Optimization of preparation technology of baicalin lipid nano foam aerosol / 中国药房

OBJECTIVE To optimize the pr eparation technology of the baicalin lipid nano foam aerosol （BC-LN-FA）. METHODS Baicalin lipid nanoparticle （BC-LN）and BC-LN-FA were prepared by the thin film dispersion method and homogeneous emulsification method ，respectively，using baicalin （BC） as the model drug. The preparation technology was optimized by Box-Behnken design-response surface methodology using particle size and encapsulation efficiency （EE）as indexes ，with dosage ， emulsifier dosage ，co-emulsifier dosage and homogenization time as factors. The morphology ，particle size ，polymerdispersity index（PDI），EE，the viscosity ，the foam dissolution rate and in vitro transdermal release of BC-LN-FA were characterized. RESULTS The optimal technology included 25 mg BC ，40 mg emulsifier （mass ratio of stearic acid-soybean lecithin-glycerol was 1∶1∶1），30 mg co-emulsifier （mass ratio of octadecanol-lactic acid was 1∶1），homogenization time of 20 min. Results of 3 times of validation tests showed that particle size of prepared BC-LN-FA was （151.70±2.40）nm，EE was （68.62±1.16）％；the deviation of them from the predicted value （particle size of 150.80 nm，EE of 67.02％）were 0.60％ and 2.39％ respectively. The BC-LN-FA prepared by the optimal process was light yellow opalescence ，uniform in particle size and round-like in shape. The viscosity，the foam dissolution rate ，the content of BC and PDI were （122.92±5.09）mPa·s，（65.32±3.22）％，（7.01±0.12）％ and（0.199±0.006），respectively. At 48 h，the cumulative release rates of BC-LN-FA in phosphate buffer saline （PBS）at pH 7.4， 6.8，5.0 were（54.12±2.69）％，（57.85±4.25）％ and（59.47±1.83）％，respectively；those of free BC in PBS at pH 7.4 was only （15.04±1.43）％. CONCLUSIONS The optimized technology is stable and feasible. Prepared BC-LN-FA has a uniform particle size，high digestion rate and certain viscosity.

Study on the salt-processing technology of Rosa laevigata and its HPLC fingerprints and chromaticity values before and after salt-processing / 中国药房

OBJECTIV E To optimize the s alt-processing technology of Rosa laevigata ，and to study high performance liquid chromatography（HPLC）fingerprints and chromaticity values of R. laevigata before and after salt-processing. METHODS The comprehensive scoring method was adopted to optimize the salt-processing technology of R. laevigata using appearance character ， moisture and polysaccharide content as index. Fingerprints were established by HPLC method before and after salt-processing ，and chromaticity values （L*，a*，b*）of the powder before and after salt-processing were determined. The multivariate statistical analysis was carried out for raw product and salt-processing product of R. laevigata by using common peak areas and chromaticity values as index. RESULTS The optimal salt-processing technology of R. laevigata was to mix it with appropriate amount of salt water ，place them in the preheated frying wok at 140 ℃，fry them for 25 min，and rotate frying wok 20 times/min. Ten common peaks were calibrated by HPLC fingerprints before and after salt-processing ，and 3 components were identified ，such as gallic acid ，catechin and ellagic acid. The chromaticity values L*，b* and E* changed significantly after salt-processing. The multivariate statistical analysis method could distinguish raw products and salt-processing products into two categories ，in which peaks 1，5，6 and 10 and chromaticity values b* and E* were important characteristic factors. CONCLUSIONS The optimized salt-processing technology is stable and reliable ，and the established fingerprint has good repeatability and stability. Fingerprint and chromaticity values combined with multivariate statistical analysis can provide reference for the identification and quality analysis of R. laevigata before and after salt-processing.

