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1.
China Pharmacy ; (12): 793-800, 2024.
Article in Chinese | WPRIM | ID: wpr-1013539

ABSTRACT

OBJECTIVE To study the extraction technology of Sophora flavescens-Phellodendron chinense drug pair and provide a reference for the development of new drugs for the treatment of anorectal diseases. METHODS Using the contents of total alkaloids of S. flavescens (matrine+oxymatrine), berberine hydrochloride and total flavonoid, and extract yield as evaluation indicators, analytic hierarchy process-entropy weight method was used to calculate the weight coefficient of each indicator, and was combined with Box-Behnken design-response surface method to study the extraction technology of S. flavescens-P. chinense drug pair and verify it. RESULTS The optimal extraction technology of S. flavescens-P. chinense drug pair was immersed in 12-fold amount of 58% ethanol for 30 minutes and extracted twice, each time for 120 minutes. The relative error between the verification experimental results and the predicted value was 1.88%. CONCLUSIONS The obtained extraction technology is stable and feasible and can provide reference for the application of S. flavescens-P. chinense drug pair and development of new drugs.

2.
Article | IMSEAR | ID: sea-219449

ABSTRACT

Besides cultivation, extraction is also a critical stage in enhancing the yield of phycocyanin production - a highly valuable compound from Spirulina biomass. In this study, the combined effect of three important variables in the ultrasonic-assisted extraction process on phycocyanin extraction yield, namely extraction temperature, sonication time, and solvent pH were investigated through a central composite design experiment. Furthermore, the response surface method was applied in order to define an optimal condition to achieve the highest extraction yield. The results showed that when temperature ranged from 35ºC to 45ºC, sonication time from 20 to 50 minutes, and solvent pH from 6 to 8, the average yield of 30.135±1.552 mg/g was obtained with an average purity of 0.871±0.043. A regression model was also successfully developed, which allowed a good prediction of extraction yield based on the three mentioned variables. On the other hand, an optimal condition for extraction was also proposed with sonication time = 43.57 minutes, extraction temperature = 37.6oC, and solvent pH = 6.7. These results were practically valuable for the improvement of phycocyanin extraction from Spirulina biomass

3.
China Pharmacy ; (12): 1071-1075, 2023.
Article in Chinese | WPRIM | ID: wpr-972949

ABSTRACT

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.

4.
China Journal of Chinese Materia Medica ; (24): 5540-5547, 2023.
Article in Chinese | WPRIM | ID: wpr-1008750

ABSTRACT

The effective components of flavonoids in the "Pueraria lobata-Hovenia dulcis" drug pair have low bioavailability in vivo due to their unstable characteristics. This study used microemulsions with amphoteric carrier properties to solve this problem. The study drew pseudo-ternary phase diagrams through titration compatibility experiments of the oil phase with emulsifiers and co-emulsifiers and screened the prescription composition of blank microemulsions. The study used average particle size and PDI as evaluation indicators, and the central composite design-response surface method(CCD-RSM) was used to optimize the prescription; high-dosage drug-loaded microemulsions were obtained, and their physicochemical properties, appearance, and stability were evaluated. The results showed that when ethyl butyrate was used as the oil phase, polysorbate 80(tween 80) as the surfactant, and anhydrous ethanol as the cosurfactant, the maximum microemulsion area was obtained. When the difference in results was small, K_(m )of 1∶4 was chosen to ensure the safety of the prescription. The prescription composition optimized by the CCD-RSM was ethyl butyrate(16.28%), tween 80(9.59%), and anhydrous ethanol(38.34%). When the dosage reached 3% of the system mass, the total flavonoid microemulsion prepared had a clear and transparent appearance, with average particle size, PDI, and potential of(74.25±1.58)nm, 0.277±0.043, and(-0.08±0.07) mV, respectively. The microemulsion was spherical and evenly distributed under transmission electron microscopy. The centrifugal stability and temperature stability were good, and there was no layering or demulsification phenomenon, which significantly improved the in vitro dissolution of total flavonoids.


