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OBJECTIVE Optimizing the water extraction technology of Xiangqin jiere granules. METHODS The orthogonal test of 3 factors and 3 levels was designed， and comprehensive scoring was conducted for the above indexes by using G1-entropy weight to obtain the optimized water extraction technology of Xiangqin jiere granules with water addition ratio， extraction time and extraction times as factors， using the contents of forsythoside A， baicalin， phillyrin， oroxylin A-7-O-β-D-glycoside， wogonoside， baicalein and wogonin， and extraction rate as evaluation indexes. BP neural network modeling was used to optimize the network model and water extraction process using the results of 9 groups of orthogonal tests as test and training data， the water addition multiple， decocting time and extraction times as input nodes， and the comprehensive score as output nodes. Then the two analysis methods were compared by verification test to find the best water extraction process parameters. RESULTS The water extraction technology optimized by the orthogonal test was 8-fold water， extracting 3 times， extracting for 1 h each time. Comprehensive score was 96.84 （RSD＝0.90%）. The optimal water extraction technology obtained by BP neural network modeling included 12-fold water， extracting 4 times， extracting for 0.5 h each time. The comprehensive score was 92.72 （RSD＝0.77%）， which was slightly lower than that of the orthogonal test. CONCLUSIONS The water extraction technology of Xiangqin jiere granules is optimized successfully in the study， which includes adding 8-fold water， extracting 3 times， and extracting for 1 hour each time.
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OBJECTIVE To evaluate the quality of Amomum tsao -ko from different origins and harvesting periods comprehensively. METHODS The contents of total volatile oil in A. tsao -ko were determined by volatile oil measurement method A stated in 2020 edition of Chinese Pharmacopoeia （part Ⅳ）；the contents of total flavonoids and total polyphenols in A. tsao -ko were determined by aluminum nitrate-sodium nitrite colorimetry and folin-ciocalteu method. The contents of α-pinene，β-pinene， 1，8-cineole，α-terpineol，geraniol and trans-nerolidol in the volatile oil of A. tsao -ko were determined by gas chromatography ；the contents of protocatechuate and vanillic acid in A. tsao -ko were determined by ulta high performance liquid chromatography. The above 11 indicators were selected ，and entropy weight TOPSIS method was used to comprehensively evaluate the quality of 16 batches of A. tsao -ko. RESULTS The contents of total volatile oil ，total flavonoids ，total polyphenols ，α-pinene，β-pinene， 1，8-cineole，α-terpineol，geraniol，trans-nerolidol，protocatechuate and vanillic acid in 16 batches of A. tsao -ko were 15.833 3- 28.000 0 μL/g，29.100 5-78.199 6 mg/g，6.789 8-35.797 7 mg/g，0.088 7-0.401 3 mg/g，0.106 3-0.408 0 mg/g，3.709 6-8.533 1 mg/g，0.259 8-0.599 6 mg/g，0.314 8-1.324 1 mg/g，0.272 3-0.576 4 mg/g，9.301 2-19.818 5 μg/g，8.180 9-27.666 3 μg/g， respectively. Entropy weight TOPSIS results showed that the top three of relative closeness rankings were A. tsao -ko produced by Yunnan Baoshan in July ，Yunnan Honghe in October ，Yunnan Wenshan in September ；the last three of relative closeness rankings were A. tsao -ko produced by Yunnan Dehong in September ，Yunnan Dehong in November ，Yunnan Dehong in December. CONCLUSIONS A. tsao -ko produced by Yunnan Baoshan in July ，Yunnan Honghe in October and Yunnan Wenshan in September present better quality.
