Optimization of water extraction process of Maxing kechuan granules / 中国药房

OBJECTIVE To optimize the water extraction process of Maxing kechuan granules. METHODS With the contents of ephedrine hydrochloride， bergenin， prim-O-glucosylcimifugin， 5-O-methylvisamin， naringin and hesperidin and the rate of extraction as the evaluation indexes， the weight was determined by the analytic hierarchy process（APH）-entropy weight method， and the comprehensive score was calculated as the response value. Based on the single-factor test， the Box-Behnken response surface method was used to investigate the factors， and the best water extraction process of Maxing kechuan granules was optimized； process validation was also carried out. RESULTS The best water extraction process of Maxing kechuan granules optimized was as follows： soaking for 40 minutes， adding 8 times water， and extracting for 180 minutes. After three validation tests， the comprehensive score was 94.82 （RSD＝0.96%， n＝3）， which had a small difference from the predicted value of 94.64. CONCLUSIONS The water extraction process of Maxing kechuan granules is stable and reliable， which can provide a reference for the development of the preparation.

Optimization of extraction process of Sarcandra glabra by combination of entropy weight method with Box-Behnken response surface method / 中国药房

OBJECTIVE To optimize the extraction process of Sarcandra glabra. METHODS The contents of rosmarinic acid and isofraxidin in S. glabra were determined by HPLC； ultrasonic time， ultrasonic temperature， solid-liquid ratio （mL/g） and methanol volume fraction were investigated by single factor test. Based on the results of single factor test， experimental scheme was designed by Box-Behnken response surface method， and the entropy weight method was used to assign the weight of each index and calculate the comprehensive score. Taking the comprehensive score as the evaluation index， the extraction process of S. glabra was optimized， and then optimized extraction process was verified. RESULTS The optimal extraction technology of S. glabra included ultrasonic time of 40 min， ultrasonic temperature of 45 ℃， liquid-solid ratio of 50∶1， methanol volume fraction of 70%. The results of 3 times of verification experiment showed that average comprehensive score was 0.988 6， and the RSD was 0.50%. The deviation between the actual value and the predicted value （0.985 1） of each comprehensive score was within ±1%. CONCLUSIONS The optimized extraction method is stable， feasible and repeatable， which can provide reference for extraction of S. glabra.

Processing Magnoliae Officinalis Cortex with ginger juice: process optimization based on AHP-CRITIC weighting method and composition changes after processing / 中国中药杂志

The weight coefficients of appearance traits, extract yield of standard decoction, and total content of honokiol and magnolol were determined by analytic hierarchy process(AHP), criteria importance though intercrieria correlation(CRITIC), and AHP-CRITIC weighting method, and the comprehensive scores were calculated. The effects of ginger juice dosage, moistening time, proces-sing temperature, and processing time on the quality of Magnoliae Officinalis Cortex(MOC) were investigated, and Box-Behnken design was employed to optimize the process parameters. To reveal the processing mechanism, MOC, ginger juice-processed Magnoliae Officinalis Cortex(GMOC), and water-processed Magnoliae Officinalis Cortex(WMOC) were compared. The results showed that the weight coefficients of the appearance traits, extract yield of standard decoction, and total content of honokiol and magnolol determined by AHP-CRITIC weighting method were 0.134, 0.287, and 0.579, respectively. The optimal processing parameters of GMOC were ginger juice dosage of 8%, moistening time of 120 min, and processing at 100 ℃ for 7 min. The content of syringoside and magnolflorine in MOC decreased after processing, and the content of honokiol and magnolol followed the trend of GMOC>MOC>WMOC, which suggested that the change in clinical efficacy of MOC after processing was associated with the changes of chemical composition. The optimized processing technology is stable and feasible and provides references for the modern production and processing of MOC.