Optimization of processing technology of Portulaca oleracea charcoal and its improvement effect on the symptom of hemorrhoid model rats / 中国药房

OBJECTIVE To optimize th e p rocessing technology of Portulaca oleracea charcoal，and to investigate its improvement effect on the symptom of hemorrhoid model rats. METHODS The effects of roasting temperature ，dosage and roasting time on the processing technology of P. oleracea charcoal were investigated with Box-Behnken response surface methodology using comprehensive score of tannin content ，water-soluble extract content and appearance properties as the index. The optimal process parameters are selected and verified. The hemorrhoid model rats were treated with P. oleracea charcoal（0.8 g/mL）prepared by the optimal processing technology ，once a day ，for 11 days. After last medication ，the perianal pathological score of hemorrhoid model rats were performed ；serum levels of tumor necrosis factor α（TNF-α），interleukin 6（IL-6）and IL- 1β were detected. RESULTS The optimal processing technology of P. oleracea charcoal included roasting temperature of 200 ℃， dosage of 150 g and roasting time of 14 min. Results of validation test showed that the comprehensive score of P. oleracea charcoal was 92.57，and relative error of it with predicted value （96.59）was －4.13％. External use of P. oleracea charcoal 0.8 g/mL prepared by the optimal processing technology could significantly promote the wound healing of hemorrhoid model rats ，reduced the amount of exudate ，and decreased the levels of TNF-α，IL-6 and IL-β in serum. CONCLUSIONS The optimized processing technology of P. oleracea charcoal is feasible. P. oleracea charcoal prepared by the optimized processing technology has good curative effect on the symptom of hemorrhoid model rats.

Optimization of formulation and preparation technology of Neuritic acid oral emulsion / 中国药房

OBJECTIVE To prepare Neuritic acid oral emulsion ，to optimize its formulation and preparation technology ，and to investigate its stability. METHODS Neuritic acid oral emulsion was prepared by mechanical method. On the basis of single factor experiment ，the appearance ，centrifugal stability ，centrifugal stability constant （Ke）and particle size of the emulsion as indexes，the formulation was optimized by orthogonal design ，taking the dosage of oleic acid ，octylphenol polyoxyethylene ether-10 and propylene glycol as factors ，the preparation technology was optimized by taking emulsification temperature ，shear time，pressure of high-pressure homogenization and cycle times of high-pressure homogenization as factors. The content of neuritic acid was determined by high performance liquid chromatography. The stability of Neuritic acid oral emulsion was investigated by high temperature test ，accelerated test and long-term test. RESULTS The optimal formulation and preparation technology were as follows：neuritic acid of 1 g，oleic acid of 5％ ，octylphenol polyoxyethylene ether- 10 of 4％ ，propylene glycol of 2％ ， emulsification temperature of 60 ℃ ，shear time of 2 min，homogenization pressure of 40 MPa and cycle times of twice. After three experiments ，the average particle size of Neuritic acid oral emulsion was 158.05 nm（RSD＝1.58％，n＝3），the average Ke was 0.39（RSD＝1.49％，n＝3），and the appearance was uniform milky white ，there was no stratification. The results of high temperature test showed that Neuritic acid oral emulsion was prone to stratification in high temperature environment ，and the content of neuritic acid increased. The results of accelerated test and long-term test showed that there was no significant change in the appearance or the content of neuritic acid when Neuritic acid oral emulsion was placed at room temperature for 6 months. CONCLUSIONS The formulation and preparation technology are stable and feasible ，and can be used for the preparation of Neuritic acid oral emulsion. Neuritic acid oral emulsion should not be placed in high temperature environment. It has good stability at room temperature for 6 months.

Optimization of Ethanol Extraction Technology of Mongolian Medicine Naru- 3 / 中国药房

OBJECTIVE：To optim ize ethanol extraction technology of Mongolian medicine Naru- 3. METHODS ：The L 9（34） orthogonal design was used to optimize ethanol extraction technology of Mongolian medicine Naru- 3 with solid-liquid ratio ，ethanol volume fraction and extraction time as factors ，using comprehensive scores for the contents of benzoylaconitine ，benzoylneoaconitine， benzoylhypoaconitine，aconitine，neoaconitine，hypoaconitine，piperine and gallic acid as indexes. RESULTS ：The optimal ethanol extraction technology was that solid-liquid ratio of 1∶10（g/mL），ethanol volume fraction of 75％，extracting for 1.5 h. After 3 times of validation tests ，average contents of above 8 components in ethanol extract from Naru- 3 were 1.69，1.48，14.69，0.28， 0.05，0.08，26.01，17.33 mg/g（RSDs were 0-4.96％，n＝3），respectively. Average comprehensive score was 19.03（RSD＝1.42％， n＝3）. CONCLUSIONS ：The optimal ethanol extraction technology of Mongolian medicine Naru- 3 is stable and feasible.

