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Objective:To evaluate the cerebral infarct volume and the nerve fiber connectivity between cortical and neurogenesis-related regions in the mouse model of reperfusion after middle cerebral artery occlusion (MCAO) by 11.7 Tesla(11.7 T) magnetic resonance imaging (MRI).Methods:MCAO models were established in SPF grade adult male C57BL/6 mice using the suture-occluded method.MRI scans were performed at 3 days before and 1 day after modeling.Infarct volumes were calculated, and nerve fiber tracking was performed on specific brain regions to analyze the nerve fiber number and the parameters of fractional anisotropy(FA), mean diffusivity(MD), axial diffusivity (AD)and radial diffusivity(RD). SPSS 26.0 was used for statistical analysis, and paired t test was used to compare the data before and after modeling. Results:(1) After MCAO-induced ischemia, the infarct volume was up to (35.11±17.57)mm 3, and the FA value of the infarct area was significantly reduced compared with that of before modeling( t=4.73, P<0.01). (2) At the anterior-posterior(AP): + 1.2 mm section, the results of fiber tracking showed that compared with before modeling, the number of fiber bundles originating from the dorsal horn of the lateral sub-ventricle zone(SVZ)to the cortex reduced ((92 584.20±14 751.00) vs (59 815.60±6 752.46), t=4.87, P<0.01), and the number of fiber bundles projected to the infarcted area reduced ((107 671.40±10 497.57) vs (61 658.60±10 178.21), t=6.43, P<0.01). FA, AD, MD, and RD values were all decreased in different degrees( t=3.38-6.43, all P<0.05). (3) At the AP: -3.8 mm section, the number of fiber bundles originating from the dorsal horn of the SVZ to the cortex decreased (after modeling(96 944.00±18 331.09), before modeling(58 767.80±16 445.25), t=2.99, P<0.05), and the values of FA, AD, MD and RD decreased after ischemia ( t=7.30, 5.05, 6.74, 4.13, all P<0.05). Conclusion:The ultra-high field strength of 11.7 T MRI can accurately detect the following results that the number of nerve fiber bundles from the SVZ to the cortex or infarct area are both significantly reduced, and diffusion tensor parameters are consistently changed in mice after 1 day of ischemia-reperfusion.
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In order to research and enhance bioavailability of chlorogenic acid and rutin[CA-R] via the oral route, chitosan coated composite phospholipid liposomes [C-CPLs] were applied to study on preparation, permeability and pharmacokinetic of C-CA-R-CPLs. TheC-CA-R-CPLs were prepared by the method of ethanol injection. The entrapment efficiency [EE], average particle sizes, polymer disperse index [PDI], zeta potential, shape and in vitro drug release were investigated to characterize physicochemical parameters of C-CA-R-CPLs. The penetration properties from C-CA-R-CPLs were studied through Caco-2 cells model and the pharmacokinetics in Sprague-Dawley [SD] rats were evaluated by rat jugular vein intubation tube. The EE of C-CA-R-CPLs of CA and R was 91.3+/-2.13% and 92.6+/-2.44%, particle size of C-CA-R-CPLs was 176.7+/-2.3 nm, PDI was 0.207+/-0.014 and zeta potential of 12.61+/-1.33 mV. CA-RCPLs and C-CA-R-CPLs were spherical or elliptical sphere and the bilayer of the CPL was observed obviously under transmission electron. The C [max], t1/2 and AUC[0-12] h values of CA and R for groups of C-CA-R-CPLs were significantly increased.In conclusion, TheC-CA-R-CPLs as a novel nano-formulation have potential to be used to enhance the oral bioavailability of poorlywater-soluble drugs after oral administration
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OBJECTIVE:To study the effects of tilianin(TIL)on brain tissue in rats with cerebral ischemia-reperfusion injury. METHODS:Totally 120 male SD rats were randomly divided into sham operation group(0.9% sodium chloride solution),model group(0.9% sodium chloride solution),nimodipine group(32 mg/kg)and TIL low-dose and medium-dose,high-dose groups(4, 8,16 mg/kg),with 20 rats in each group. The rats were given relevant medicine intragastrically,once a day,for consecutive 7 d. 15 min after last medication,cerebral ischemia-reperfusion injury model was established by reforming suture-occluded method. The neurological deficit score in rats were evaluated, and percentage of cerebral infarction volume of rats was determined. Histopathological changes of brain tissue were observed by HE staining. The activities of SOD,CAT and LDH,MDA content in cerebral tissue of rats were determined. The expression of calcitonin gene-related peptide(CGRP)and peripheral vascular endothelial growth factor receptor 2 (VEGFR2) protein were determined by Western blot assay. RESULTS:Compared with sham operation group,neurological deficit score and percentage of cerebral infarction volume of model group were increased significantly(P＜0.01);the nerve cells in brain tissue were significantly reduced and the interstitial edema was obvious. SOD and CAT activities were decreased significantly,LDH activity was increased significantly,MDA content was decreased significantly,protein expression of CGRP and VEGFR2were increased significantly(P＜0.05 or P＜0.01). Compared with model group,neurological deficit score of nimodipine group,TIL medium-dose and high-dose groups were decreased significantly;percentage of cerebral infarction volume was decreased significantly (P＜0.05 or P＜0.01);above pathological conditions of cerebral tissue in rats were relieved significantly;SOD and CAT activities were strengthened significantly,MDA content and LDH activities were decreased significantly,protein expression of CGRP and VEGFR2were increased significantly (P＜0.05 or P＜0.01). CONCLUSIONS: TIL has certain protective effects on cerebral ischemia-reperfusion injury model rats,and its mechanism may be related to the up-regulation of CGRP and VEGFR2expression.