Study on the extraction of polysaccharides from Dendrobium officinale and its improvement effect on acute lung injury in mice / 中国药房

OBJECTIVE To optimize the extraction process of polysaccharides from Dendrobium officinale， and preliminarily study its effect on acute lung injury （ALI） in mice. METHODS Using D. officinale as raw material， the polysaccharides were extracted from D. officinale by ultrasonic-assisted hot water immersion. Using the extraction rate of D. officinale polysaccharides as response value， the single-factor experiments and Box-Behnken response surface method were used to optimize the ratio of material to liquid， extraction time and extraction temperature. ALI mice were induced by lipopolysaccharide. Using prednisone acetate （5 mg/kg） as the positive control， the effects on the mass ratio of wet and dry lung and pathological changes of lung tissue （HE staining and Masson staining） of low-dose， medium-dose and high-dose D. officinale polysaccharides （50，100，200 mg/kg） were investigated. RESULTS The optimal extraction technology of D. officinale polysaccharides was as follows： the ratio of material to liquid was 1∶25 （g/mL）， the extracting time was 1 h， and the extracting temperature was 58 ℃ . Under these conditions， the average extraction rate of D. officinale polysaccharides was 37.75% （RSD＝1.12%，n＝3）， the relative error of which with predicted value （38.63%） was 2.28%. Compared with the model group， the ratios of wet and dry lung in the positive control group and D. officinale polysaccharides groups were all decreased significantly （P＜0.05 or P＜0.01）， and the pathological changes in lung tissue （severe destruction of alveolar structure， significant widening of alveolar septa， extensive infiltration of inflammatory cells and proliferation of fibroblasts） were alleviated to varying degrees. CONCLUSIONS The optimal extraction process of D. officinale polysaccharides is feasible； the obtained polysaccharide extract has a certain improvement effect on ALI in mice.

Optimization of molding process and physical fingerprint of Shuangye pipa granules based on QbD concept / 中国药房

OBJECTIVE To optimize the molding process of Shuangye pipa granules based on the concept of quality by design （QbD） and analyze its physical fingerprint. METHODS The dry extract of Shuangye pipa granules was used as the main drug. The retention rate of total flavonoid， moisture absorption rate， dissolution rate， angle of repose and molding rate of the granules were selected as evaluation indexes. The single-factor test combined with the entropy weight method and Box-Behnken response surface design was used to optimize the molding process， and validation test was conducted. The physical fingerprints of 10 batches of Shuangye pipa granules prepared by the optimal process were comprehensively analyzed by eight secondary physical indexes （relative homogeneity， moisture， moisture absorption rate， Hausner ratio， angle of repose， bulk density， tap density and porosity）. RESULTS The optimal molding process of Shuangye pipa granules was as follows： soluble starch-maltodextrin-mannitol was 1∶1∶1 （m/m/m）， 95% ethanol was as wetting agent and the amount of it was 37%， the drug-assisted ratio was 1∶0.8 （m/m）， the drying temperature was 59 ℃， drying time was 28 min. The results of 3 validation tests showed that the average comprehensive score was 0.879 6， the RSD of which with prediction value （0.881 9 score） was 1.97%. The similarity between the physical fingerprints of 10 batches of Shuangye pipa granules and the control physical fingerprint was higher than 0.99. CONCLUSIONS The optimized molding process of Shuangye pipa granules is stable and feasible， and the physical property of Shuangye pipa granules is stable and controllable.

Optimization of the formulation of a porcine fibrin patch / 中国药房

OBJECTIVE To optimize the formulation of a porcine fibrin patch （abbreviated as “DBT”）. METHODS Based on single-factor tests， with the contents of fibrinogen， thrombin and collagen before freeze-drying as the factors， with the overall desirability （OD） value of adhesion strength， holding viscosity and water absorption as response value， the formulation of DBT was optimized by Box-Behnken-response surface methodology， and the verification tests were conducted. RESULTS According to the results of the single factor tests and Box-Behnken-response surface methodology， combined with the actual production， the optimal formulation of DBT was 6.5 mg/cm2 of fibrinogen， 8.0 IU/cm2 of thrombin and 5.6 mg/mL of collagen. The average OD value of 3 validation tests was 0.726 6 （RSD＝0.58%， n＝3）， and the relative error of which with the predicted value （0.733 0） was －0.87%. CONCLUSIONS The optimal formulation of DBT is stable and feasible.

