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Objective: To prepare valsartan tablets and optimize the parameters of rolling granulation process. Methods: The par-ticle size (D50, Y1/μm), tablet hardness (Y2/N), and 30-min drug dissolution (Y3/%) as the evaluation indices, the critical process variables were studied by Plackett-Burman experiment design firstly, and then Box-Behnken response surface method was used to optimize the parameters of rolling granulation process. Results: Plackett-Burman experimental design showed that the rolling pressure and mesh size had significant effect on the granule size (P<0. 05). The rolling pressure, rolling nip and mesh size had significant effect on the tablet hardness (P<0. 05). The optimum rolling parameters based on Box-Behnken response surface method were as fol-lows: the rolling pressure was 30 bar, the rolling nip was 3. 0 mm and the mesh size was 2. 0 mm. Valsartan tablets had good compres-sibility and high drug dissolution, which was similar to the in vitro dissolution profile of commercial reference preparations. Conclu-sion: The experimental designs to optimize the rolling granulation process of valsartan tablets can improve the controllability of the prod-uct quality.
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Objective: To prepare norcantharidin albumin nanoparticles and evaluate the physical characteristics of the albumin nanoparticles. Methods:Norcantharidin albumin nanoparticles were prepared by ultra-high pressure microfluidization technology. The average particle size and the drug entrapment efficiency of albumin nanoparticles were used as the evaluation indices. Firstly,Plackett-Burman experimental design was used to screen the formula and process variables which had significant effects on the properties of albu-min nanoparticles,and then Box-Behnken experimental design was used to optimize the variables range. The morphology,particle size distribution,zeta potential and in vitro drug release behavior were investigated. Results:The average particle size of norcantharidin al-bumin nanoparticles was (105.2 ± 30.1) nm,the PdI was 0.127,and the zeta potential was( -24.7 ± 1.9) mV. In 0.5% Tween-80 phosphate buffered saline (pH 7.4),the in vitro cumulative release of norcantharidin albumin nanoparticle suspension reached up to 81.4% in 24 h. Conclusion:The preparation technology of norcantharidin albumin nanoparticles by ultra-high pressure microfluidi-zation technology is simple and feasible. The preparation technology can be used in industrial production.
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Objective: To prepare celecoxib-loaded micelles with polyethylene glycol monomethyl ether-polylactic acid ( mPEG-PLA) block copolymer as the carrier material and evaluate the physical and chemical properties .Methods:Celecoxib-loaded micelles were prepared by a film dispersion method .The micelle formula and preparation process were screened by single factor experiment and further optimized by Box-Behnken response surface method .The physical and chemical properties of celecoxib-loaded micelles such as microscopic morphology , particle size distribution and zeta potential were evaluated .The in vitro drug release of celecoxib-loaded mi-celles was investigated by dynamic membrane dialysis .Results:Celecoxib-loaded micelles prepared according to the optimized formula showed the following properties:the particle size distribution was (35.6 ±15.1) nm, PdI was (0.152 ±0.05), and the zeta potential was (-24.6 ±2.9) mV.In 0.5％SDS phosphate buffered saline (pH 6.8), the in vitro cumulative release of celecoxib-loaded mi-celles reached up to 81 .5％in 24 h.Conclusion:It is simple and feasible to prepare celecoxib-loaded micelles by the thin film dis-persion method .