Optimization of the Extraction Technology of Phenolic Acid from Amomum tsaoko / 中国药房

OBJECTIVE：To opt imize the extraction technology of phenolic acid from Amomum tsaoko . METHODS ：The extraction technology of phenolic acid from A. tsaoko was optimized by using Box-Behnken design-response surface methodology with ethanol volume fraction ，liquid-solid ratio and extraction time as factors ，using the total contents of protocatechuic acid and vanillic acid as response value. The optimizd extraction technology was vlidated. RESULTS ：The optimal extraction technology was as follows ：ethanol volume fraction 65％，liquid-solid ratio 4∶1（mL/g），extraction time 2.5 h. After 3 times of validation tests ， average total content of protocatechuic acid and vanillic acid were 12.32 mg/g（RSD＝0.26 ％，n＝3），average relative error of which with predicted value （12.63 mg/g）was 2.45％. CONCLUSIONS ：The optimal technology is stable and feasible .

Optimization of Processing Technology of Paeonia lactiflora Stir-baked with Wine and Investigation of Its Anticoagulant Effect / 中国药房

OBJECTIVE：To optimize the processing technology of Paeonia lactiflora stir-baked with wine ，and to investigate its in vitro anticoagulant effect. METHODS ：The weight coefficient of each index was determined and the comprehensive score was calculated with analytic hierarchy process （AHP），Criteria Importance Though Intercrieria Correlation （CRITIC）and AHP-CRITIC weighting method ，using the contents of oxypaeoniflorin ，albiflorin，paeoniflorin，benzoic acid and water-soluble extract as index. Box-Behnken response surface methodology was used to optimize the parameters of P. lactiflora stir-baked with wine ，such as moistening time ，frying time and frying temperature. Then in vitro anticoagulant experiment was used to investigate the pharmacodynamics of P. lactiflora stir-baked with wine prepared according to the optimal processing technology. RESULTS ：The weight coefficients of albiflorin ，oxypaeoniflorin，paeoniflorin，benzoic acid and water-soluble extract determined by AHP-CRITIC weighting method were 0.233 9，0.131 7，0.183 3，0.078 9，0.372 3，respectively；the optimal processing technology of P. lactiflora stir-baked with wine included moistening time of 35 min，frying time of 20 min and frying temperature of 120 ℃. The results of in vitro anticoagulant test showed that P. lactiflora and P. lactiflora stir-baked with wine could significantly prolong the time of thrombin time ，prothrombin time ，activated partial thrombin time of plasma ；the effects of P. lactiflora stir-baked with wine were significantly better than those of P. lactiflora （P＜0.05）. CONCLUSIONS ：The optimized processing technology of P. lactiflora stir-baked with wine is stable and feasible. The in vitro anticoagulant effect of P. lactiflora stir-baked with wine prepared by this tehcnology is better than that of raw products.

Content Determination of 10 Kinds of Active Componets in Tibetan Medicine Siwei Jianghuang Prescription and Its Decoction Technology Optim ization / 中国药房