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The present study was undertaken to optimize the preparation conditions of total flavonoids extract from Dracocephalum Moldavuca composite phospholipid liposome [TFDMCPL]by response surface methodology [RSM] and to investigate the in vitro release [IVR] of TFDMCPL. Method of ethanol injection was adopted to prepare TFDMCPL. The single factor experiments were used for the key experimental factors and their test range. Based on the single factor experiments, with encapsulation efficiency [EE] Size of TFDMCPL and polymey disperse index [PDI] as dependent variable, central composite design was adopted to optimize preparation technology by taking content of phospholipid and content of cholesterol as independent variables, fitting of various mathematical equations were performed using a statisitical software of Design-Expert 8.0.6. Preparation parameters were optimized through response surface plotted by optimum fitting equations, optimized procedure was validated through experimental preparation of TFDMCPL. Optimum preparation technology was as following: phospholipid 505mg and cholesterol 50mg. Under these condition, encapsulation efficiency was 90.2+/-1.2%, size of TFDMCPL was 115.6+/-4.3nm, PDI was 0.169+/-0.015 and Zeta potential was -15.38+/-0.5. These indicated that TFDMCPL with high entrapping efficiency and small particle size could be prepared by the ethanol injection method. And TFDMCPL were found to enhance the release of drugs more effectively than TFDM based on the in vitro model
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In Vitro Techniques , Plant Extracts , Phospholipids , Liposomes , FlavonoidsABSTRACT
OBJECTIVE:To establish a method for content determination of rosmarinic acid and total polysaccharide in Hysso-pus. offcinalis. METHODS:HPLC was conducted to determine the content of rosmarinic acid in H. offcinalis. The column was Shim-pack VP-ODS with mobile phase of acetonitrile-0.5% formic(17:83,V/V) at flow rate of 1.0 ml/min,detection wavelength was 330 nm,column temperature was 30 ℃,and the injection volume was 10 μl. UV-visible spectrophotometry was conducted to determine the content of total polysaccharide,detection wavelength was 620 nm. RESULTS:The linear range was 10.86-54.30 μg/ml (r=0.999 8)for rosmarinic acid and 1.996-15.97 μg/ml for total polysaccharide(r=0.999 6);RSDs of precision,stability and re-producibility tests were lower than 1.0% and 2.0%,respectively;recoveries were 98.20%-101.79%(RSD=1.68%,n=6) and 96.62%-101.68%(RSD=1.88%,n=6). CONCLUSIONS:The method is simple and reproducible,and can be used for the con-tents determination of rosmarinic acid and total polysaccharide in H. offcinalis.
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Hot-melt extrusion (HME) is the process of pumping raw materials with a rotating screw under the elevated temperature and pressure through a die to from a product with the uniform shape. This technique combines many advantages of solid dispersion technology and mechanical preparation, including dust reduction, short duration of extrusion process, without use of organic solvents and water, without heat drying and hydrolysis, etc. In addition, it has the superiority in solubility, taste masking, drug stability and drug release. Besides, this technique has good reproducibility, high production efficiency, and it can be online monitored in the mass production. Therefore, this technique is widely used in the research and development of drug dosage forms involved in rapid and immediate drug release, sustained drug release, gastrointestinal drug site-specific release, transdermal drug delivery systems and so on. This paper reviews the advantages of HME and its recent application in the pharmaceutical research.