Formulation optimization of emodin nanostructured lipid carriers by Box-Behnken response surface method and in vitro quality evaluation / 中国中药杂志

Emodin nanostructured lipid carriers(ED-NLC) were prepared and their quality was evaluated in vitro. Based on the results of single-factor experiments, the ED-NLC formulation was optimized by Box-Behnken response surface method with the dosages of emodin, isopropyl myristate and poloxamer 188 as factors and the nanoparticle size, encapsulation efficiency and drug loading as evaluation indexes. Then the evaluation was performed on the morphology, size and in vitro release of the nanoparticles prepared by emulsification-ultrasonic dispersion method in line with the optimal formulation, i.e., 3.27 mg emodin, 148.68 mg isopropyl myristate and 173.48 mg poloxamer 188. Under a transmission electron microscope(TEM), ED-NLC were spherical and their particle size distribution was uniform. The particle size of ED-NLC was(97.02±1.55) nm, the polymer dispersion index 0.21±0.01, the zeta potential(-38.96±0.65) mV, the encapsulation efficiency 90.41%±0.56% and the drug loading 1.55%±0.01%. The results of differential scanning calorimeter(DSC) indicated that emodin may be encapsulated into the nanostructured lipid carriers in molecular or amorphous form. In vitro drug release had obvious characteristics of slow release, which accorded with the first-order drug release equation. The fitting model of Box-Behnken response surface methodology was proved accurate and reliable. The optimal formulation-based ED-NLC featured concentrated particle size distribution and high encapsulation efficiency, which laid a foundation for the follow-up study of ED-NLC in vivo.

Optimization of the Honey-stir-fired Technology of Chelidonium majus / 中国药房

OBJECTIVE：To optimize the honey-stir-fried technology of Chelidonium majus . METHODS ：Taking the mass ratio of water to honey ，the ratio of honey water to C. majus ，stir-fired temperature ，stir-fired time as the factors ，the total contents of chelidonine ，coptisine hydrochloride ，sanguinarine，berberine，chelerythrine as response values ，Box-Behnken response surface method was used to optimize the processing technology ，and valifation test was conducted. RESULTS ：The optimum process conditions were as follows the ratio of water to refined honey 1∶1.9（g/g），the ratio of honey water to C. majus 21∶100（g/g）， stir-fried temperature 122 ℃，stir-fried time 10.40 min. After 3 times of validation ，average total contents of 5 components was 10.37 mg/g（RSD＝0.23％），relative error of which with predicted value （10.39 mg/g）was 0.19％. CONCLUSIONS ：The optimized honey-stir-fried technology of C. majus is stable and feasible.

Optimization of extraction process of Compound Guizhi Shaoyao Zhimu Granules by combination of response surface methodology with entropy weight method / 中草药

Objective: To optimize the extraction process parameters of Guizhi Shaoyao Zhimu Granules (GSZG). Methods: Using high performance liquid chromatography and Elisa, the extraction rate of trans-cinnamaldehyde, paeoniflorin, mangiferin, glycyrrhizic acid, the dry extract yield of extracted herbs and inflammatory factor IL-6 were comprehensively evaluated. The information entropy weighting method was used to determine the objective weight of each index, and response surface methodology was adopted to optimize the extraction process parameters of GSZG. Results: The method had good linear relationship within the range of 3.27-104.64 μg/mL for trans-cinnamaldehyde (r = 0.999 9), 8.16-261.03 μg/mL for paeoniflorin (r = 1.000 0), 1.39-89.27 μg/mL for mangiferin (r = 0.999 9), and 1.00-33.00 μg/mL for glycyrrhizic acid ammonium salt (r = 0.999 9). Guizhi-Shaoyao-Zhimu extraction had the effect of inhibiting the proliferation of MH7A cells (molded by TNF-α) with IC50 of 1.02 mg/mL, and had anti-inflammatory activity. Entropy method was more scientific, reasonable and stable. According to the comprehensive scoring results and practical situation, it was determined that the best extraction process of the preparation was to add 16 times the amount of water, and decocted three times for 1 h each time. The RSD of the predicted value was less than 3% compared with the measured value. Conclusion: The preferred process has high extraction rate, with good stability and repeatability, which is suitable for the mass production of GSZG.

