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1.
Article in Chinese | WPRIM | ID: wpr-879012

ABSTRACT

To evaluate the effects of Hydroxypropyl methylcellulose acetate succinate(HPMCAS MF) on absorption of silybin(SLB) from supersaturable self-nanoemulsifying drug delivery system which was pre-prepared at the early stage experiment. The cell toxicity of self-emulsifying preparation was evaluated by the MTT method, and the in vitro membrane permeability and absorption promoting effect of the self-emulsifying preparation were evaluated by establishing a Caco-2 cell monolayer model. The in vivo and in vitro supersaturation correlation was evaluated via the blood concentration of SLB. The results of MTT showed that the concentration of the preparation below 2 mg·mL~(-1)(C_(SLB) 100 μg·mL~(-1)) was not toxic to Caco-2 cells, and the addition of polymer had no significant effect on Caco-2 cells viability. As compared with the solution group, the transport results showed that the P_(app)(AP→BL) of the self-emulsifying preparation had a very significant increase; the transport rate of silybin can be reduced by polymer in 0-30 min; however, there was no difference in supersaturated transport between supersaturated SLB self-nanoemulsion drug delivery system(SLB-SSNEDDS) and SLB self-nanoemulsion drug delivery system(SLB-SNEDDS) within 2 hours. As compared with SLB suspension, pharmacokinetic parameters showed that the blood concentration of both SLB-SNEDDS and SLB-SSNEDDS groups were significantly increased, and C_(max) was 5.25 times and 9.69 times respectively of that in SLB suspension group, with a relative bioavailability of 578.45% and 1 139.44% respectively. C_(max) and relative bioavailability of SLB-SSNEDDS were 1.85 times and 197% of those of SLB-SNEDDS, respectively. Therefore, on the one hand, SSNEDDS can increase the solubility of SLB in gastrointestinal tract by maintaining stability of SLB supersaturation state; on the other hand, the osmotic transport process of SLB was regulated through the composition of its preparations, and both of them could jointly promote the transport and absorption of SLB to improve the oral bioavailability of SLB.


Subject(s)
Administration, Oral , Biological Availability , Caco-2 Cells , Drug Delivery Systems , Emulsions , Humans , Methylcellulose/analogs & derivatives , Nanoparticles , Particle Size , Silymarin , Solubility
2.
Article in Chinese | WPRIM | ID: wpr-878946

ABSTRACT

To verify the appropriate preparation process of extracts for the solid substance benchmark of Linggui Zhugan Decoction. The extracts were prepared by different preparation processes, namely the traditional process(process 1), the extract combined with volatile oil separated from traditional process extract liquid(process 2), the modern secondary reflux extraction process(process 3) and the process that volatile oil was extracted first, then prepared according to the traditional process, and combined with extract(process 4); based on the characteristic spectrum, index components of cinnamaldehyde, glycyrrhizin, ammonium glycyrrhizinate, cinnamic acid, and the dry extract rate of process 1, the differences and similarities of four extracts were compared. The results showed that the similarity of the characteristic spectrum of process 2, process 4 and process 1 were all greater than 0.97, while there was no significant difference for the content of 4 quality control components and dry extract rate; the similarity of the characteristic spectrum of process 3 and process 1 was 0.91, the absolute peak area of 13 out of 21 peaks and the relative peak area of 7 peaks increased significantly, and the content of 3 out of 4 quality control components and dry extract rate also significantly increased. In conclusion, the material standards of extracts by the process 2 and 4 are consistent with that of the traditional process, so the two processes are suitable.


Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Glycyrrhizic Acid , Oils, Volatile , Quality Control , Reference Standards
3.
Article in Chinese | WPRIM | ID: wpr-828399

ABSTRACT

In order to improve the supersaturation and maintenance time of drug dispersion in curcumin self-nanoemulsion(CUR-SNEDDS), precipitation inhibitors(PPIs) were introduced to prepare curcumin supersaturated self-emulsion(CUR-SSNEDDS). The composition of CUR-SNEDDS prescriptions was selected through the solubility test, the compatibility of oil phase and surfactant, the investigation of the emulsifying ability of the surfactant and the drawing of the pseudo-ternary phase diagram. Analytic hierarchy process was used in combination with central composite design-response surface method to optimize the prescription. The type and dosage of precipitation inhibitors(PPIs) were selected to maintain the supersaturated concentration and duration of CUR in artificial gastrointestinal fluids. At the same time, polarizing microscope was used to evaluate the crystallization inhibition effect and the quality and in vitro release behavior of CUR-SSNEDDS. The prepared CUR-SSNEDDS prescription was capryol 90-kolliphor RH40-transcutol HP-Soluplus(7.93∶66.71∶25.36∶5), with the drug loading of(65.12±1.25) mg·g~(-1). CUR-SSNEDDS was transparent yellow, and the nanoemulsion droplets were spherical with uniform distribution. The emulsification time was(21.02±0.13) s, the average particle size was(57.03±0.35) nm, the polydispersity index(PDI) was(0.23 ± 0.01), and the Zeta potential was(-18.10±1.30) mV. CUR-SSNEDDS significantly inhibited the generation and growth of crystals after in vitro dilution. The supersaturation could be maintained above 10 within 2 h, and the dissolution rate and degree of CUR in artificial gastrointestinal fluid were significantly increased. Soluplus could effectively maintain the supersaturated state of CUR and enhance CUR dissolution in vitro.


Subject(s)
Biological Availability , Curcumin , Emulsions , Nanoparticles , Particle Size , Solubility , Surface-Active Agents
4.
Acta Pharmaceutica Sinica ; (12): 2289-2295, 2019.
Article in Chinese | WPRIM | ID: wpr-780329

ABSTRACT

This study aimed to investigate the influence of combinating Huangqi with Fuzi on the pharmacokinetics of six Aconitum alkaloids, i.e. aconitine (AC), hypaconitine (HA), mesaconitine (MA), benzoylaconine (BAC), benzoylhypaconine (BHA) and benzoylmesaconine (BMA). The plasma concentrations of the drugs were determined by LC-MS for dose response and time dependent curves. The pharmacokinetic parameters were calculated by DAS 3.3, and SPSS 12.0 was used to analyze the differences of main pharmacokinetic parameters between the two groups. Comparing with Fuzi group, the AUC0-t and AUC0-∞ of six alkaloids in Fuzi-Huangqi group was significantly decreased, the CLz/Fof six alkaloids except HA was significantly increased; the Cmax was decreased and the tmax was prolonged in 3 monoester alkaloids, and the apparent volume of distribution of BMA and MA (Vz/F) increases. These data indicated that Huangqi can inhibit the absorption of aconite alkaloids, induce the distribution of aconite alkaloids to the whole body, and accelerate the elimination of aconite alkaloids. The animal experiment scheme in this study has been approved by the Experimental Animal Ethics Committee of Jiangxi University of Traditional Chinese Medicine.