OBJECTIVE：To e stablish the method for simultaneous determination of 10 kinds of active components in Tibetan medicine Siwei jianghuang prescription ，and to optimize its decoction technology. METHODS ：HPLC method was adopted. Using soaking time ，the amount of added water ，decoction time and decoction times as factors ，comprehensive score of the contents of 10 kinds of components and solid extracts rate as response values ，one the basis of single factor test ，Box-Behnken response surface method was used to optimize its decoction technology. RESULTS ：The linear range of gallic acid ，corilagin，magnoflorine， ellagic acid ， hydrochloric jatrorrhizine ， hydrochloride palmatine ， hydrochloride berberine ， bisdemethoxycurcumin， demethoxycurcumin and curcumin were 0.280 6-1.683 6，0.289 6-1.737 6，0.320 8-1.924 8，0.116 0-0.696 0，0.018 9-0.113 5， 0.013 3-0.079 9，0.092 3-0.553 8，0.025 5-0.153 0，0.036 1-0.216 3，0.041 0-0.245 7 µg（all r were 0.999 9），respectively. The limits of quantitation were 0.28，14.48，3.21，11.60，1.89，4.44，0.46，0.26，0.36，0.41 ng，respectively. The limits of detection were 0.11，4.14，1.24，3.32，0.58，1.33，0.13，0.09，0.14，0.12 ng，respectively. RSDs of precision ，stability and reproducibility tests were all lower than 3％. The recoveries were 92.56％-103.69％（RSDs were 0.90％-3.81％，n＝6）. The optimal decoction technology included soaking 60 min，adding 8-fold（mL/g）water，decoction for twice ，lasting for 65 min each time. In 6 validation tests ，comprehensive scores were 3.323 2-3.422 4，and the absolute value of the relative error with the predicted value （3.437 4）was less than 2％.CONCLUSIONS：Established method is simple and repeatable ，and can be used for simultaneous determination of 10 kinds of active components in Siwei jianghuang prescription. Optimized decoction technology is stable and feasible.

Preparation of Chelerythrine Solid Dispersion and Study on Its Physicochemical Properties and Antioxidant Activity / 中国药房

OBJECTIVE：To prepare Cheler ythrine （CHE） solid dispe rsion （SD），optimize the formulation technology ， characterize its preparation and investigate its in vitro antioxidant activity. METHODS ：The content of CHE in SD was determined by UV spectrophotometry. Based on single factor tests ，using the product yield as index ，using preparation method ，carrier material type，carrier material proportion （drug-carrier material mass ratio ）as factors ，the formulation technology of SD was optimized by L（9 34）orthogonal test and validated. Based on solubility and accumulative dissolution determination ，the product was characterized with thermal analyssis ，X-ray diffraction and scanning electron microscope. Using ascorbic acid as positive control ，in vitro antioxidant activity of the product was determined by DPPH method. RESULTS ：The linear range of CHE was 2.4-5.6 μg/mL； quantitation limit and detection limit were 0.066 9，0.022 1 μg/mL；RSDs of precision ，stability and reproducibility tests were all lower than 2％；recoveries were 97.50％-99.25％（RSD＜1％， n＝3）. The optimal preparation technology included using PEG 6000 as carrier material ，carrier material ratio of 1 ∶ 3， prepared by solvent method. Three batches of CHE-PEG-SD were prepared. Verification test results showed that the 话：0539-80311889。E-mail：zhenshengao@163.com accumulative dissolution of CHE-PEG-SD was （61.72 ± 0.67）％ at 15 min，and the yield was （99.04±0.83）％. The results of characterization showed that after CHE-PEG-SD prepared ， its solubility （3.725 mg/mL）and accumulative dissolution （61.25％，15 min）were higher than CHE raw material [ 0.098 mg/mL， 6.24％（180 min）]. The endothermic peak and crystal absorption peak moved or even disappeared compared with raw material and the carrier material ，and CHE was uniformly dispersed in the carrier material as an amorphous state. Results of in vitro antioxidation test showed that different concentration of CHE-PEG-SD showed certain ability of DPPH free radical scavenging ，and the IC 50 was 0.124 mg/mL，higher than 0.041 mg/mL of ascorbic acid. CONCLUSIONS ：Established content determination method is simple and accurate. The optimal SD formulation technology is stable and feasible. The solubility of prepared CHE-PEG-SD increases，and the dissolution in vitro increases，showing certain in vitro oxidation resistance.