Subject(s)
Polysorbates/chemistry , Flavonoids , Pueraria , Surface-Active Agents/chemistry , Ethanol , Emulsions , Particle Size , Solubility
5.
China Pharmacy ; (12): 2745-2749, 2023.
Article in Chinese | WPRIM | ID: wpr-998559

ABSTRACT

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.

6.
China Pharmacy ; (12): 2323-2327, 2023.
Article in Chinese | WPRIM | ID: wpr-996386

ABSTRACT

OBJECTIVE To optimize the extraction process of blumeatin from Blumea balsamifera and to evaluate its antibacterial and anti-inflammatory activity. METHODS The content of blumeatin in the extract of B. balsamifera was determined by HPLC. On the basis of the single factor experiment, the extraction technology of blumeatin was optimized by the Box-Behnken response surface method with the volume fraction of ethanol, liquid-solid ratio and extraction time as the factors, using the yield of blumeatin as index. Microdilution method was used to determine the antibacterial activity of blumeatin against Streptococcus pyogenes, Staphylococcus aureus, Streptococcus agalactiae, Streptococcus mutans, Bacillus subtilis and Micrococcus luteus. The anti-inflammatory activity of blumeatin was evaluated by ear swelling test and capillary permeability test in mice. RESULTS The optimal extraction technology was as follows: ethanol concentration of 90%, liquid-material ratio of 15∶1, extraction time of 2 h at 80 ℃; the yield of blumeatin using this extraction process was 1.97 mg/g. The minimum inhibitory concentrations of blumeatin for S. pyogenes, S. aureus, S. agalactiae, S. mutans, B. subtilis and M. luteus were 50.00, 200.00, 400.00, 400.00, 800.00 and 1 600.00 μg/mL, respectively; the minimum bactericidal concentrations of blumeatin for S. pyogenes and S. aureus were 400.00 and 1 600.00 μg/mL, respectively. Blumeatin could significantly inhibit the ear swelling induced by xylene and capillary permeability induced by acetic acid in mice(P<0.05 or P<0.01). CONCLUSIONS The optimized extraction technology of blumeatin is stable and feasible. The extracted blumeatin has a certain antibacterial effect against S. pyogenes and a good anti-inflammatory activity.

7.
China Pharmacy ; (12): 2095-2100, 2023.
Article in Chinese | WPRIM | ID: wpr-987138

ABSTRACT

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.

8.
International Journal of Traditional Chinese Medicine ; (6): 56-60, 2022.
Article in Chinese | WPRIM | ID: wpr-930099

ABSTRACT

Objective:To optimize the ethanol reflux extraction process of total saponins in total saponins of Trillium tschonoskii Rhizome. Methods:On the basis of single factor tests, making the total extraction rate of three main compounds [paris saponin Ⅵ, paris saponin Ⅶ and pennogenin-3- O-α-L-rhamnopyranosyl-(1→4)-[O-α-L-rhamnopyranosyl (1→2)]- O-β-D-glucopyranoside (PRRG)] as the indicator, the optimal extraction parameter was selected with the main influencing factors: the ethanol concentration, solid-liquid ratio, and extraction time by the central composite design-response surface method.Results:The optimal extraction parameter for the ethanol extract of total saponins of Trillium tschonoskii Rhizome was as follows: ethanol concentration 69%, extraction time 1.9 h, and solid liquid ratio 1∶9.7. The binomial fitting complex correlation coefficient r = 0.966 1, and the deviation between the extracted predicted value and the actual value is 4.68%. Conclusion:The central composite design-response surface method is simple and reliable for the optimization of extraction process of total saponins of Trillium tschonoskii Rhizome.