5.
Article in Chinese | WPRIM | ID: wpr-690523

ABSTRACT

This study attempts to establish a method for the anti-thrombin activty bioassay of musk, explore the impact of species and producing areas on the anti-thrombin activty of musk, and provide scientific basis for its biological quality evaluation. Anti-thrombin activty of musk was analyzed by thrombin titration, and the influence factors such as musk solution concentration, fibrinogen concentration, thrombin concentration and titration interval were optimized to evaluate the effect of different species and producing areas on anti-thrombin activty of musk. As a result, there was a good linear relationship between musk solution concentration and thrombin consumption volume within the range of 0.01-0.02 g·mL⁻¹ (=0.991 4) under the experimental condition as follows: fibrinogen concentration was 0.5%, the thrombin concentration was 10 U·mL⁻¹; titration time interval was once every minute, and each titration volume was 2 μL. The average anti-thrombin activty potency of Moschus berezovskii from different producing areas was (105.0±10.4) U·g⁻¹, (102.4±5.5) U·g⁻¹ for M. sifanicus from different producing areas, (97.7±6.6) U·g⁻¹ for M. moschiferus from Anhui province, and (58.6±6.4) U·g⁻¹ for artificial musk. The results indicated that this anti-thrombin activty bioassay method could be applied to evaluate the anti-thrombin activty of musk quickly, conveniently, sensitively and exactly. It was also suggested that different species and producing areas had effects on the anti-thrombin activty of musk, so it is necessary to pay attention to species and producing areas in the process of musk domestication; meanwhile, the artificial musk and natural musk also showed great differences in anti-thrombin activty, suggesting that ratio in artificial musk prescription needs to be further optimized.

6.
Article in Chinese | WPRIM | ID: wpr-275460

ABSTRACT

To study the correlation of four properties of traditional Chinese medicine and the function of reversing multidrug resistance (MDR) of tumor cells, with 580 herbs in Chinese Pharmacopoeia 2015 version as the research objects. CNKI, CBA, Wanfang, VIP, and PubMed were searched to screen the documents related to the reversal of MDR for collection, summarizing and analysis. The results of the research showed that a total of 114 species Chinese herbs had been reported to be associated with reversal of MDR in tumor cells. Among 15 Chinese herbs with heat nature, 7 herbs had the function of reversing MDR in tumor cells, accounting for 46.7%. Among the 48 herbs with cool nature, 12 herbs had the function of reversing MDR, accounting for 25%. Among the 211 herbs with cold nature, 46 herbs had the function of reversing MDR, accounting for 21.8%. Among the 179 herbs with warm nature, 34 herbs had the function of reversing MDR, accounting for 19%. Among the 127 herbs with neutral nature, 15 herbs had the function of reversing MDR, accounting for 11.8%. Through the analysis on the relationship between four properties of 114 kinds of traditional Chinese medicines and reversing multidrug resistance of tumor cells, this paper speculated that there was a certain correlation between four properties of traditional Chinese medicine and the function of reversing multidrug resistance of tumor cells.

7.
Article in Chinese | WPRIM | ID: wpr-256077

ABSTRACT

The purpose of this study was to investigate the effect of key physical properties of hawthorn leaf granule on its dissolution behavior. Hawthorn leaves extract was utilized as a model drug. The extract was mixed with microcrystalline cellulose or starch with the same ratio by using different methods. Appropriate amount of lubricant and disintegrating agent was added into part of the mixed powder, and then the granules were prepared by using extrusion granulation and high shear granulation. The granules dissolution behavior was evaluated by using equilibrium dissolution quantity and dissolution rate constant of the hypericin as the indicators. Then the effect of physical properties on dissolution behavior was analyzed through the stepwise regression analysis method. The equilibrium dissolution quantity of hypericin and adsorption heat constant in hawthorn leaves were positively correlated with the monolayer adsorption capacity and negatively correlated with the moisture absorption rate constant. The dissolution rate constants were decreased with the increase of Hausner rate, monolayer adsorption capacity and adsorption heat constant, and were increased with the increase of Carr index and specific surface area. Adsorption heat constant, monolayer adsorption capacity, moisture absorption rate constant, Carr index and specific surface area were the key physical properties of hawthorn leaf granule to affect its dissolution behavior.