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OBJECTIVE：To study the pharmacokinetics and tissue distribution characteristics of Hydroxycamptothecin （HCPT） nanoparticles in rats ，and to investigate their targeting. METHODS ：Male SD rats were randomly divided into 2 groups，with 6 rats in each group. They were given HCPT nanoparticles and HCPT injection （4 mg/kg based on HCPT ）via tail vein respectively. 500 μL fundus venous plexus blood were sampled at 5，30，60，120，240，360，480，600 and 720 min after administration. The plasma concentration of HCPT in rats were measured by HPLC at different time points. The pharmacokinetic parameters were calculated by DAS 3.0 software. Male SD rats were randomly divided into two groups ，with 24 rats in each group. They were given HCPT nanoparticles and HCPT injection （0.6 mg/kg based on HCPT ）via tail vein ，respectively. Blood was immediately taken from the abdominal aorta ，and heart ，liver，spleen，lung，kidney and brain were removed at 30，60，120，240 min after administration. The plasma and tissue concentration of HCPT in rats were measured by HPLC. The distribution of HCPT ineach tissue and targeting were investigated. RESULTS ：HCPT nanoparticles and its injection conformed to a two-compartment model in rats. Compared with HCPT injection ，AUC0-720 min andAUC0- ∞ increased by 1.89 and 1.87 times respectively ， MRT0-720 min and MRT 0- ∞ increased by 2.74 and 3.00 times respectively， t1/2 β increased by 2.75 times，with statistical significance（P＜0.05）. At 30 min after administration ，HCPT nanoparticles and HCPT injection had the highest concentration in lung；with the passage of time ，the drug gradually accumulated in the liver and reached the highest concentration at 60 min. The relative liver uptake rate of HCPT nanoparticles was the highest （6.28）. Taking liver ad target organ ，and the targeting efficiencies of it in heart ，spleen，lung，kindey，brain and plasma were higher than those of HCPT injection. The selectivity index of HCPT nanoparticles in heart ，lung（except for 30 min after administration ），kidney，brain and plasma were significantly higher than those of HCPT injection at 30-120 min after administration. CONCLUSIONS ：HCPT nanoparticles extend the half-life of the drug ， increase its plasma concentration ，and prolong its action time in vivo ，with significant liver targeting.
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OBJECTIVE：To stud y the pharmacok inetics of PELGE-crebanine nanopartic les （PELGE-Cre-NPs） in rabbits. METHODS：Totally 6 rabbits were collected ，and injected with PELGE-Cre-NPs （3.5 mg/kg）via ear vein. 1 mL of blood samples were collected at 5，15，30，60，90，120，150，180，240，300 min after administration from the ear vein. After the plasma were isolated and Cre were extracted with ethyl acetate ，HPLC method was adopted to determine the plasma concentration of Cre by using verapamil hydrochloride as internal standard. The plasma concentration-time curve was drawed and pharmacokinetic parameters were calculated by using DAS 2.0 software. Chromatographic conditions such as the chromatographic column was Agilent ZORBAX Extend-C 18；the mobile phase consisted of methanol- 0.01％ triethylamine solution （75 ∶ 25，V/V）；the flow rate was 1 mL/min；the detection wavelength was 280 nm；the column temperature was 30 ℃；the injection volume was 20 μL. RESULTS：The linear range of Cre were 45.0-3 600 µg/L（R2＝0.999 9）. RSDs of inter-day and intra-day precision and stability tests were all lower than 5％（n＝6 or n＝12）；the accuracies were （97.44±2.41）％-（98.45±3.87）％（n＝6）. PELGE-Cre-NPs was in a two-compartment model in rabbits. Main pharmacokinetic parameters included that t1/2 was（109.357±33.917）min；CL was（0.016±0.001）L/（min·kg）；MRT was （76.733±7.502）min；cmax was（3 699.458±287.713）μg/L. CONCLUSIONS：The half-life period of PELGE-Cre-NPs in rabbits is longer than that of Cre injection；its retention time in the body is prolonged ，and sustained-release effect is obvious.