Synthesis and Technology Optimization of Dapoxetine Hydrochloride / 中国药房

OBJECTIVE：To optimize the synthesis process of dapoxetine hydrochloride. METHODS ：By chiral synthesis ， asymmetric reduction was carried out by using 3-chlorophenylacetone as raw material ，（1S，2R）-（-）-1-amino-2-indanol as catalyst，and borane- N，N-diethylaniline （DEANB） as reducing agent. Then ，it was reacted with α-naphthol etherification， sulfonation，dimethylamine substitution ，and HCl salt formation reaction to obtain the final products. The products were characterized by NMR and MS. The synthesis reaction of intermediate Ⅰ，intermediate Ⅱ，intermediate Ⅲ and the final product were optimized. RESULTS ：The final product was dapoxetine hydrochloride with purity of 99.8％ and yield of 58.9％. Compared with traditional splitting technology ，the chiral synthesis technology of this study did not need splitting ，and the yield of the technology was significantly higher than that of splitting technology reported in literature （31.9％）. The optimized technology reduced the generation of impurities and improved the product quality. CONCLUSIONS ：The improved technology has milder reaction conditions ，shorter synthesis route and higher yield.

Optimization of Preparation Technology of Tetracaine Hydrochloride Ethosomes / 中国药房

OBJECTIVE： To establish a method for determining the content of tetracaine hydrochloride （TCH） ethosomes， and to optimize the preparation technology. METHODS： The content of TCH was determined by HPLC. TCH ethosomes were prepared with injection-ultrasonic method. Using drug-loading amount， egg lecithin concentration and ethanol volume fraction as factor， encapsulation efficiency as index， central composite design-response surface methodology was used to optimize the prescription based on the single factor test. The prepared ethosomes were characterized and the stability was evaluated. RESULTS： The linear range of TCH was 10-100 μg/mL （r＝0.999 5）； the limit of quantification was 0.045 μg/mL， and detection limit was 0.021 μg/mL. RSD of precision， stability and repeatability tests were less than 2％. The recoveries ranged 97.80％-103.20％ （RSD＝0.36％， n＝9）. The optimal preparation technology included that the adding amount of TCH control was 1 mg； the concentration of egg lecithin was 7 mg/mL， and ethanol volume fraction was 33％. Under this technology， the average encapsulation efficiency was 64.50％ （n＝3）， the relative error of which from the predicted value （64.92％） was 0.64％. TCH ethosome was a clear blue liquid with a blue opalescence. Its appearance was spherical， its shape was round， smooth， uniform in size； the average particle size was （80.33±2.24） nm， and the average Zeta potential was （－22.6±1.33） mV. TCH ethosome was stable during 10 days under 4 ℃， sealed and protected from light. CONCLUSIONS： The optimal preparation process is stable and feasible. Established method is simple and rapid.

Optimization of Water Extraction Technology of Total Polysaccharide of Shuanghu Capsules by Orthogonal Design / 中国药房

OBJECTIVE： To optimize the water extraction technology of total polysaccharide of Shuanghu capsules. METHODS： The total alkaloid was firstly extracted from Dendrobium nobile and Dendrobium officinale mixture of Shuanghu capsules with ethanol， and then total polysaccharide was extracted with water. Using glucose as control， total polysaccharide was treated with phenol-sulfuric acid method and its content was determined at 488 nm. Using comprehensive score calculated with the yield of the extract and the content of total polysaccharide as index， the effects of material-liquid ratio， extraction temperature， extraction time and times on the extraction were investigated by single factor test. Then L9（34） orthogonal test was used to optimize solid-liquid ratio，extraction temperature，extraction time and extraction times according to the results of single factor test. The optimized technology was validated. RESULTS： The linear range of glucose were 0.041 4-0.207 0 mg/mL（r＝0.999 9）. RSDs of intra-day and inter-day ranged 3.61％-8.24％ （n＝3，n＝5）， and RSD of repeatability test was 1.49％ （n＝6）. Average recovery rate was 98.65％（RSD＝1.45％，n＝6）. The optimal water extraction technology included solid-liquid ratio of 1 ∶ 25（g/mL），extraction temperature of 100 ℃，extracting for 90 min， extracting once. Results of validation tests showed that average content of total polysaccharide was 379.292 8 mg/g （RSD＝1.93％，n＝3） and average yield of the extract was 22.75％（RSD＝2.41％，n＝3）. CONCLUSIONS： Established phenol-sulphuric acid method is simple， precise and accurate. The optimal water extraction technology is stable and feasible， which can be used for the extraction of total polysaccharides from Shuanghu capsules.