8.
Article in Chinese | WPRIM | ID: wpr-338189

ABSTRACT

The study was aimed to establish a liquid chromatography-tandem mass spectrometric method for the determination of the docetaxel concentration in rat plasma, and study the effect of coumarin constituents (imperatorin, isoimperatorin and oxypeucedanin) in Angelica dahurica on pharmacokinetics of docetaxel.Plasma was precipitated with acetonitrile and determined by LC-MS method with Paclitaxel as an internal standard. The specificity, linearity, range, accuracy, precision and stability of the method were suitable for the determination of docetaxel in plasma.Six sprague-dawley rats in each group received intragastric administration of docetaxel (50 mg•kg⁻¹), oxypeucedanin (8 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹), imperatorin (15 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹), and isoimperatorin(15 mg•kg⁻¹) combined with docetaxel (50 mg•kg⁻¹).Their drug plasma concentration was determined by LC-MS with Paclitaxel as an internal standard to draw plasma concentration-time curve, and the phamacokinetic parameters were calculated by DAS 2.0. The results showed that the phamacokinetic parameters of docetaxel all had notable changes when combined with imperatorin, isoimperatorin, and oxypeucedanin, respectively. The phamacokinetic parameters AUC and Cmax were significantly increased, indicating that coumarin constituents in Angelica dahurica could promote the oral bioavailability of docetaxel, and their effects were in the following order: oxypeucedanin> isoimperatorin> imperatorin.

9.
Article in Chinese | WPRIM | ID: wpr-284743

ABSTRACT

To establish a method for the determination of chemical specific chromatograms and five components in Yinqiao powder decoction, and provide basis for elucidating the scientific connotation of ″taking in when the fragrance volatilized fiercely″. Yinqiao powder decoctions with different decocting times were prepared to study the changes of chemical components during decocting process. Specific chromatograms and contents of chlorogenic acid, phillyrin, arctiin, liquiritin and glycyrrhizin were determined by high performance liquid chromatography. According to the results, the similarities of Yinqiao powder decoctions with different decocting times were high, which indicated that their chemical compositions were similar. The dissolutions of the five components in Yinqiao powder reached more than 39.7% of 2 hour maximum dissolution amounts (MDA) after 20 minutes of soaking, more than 69.5% of MDA when boiling, more than 79.1% of MDA at the 5th minute after boiling, and more than 85.7% of MDA at the 10th minute after boiling. The concentrations of five components were not increasing obviously after 15 minutes of boiling (RSD<4.3%). The fragrance volatilized fiercely at about the 5th minute after boiling, which indicated that the contents of volatile components in Yinqiao powder decoctions were high, but it became weak after boiling for 15 minutes, which indicated that the contents of volatile components in Yinqiao powder decoctions were low. The results showed that the contents of five components in Yinqiao powder decoctions were heavily influenced by the decocting time. When boiling for about 5 minutes, the fragrance volatilized fiercely, both the contents of volatile components and non-volatile components were high. It is suggested that the traditional decocting method has a certain scientific basis.

10.
Article in Chinese | WPRIM | ID: wpr-250415

ABSTRACT

To study the improvement of powder flowability and hygroscopicity of traditional Chinese medicine extract by surface coating modification technology. The 1% hydrophobic silica nanoparticles were used as surface modifier, and andrographis extract powder was taken as a model drug. Three different techniques were used for coating model drugs, with angle of repose, compressibility, flat angle and cohesion as the comprehensive evaluation indexes for the powder flowability. The powder particle size and the size distribution were measured by Mastersizer 2000. FEI scanning electron microscope was used to observe the surface morphology and structure of the powder. The percentage of Si element on the powder surface was measured by energy dispersive spectrometer. The hygroscopicity of powder was determined by Chinese pharmacopoeia method. All of the three techniques can improve the flowability of powder extract. In particular, hygroscopicity of extract powder can also be improved by dispersion and then high-speed mixing, which can produce a higher percentage of Si element on the powder surface. The improvement principle may be correlated with a modifier adhered to the powder surface.