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OBJECTIVE： To establish a method for concentration determination of sinoacutine in rabbit plasma， and to conduct its pharmacokinetic study. METHODS： The rabbits were grouped according to gender， 6 rabbits in each group. Rabbits were injected with sinoacutine solution （5 mg/kg） via ear vein. Each blood sample 1 mL was collected before medication and 5， 10， 15， 30， 45， 60， 90， 120， 180， 240 min after medcation. After the plasma isolated and extracted with ethyl acetate， HPLC method was adopted by using sinomenine as internal standard. The determination was performed on Agilent Zorbax Extend-C18 column with mobile phase consisted of methanol-2 mmol/L disodium hydrogen phosphate aqueous solution （containing 0.016％ triethylamine， pH 9.8） （45 ∶ 55， V/V) at the flow rate of 1 mL/min. The detection wavelength was set at 262 nm， and column temperature was 30 ℃. The sample size was 20 μL. The pharmacokinetic parameters were calculated by using DAS 3.0 software. The difference of 2 groups were investigated by t-test. RESULTS： The linear range of sinoacutine were 0.1-5.0 mg/L； the limit of quantitation was 0.1 mg/L， and the lowest detection limit was 0.08 mg/L. RSDs of intra-day and inter-day were both less than 10％； the accuracy ranged from （99.80±8.21）％-（103.61±8.55）％. The extraction method did not affect the quantitative analysis of the substance to be measured. The average plasma-time curve of sinomenine with single intravenous injection in rabbits was in line with the two-compartment model. The distribution half-life of all rabbits was （10.99±2.52） min， and the elimination half-life was （147.08±32.41） min. AUC0-t was （190.82±30.82）mg·min/L， and AUC0-∞ was （289.82±73.27） mg·min/L. There was no statistical significance in pharmacokinetic parameters between female and male rabbits （P＞0.05）. CONCLUSIONS： Established HPLC method is simple， specific and sensitive， and can be used for plasma content determination of sinoacutine. Pharmacokinetic study shows that the pharmacokinetic process of the compound is in line with two-compartment model in rabbits. The pharmacokinetic parameters of the compound have no sex difference， and the compound is distributed rapidly and eliminated fast.
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OBJECTIVE:To prepare and characterize Fluorescent dye 1,1′-octacosyl-3,3,3′,3′-tetramethylindocarbocyanine iodide(DiR)-loading polyethylene glycol-poly lactic-co-glycolic acid(DiR-PEG-PLGA)nanocapsules,and to evaluate its biocompatibility in vitro. METHODS:Using PLGA and PEG-PLGA as carrier,DiR-PEG-PLGA nanocapsules were prepared by modified ultrasonic emulsification method. The particle size,Zeta potential,morphology,stability and fluorescence in vitro of nanocapsules were detected respectively. MTT assay was used to evaluate cytotoxicity in vitro of nanocapsules to human-derived HL7702 hepatocytes,and hemolysis test was carried out to investigate its hemolysis effects. RESULTS:Prepared DiR-PEG-PLGA nanocapsules were spherical with a clear core-shell structure. The average particle size was(507.53 ± 7.87)nm,polydispersity coetficient of particle size was 0.306 1±0.001 5 and Zeta potential was(-35.20±0.92)mV with good stability within 6 months under 4℃. Fluorescence signal intensity(y)of nanocapsules was increased linearly with DiR mass concentration(x)in vitro. The linear eguation was y=0.345 2x+0.433 4(R2=0.997 3).The toxicity of nanocapsules to HL7702 cells was between 0-1 degree,and no hemolytic effect was observed. CONCLUSIONS:The study successfully prepare fluorescent DiR-PEG-PLGA nanocapsules with high biocompatibility in vitro,which is further expected to become a safe optical drug carrier.
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Objective To optimize the preparation technology ofCangai volatile oil dextrin inclusion compound/ in situ nasal thermosensitive gel by the central composite design-response surface method.Methods In the design, the investigation factors were the amounts of poloxamer 407 and poloxamer 188, and the evaluation index was the gel temperature. Quadratic models were used to evaluate the mathematic relation between the evaluation index and two investigation indexes to identify the optimum prescription, and then the optimum prescription was verified. Results According to the quadratic models, it was found that there was reliable quantitative relation between the evaluation index and two investigation indexes, among which the optimum dosage was 19.37% for poloxamer 407 and 2.73% for poloxamer 188.Conclusion The optimum model ofCangai volatile oil dextrin inclusion compound/ nasal thermosensitive gel can be obtained from central composite design-response surface method based on quadratic models. This method is reliable and feasible, which can realize the prescription optimization of the in situ gel.