Preparation and pharmacodynamic study of Oral Disintegration Tablets of "Hugan I" / 中草药

Objective: To optimize the prescription and preparation process of "Hugan I" Orally Disintegrating Tablets, and investigate its efficacy against acute liver injury in mice. Methods: Single factor method was used for disintegrants, lubricants, and fillers screening. Taking the appearance, hardness, friability and disintegration time of the tablets as the comprehensive evaluation index, the dosage of disintegrant, micro-silica gel and magnesium stearate was selected as the investigation factor. The Box-Behnken response surface method was used to optimize the orally disintegrating tablets. Acetaminophen (APAP, 500 mg/kg) was used to replicate acute liver injury model by one-time high-dose intragastric administration to investigate the effects of orally disintegrating tablets on the activities of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in serum, the content of glutathione (GSH) and malondialdehyde (MDA) and morphological changes in liver tissue. Results: The optimal prescription was as following: dry paste powder 22.00%, microcrystalline cellulose 18.00%, sorbitol 20.00%, mannitol 16.00%, Aspartame 0.50%, citric acid 0.50%, disintegration agent L-HPC 20.00%, micro-powder silica gel 2.50% and magnesium stearate 0.50%. The hardness of the orally disintegrating tablets was 4-7 kg, the mean disintegration time was about 50 s, and the mean friability was around 0.85%. Compared with the model group, there were significant differences (P < 0.01) in Biphenyl diester control group, "Hugan I" Decoction group and "Hugan I" Orally Disintegrating Tablets group, and the levels of ALT and AST in the serum of the mice were significantly decreased, The content of MDA in the liver tissue was decreased, which improved the damage of APAP to liver tissue. Conclusion: The formulation of the "Hugan I" Orally Disintegrating Tablet is feasible and easy to operate, which achieves the same effect with "Hugan I" Decoction that effectively prevent liver damage caused by acetaminophen with no significant differences.

Formulation Optimization of Compound Renshen Jianti Formulation and Study on Its Anti-fatigue Activity and Acute Toxicity / 中国药房

OBJECTIVE：To optimi ze the ratio of four comp onents of Compound renshen jianti formulation （Panax ginseng ， Dioscorea oppositifolia ，Lycium barbarum fruit，Alpinia oxyphylla ），and to investigate its anti-fatigue activity and acute toxicity. METHODS：The water extract of Compound renshen jianti formulation was prepared by water extraction ，concentration and decompression drying. By single factor tests ，using weight-bearing swimming time as index ，the effects of four factors were investigated，such as the amount of P. ginseng ，D. oppositifolia ，L. barbarum fruit，A. oxyphylla . On the basis of single factor tests，using comprehensive score of weight-bearing swimming time ，serum urea nitrogen content ，liver glycogen content and AUC of blood lactate after exercise as index ，the formulation was optimized by Box-Behnken response surface method. The mice was divided into blank control group （water），positive control group （Renshen hongjingtian capsules ，0.135 g/kg）and compound low-dose，medium-dose and high-dose groups [the optimal ratio of Compound renshen jianti formulation extract （called“optimal compound formulation ”for short ）4.08，8.16，12.24 g/kg，by crude drug] ，intragastric administration of drug or distilled water 20 mL/kg，once a day ，for consecutive 30 d. The weight-bearing swimming time ，the contents of serum urea nitrogen ，liver glycogen and blood lactate AUC after exercise were used to optimize its anti-fatigue activity of optimal compound formulation. The comprehensive score was calculated based on the measured data of mice in the compound formulation middle-dose group ， and the difference between it and the theoretical prediction value was compared. The mice were given optimal compound formulation intragastrically （total dose 16.00 g/kg， by extract）. The general state ， body mass change ， toxic characteristics and death of mice were observed and recorded for 14 days. Median lethal dose （LD50）and maximum tolerated dose （MTD）were measured. RESULTS ：The optimal formulation ratio of Compound renshen jianti formulation included that P. ginseng 1.5 g，D. oppositifolia 10 g，L. barbarum fruit 10 g，A. oxyphylla 3 g. Results of anti-fatigue activity validation test showed that the optimal compound formulation could significantly prolonged weight-bearing swimming time ，reduced serum content of urea nitrogen ，blood lactate content and its AUC （except for low-dose group ），while significantly increased the content of liver glycogen （P＜0.05 or P＜0.01）. Average comprehensive score of medium-dose group was 96.95，which was only 0.06％ different from the theoretical prediction value of 97.01. The results of acute toxicity test showed that there was no death in mice. The oral MTD of the optimal compound formulation was more than 15 g/kg，which was non-toxic. CONCLUSIONS ：The optimal Compound renshen jianti formulation has effective anti-fatigue activity of mice ，and has no significant toxic effect.