11.
Article in Chinese | WPRIM | ID: wpr-307153

ABSTRACT

To establish a method for the determination of three volatile components: menthone, menthol and pulegone in Yinqiao powder (YQP) decoction, explore the change rules of volatile components in decocting process, and provide evidence for elucidating the scientific connotation of its traditional decocting method "taking when the fragrance is volatilized fiercely". YQP decoctions with different decocting time were prepared, and GC-MS was used to qualitatively analyze the volatile components and determine the contents of menthone, menthol and pulegone in decoctions. Then the effects of different decocting time on contents of volatile components were investigated. The results showed that the volatile components in YQP decoctions mainly come from Menthae Haplocalycis Herba, Schizonepetae Herba and Forsythiae Fructus. With the extension of decocting time, the concentrations of all the above 3 volatile components in Yinqiao powder decoction were first increased and then decreased. When soaking for 30 minutes, as well as boiling for 0, 5, 10, 15, 20, 30, 40, 50, 60 minutes, the concentrations of menthone in YQP decoction were 0.058, 0.268, 0.216, 0.073, 0.065, 0.048, 0.048, 0.041, 0.038, 0.034 mg•L ⁻¹; the concentrations of menthol were 0.965, 2.847, 3.633, 2.420, 1.539, 1.189, 1.273, 1.188, 0.905, 0.663 mg•L ⁻¹; the concentrations of pulegone were 0.355, 0.522, 0.598, 0.477, 0.374, 0.374, 0.339, 0.355, 0.248, 0.251 mg•L ⁻¹; and the total concentrations were 1.377, 3.637, 4.446, 2.970, 1.979, 1.611, 1.660, 1.583, 1.191, 0.947 mg•L ⁻¹, respectively. The results showed that the contents of menthone, menthol and pulegone in YQP decoctions were heavily influenced by the decocting time. The fragrance was volatilized fiercely at about 5 minutes after boiling, with larger concentrations of the above three volatile components in decoction; the fragrance got weak after 15 minutes of boiling, the concentrations of menthone, menthol and pulegone in YQP decoctions were significantly decreased, indicating that the traditional decocting method "taking when the fragrance is volatilized fiercely" has some scientific foundation.

12.
Article in Chinese | WPRIM | ID: wpr-310997

ABSTRACT

The impact of key physical properties on granulated products by the high-speed mixing wet method was studied. Andrographis extracts were utilized as the model drug. Four processing methods were adopted to prepare mixed powder of microcrystalline cellulose (MCC) and starch with the mass ratio 1:0.5, 1:1 and 1:2 by the high-speed mixing wet method. The properties of the prepared granules were evaluated with such indexes as granule yield, the ratio of lumps and fine powder, granule-AOR and granule-HR. The impact of key physical properties on granulated products was analyzed through stepwise regression analysis. The results showed that angle of repose, moisture content, pore volume, density and contact angle with water were key physical properties of the powder. The key physical properties of Chinese medical extracts powder are the important factor impacting granulated products made by the high-speed mixing wet method. In this study, the impact of key physical properties on granulated products of Chinese medical extracts was analyzed from the physical angle.


Subject(s)
Andrographis , Chemistry , Drug Compounding , Methods , Drugs, Chinese Herbal , Chemistry , Particle Size , Powders , Chemistry
13.
Article in Chinese | WPRIM | ID: wpr-319622

ABSTRACT

With the content of gallic acid, loganin, paeoniflorin and paeonol as the indexes, to screen out dissolution determination conditions, establish the dissolution determination method for multi-index components in Liuwei Dihuang concentrated pills, calculate and map the accumulative dissolution curve, and then compare the dissolution of products from different pharmaceutical factories through the similarity factor (f2). According to the results, the optimum dissolution determination conditions were the paddle method, with 250 mL 0.1 mol x L(-1) hydrochloric acid as the dissolution medium, and a rotation rate of 100 r x min(-1). The similarity factor values (f2) of the dissolution curves of the four main components of Liuwei Dihuang concentrated pills from different pharmaceutical factories were mostly less than 50. This demonstrated a significant difference in the dissolution of Liuwei Dihuang concentrated pills from different pharmaceutical factories, and provided scientific basis for improving the equality evaluation of Liuwei Dihuang concentrated pills.