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Objective To investigate the effects of moldavica total flavone on vascular endothelial growth factor (VEGF), intercellular adhesion molecule-1 (ICAM-1), nitric oxide (NO) and endothelin-1 (ET-1) in ovalbumin-induced bronchial asthmatic rats, and explore its mechanism. Methods A total of 60 SD rats was randomly divided into control group, model group, dexamethasone (1 mg/kg) group and moldavica total flavone low (90 mg/kg), medium (180 mg/kg) and high (360 mg/kg) dose group. Rats asthma model was established by ovalbumin challenge methods except the control group. After modeling, rats in control and model groups were intragastrically given distilled water, rats in medicine groups were intragastrically given moldavica total flavone and dexamethasone for 30 d. VEGF in lung tissue and ICAM-1 in bronchoalveolar lavage fluid (BALF) were detected respectively by ELISA. The content of ET-1 and NO in BALF were analyzed with radioimmunity method and nitric acid reductase method. Results The VEGF in lung tissue and ICAM-1, NO and ET-1 in BALF were decreased by moldavica total flavone at 180 and 360 mg/kg (P<0.05, P<0.01) in ovalbumin-induced bronchial asthmatic rats. Conclusion Moldavica total flavone is effective in adjusting abnormal increase of VEGF, ICAM-1, ET-1 and NO of bronchial asthma rats.
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<p><b>OBJECTIVE</b>To observe the uptake of tiliani in Caco-2 Cell.</p><p><b>METHOD</b>A human intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study the kinetics of uptake, transport and efflux kinetics of tiliani at small intestine. The effect of time, pH, drug concentration and inhibitors on the uptake of tiliani were investigated. The determination of tiliani was performed by HPLC.</p><p><b>RESULT</b>Tiliani in Caco-2 cell uptake was time-dependent. Tiliani in Caco-2 cell uptake was concentration-dependent at 4-16 mg x L(-1) consistent with passive diffusion process. The acid condition was good for the uptake of tiliani at pH 5-8. Compared with the control group, tiliani cell uptake was significantly higher after additional treatmeant with verapamil (1.545 +/- 0.010) mg x g(-1), (P < 0.05), and tiliani cell uptake was significantly lower after additional treatmeanet with sodium azide (0.994 +/- 0.003) mg x g(-1) (P < 0.05), with 2,4-dinitrophenol (1.174 +/- 0.030) mg x g(-1) (P < 0.05), and with phloridzin (1.098 +/- 0.021) mg x g(-1) (P < 0.05). Compared with the control group, tiliani cell uptake was not significantly after additional treatmeant with lactose (1.470 +/- 0.025) mg x g(-1), Papp of Basolateral to Apical was much more than that of Apical to Basolateral (1.10 Fold).</p><p><b>CONCLUSION</b>P-glycoproteins and SGLT1 participate in the conveying process of tiliani in Caco-2 cells. The uptake of tiliani has no relationship to LPH. passive transport and carrier-mediated transport participate in the uptake process of tiliani in Caco-2 cells.</p>
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Humans , Biological Transport , Caco-2 Cells , Chromatography, High Pressure Liquid , Flavonoids , Pharmacokinetics , Glycosides , Pharmacokinetics , Intestinal Absorption , Kinetics , Verapamil , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To optimize the formulation of gel matrix of Saussurea involucrate.</p><p><b>METHOD</b>The formulation of gel containing carbopol, azone, trimethylene glycol and alcohol was optimized by orthogonal design with evaluation indexes such as consistency in room temperature, consistency of average temperature of skin, yield value and rheopexy in room temperature.</p><p><b>RESULT</b>The optimal proportion of matrix components was made from carbopol-azone-trimethylene glycol-absolute alcohol (2. 0: 2. 0:15.0 : 30.0).</p><p><b>CONCLUSION</b>The optimal formulation of S. involucrate gel based the optimal formulation is well-distributed and transparent, it has proper consistency and well rheopexy.</p>
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Chemistry, Pharmaceutical , Dosage Forms , Drugs, Chinese Herbal , Chemistry , Saussurea , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To optimize the extraction process of compund kaliziran gel.</p><p><b>METHOD</b>Orthogonal design was used to optimize the extracting process of eight herb medicines with the extract yield, the content of psoralen, isopsoralen and osthole as indexes, and to optimize the extracting process of Polygonum multflorumi and Seman sinapis albae with the extract yield and the content of 2,3,5,4'-tetrehydroxy-stilbene glucoside as indexes.</p><p><b>RESULT</b>The optimum extraction progress was as follows:eight herb medicines were extract 2 times for 1 hour with 8 times of 60% alcohol; P. multflorumi and S. sinapis albae were extract 2 times for 1 hour with 8 times of 40% alcohol.</p><p><b>CONCLUSION</b>The optimum extraction processes are stable and feasible.</p>