Preparation and in vitro quality evaluation of self-microemulsion co-loaded with tenuifolin and β-asarone / 中国中药杂志

To prepare and optimize the self-microemulsion co-loaded with tenuifolin and β-asarone(TF/ASA-SMEDDS) and evaluate its quality. The prescription compositions of TF/ASA-SMEDDS were screened by solubility test, single factor test and pseudo-tern-ary phase diagram, and the prescriptions were further optimized by Box-Behnken response surface method, with the drug loading and particle size as the evaluation indexes. Then the optimized TF/ASA-SMEDDS was evaluated for emulsified appearance, particle size, morphology and drug release in vitro. The optimized prescription for TF/ASA-SMEDDS was as follows: caprylic citrate triglyceride polyoxyethylene castor oil-glycerol(10.8∶39.2∶50), drug loading of(5.563±0.065) mg·g~(-1) for tenuifolin and(5.526±0.022) mg·g~(-1) for β-asarone; uniform and transparent pan-blue nanoemulsion can be formed after emulsification, with particle size of(28.84±0.44) nm. TEM showed that TF/ASA-SMEDDS can form spherical droplets with a uniform particle size after emulsification; In vitro release test results showed that the drug release rate and cumulative release of tenuifolin and β-asarone were significantly improved. The preparation process of TF/ASA-SMEDDS was simple and can effectively improve in vitro release of tenuifolin and β-asarone.

Optimization of the formulation of fe3o4 nanoparticles by box-behnken response surface method and its drug release mechanism in vitro / 中国药学杂志

OBJECTIVE: To optimize the formulation of Fe3O4 nanoparticles modified with polyethylene glycol (PEG)through Box-Behnken response surface method.To investigate its release properties in vitro to provide references for the study of drug delivery system. METHODS: Firstly, the formulationof Fe3O4 nanoparticles was optimized by Box-Behnken response surface method. Secondly, the physical and chemical stabilities of Fe3O4 nanoparticles were determined at different stages. Next, doxorubicin hydrochloride, scutellarin and 5-fluorouracil were respectively loaded into Fe3O4 nanoparticles by ultrasonic stirring method and the drug release ability of Fe3O4 nanoparticles was studied by dialysis method. Finally, different mathematical models were applied to fit the release data to explain the release mechanism, and the release ability of Fe3O4 nanoparticles was investigated at different temperatures to clarify the effect of photothermal effect on drug release. RESULTS The particle size of Fe3O4 nanoparticles was from 20 to 30 nm at room temperature. Fe3O4 nanoparticles loading with water-soluble drugs 5-fluorouracil was incompatible with the five models. However, when doxorubicin hydrochloride was loaded, its release fitted well with the Higuchi equation. And both zero-order equation and the Hixson-Crowell equation can match well with such Fe3O4 nanoparticles loading with scutellarin. Finally, it can be clarified with mechanism-verified Ritger-Peppas equation that the simple diffusion motivated the drug release of Fe3O4 nanoparticles loaded with hydrophilic drugs, and the Zero dissolution release mechanism worked when loaded with hydrophobic drugs.As the temperature increases, the release ability of Fe3O4 nanoparticles was increases. CONCLUSION: Hydrophobic drugs can be loaded with SCU in the Fe3O4 nanoparticles by ultrasonic stirring method to improve the biocompatibility of the drugs, which provide some experimental foundation for the research and development of new formulations of poorly soluble drugs.