Subject(s)
Drugs, Chinese Herbal , Chemistry , Humans , Organic Chemicals , Quality Control , Solvents , Chemistry
14.
Article in Chinese | WPRIM | ID: wpr-341862

ABSTRACT

It was difficult to prepare traditional Chinese medicine pellets due to the adverse characteristics of the herbal extract. In this study, Danshen extract (DS) powder mixed with different proportions of microcrystalline cellulose (MCC), lactose and starch were made into pellets by extrusion-spheronization. Particle size, span, bulk density, tapping density, compressibility, Hausner ratio and angle of repose were used to evaluate the micromeritic properties of mixing powders. Feret diameter, aspect ratio, yield, density and friability were used to evaluate the properties of the pellets. The correlations between micromeritic properties of raw material powders and the formability of their pellets were analyzed by cluster analysis, principal component analysis and partial least squares regression analysis. As a result, the particle size of the powders was negatively correlated with the size, density, yield, and was positively correlated with the friability of their pellets. The span, density, compressibility and angle of repose of the powders were positively correlated with the size, density, yield, and were negatively correlated with the friability of their pellets. So there were certain correlations between the micromeritic properties of raw material powders and the properties of their pellets prepared by extrusion-spheronization. This research provided a foundation for the technology and method of traditional Chinese medicine extract pellets.


Subject(s)
Cellulose , Chemistry , Drug Compounding , Methods , Drug Implants , Chemistry , Drugs, Chinese Herbal , Chemistry , Excipients , Chemistry , Lactose , Chemistry , Medicine, Chinese Traditional , Methods , Particle Size , Powders , Chemistry , Starch , Chemistry
15.
Chinese Pharmaceutical Journal ; (24): 572-577, 2014.
Article in Chinese | WPRIM | ID: wpr-859780

ABSTRACT

OBJECTIVE: To investigate the relationship between the process parameters and granulation behavior during high shear granulation process. METHODS: Andrographis extract was utilized as a model drug and mixed with microcryslalline cellulose (MCC) or soluble starch at the ratio of 1:1 by weigh, respectively. The process parameters were selected according to fractional factorial experiment. The granules were prepared by using high shear granulation. The aggregation behavior was evaluated by granule yield and ratio of lumps and fine powder. The effect of process parameters on granulation behavior was analyzed through stepwise regression. Standard least squares regression analysis was used to establish the mathematical model of granule yield. RESULTS: The process parameters had different effects on the granulation behaviors of MCC and starch mixtures. The granule yield predicted by the fitting model was (66.66 ± 3.7)%, and the measured values for MCC and starch mixture were 68.9% and 66.1%, respectively. CONCULSION: The established mathematical model is useful in predicting the performance of materials duing high shear granulation process. Understanding the impact of process parameters on granulation behavior provides the basis of modulating granulation parameters in order to optimize product performance and improve the yield.

16.
Article in Chinese | WPRIM | ID: wpr-854795

ABSTRACT

Objective: To explore the dynamic distribution of moistening agent in Andrographis paniculata granule (APG) during the high shear wet granulation (HSG). Methods: A. paniculata extract was utilized as a model drug and mixed with microcrystalline cellulose (MCC) with the ratio of 1∶1.5 by weight. The granules were prepared using HSG with 60% ethanol as the moistening agent. Sodium fluorescein was incorporated as a tracer in the moistening agent in order to detect its distribution in the granules during the process. Results: The moistening agent was heterogeneously distributed at the beginning of the process, fractional powder was over wetted, meanwhile partial powder was not wetted, and granule size distribution was polarization. The moistening agent tended to be evenly distributed and the granule size distribution presented nearly unimodal distribution with the increase of granulation time. Conclusion: The distribution of moistening agent obeys the first-order kinetics model during HSG of APG.