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Alcohols , Chemistry , Chemical Fractionation , Methods , Drugs, Chinese Herbal , Plants, Medicinal , Chemistry , Technology, Pharmaceutical , MethodsABSTRACT
AIM:To select an optiomal formulation of liposome entrapped alkanin prepared with ethanol injection in the combination of orthogonal design and central composite design/Response surface method.METHODS:Five influencing factors,including ratio of alkanin to liposome and soyabean lecithin to cholesterol,volume ratio of ethanol phase to water phase,soybean concentration and mannitol concentration were chosen as indices by orthogonal design.Then the method utilized the central composite design,which fitted multivariate linear and second/third order nonlinear regression equation,to find out the optimal formulation.RESULTS:Third order regression equation gained made the good prediction about entrapment(85.4%)and alkanin load(5.16%),and exhibited no significant difference between theoretic value and measured value.CONCLUSION:The combination of orthogonal design with central composite design is a feasible and convenient method to optimize the prescription of alkanin-liposome.
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<p><b>OBJECTIVE</b>To study the effects of different penetration enhancers on the transcutaneous permeability of syringin, chologenic acid and rutin in Xuelian cataplasm in vitro and to determine the effective enhancer.</p><p><b>METHOD</b>Using improved Franz-type diffusion cell and excised big mouse skin in vitro as transdermal barrier, the kinetics parameters of syringin, chologenic acid and rutin in Xuelian cataplasm such as cumulative permeation quantity, permeation rate were determined by HPLC. The enhancement ability of azone (A-zone), propylene glycol (PG) was investigated when used either uniquely or combinatively.</p><p><b>RESULT</b>With the 7% azone, the syringin, chologenic acid and rutin in Xuelian cataplasm could penetrate through the skin of rats well.</p><p><b>CONCLUSION</b>The selection of the best penetration enhancers provide reference for Xuelian cataplasm.</p>
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Animals , Mice , Rats , Drug Carriers , Chemistry , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Glucosides , Chemistry , Pharmacokinetics , In Vitro Techniques , Permeability , Phenylpropionates , Chemistry , Pharmacokinetics , Propylene Glycol , Rutin , Chemistry , Pharmacokinetics , Skin AbsorptionABSTRACT
Objective To study the technological parameters of the purification process for active cons-tituents from Saussurea involucrata.Methods Using absorption and desorption rates of syringin,chologenic acid,and rutin as the primary screening indexes,four resins were selected,and the conditions of absorption and desorption were optimized for active constituents.Results Resin HPD400 gave good separation performance and was selected to purify the active constituents in S.involucrata.The optimum parameters were established as followings:4 BV(bed volume)sample extract whose pH value was adjusted to pH 2-3 by HCl was passed through the column with a flow rate of 1 BV/h,12 h later,the column was washed with 4 BV water,6 BV 30% ethanol and 4 BV 50% ethanol,respectively.The combined 30% and 50% ethanolic elutes were taken as object products.Conclusion The contents of active constituents were increased to about five times.Macroporous absorption resin HPD400 could be well used in separating and purifying the active constittuents from S.involucrata.
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Objective: To establish the quality standard for Shentaipikang Granules (Cornu Cervi Pantotrichum, Herba Epimedii, Herba Cistanches, Cortex Phellodendri, etc). Methods: Counu Cervi Pantotrichum in this prescription was examined by microscopical identification. Cortex Phellodendri, Rhizoma Dioscoreae and Rhizoma Atractylodis Macrocephalae were identified by TLC. Radix Rehmanniae was identified by HPLC. Icariin was determined by HPLC. Results: Cornu Cervi Pantotrichum could be examined by microscopical identification, Cortex Phellodendri, Rhizoma Dioscoreae and Rhizoma Atractylodis Macrocephalae by TLC, and Radix Rehmanniae by HPLC. Icariin showed a good linear relationship at a range of 0.104 ～ 0.624 ?g , r = 0.9998 . The average recovery was 100.1% and RSD was 1.3% ( n =9) respectively. Conclusion: These methods are simple, accurate and specific and can be used for the quality control of Shentaipikang Granules.