Optimization of Water Extraction Technology of Taohe Chengqi Decoction by Response Surface Methodology Combined with Information Entropy Theory / 中国药房

OBJECTIVE： To optimize the water extraction technology of classic formula Taohe chengqi decoction. METHODS： Based on single factor test， combined with response surface methodology and information entropy theory， the soaking time， solid-liquid ratio and extraction time were investigated. Using the contents of rhein， amygdalin， cinnamaldehyde and glycyrrhizic acid in Taohe chengqi decoction as indexes， information entropy theory was used to assign weight coefficients to each evaluation index and calculate the comprehensive score. Through Design-Expert 10 software， the interactions of each factor were analyzed. Water extraction technology was optimized， and validation test was also performed. RESULTS： According to information entropy theory， the weight coefficients of rhein， amygdalin， glycyrrhizic acid and cinnamaldehyde were located at 0.097 6， 0.363 2， 0.173 5 and 0.365 7. The results of interaction analysis showed that the material-liquid ratio had a greater impact on the comprehensive score. The optimal water extraction technology of Taohe chengqi decoction were determined as that soaking time was 60 min； the ratio of material to liquid was 1 ∶ 10 （g/mL）； total extraction time was 130 min （extracting for 3 times， lasting for 65， 33， 32 min each time）. The results of verification test showed that RSD of content of each index component and the comprehensive score was less than 3％. CONCLUSIONS： The optimal water extraction technology is proved to be stable and feasible， which can provide the basis for the further development and utilization of Taohe chengqi decoction.

Preparation of Peppermint Oil Moisturizing Microemulsion for Nasal Mucosa and Study on Its Mucosal Adhesion and Cilia Toxicity / 中国药房

OBJECTIVE： To prepare the Peppermint oil moisturizing microemulsion for nasal mucosa and survey its mucosal adhesion and cilia toxicity. METHODS： The polyoxyethylene hydrogenated castor oil was used as emulsifier to prepare the Peppermint oil moisturizing microemulsion for nasal mucosa， and the preparation technology was optimized on the basis of comprehensive score by orthogonal design. The microemulsion was characterized and the menthol content was determined by GC. The mucosal adhesion was evaluated by measuring the transport rate by cilia in vivo， and the cilia toxicity of microemulsion was evaluated by measuring the sustained movement time of cilia in vitro. RESULTS： The optimal preparation technology of self-made microemulsion was to firstly disperse the peppermint oil and the emulsifier， then add anhydrous ethanol， edible glycerin and distilled water， and stir at 1 200 r/min for 2 h. The average contents of menthol in the three batches of the microemulsion were 2.682， 2.507 and 2.496 mg/mL （RSD＝2.89％，n＝3）， respectively. The cilia transport rates in vivo were （0.65±0.01）， （0.78±0.03）and （0.92±0.04） cm/min in high-dose， medium-dose， and low-dose groups of self-made microemulsion （2.561， 0.256， 0.128 mg/mL of menthol） respectively， which were significantly lower than normal saline group and compound menthol nasal droups （P＜0.05）. The cilia movement time in vitro were（206.7±4.9）， （226.0±13.5）， （269.3±12.9）min， which were significantly longer than sodium deoxycholate group （P＜0.05）. CONCLUSIONS： The preparation technology of self-made microemulsion is easy-to-handle and controllable in quality. The prepared microemulsion shows good mucosal adhesion without cilia toxicity．

Study on Preparation Phase Identification and Release Rate in vitro of Inclusion Compound of Indapamide- β-cyclodextrin Inclusion Compound / 中国药房