9.
Journal of Pharmaceutical Practice ; (6): 28-33, 2022.
Article in Chinese | WPRIM | ID: wpr-907150

ABSTRACT

Objective To prepare berberine hydrochloride nanoemulsion, optimize its formulation composition and preparation process, and investigate its in vitro characteristics. Methods BBR-NE was prepared by water drop addition and pseudo-ternary phase diagram was drawn. The formulation of NE was optimized by central composite design-response surface methodology to choose the optimal formulation composition. The particle size, potential and appearance of the prepared BBR-NE were characterized. Results The optimal prescription of BBR-NE was determined as the oil phase Capryol 90 accounted for 32.84% of the system, the surfactant Tween-80 accounted for 33.90%, the co-surfactant 1,2-propylene glycol accounted for 16.95%, and water relative system accounted for 15.25%. The prepared NE was clear and transparent in appearance, regular in shape and uniform in size, with an average particle diameter of (68.85±8) nm, polydiseperse index of (0.245±0.03) and drug loading of 0.83 mg/g. The in vitro drug release results of NE showed that the in vitro drug release behavior was passive diffusion, which had a certain slow releasing effect and met the first-order release equation. Conclusion The BBR-NE can provide a new dosage form for the clinical use of berberine.

10.
International Journal of Traditional Chinese Medicine ; (6): 1234-1239, 2021.
Article in Chinese | WPRIM | ID: wpr-907701

ABSTRACT

Objective:To optimize the preparation technic of Chuanxiong Rhizoma with vacuum steam method, and to investigate the anti-inflammatory and analgesic activity of Chuanxiong Rhizoma decoction pieces with Central Composite Design-Response Surface Method. Methods:Taking the content of ferulic acid as the evaluation index and the moistening temperature, moistening time and vacuum time as the observation indexes, the moistening technic of Chuanxiong Rhizoma was optimized by Response Surface Method, and selected the optimized plan. The anti-inflammatory and analgesic activities of Chuanxiong Rhizoma were investigated by auricle swelling induced by xylene and writhing induced by glacial acetic acid. Results:The optimum vacuum moistening technic was that the softening temperature was 80 ℃, the softening time was 50 min and the vacuum time was 45 min. The content of ferulic acid in Chuanxiong Rhizoma produced by this technic is highand could decreased the times of wrinkle reaction induced by acetic acid in mice, prolonged the latent period, and obviously or partially inhibitied the ear swelling degree induced byxylene in rats. Conclusions:The Response Surface Method technic of Chuanxiong Rhizoma is easy to operate with high accuracy. The vacuum steam treatment was more obvious than traditional technology group. It provides reference for the subsequent production of Chuanxiong Rhizoma decoction pieces and have the certain value for its promotion and application.

11.
International Journal of Traditional Chinese Medicine ; (6): 887-892, 2021.
Article in Chinese | WPRIM | ID: wpr-907648

ABSTRACT

Objective:Response surface methodology was used to optimize the optimal extraction conditions of red ginseng polysaccharide and to study the antioxidant activity of red ginseng polysaccharide.Methods:Supercritical CO 2 extraction method was used to extract polysaccharides from red ginseng. The effects of solid-liquid ratio, extraction time, extraction temperature and extraction pressure on the extraction of polysaccharides from red ginseng were investigated. Box-behnken Design method was used to optimize the extraction process of red ginseng polysaccharide, and Logit method was used to calculate the semi-inhibitory concentration of red ginseng polysaccharide on DPPH clearance (half maximal inhibitory concentration, IC 50). Results:The optimal extraction conditions were as follows: extraction temperature 61.12 ℃, extraction pressure 20.64 MPa, extraction time 128.37 min, solid-liquid ratio 1∶25.61 g/ml, and the extraction yield of red ginseng polysaccharide was 36.89%. The results of three groups of repeatability tests showed that the relative error of polysaccharide yield of red ginseng was in the range of 5%. When the mass concentration of red ginseng polysaccharide was 25 μg/ml, it had better antioxidant activity and IC 50 was 10.97 μg/ml. Conclusion:The optimized extraction conditions of red ginseng polysaccharide were reasonable and reliable, and the antioxidant activity of red ginseng polysaccharide was strong, which could provide reference for the follow-up research.