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Abstract The application of high-potential thermotolerant yeasts is a key factor for successful ethanol production at high temperatures. Two hundred and thirty-four yeast isolates from Greater Mekong Subregion (GMS) countries, i.e., Thailand, The Lao People's Democratic Republic (Lao PDR) and Vietnam were obtained. Five thermotolerant yeasts, designated Saccharomyces cerevisiae KKU-VN8, KKU-VN20, and KKU-VN27, Pichia kudriavzevii KKU-TH33 and P. kudriavzevii KKU-TH43, demonstrated high temperature and ethanol tolerance levels up to 45 °C and 13% (v/v), respectively. All five strains produced higher ethanol concentrations and exhibited greater productivities and yields than the industrial strain S. cerevisiae TISTR5606 during high-temperature fermentation at 40 °C and 43 °C. S. cerevisiae KKU-VN8 demonstrated the best performance for ethanol production from glucose at 37 °C with an ethanol concentration of 72.69 g/L, a productivity of 1.59 g/L/h and a theoretical ethanol yield of 86.27%. The optimal conditions for ethanol production of S. cerevisiae KKU-VN8 from sweet sorghum juice (SSJ) at 40 °C were achieved using the Box-Behnken experimental design (BBD). The maximal ethanol concentration obtained during fermentation was 89.32 g/L, with a productivity of 2.48 g/L/h and a theoretical ethanol yield of 96.32%. Thus, the newly isolated thermotolerant S. cerevisiae KKU-VN8 exhibits a great potential for commercial-scale ethanol production in the future.
Subject(s)
Pichia/metabolism , Saccharomyces cerevisiae/metabolism , Ethanol/metabolism , Pichia/isolation & purification , Pichia/genetics , Pichia/chemistry , Asia, Southeastern , Saccharomyces cerevisiae/isolation & purification , Saccharomyces cerevisiae/genetics , Saccharomyces cerevisiae/chemistry , Sorghum/metabolism , Glucose/metabolism , Hot TemperatureABSTRACT
Objective:To optimize the flash extraction process of Isatidis Radix by Box-Behnken experimental design. Methods:A flash extraction method was used with the extraction voltage, material-liquid ratio and extraction time as the independent variables. A Hassan’s method was used to calculate the normalized value(OD) of comprehensive evaluation of the dry extract yield and the epi-goitrin extraction rate in order to establish the mathematical relationship between the comprehensive evaluation OD and the independent variables, and the response surface method was used to predict the best process conditions. Results:The optimum process conditions were as follows:voltage of 88 V, material-liquid ratio of 19. 62, and extraction time of 2. 03 min. The rate of dry extract and epigoitrin extraction was 37. 902% and 0. 1887%, respectively. Conclusion:The measured value is close to the predicted one,which indicates the comprehensive flash extraction parameters optimized by Box-Behnken experimental design can be used for the extraction for Isatidis Radix.
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Objective:To optimize the extraction parameters for anthraquinones in Semen Cassiae by Box-Behnken experimental design. Methods:Based on single factor screening, a three-factor and three-level Box-Behnken experimental design was employed with the ethanol concentration, material to liquid ratio and extraction time as the independent variables. The dependent variables including the extration rates of chrysophand and aurantio-obtusin were transformed into desirability mathematically by Hassan 's method. The mathematical relationship was established between the dependent variables and the independent variables. The optimum experimental conditions were selected from the stationary point of the response surfaces. Results:The optimum extraction conditions were as follows:12-fold amount of 44％ ethanol as the solvent, extracted three times with 2. 65h for each time. The extraction rate of chrysophanol and aurantio-obtusin was 1. 921％ and 3. 244％, respectively. Conclusion:The measured value is close to the predicted one,which indi-cates the comprehensive extraction parameters optimized by Box-Behnken experimental design can be used for the extraction of chry-sophanol and aurantio-obtusin from Semen Cassiae.
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Objective To optimize the processing parameters for the extraction of chlorogenic acid in Fule Granula by Box-Behnken experimental design.Methods The content of chlorogenic acid in Fule Granula was determination.The separation was performed on a Agilent ZORBAX Eclipse XDB C18 column(4.6 mm ×250 mm, 5 μm), and column temperature 30 ℃.Aetonitrile-0.2% H3PO4 was used as the mobile phase.The detection wavelength was at 327 nm.A three-factor and three-level Box-Behnken experimental design was employed to investigate effects of extraction time, solid-liquid ratio and extraction times on composite score of extracting amount of chlorogenic acid.Results Optimum process conditions were as follows:12 times the amount of water extracted three times, each time 60 min; chlorogenic acid extraction rate of 3.379%.Conclusion This optimized extraction technology has good predictability by Box-Behnken experimental design, and overall desirability, it provides a reference for application of Fule Granula.
