate 20, Polyethylene glycol 400, Polyethylene glycol 600, Poloxamer 188 and Polysorbate 80 of high concentration (0.75% - 1%), Shengmai injection had hemolytic effect. CONCLUSIONS: The absorption spectrometry is more reliable for the judgement of hemolysis than macroscopic observation, and it is helpful to improve the accuracy to select the solubilizing excipients for the TCM injection. Polysorbate 80 can be used as solubilizing excipient of Shengmai injection, which is safe in the concentration range of 0.1% to 0.5%.

[Research advances of macroporous resin].

We surveyed the literatures domestic and abroad, and summarized the physical and chemical characterizations as well as preparation and applications of macroporous resin. The research of physical parameter and chemical parameter includes the measurement of the organic residue, the application research includes the separation and purification methods of the phytochemical ingredients. Macroporous resin show its advantages in the field of phytochemical studies, traditional Chinese medicine development and production, but there exist some disadvantages in its performance and application. It's necessary to establish the quality standard and the technical specifications to promote the standardization of the research and the application of the macroporous resin.

[The research of the adsorption and desorption behaveior of macroporous resin for glycyrrhizic acid].

OBJECTIVE: To investigate the performance of static and dynamic adsorption and desorption of the three macroporous resins of AB-8, D-101 and H-103. METHOD: Compare the adsorption and desorption of the three macroporous resins for glycyrrhizic acid by determining the static adsorption, static desorption, dynamic adsorption and dynamic desorption through detecting the glycyrrhizic acid content by HPLC method. RESULT: The saturation of AB-8 is 0.75 g (crude drug)/mL (macroporous resins), the best elution reagent is 50% EtoH and it's eluation ration is 68.81% . The saturation of D-101 is 0.75 g (crude drug)/mL (macroporous resins), the best elution reagent is 60%EtoH and it's eluation ration is 64.67%. The saturation of H-103 is 0.5 g (crude drug)/mL (macroporous resins), the best elution reagent is 50%E-toH and it's elution ration is 51.18%. CONCLUSION: AB-8 and D-101 are the superior absorbents for glycyrrhizic acid.