12.
Chinese Journal of Blood Transfusion ; (12): 26-29, 2021.
Article in Chinese | WPRIM | ID: wpr-1003915

ABSTRACT

【Objective】 To optimize the purification conditions of heparin affinity chromatography in the purification of human coagulation factor Ⅸ by response surface method and establish the optimal chromatography process parameters. 【Methods】 The effect of sample loading temperature on purification efficiency was analyzed through single factor test. Three-factor three-level response surface method was used to optimize the chromatographic elution conditions. The Folin phenol method and the automatic hemagglutination analyzer were used to determine the total protein content and human coagulation factor Ⅸ titer, respectively. The purification effect was evaluated by activity index and process recovery rate. 【Results】 The optimized optimal chromatographic conditions were loading at 5 ℃, washing 4 CV, eluent formulation of sodium citrate 20 mmol/L, arginine hydrochloride 18.7 mmol/L, NaCl 611.6 mmol/L and pH 7.5; under this optimal setting, the recovery rate of the chromatographic process was (46.6±2.9) %, titer of factor Ⅸ rated to (68.4±4.7) IU/mL and specific activity was (62.8±3.3) IU/mg. 【Conclusion】 The optimized parameters of heparin affinity chromatography process by response surface method can produce better purification effect on human coagulation factor Ⅸ.

13.
China Pharmacy ; (12): 2383-2387, 2021.
Article in Chinese | WPRIM | ID: wpr-886921

ABSTRACT

OBJECTIVE:To optimize the formulation of Curcumin (CUR)transethosomes(CUR-TEs). METHODS :The contents of CUR in CUR-TEs were determined by HPLC. CUR-TEs were prepared by injection method. Using comprehensive score of encapsulation efficiency and drug loading as index ,based on signal factor test ,Box-Behnken design-response surface method was used to optimize and validate the formulation. The property of CUR-TEs prepared by the optimal formulation was investigated. RESULTS:The optimal formulation of CUR-TEs was as follows as lecithin of 4%,CUR of 0.13%,1,2-propylene glycol of 25%,tween-80 of 1%. Results of validation test of optimal formulation showed that comprehensive score of encapsulation efficiency and drug loading of CUR-TEs was 93.04±2.16,relative error of which to predicted value (91.19)was 2.03%. The encapsulation efficiency of CUR-TEs prepared by optimal formulation was (91.17±1.35)%,and its drug loading was (0.94± 0.02)%. The particle size was (190.64±15.97)nm with polydispersity index of 0.086±0.007,and Zeta potential was (-12.74± 1.60)mV. CONCLUSIONS :The optimized formulation of CUR-TEs is stable ,feasible and repeatable ,with good stability.