17.
Article in Chinese | WPRIM | ID: wpr-315019

ABSTRACT

<p><b>OBJECTIVE</b>To study the transport mechanism of baicalin of Scutellariae Radix extracts and the effect of Angelica dahurica extracts on the intestinal absorption of baicalin by using Caco-2 cell monolayer model, in order to analyze the effect mechanism of Angelica dahurica extracts on the intestinal absorption of baicalin.</p><p><b>METHOD</b>The Caco-2 cell monolayer model was established with human colonic adenocarcinoma cells, and used to study the effect of pH, time, drug concentration and temperature on the transport of baicalin in Scutellariae Radix extracts, the effect of P-gp and MRP protein-dedicated inhibitors on the bidirectional transport of baicalin in Caco-2 cell model, and the effect of angelica root extracts on baicalin absorption and transport.</p><p><b>RESULT</b>Baicalin was absorbed well at 37 degrees C and under pH 7.4 condition and concentration dependent. Its proteins became inactive at 4 degrees C, with a low transport. The bi-drectional transfer PDR was 0. 54. After P-gp inhibitor verapamil and MRP inhibitor probenecid were added, the value of PappBL-AP of baicalin decreased, but without any difference in PDR. The transport of baicalin was improved by 2.34, 3.31 and 3.13 times, after A. dahurica extract coumarin, volatile oil, and mixture of coumarin and volatile oil.</p><p><b>CONCLUSION</b>The transport mechanism of baicalin is mainly passive transfer and supplemented with efflux proteins involved. A. dahurica extracts can enhance the absorption of baicalin, which may be related to the passive transfer merchanism of baicalin. A. dahurica extracts' effect in opening the close junction among cells may be related to its expression or function in inhibiting efflux proteins.</p>


Subject(s)
ATP Binding Cassette Transporter, Subfamily B, Member 1 , Metabolism , Angelica , Chemistry , Biological Transport , Caco-2 Cells , Cell Line, Tumor , Coumarins , Chemistry , Pharmacology , Drug Interactions , Drugs, Chinese Herbal , Chemistry , Pharmacology , Flavonoids , Pharmacokinetics , Humans , Intestinal Absorption , Physiology , Oils, Volatile , Chemistry , Pharmacology , Plant Extracts , Chemistry , Pharmacology , Plant Roots , Chemistry , Probenecid , Pharmacology , Scutellaria baicalensis , Chemistry , Verapamil , Pharmacology
18.
Chinese Pharmaceutical Journal ; (24): 899-903, 2013.
Article in Chinese | WPRIM | ID: wpr-860368

ABSTRACT

OBJECTIVE: To prepare Panax notoginseng saponins-loaded complex nano vesicles (PNS-CNV) with MPEG-PLGA nanoparticles as the core and investigate the physicochemical property of PNS-CNV and protective action on acute myocardial ischemia in rats. METHODS: Double emulsification-solvent evaporation method was used to prepare Panax notoginseng saponins-loaded nanoparticles using different molecular weight MPEG-PLGA (PNS-NP). Thin-film hydration method was applied to entrap PNS-NP as the core to form PNS-CNV. Ultrafiltration, transmission electron microscope, dynamic light scattering and electrophoretic light scattering were employed to study the entrapment efficiency of each index component in PNS and physicochemical parameters of PNS-CNV. Acute myocardial ischemia model in rats was established to investigate the protective effect of PNS-CNV. RESULTS: The molecular weight of MPEG-PLGA did not affect the entrapment efficiency, particle size and Zeta potential of PNS-CNV. The pharmacodynamic experiment indicated that comparing with PNS solution group, the SOD activity of rat myocardium in PNS-CNV group was elevated with markedly decreased H2O2, MDA and serum LDH activity (P<0.05). The protective effect of PNS-CNV with MPEG5000-PLGA was the most significant. CONCLUSION: CNV may be used as potential new oral drug delivery carriers.