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Objective: To optimize the ultrahigh pressure extraction ( UPE) process for forsythoside from Forsythia suspensa by Box-Behnken experimental design. Methods:On the basis of single factor screening, a three-factor and three-level Box-Behnken ex-perimental design was employed with liquid/material ratio( X1 ) , extraction pressure ( X2 ) and extraction time ( X3 ) as the independent variables. The response variable was the extraction yield of forsythoside. Results:The optimal UPE conditions for forsythoside were as follows:the ratio of solvent to material (ml·g-1) was 70, the extraction pressure was 151 MPa, and the extraction time was 114 s. With the optimal extraction process, the extraction yield of forsythoside was 13. 15 mg·g-1 . Conclusion:As a novel extraction tech-nology for Chinese herbal medicines, UPE procedure has higher extraction yield, lower extraction temperature, shorter extraction time and less power consumption, which provides a brand-new method for the extraction of forsythoside from Forsythia suspensa.
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Objective To screen the best processing technology of prepared Rhubarb by multi- component composite score combined with response surface.Methods The composite score of seven components, i.e., gallicacid, chrysophanol-8-O-β-D-glucopyranoside, aloeemodin, rhein, emodin, chrysophanol, physcion, was taken as indicators. Three factors and three levels of response surface Box-Behnken were used in experimental design. The effects of factors including rice wine volume, moistening time, and steaming time on processing technology of stewed Rhubarb were studied, and the optimized processing parameters were chosen.Results Design Expert 8.05 software was used for data analysis. Multivariate quadratic mathematical model of the sample and examine factors composite score regression equation of seven ingredients content were set up. The best processing conditions of prepared Rhubarb were as following:adding 36.6 mL rice wine into per 100 g raw material;moistening time continued for 2.16 hours;steaming time continued for 10.96 h. According to actual production, the optimized processing conditions of prepared Rhubarb are as following:adding 35 mL rice wine per into 100 g raw material;moistening time continued for 2 h;steaming time continued for 11 h.Conclusion The optimized processing technology can reasonably control the quality of prepared Rhubarb, and provide the basis for the quality standards of its decoction pieces and clinical application.
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OBJECTIVE: To optimize the ultrahigh pressure extraction (UPE) process of effective constituents from Jinqiao Reduqing granules by Box-Behnken design-response surface methodology. METHODS: On the basis of single factor screening, a three-factor and three-level Box-Behnken experimental design was employed, with solvent ratio (X1), extraction pressure (X2) and extraction time(X3) as independent variables. Dependent variables were transformed into desirabilities mathematically by Hassan's method. Data of overall desirabilities were fitted to a second order polynomial equation, through which three dimensional response surface graphs were produced. Optimum experimental conditions were selected from the stationary point of the response surfaces. RESULTS: Regression coefficient of binomial fitting complex model was as high as 0.9878. The optimum conditions of UPE were as follows: the materials were extracted for 38 s with 24 times amount of water, the extraction pressure was 112.1 MPa, and the extraction was performed for one tine. The bias between observed and predicted values was 5.27%. CONCLUSION: As a novel extraction technology for Chinese herbal medicine, the UPE procedure has higher extraction yield, lower extracting temperature, shorter extracting time and less power consumption. The UPE has provided a brand new method for extraction of chlorogenic acid and forsythiaside from Jinqiao Reduqing granules.
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Objective: To optimize the formulation parameters of solid lipid nanoparticles (SLN) of Silymarin by Box-Behnken experimental design. Methods: A three-factor and three-level Box-Behnken experimental design was employed using emulsion evaporation-low temperature solidification technique to prepare SLN with Silymarin as model drug. Response surface methodology was used to investigate the factors affecting entrapment efficiency (EE), drug loading (DL), and particle size. Binomial mathematical model-optimized formulation was established with EE, DL, and particle size as response values. Results: The optimal formulation was as follows: the amount of glycerol monostearate was 5.05%, the concentration of Poloxamer 188 was 7.25%, and the amount of drug was 15%. Conclusion: The Box-Behnken experimental design could be used to optimize the SLN of silymarin.