Formulation Optimization of Hydrophobically-Pullulan Nanoparticles by Box-Behnken Response Surface Methodology / 中国药学杂志

OBJECTIVE: To optimize the preparation of self-assembled doxorubicin-loaded cholesterol-modified pullulan nanoparticles(DOX-CHSP-SAN) by response surface methodology. METHODS: DOX-CHSP-SAN was prepared by dialysis method with the amphiphilic carrier of cholesterol-modified pullulan (CHSP) and the model drug of doxorubicin(DOX). Box-Behnken Design (BBD) response surface method was used to optimize the preparation process of DOX-CHSP-SAN. The morphology, average particle size, Zeta potentia, the encapsulation efficiency, drug loading of doxorubicin and the drug release characteristics in vitro were determined. RESULTS: The optimized DOX-CHSP-SAN has a round spherical shape with an average particle size of (117.1±3.4) nm, PDI of (0.205±0.023), Zeta potential of (-26.1±0.135) mV, the encapsulation efficiency was (68.17±0.93)%, and the drug loading was (6.84±0.47)%. The in vitro release behavior in PBS of pH 7.4 was consistent with the Weibull equation. CONCLUSIO:N The DOX-CHSP-SAN prepared by the dialysis method and optimized by the response surface method is round and smooth, the particle size is small and uniform, the encapsulation efficiency and the drug loading amount are high, and the in vitro release has the sustained release characteristics.

Extraction and purification of components from Bufonis Venenum / 中草药

Objective: To optimize the extraction and purification technology of liposoluble constituents from Bufonis Venenum. Methods: The total content of cinobufagin and resibufogenin was taken as the index, and the ethanol potency, solvent multiplication and extraction time were taken as the investigation factors. The optimum extraction process parameters was determined by orthogonal test. Through single factor investigation experiment combined with Box-Behnken response surface method, taking the expansion agent ratio, ratio of diameter to height, adsorbent and sample quantity as the investigation factors, the optimum purification process was selected and determined. Results: It was determined that the optimum extraction process for the addition was 10 times 85% ethanol for 90 minutes’ extraction, the best purification process for the expansion agent cyclohexane-chloroform- acetone was 4:3:3, column height and diameter was 7:1, adsorbent and sample volume was 5.5:1. The content of two kinds of toad poison base purified was up to 66.51%. Through the verification of three batches of amplification process, it was shown that the model fit well, and the separation and purification of toad poison ligand by silicone column chromatography had the advantages of simple operation, fast separation speed, and good separation effect. Conclusion: The selected process is reasonable and feasible, which provides technical reference and basis for the industrialization application of the product in the future.

Optimization of extraction process of Modified Yangyin Qingfei Decoction by Box-Behnken response surface methodology based on analytic hierarchy process / 中草药

Objective: To optimize the extraction process of Modified Yangyin Qingfei Decoction (MYQD). Methods: The effects of ethanol concentration, extraction time and extraction times on the optimization of extraction process of MYQD were investigated by multiple indicators comprehensive scoring and Box-Behnken response surface methodology. The content of verbascoside, chlorogenic acid, paeonol, and glycyrrhizic acid was simultaneously determined by HPLC, and the method of analytic hierarchy process was used to calculate the weight coefficient. Results: The optimum extraction process was as follow: using 69% ethanol for once extraction for 68 min. Conclusion: The optimum extraction process is simple and feasible, and the extraction efficiency of components is high, which can provide reference for the extraction process of MYQD.

Extraction parameters and drying methods of Cistanche deserticola / 中草药

Objective: The optimum extraction process parameters of Cistanche deserticola were selected to study the effects of different drying methods on five phenylethanoid glycosides. Methods: Single factor screening combined with Box-Behnken response surface method was used to optimize the extraction process. After optimal conditions were extracted, HPLC method was used to detect the content of echinacoside, cistanche A, verbascoside, isoacteoside, and 2’-acetylacteoside in different drying methods, and one-way ANOVA, cluster analysis, principal component analysis and close value analysis were used to analyze the content of five phenylethanoid glycosides to choose the best drying method. Results: Optimal extraction process was as following: methanol volume fraction was 55.14%, liquid to material ratio was 46.39, extraction time was 38.50 min. Cluster analysis, principal component analysis, and close value analysis showed that the quality of C. deserticola obtained by freeze-drying method was the best, followed by drying at 80 ℃ and the lowest at 40 ℃. Conclusion: Using this process to extract C. deserticola, the five phenylethanoid glycosides are completely and fully extracted. Although the freeze-drying method of C. deserticola has the highest active ingredient retention, from the production point of view, the 80 ℃ drying method can achieve a balance of cost and efficiency.

