Optimization of ethanol reflux extraction process of Ziziphi Spinosae Semen- Schisandrae Sphenantherae Fructus based on network pharmacology combined with response surface methodology / 中国中药杂志

The present study optimized the ethanol extraction process of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus drug pair by network pharmacology and Box-Behnken method. Network pharmacology and molecular docking were used to screen out and verify the potential active components of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus, and the process evaluation indexes were determined in light of the components of the content determination under Ziziphi Spinosae Semen and Schisandrae Sphenantherae Fructus in the Chinese Pharmacopoeia(2020 edition). The analytic hierarchy process(AHP) was used to determine the weight coefficient of each component, and the comprehensive score was calculated as the process evaluation index. The ethanol extraction process of Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus was optimized by the Box-Behnken method. The core components of the Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus drug pair were screened out as spinosin, jujuboside A, jujuboside B, schisandrin, schisandrol, schisandrin A, and schisandrin B. The optimal extraction conditions obtained by using the Box-Behnken method were listed below: extraction time of 90 min, ethanol volume fraction of 85%, and two times of extraction. Through network pharmacology and molecular docking, the process evaluation indexes were determined, and the optimized process was stable, which could provide an experimental basis for the production of preparations containing Ziziphi Spinosae Semen-Schisandrae Sphenantherae Fructus.

Optimization of formulation of paclitaxel nanosuspension encapsulated by erythrocyte membrane based on Box-Behnken method / 中国中药杂志

In view of the longevity and innate immune escape of red blood cells, this study designed the red blood cell membrane-coated paclitaxel nanosuspension [RBC-(PTX)NS] and investigated its physicochemical properties and antitumor effect in vitro. Paclitaxel nanosuspension [(PTX)NS] was prepared by ultrasonic precipitation and then RBC-(PTX)NS by ultrasonic coating. The formulation of(PTX)NS was optimized with Box-Behnken method and indexes of particle diameter, zeta potential, and stability. The morphology, particle diameter, stability, in vitro dissolution, and antitumor effect of(PTX)NS and RBC-(PTX)NS were characterized. The results showed that the particle diameter and zeta potential were(129.38±0.92) nm and(-22.41±0.48) mV, respectively, for the optimized(PTX)NS, while(142.5±0.68) nm and(-29.85±0.53) mV, respectively, for RBC-(PTX)NS. Under the transmission electron microscope,(PTX)NS was spherical and RBC-(PTX)NS had obvious core-shell structure. RBC-(PTX)NS remained stable for 5 days at 4 ℃. The in vitro dissolution test demonstrated that the cumulative release rate of RBC-(PTX)NS reached 79% within 20 min, which was significantly higher than that(25%) of(PTX)NS(P<0.05). As evidenced by MTT assay, RBC-(PTX)NS highly inhibited the proliferation of HepG2 cells in a dose-dependent manner. The cell membrane-coated nano-preparation preparation method is simple and reproducible. It improves the solubility of PTX and endows RBC-(PTX)NS with higher stability and stronger cytotoxicity. Thus, it is a new method for the delivery of PTX via nanocrystallization.

Optimization of Preparation Process of Fast-Dissolving Microneedles by Box-Behnken Method / 中国药学杂志

OBJECTIVE: To optimize the formulation and preparation process of fast-dissolving PVP microneedles, and provide a high-quality carrier for PVP drug-loaded microneedle research. METHODS: On the basis of single factor, the needle tips dissolution time and insertion ratio were used as the evaluation indexes, and the optimal preparation process of microneedle was optimized by Box-Behnken method. RESULTS: From the single factor test and the Box-Behnken test, it was known that the optimum preparation conditions were as follows: the needle tip concentration was 0.70 g•mL-1, the temperature was 40 ℃, and the humidity was 40%. The microneedle height was 600 μm, the width was 200 μm, the pitch was 500 μm, quadrangular pyramid. The area of the microneedle patch was 0.56 cm2, the dissolution time in water was (41.00±3.74)s, and the insertion ratio was (93.19±5.25)%. CONCLUSION: The PVP fast-dissolving microneedles can be prepared simply and conveniently by the Box-Behnken method, which provides a reference for the preparation of further drug-loaded microneedles.

Preparation of andrographolide-loaded solid dispersions / 中成药

AIM To prepare the andrographolide-loaded solid dispersions.METHODS Differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD) were used for the analysis of solid dispersions previously prepared from the mixture of andrographolide and PVPK30 (1 ∶ 9) in autoclave.In addition to the evaluation index of in vitro dissolution rate,the influencing factors of pressure,temperature and reaction time were taken into consideration for the preparation optimization by Box-Behnken method.RESULTS Andrographolide was totally dispersed in solid dispersions in an amorphous state,manifesting an inhibited crystal diffraction peaks' formulation.Under the optimal conditions of 21.26 MPa for pressure,40.76 ℃ for temperature,and 1.13 h for reaction time,the in vitro dissolution rate was 85.49％.CONCLUSION After andrographolide is made into solid dispersions,its in vitro dissolution rate is obviously increased.

Optimization of ultrasonic extraction process for Xiaoqinglong granules by Box-Behnken in condition of medium scale / 中国中药杂志

This paper is to investigate the optimization conditions of ultrasonic technique for extraction process of Xiaoqinglong granules in medium scale. First of all, single factor experiment was used to determine the overall impact tendency and range of each factor； secondly, Box-Behnken method was used for optimization and detecting the content of paeoniflorin, ephedrine hydrochloride, glycyrrhizic acid of the liquid medicine. Their respective extraction rate was calculated and the comprehensive evaluation was carried out. The results were used as the evaluation basis for the efficacy of Xiaoqinglong granules ultrasonic extraction. The test results showed that the optimum extraction process of Xiaoqinglong granules by ultrasonic extraction was under the following conditions: ultrasonic power 600 W, liquid-solid ratio 10∶1, extraction for 31 min. Under this condition, the predicted value of extraction rate for Xiaoqinglong granules was 85.90%, and the test value was 85.87%. The mathematical model(P<0.01) established in this paper was significant, and can be used for the analysis and prediction of the ultrasonic extraction process of Xiaoqinglong granules.

Optimization of microwave extraction process of Corydalis Rhizoma by Box-Behnken in condition of pilot scale / 中草药

Objective: To optimize the conditions of microwave technique in extraction of effective ingredients in Corydalis Rhizoma in the condition of pilot scale. Methods: Medicinal materials processing, microwave power, solvent concentration, liquid to solid ratio, extraction time and so on were investigated by single factor test on the extraction rate of tetrahydropalmatine, and on this basis, using the method of Box-Behnken the microwave extraction process of Corydalis Rhizoma was optimized. Results: The optimum process of microwave extraction of Corydalis Rhizoma was as follows: using drinking water as the extraction solvent, microwave power of 7 kW, liquid to solid ratio of 10:1, and extraction for 21 min. Under these conditions, the extraction rate of tetrahydropalmatine predictive value was 83.60%, and the verified value was 83.74%; and compared with water extraction, dry extract rate decreased by 70%. Conclusion: The mathematical model established is significant (P<0.01) and can analyze and forecast the microwave extraction technology of Corydalis Rhizoma.