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Aim To investigate the effect of isocorydine on arrhythmia in rats induced by myocardial ischemia/reperfusion injury. Methods SD rats were randomly divided into 6 groups: sham group, myocardial ische-mia/reperfusion group, verapamil group and isoc-orydine group of 2. 5 , 5 , 10 mg · kg-1 , each group having 16 rats. Left anterior descending ( LAD ) was tied up to establish the injury model of myocardial is-chemia. ECG was recorded for analysis. The ischemic and infarction area was measured and indexes of SOD, MDA, GSH-Px in the myocardial were determined. Re-sults Isocorydine could significantly reduce the inci-dence of arrhythmia induced by ischemic/reperfusion, including VT, VF;and reduce ischemic and infarction area. Further study demonstrated that isocorydine could increase myocardial SOD and GSH-Px, but de-crease myocardial MDA. Conclusion Isocorydine has a protective effect on the myocardial ischemia/reperfu-sion injury, which might be related to its anti-oxidative function.
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Paecilomyces hepialid was obtained through separation from cordyceps. Its name comes from studies on identification, cultivation, and morphology. It is one of the common substitutes of cordyceps. This article made a summary from the aspects of review, cultivation methods, active constituents, pharmacological effects, and product development. It also discussed the major issues remaining in the current researches and made suggestions for future studies.
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Objective To develop a RP-HPLC method for the determination of Brucine and Strychnine in Semen Strychni and its extractive of total alkaloids. Methods A chromatographic column of Licrospher C18 (4.6 mm×250 mm, 5 μm) was used with the mobile phase of acetonitrile∶0.01 mol/L sodium heptane sulfonate and 0.02 mol/L potassium dihydrogen phosphate mixed with equal amount (adjusted pH to 2.8 with 10% phosphonic acid)=27∶73, detection wavelength at 260 nm, column temperature of 30 ℃ and flow rate of 1 mL/min. Results The calibration curves of Brucine and Strychnine were both in good linearity in the ranges of 0.1-1.0 μg and 0.12-1.2 μg (r=1.000) respectively. The average recovery rates of Brucine and Strychnine were 99.88% (RSD=1.06%) and 100.06% (RSD=0.78%) respectively. Conclusion The method is realiable and accurate, which can be applied to determination of Brucine and Strychnine in Semen Strychi and its extractive.
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Objective To investigate the effects of volatile oils of Rhizoma Acori Tatarinowii (RAT), Semen Myristicae (SM) and Pericarpium Citri Reticulatae (PCR) on percutaneous penetration of total alkali of Shortstalk Monkshood Root through mouse skin in vitro. Methods By using an improved Franz diffusion cells, the effects of these 3 kinds of volatile oil on the percutaneous penetration of total alkali of Shortstalk Monkshood Root were observed and compared with Azone, and the cumulative amount of Bullatine A was determined by HPLC. Results 7% (v/v) volatile oil RTA and SM, 5% (v/v) volatile oil of PCR and 3% (v/v) Azone were best concentration, the penetration coefficient were 5.88, 6.91, 5.30, 5.75, respectively. Compared with the group without penetration enhencers, the enhancement ratios were 1.09,1.28, 0.98, 1.06, respectively. Conclusion The volatile oil of RAT and SM enhance penetration of total alkali of Shortstalk Monkshood Root. The volatile oil of PCR cannot enhance penetration.
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Objective: To study the effect of volatile oil of Fructus Litseae(FL) ,Rhizoma Zingiberis(RZ) and Rhizoma Acori Talarinowii(RAT) on percutaneous penetration of aconitine through mouse skin in vitro.Methods :By using improved Franz diffusion cells,the effects of these 3 volatile oils on the percutaneous penetration of aconitine were observed and compared with azone,and the cumulative amount of aconitine was determined by HPLC.Results : The penetration coefficient of aconitine with 7%(v/v) volatile oil of FL,RZ and RAT and 3% azone were 10.79,5.82,5.40,3.91,respectively;Compared with the group without penetration enhancers,the differences were significannt;and the enhancement ratios were 3.87,2.09,1.94 and 1.40,respectively,which showed the enhancement ratios of 7% of the 3 volatile oils were higher than that of 3% azone.Conclusion :The 7% volatile oils of FL,RZ and RAT enhance the permeation of aconitine effectively.