14.
China Journal of Chinese Materia Medica ; (24): 2537-2546, 2021.
Article in Chinese | WPRIM | ID: wpr-879158

ABSTRACT

This research was used with high performance liquid chromatography(HPLC), combined with information entropy-response surface method(RSM) to investigate the ethanol concentration, extraction time, liquid-to-material ratio. Taking the content of four chromogens as evaluation indexes, the weight coefficients of each index were given, and the comprehensive score was calculated to optimize the extraction process. Then, prim-O-glucosylcimifugin was used as the reference, the relative calibration factors(RCFs) of cimifugin, 4'-O-β-D-glucosyl-5-O-methylvisamminol and sec-O-glucosylhamaudo to prim-O-glucosylcimifugin were calculated respectively. The contents of four components in Saposhnikoviae Radix were determined by both external standard method(ESM)and quantitative analysis of multi-components by single marker(QAMS) method, and the results were compared. At last, combined with principal component analysis(PCA) and orthogonal partial least squares discriminant analysis(OPLS-DA) to evaluate the quality of the Saposhnikoviae Radix in different production areas. The optimal extraction process parameter of the Saposhnikoviae Radix was as follows: liquid-to-material ratio is 60∶1(mL·g~(-1)), extraction time is 35 min, and ethanol concentration is 70%. The repeatability of the RCFs was perfect, and the results calculated by the QAMS were consistent with the results from the ESM. The stoichiometric results indicate that there are obvious differences in the distribution of Saposhnikoviae Radix in different production areas, and cimifugin and prim-O-glucosylcimifugin are the characteristic compounds that cause this difference. In this study, the optimal extraction process is stable and feasible, and the method of QAMS is accurate and reliable. From the perspective of four chromogens, there are differences in the quality of the Saposhnikoviae Radix in different production areas. Therefore, the established extraction process combined with the method of QAMS can be used to evaluate the quality of Saposhnikoviae Radix and provide a scientific basis for the quality control of Saposhnikoviae Radix.


Subject(s)
Apiaceae , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Entropy , Plant Roots
15.
China Pharmacy ; (12): 1473-1479, 2021.
Article in Chinese | WPRIM | ID: wpr-881284

ABSTRACT

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.

16.
Journal of Pharmaceutical Practice ; (6): 27-34, 2020.
Article in Chinese | WPRIM | ID: wpr-782380

ABSTRACT

Objective To optimize the extraction process of the compound herba lysimachiae by orthogonal experiment and response surface method. Methods The sum of the peak areas of multiple representative components in the compound herba lysimachiae was used as the evaluation index. The ultrasonic extraction time, ultrasonic temperature and ethanol ratio were analyzed to optimize the extraction process conditions by orthogonal experiment and Box-Behnken response surface analysis method. Results Ultrasonic extraction time and ethanol ratio are important factors in the extraction process of the compound herba lysimachiae. The effect of ultrasonic temperature in the extraction process is not significant. The optimal extraction condition for compound herba lysimachiaeare is 10 min ultrasonic extraction time at 55 ℃ with 55% ethanol. Conclusion The optimal extraction process parameters obtained by combining orthogonal experiment and Box-Behnken response surface method can be used for the extraction of representative components from the compound herba lysimachiae and pharmaceutical research in the future.

17.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 124-131, 2020.
Article in Chinese | WPRIM | ID: wpr-872835

ABSTRACT

Objective:To optimize the processing technology of salt-processed products of Plantaginis Semen with the specific process parameters, and verify the obtained processing technology by pharmacodynamic research, so as to provide experimental basis for the standardized production and quality control of this decoction pieces. Method:Taking composite score of appearance character score, dry extract yield and contents of three components (geniposidic acid, acteoside and isoacteoside) as index, the analytic hierarchy process (AHP)-criteria importance through intercrieria correlation (CRITIC) mixed weighting method was used to determine the weight coefficient of each index. Based on single factor tests, the response surface method was used to investigate the effects of frying time, frying temperature, salt amount and water amount on the processing technology of salt-processed products of Plantaginis Semen, and the processing technology was verified by diuretic experiment with furosemide tablets as the positive drug (administration dose of 0.01 g·kg-1). Result:The weight coefficients of geniposidic acid content, acteoside content, appearance character score, isoacteoside content and dry extract yield were 0.319, 0.193, 0.207, 0.273 and 0.008, respectively. The optimal process parameters were as following:fried at 150-180 ℃ for 10 min (obtained from the single factor tests), 100 g of Plantaginis Semen sprayed evenly with 2 g of salt (2 g of salt dissolved in 20 mL of water), and fried at 150-180 ℃ for 15 min. Compared with the blank group, both of the raw products group and the salt-processed products group could significantly increase the secretion of urine volume (P<0.01), but the excretion of Na+ in the urine of rats in the salt-processed products group was significantly higher than that in the raw products group (P<0.05). Conclusion:The optimized processing technology is simple and feasible, which can provide reference for standardizing the industrial production of salt-processed products of Plantaginis Semen. At the same time, combined with inherent quality and appearance of the salt-processed products, and verified by pharmacodynamic test, the obtained results are reasonable and reliable, which can be used for quality control of this decoction pieces.