OBJECTIVE： To establish a method for content determination of indapamide （IDP）-β-cyclodextrin （β-CD） inclusion compound， optimize the preparation technology， carry out phase identification and in vivo release study of it. METHODS： UV spectrophotometry was used to determine the content of IDP in IDP-β-CD inclusion compound. IDP-β-CD inclusion compound was prepared by the solution-stirring method and the preparation technology was optimized by the orthogonal experiment using inclusion rate as index. The inclusion rate and drug-loading rate were compared between different drying methods. Phase identification of IDP-β-CD inclusion compound was verified by IR and DSC. The cumulative release rate of inclusion compound was tested by in vitro experiment. RESULTS： The linear range of concentration of IDP was 2.0-14.0 μg/mL （r＝0.999 7）. The quantitative limit and detection limit were 0.204， 0.067 μg/mL， respectively. RSDs of precision， stability and repeatability tests were all less than 2％. The recoveries range was 98.8％-101.8％（RSD＝1.10％，n＝6）. The optimum technology conditions were as follows the molar ratio of β-CD to IDP was 3 ∶ 1， the inclusion time was 3 h， and the stirring speed was 300 r/min. Average inclusion rate of IDP-β-CD inclusion compound was 72.81％. IR and DSC analysis showed that IDP and β-CD formed inclusion compound through physical interaction. After spray drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （60.96±0.25）％ and （4.18±0.12）％. After freeze-drying， the inclusion rate and drug-loading rate of IDP-β-CD inclusion compound were （77.31±0.51）％ and （5.31±0.27）％. Accumulative release rates of IDP， IDP-β-CD inclusion compound （by freeze-drying and spray drying） were 37.2％， 42.5％ and 81.9％ within 12 h， respectively. Compared with IDP raw material， accumulative release rate of IDP-β-CD inclusion compound increased significantly after spray drying. CONCLUSIONS： Established method is simple and accurate. The optimal preparation technology of inclusion compound is stable and feasible. IDP-β-CD inclusion compound is prepared successfully. The inclusion compound prepared by spray drying shows higher release rate.

Study on the Optimization of Water-extraction Technology of Yao Medicine Jasminum lanceolarium and the Anti-inflammatory and Analgesic Effect of Its Water Extract / 中国药房

OBJECTIVE:To optimize the water-extraction technology of Yao medicine Jasminum lanceolarium and study the anti-inflammatory and analgesic effect of its water extract. METHODS:The single factor test and orthogonal test were used to investigate the effects of extraction time,liquid-solid ratio and extraction times on water-extraction technology and optimize extraction technology using ferulic acid content and dry extract yield as index. The validation test was also conducted. With aspirin as positive control,the method of ear edema induced by xylene and paw edema induced by carrageenan in mice were used to observe the anti-inflammation effects of low-dose,medium-dose and high-dose(3,6,12 g/kg,by crude drug)of J. lanceolarium water extract;the analgesic effect of those was investigated by hot-plate induced pain response test and mice writhing response test. The contents of TNF-α and IL-1 β were determined by ELISA after carrageenan induced inflammation in mice. The contents of PGE2in serum and inflammation tissue were detected by UV spectrophotometry.RESULTS:The optimal extraction technology was as follows as extraction time of 120 min,liquid-solid ratio of 16:1(mL/g),extracting for 3 times.Compared to model group,the ear edema degree and paw edema rate of mice were raduced,writhing response times were lessened,and pain response threshold was enhanced significantly in low-dose,medium-dose and high-dose groups of J. lanceolarium water extract(P<0.05 or P<0.01). Compared to model group,the contents of TNF-α,IL-1β and PGE2in serum and the content of PGE2in inflammation tissue of mice were raduced significantly in low-dose,medium-dose and high-dose groups of J. lanceolarium water extract(P<0.05 or P<0.01). CONCLUSIONS:The optimized water-extraction technology of Yao medicine J. lanceolarium shows high efficiency,stable and feasible.Water extract shows significant anti-inflammatory and analgesic effects through reducing the contents of TNF-α,IL-1β and PGE2.

Optimization of Extraction Technology of Protein from Cryptotympana pustulata and in vitro Antioxidant Activity Study / 中国药房