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Objective: To evaluated the granules stabilities in four conditions by taking the change of Baricalin content and granules surface color as stability test markers. Methods: The content of baicalin was determined by dual wave length iso absortion method and the granules surface color was determined by the diffuse reflectrance spectroscopy. ① The granules were tested in a simulated summer environment (30 ?C , RH92.5%, 1month) and in a high intensity light condition (3000LX, 10dyas). ② The influence of humidity on the stability of the granules was investigated. ③ The expiry date of the granules was predicted by the mutivariate linear regression analysis and compared with the result of the classical constant temperature method. ④ The influences of temperature and humidity on the granules stability were etudied by orthogonal test. Results: ① There was hardly any change in baicalin content of samples in a simulated summer environment and in a high intensity light condition. ② The results showed that the decrease of baicalin content and charge of granules color were obvious when the relative humidity of environment was high and the granules color was more easily influenced by the humidity. ③ The expiry date was about 2.87 years. ④ The results indicated that both temperature and humidity had effects on the change of baicalin content. Conclusion: We tried to estimate the stability of the granules by two indexes. The results showed that Qingrejedu granules was stable in different conditions. It satisfied the stability requirements of solid dosage form.
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AIM:To select an optiomal formulation of liposome entrapped alkanin prepared with ethanol injection in the combination of orthogonal design and central composite design/Response surface method.METHODS:Five influencing factors,including ratio of alkanin to liposome and soyabean lecithin to cholesterol,volume ratio of ethanol phase to water phase,soybean concentration and mannitol concentration were chosen as indices by orthogonal design.Then the method utilized the central composite design,which fitted multivariate linear and second/third order nonlinear regression equation,to find out the optimal formulation.RESULTS:Third order regression equation gained made the good prediction about entrapment(85.4%) and alkanin load(5.16%),and exhibited no significant difference between theoretic value and measured value.CONCLUSION:The combination of orthogonal design with central composite design is a feasible and convenient method to optimize the prescription of alkanin-lipo-some.
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AIM: To establish the quality standard for Hanshi Tougu Tablets(Radix Aconiti Praeparata,Radix Aconiti Kusnezoffii Praeparata,Ramulus Cinnamomi,Rhizoma Atractylodis, Semen Sinapis,Radix Aucklandiae,Radix Glycyrrhizae). METHODS: Rhizoma Atractylodis,Semen Sinapis,Radix Glycyrrhizae in Hanshi Tougu Tablet were identified by TLC.The content of cinnamaldehyde and costunolide in Hanshi Tougu Tablets were determinded by HPLC. RESULTS: Rhizoma Atractylodis,Semen Sinapis,Radix Glycyrrhizae,Radix Aconiti Praeparata and Radix Aconiti Kusnezoffii Praeparata could be identified by TLC.Cinnamaldehyde showed a good linear relationship at the range of 2.104 ?g?mL~(-1)-52.60 ?g?mL~(-1),r=0.999 8(n=5), and the recovery was(99.62%,) RSD was(0.88%).Costunolide also showed a good linear relationship at a range of(0.036) mg?mL~(-1)-0.54 mg?mL~(-1),r=(0.999 9)(n=5),and the recovery was 96.10%,RSD was 0.15%. CONCLUSION: The method is simple,accurate and with strong specificity and can be used for the quality control of Hanshi Tougu Tablets.
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AIM: To establish the quality standard for Baixuan Xitare Tablets (Alone, Herba Euphorbiae Humifusae, Fructus Chebulae, etc.) METHODS: Herba Euphorbiae Humifusae and Scammonia resin were identified by TLC. The content of aloin was determined by HPLC. RESULTS: Herba Euphorbiae Humifusae and Scammonia resin could be identified by TLC. Aloin showed a good linear relation in a range of 0.9360?g～ 2.184?g, r=0.9995(n=5). The average recovery was 98.54% and RSD was 0.67%(n=9), respectively. CONCLUSION: The method is simple, accurate and specific and can be used for the quality control of Baixuan Xitare Tablets.
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Objective: To select the prescription of Harmine HCl ointment. Methods: The orthogonal design was used for selecting the prescription with transdermal absorption rate constant (K) and flow energy of activition (E ?) as selecting standard. Results: The optimum prescription is as follows: Azone (2.0%), Span-80 ( 0.2%), Tweens-80 (0.4%), Glycerylmonostearate (2.5%), Vaselin (4.0%), Liquid (11%). Conclusion: The prescription design is available, and the ointment has a good stability.