18.
Chinese Traditional and Herbal Drugs ; (24): 84-90, 2020.
Article in Chinese | WPRIM | ID: wpr-846695

ABSTRACT

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.

19.
Chinese Traditional and Herbal Drugs ; (24): 43-50, 2020.
Article in Chinese | WPRIM | ID: wpr-846690

ABSTRACT

Objective: To optimize the prescription process of curcumin-piperine polymeric compound micelles (Cur/Pip F127/P123-PM) by central composite design-response surface method. Methods: The content of curcumin and piperine was determined by UPLC. The Cur/Pip F127/P123-PM was prepared by thin film hydration method. Based on the single factor test, the dosage, the mass ratio of F127 and the volume of water were used as independent variables, and the drug loading and entrapment efficiency of curcumin, entrapment efficiency of piperine and the micelle size were dependent variables, and next central composite design-response surface method of three factors and five levels was carried out. The analysis results showed and verified the optimal prescription. Finally, the optimal lyophilization conditions of the micelle preparation were initially screened. Results: The optimal preparation process was as follow: the dosage of curcumin and piperine was 12.96 mg and 0.69 mg, respectively; The mass ratio of F127 was 0.46, and the volume of water was 8.85 mL. The compound curcumin micelles prepared by the optimum formulation had the loading capacity of 5.63%, solubility of 1.27 mg/mL and entrapment rate of curcumin was 86.86%. The entrapment rate of piperine was 77.54%; The micelle size was 66.79 nm and the Zeta potential was close to zero. The lyophilized products prepared by using 8% mannitol as a protective agent had a good redispersion. Conclusion: The model established by central composite design-response surface method can be used to optimize the prescription of compound curcumin micelles, and the method had a high accuracy and good predictability advantage.

20.
Chinese Traditional and Herbal Drugs ; (24): 2418-2426, 2020.
Article in Chinese | WPRIM | ID: wpr-846452

ABSTRACT

Objective: To optimize the formulation of 1,8-cineole self-microemulsifying drug delivery system (1,8-Cin-SMEDDS), characterize it and investigate its cell uptake. Methods: By drawing pseudo-ternary phase diagram, the effective self-emulsifying region of 1,8-Cin-SMEDDS was determined, and the preliminary prescription was screened. Taking the particle size and drug loading as the index, the central composite design-response surface method was used to optimize and verify the prescription. Fluorescence microscope was used to observe the uptake of human umbilical vein endothelial cells (HUVEC) injured by high glucose. Results: The results showed that the best prescription of 1,8-Cin-SMEDDS was a mixture of soybean oil (7.5%) and 1,8-Cin (22.5%), HS15 (56%) as emulsifier, ethanol (14%) as co-emulsifier, and dripping pure water to 8 mL to obtain a translucent slightly bluish emulsion. The appearance of spherical droplets was observed by transmission electron microscope, and the average particle size and Zeta potential measured by laser particle size Zeta tester was (131.68 ± 1.44) nm and (-10.03 ± 1.63) mV, respectively; The entrapment efficiency estimated by HPLC was (99.890 ± 0.012)%, and the drug loading was (224.750 ± 0.028) mg/g. The results of HUVEC cell uptake assay showed that the uptake of 1,8-Cin-SMEDDS by cells was higher than that of free 1,8-Cin. Conclusion: The preparation method of 1,8-Cin-SMEDDS is simple and reproducible. The obtained method has good appearance, high entrapment efficiency, stable physical, and chemical properties, which can also promote cell uptake.

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