OBJECTIVE:To optimize extraction technology of protein from Cryptotympana pustulata and investigate its in vitro antioxidant activity,so as to provide reference for further research of protein from C. pustulata. METHODS:Using extraction amount of protein as response value,based on single factor test,Box-Behnken response surface methodology was used to optimize the ratio of liquid to material,ultraonic time and extraction times.Validation test was conducted. Using Vitamin C(VC)as positive control, in vitro antioxidant activity of protein from C. pustulata was evaluated by using scavenging rate of 1, 1-diphenyl-2-picrylhydrazyl(DPPH)and 2,2′-azino-bis(3-ethyl benzothiazoline-6-sulfonic acid)(ABTS)free radical as index. RESULTS:The optimal extraction condition of protein from C.pustulata was as follows as the ratio of liquid to material 28:1(mL/g), ultrasonic time of 65 min,extracting for twice. In validation test,average extraction amount of protein from C. pustulata was 65.45 mg/g(RSD=1.68%,n=3),relative error of which to predicted value was 5.48%. The protein from C. pustulata showed strong scavenging effect on ABTS and DPPH free radicals. When the concentration of protein from C. slough was 0.2 mg/mL,and the scavenging rate of it to ABTS free radicals was 97%,the effect of which was similar to VC.The protein from C. pustulata showed weak scavenging ability to DPPH free radical,IC50was 0.96 mg/mL,the effect of which was not as good as VC. CONCLUSIONS:The extraction technology of protein from C. pustulata optimized by Box-Behnken response surface methodology shows high accuracy and good reliability.The protein from C.pustulata shows certain antioxidant activity in vitro.

Optimization of the Extraction Technology of Total Flavonoids from the Roots and Stems of Angelica sinensis / 中国药房

OBJECTIVE: To optimize reflux extraction technology of total flavonoids from the roots and stems of Angelica sinensis. METHODS: The reflux extraction technology of total flavonoids from the roots and stems of A. sinensis was optimized by Box-Behnken design-response methodology based on single factor test using volume fraction of extraction solvent ethanol, solide-liquid ration, extraction time, extraction times as investigation factors, the content of total flavonoids in extract as evaluation index. RESULTS: The optimal extraction technology of total flavonoids from the roots and stems of A. sinensis was that volume fractions of ethanol were 70％ and 50％; solid-liquid ratios were 1: 40 and 1: 30; extraction time were 1. 3 h and 1. 7 h; The number of extraction times is two times. In verification test, the contents of total flavonoids were 7. 253 6, 25. 144 1 mg/g (RSD= 1. 57％, 1. 49％, n = 3); relative errors of those to predicted value (6. 942 8, 25. 703 5 mg/g) were 4. 28％, 2. 24％. CONCLUSIONS: Optimized extraction technology for total flavonoids from the roots and stems of A. sinensis is simple, reproducible and predictable.

Optimization of Ultrasonic Extraction Technology for Tianshu Capsules by Orthogonal Test / 中国药房

OBJECTIVE:To optimize the ultrasonic extraction technology for Tianshu capsules. METHODS:Using the transfer rate of active ingredient ferulic acid in Ligusticum chuanxiong and gastrodin in Gastrodia elata of Tianshu capsules as investigation indexes,L9(34)orthogonal design test was adopted to investigate the effects of ethanol volume fraction,ethanol amount,extraction time and ultrasonic power on the extraction rate. Ultrasonic extraction technology for Tianshu capsules was optimized,and verifica-tion test was carried out. RESULTS:The optimized extraction technology for Tianshu capsules was as follow as 8-fold 70% etha-nol,extracting twice under 350 W,extracting 1.5 h every time. Results of verification test showed the average transfer rate was 94.06% for ferulic acid(RSD=0.18%,n=3)and 95.02% for gastrodin(0.47%,n=3). CONCLUSIONS:The optimized tech-nology is rapid,simple,stable and feasible,and can be used for extracting the active ingredients in Tianshu capsules.

Optimization of Extraction Technology for Tibetan Medicine Duoxuekang by Uniform Design / 中国药房

OBJECTIVE:To optimize the extraction technology of Duoxuekang. METHODS:Using comprehensive score of salidroside,gallic acid content and extraction yield as indexes,U6(63)uniform design was designed to optimize the liquid-solid ra-tio,ethanol volume fraction and extraction time of Duoxuekang,then optimize extraction times,and verification test was conduct-ed. RESULTS:The optimal extraction technology was as follows as 50% ethanol,liquid-solid ratio of 1:14,soaking time of 1.5 h,reflux extraction for 1 h and repeated twice;the average extraction yield in 3 tests was 50.18%,contents of salidroside and gal-lic acid were 1.82 mg/g,16.54 mg/g (RSD≤0.84%,n=3). CONCLUSIONS:The optimized extraction technology for Duox-uekang is reasonable,simple and feasible.