Study on formulation of liquid-solid compressed tablets of total triterpenoids from Sclerotii Poriae Cortex / 中草药

Objective: To improve the dissolution rate of total triterpenoids from Sclerotii Poriae Cortex. Central composite design response surface methodology was used to optimize formulation of liquid-solid compressed tablets. Methods: The types and ratio of excipients were determined by preliminary test and single factor experiments. Central composite design response surface methodology was used in the optimization of formulation, with dissolution rate as the index. Liquisolid compacts powders, crude drugs, and excipients were characterized by differential scanning calorimetry (DSC). Results: The best prescription was as follow: Liquid ratio was 1:1.67; R value was 18.25; Disintegrating agent was 8%; The ratio of PVPPXL-10 and CMSNa was 1.27 and the tablets hardness was 40-50 N. DSC showed that the characteristic peaks of drug in liquisolid tablets had vanished, and suggested that drugs might be present in liquid-solid compressed tablets as amorphous substance. Conclusion: The formulation of liquid-solid compressed tablet is reasonable. Liquisolid compacts can increase the dissolution rate of total triterpenoids from Sclerotii Poriae Cortex, and suggest that drugs may be present in liquid-solid compressed tablets as amorphous substance.

Optmization for cutting procedure of astragali radix with Box-Behnken design and response surface method / 中国中药杂志

Astragali Radix was firstly recorded in the "Shen Nong's Herbal Classic" as a top-grade and commonly used traditional Chinese medicine. Its frequently used slices include raw Astragali Radix and honey-processed products. In current studies, many reports were made on honey-processed Astragali Radix, whereas fewer study reports were made on the cutting process of Astragali Radix. Currently, because Astragali Radix is primarily cut by drug workers according to their operating experience, but with out specific cutting parameters, it is easy to cause the loss or mildew of active ingredients. As a result, the quality of Astragali Radix circulated in the market is not guaranteed, and the quality of their slices and preparations are hard to be controlled, which seriously impact the clinical efficacy. In response, this experiment was performed, in which the optimum cutting process of Astragali Radix was taken as the study objective, the Box-Benhnken central composite design in the response surface analysis was adopted, and the content and appearance character of astragaloside and calycosin-7-glucoside were regarded as the study indicators. Three factors, namely the softening time, the drying temperature and the drying time, were selected to optimize the cutting process of Astragali Radix and obtain the optimum cutting process parameters as follows: the softening time was 3 hours, the drying temperature was 50 degrees C, and the drying time was 4 hours. According to the verification test, the Astragali Radix cutting process is steady and feasible, which has certain significance for normalizing the cutting process of Astragali Radix.

Plasma concentration and pharmacokinetics of ursolic acid carried in self-microemulsifying drug delivery system in rats studied by UPLC-MS/MS / 药学学报

This study is to report the establishment of an UPLC-MS/MS method for the determination of plasma concentration of UA carried in self-microemulsifying drug delivery system (SMEDDS) and its pharmacokinetics in rats. It was used for determination and analysis when serum with internal standard was extracted from C18 solid-phase column. Acquity UPLC BEH C18 column (100 mm x 2.1 mm, 1.7 microm) was used for separation. The mobile phase was acetonitrile -0.1% ammonia with gradient elution at the flow rate of 0.2 mL x min(-1). The column temperature was 40 degrees C and the detection wave length was 210 nm. It was detected by negative ion using electrospray ionization source (ESI) and scanned by multiple reaction ion monitoring (MRM) mode. The liner relationship of UA was very good in the range of 1.19-3 815.00 ng x mL(-1) (r = 0.999 0). Recovery rate of different concentrations were 87.42%-89.95%. The precision of inter-day and intra-day were less than 11%. The method developed in our study was proved to be sensitive, rapid and simple. It is suitable for the pharmacokinetic study of UA-SMEDDS in rats.

Optimization of Scutellaria baicalensis extraction process by orthogonal experiment combined with pharmacodynamic index / 中国中药杂志

To optimize the Scutellaria baicalensis extraction process, the filter paper method and the bacteriostatic ratio method were adopted to determine the in vitro bacteriostatic efficacy of water extracts and 60% alcohol extracts from S. baicalensis. The quantitative analysis of multi-components by single-marker (QAMS) was used to determined the contents of four active components, baicalin, wogonoside, baicalein and wogonin. In addition, with the bacteriostatic ratio and the overall desirability of the contents of four active components as indexes, the orthogonal experiment was adopted to detect the effect of water addition, extraction frequency and extraction time. The optimal extraction process was to add 12 times of water for the first time, 10 times of water for the second time, extract for 2 time, 2 h for each time. This optimization process is stable and feasible, with a higher bacteriostatic ratio in extracts.