19.
Acta Pharmaceutica Sinica ; (12): 256-260, 2012.
Article in Chinese | WPRIM | ID: wpr-323048

ABSTRACT

This study is to investigate the effect of ferulic acid on learning and memory impairments of vascular dementia (VD) rats and its mechanism of action. VD rats model was replicated by permanent bilateral common carotid artery occlusion (2VO). The learning and memory capability of VD rats was evaluated by Morris water maze. The activity of acetylcholinesterase (AChE) and superoxide dismutase (SOD) and the content of glutamic acid (Glu) and malondialdehyde (MDA) in hippocampus of VD rats' brain were determined, separately. The results showed that ferulic acid could alleviate learning and memory deficits of VD rats significantly. Ferulic acid was found to inhibit the activity of AChE and increased the activity of SOD in rat hippocampus. In addition, ferulic acid could also decrease the content of Glu and MDA in rat hippocampus. These results suggested that ferulic acid could alleviate VD rats' learning and memory deficits, which might be due to antioxidation, the improvement of cholinergic system in brain, or the inhibitory of nerve injury by excitatory amino acids.


Subject(s)
Acetylcholinesterase , Metabolism , Animals , Anticoagulants , Pharmacology , Therapeutic Uses , Coumaric Acids , Pharmacology , Therapeutic Uses , Dementia, Vascular , Metabolism , Glutamic Acid , Metabolism , Hippocampus , Metabolism , Male , Malondialdehyde , Metabolism , Maze Learning , Memory , Memory Disorders , Drug Therapy , Random Allocation , Rats , Rats, Sprague-Dawley , Superoxide Dismutase , Metabolism
20.
Acta Pharmaceutica Sinica ; (12): 232-237, 2011.
Article in Chinese | WPRIM | ID: wpr-348972

ABSTRACT

To explore the mechanism of the absorption enhancement of Angelica dahurica extract (Ade), the absorption mechanism of baicalin in the Scutcllaria water extraction as well as the effect of Angelica dahurica extract on absorption of baicalin were investigated. In order to determine the main absorption site, everted intestinal sac model was used to study the effect of Angelica dahurica extract on the absorption of baicalin at duodenum, jejunum, ileum and colon. In situ single pass intestinal perfusion model was performed to study the absorption of various concentrations of baicalin and the effect of Angelica dahurica extract on the absorption of baicalin at the main absorption site. To authenticate the consequence of perfusion by getting the blood from the hepatic portal vein and determine the concentration of the baicalin in the blood. The result showed that baicalin could be absorbed at all of the four intestinal segments with increasing absorption amount per unit as follows: ileum > colon > jejunum > duodenum. The absorption ofbaicalin in the duodenum significantly increased with Angelica dahurica extract, thus, duodenum was chosen to be the studying site. Apparent permeability values (Papp) and absorption rate constant (Ka) of baicalin in the duodenum increased gradually with higher concentrations. When the concentration of baicalin rises to a certain degree, the absorption increase had a saturable process, the absorption of baicalin may be an active transportation. Baicalin may be not a substrate of P-gp as verapamil which had not significantly affected the Papp and Ka of baicalin. The absorption of baicalin in the duodenum significantly increased (P < 0.01) in the two models with Angelica dahurica extract and the concentration of baicalin in the blood from the hepatic portal vein showed that the Angelica dahurica extract can increase the absorption of baicalin.


Subject(s)
Angelica , Chemistry , Animals , Drug Synergism , Drugs, Chinese Herbal , Pharmacology , Duodenum , Metabolism , Flavonoids , Pharmacokinetics , Herb-Drug Interactions , Intestinal Absorption , Intestines , Metabolism , Male , Perfusion , Permeability , Plants, Medicinal , Chemistry , Portal Vein , Metabolism , Rats , Rats, Sprague-Dawley , Scutellaria , Chemistry , Verapamil , Pharmacology
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