Optimization of test solutions preparation of Panax notoginseng in Chinese Pharmacopoeia by Box-Behnken response surface methodology / 中草药

Objective: To study and optimize the preparation method of test solution from Panax notoginseng. Methods: The effects of extraction solvent, liquid-material ratio and extraction temperature on the optimization of the preparation method of test solution of notoginsenoside and ginsenosides in P. notoginseng were investigated by Box-Behnken response surface methology. The content of notoginsenoside R1, ginsenoside Rg1, and ginsenoside Rb1 was simultaneously determined by HPLC. Results: The optimum method was as follow: 75% methanol was used for once reflux extraction, the ratio of liquid-material ratio was 1:40, the extraction temperature was 100 ℃. Conclusion: The optimum preparation of test solution is simple and feasible, and the extraction rate of components is high, which provides a reference for the preparation of test solution from P. notoginseng.

Preparation and characterization of PEGylated long-circulating liposomes encapsulating costunolide and dehydrocostus lactone / 中草药

Objective: To prepare pegylated long-circulating liposomes co-encapsulated by costunolide (Cos) and dehydrocostus lactone (DL), optimize the formulation and process, and evaluate the quality. Methods: The pegylated long-circulating liposomes co-encapsulated by Cos and DL were prepared by film hydration method. Single factor test and Box-Behnken response surface methodology were used to optimize the preparation process with encapsulation efficiency of Cos and DL as the index. The particle size, surface potential, encapsulation efficiency and in vitro release of the liposomes were evaluated. Results: The optimal preparation conditions were as follows: drug-to-lipid ratio was 0.14, ratio of cholesterol to phospholipid was 0.05, mPEG-2000-DSPE addition amount was 6%, hydration time was 30 min, and probe ultrasonic time was 4 min. The obtained liposome was round and uniform in distribution, with an average particle size of (104.8 ± 2.48) nm, a polydispersity index (PDI) of (0.245 ± 0.031), and a Zeta potential of (-9.7 ± 0.23) mV, the encapsulation efficiency of Cos and DL were (91.9 ± 2.6)% and (94.41 ± 1.23)%, respectively. Conclusion: The PEGylated long-circulating liposome prepared by the process and prescription optimization has good appearance and high encapsulation efficiency, which can meet the application requirements.

Optimization of preparation process and evaluation of physical fingerprint of Angelicae Sinensis Radix cellwall broken powder / 中草药

Objective: To optimize the preparation process of Angelicae Sinensis Radix cellwall broken powder (ASR CBP) and evaluate the physical quality of powder. Methods: A HPLC method was established for the determination of five active constituents (ferulic acid, senkyunolide I, coniferyl ferulate, ligustilide and n-butylidenephthalide) of ASR. The Box-Behnken response surface design method was used. The pulverization time, pulverization temperature and sampling capacity in the pulverization process were investigated. The particle size distribution (D90) of the broken wall powder of ASR and the five active ingredients content were used as the response value to construct the response surface model. Under the premise of D90 < 45 μm, the maximum value of the five active ingredients was calculated to optimize the superfine grinding process parameters. A total of 13 physical indicators of D90, coefficient of nonuniformity, particle size distribution width, bulk density, tap density, interparticle porosity, Karl index, specific surface area, pore volume, Hausner ratio, angle of repose, loss on drying and hygroscopicity were used to establish the physical fingerprint of ASR CBP. The similarity evaluation method was used to evaluate the similarity of different batches of ASR CBP. Results: The methodological results of the HPLC method for the determination of the five active ingredients were in accordance with the guidelines. Results of response surface method showed the optimized preparing parameters of ASR CBP technology as follows: 35 min of pulverization time, -10 ℃ of pulverization temperature, and 580 g of sampling capacity. The RSD values between the content and the response surface fitting results of five active ingredients of three batches of cellwall broken powder prepared by the optimal process were all less than 3%. The similarity of the three batches of the optimal process of ASR CBP was above 99.4%. Conclusion: Box-Behnken optimized preparation method of ASR CBP has obvious advantages in retaining the content of active ingredients, especially volatile components. Physical fingerprinting has good practical effects as a tool to evaluate the consistency of physical properties of Chinese material medica powder. The combination of applications helps to achieve a higher quality control level of Chinese medicine cellwall broken powder production.