Showing papers in "The Chinese Pharmaceutical Journal in 2006"

Studies on Chemical Constituents of Astragalus membranaceus(Fisch.) Bge.var.mongholicus(Bge.) Hsiao

Abstract: OBJECTIVE To study the active constituents of Astragalus membranaceus(Fisch) Bgevarmongholicus(Bge) HsiaoMETHODS Various chromatographic techniques were used to isolate and purify the constituents,their physico-chemical properties and spectral data were determined to elucidate the structuresRESULTS Seventeen compounds were isolated and identified as: astragaloside IV(ZD_(1)),isoastragaloside Ⅱ(ZD_(2)),astragaloside Ⅱ(ZD_(3)),astramembrannin Ⅱ(ZD_(4)),astragaloside Ⅰ(ZD_(5)),acetylastragaloside Ⅰ(ZD_(6)),isoastragaloside I(ZD_(7)),formononetin(ZD_(8)),β-sitosterol(ZD_(9)),2′,4′-Dimethoxy-3′-hydroxy-isoflavan-6-O-β-glucopyranoside(ZD_(10)),(6aR,11aR)9,10-dimethoxypteroca-rpan-3-O-β-D-glucoside(ZD_(11)),(6aR,11aR)3,9-dimethoxy-10-hydroxypterocarpan(ZD_(12)),calycosin(ZD_(13)),(3R)8,2′-dihydroxy-7,4′-dimethoxyisoflavan(ZD_(14)),daucosterol(ZD_(15)),formononetin-7-O-β-D-glucoside(ZD_(16)),afrormosin(ZD_(17))CONCLUSION Compound ZD_(2),ZD_(4),ZD_(6),ZD_(7),ZD_(10) and ZD_(14) are isolated from this plant for the first time

Studies on Preparation of Puerarin Phytosomes and Their Solid Dispersions

Abstract: OBJECTIVE To optimize preparation techniques for puerarin phytosomes and explore their solid dispersions to increase the dissolution of puerarin in vitro.METHODS The preparation conditions for puerarin phytosomes were optimized by means of orthogonal design,and the puerarin-phytosome-PVP coprecipitates were prepared by means of solvent evaporation.The accumulative dissolution rate of puerarin in coprecipitates with different ratios of puerarin-phytosomes to PVP was investigated according to dissolution release in vitro.RESULTS The optimized preparation conditions for puerarin phytosomes were obtained as follows.Solvent was ethanol.The ratio of puerarin to phospholipid was 1 to 1.2.Temperature was 30 ℃.Reaction time was 0.5 h.The solubility of puerarin was enhanced by 2.08,1.42 and 1.82 times in three media with different pH and its oil/water apparent partition coefficient was also enhanced by 1.11,1.25 and 1.30 times respectively by phospholipid.The accumulative dissolution rate of puerarin-phytosome-PVP coprecipitate(ratio of mass was 1 to 3) was significantly higher than that of its physical mixture and puerarin phytosome.CONCLUSION Phospholipid can effectively enhance the solubility and oil/water apparent partition coefficient of puerarin,and the coprecipitate of puerarin-phytosome and PVP can improve its dissolution in vitro,but the pharmacokinetics needs further study.

Study on Constituents from Leaves of Phyllostachys pubescens

Abstract: OBJECTIVE To study the chemical constituents from the leaves of Phyllostachys heterocycla.METHODS The seperation was performed on the silic gel CC,Sephadex LH-20 CC as well as preparative HPLC,and the constituents isolated were identified by spectral method.RESULTS Five compounds were isolated from the leaves of Phyllostachys heterocycla,and identified as p-hydroxybenzoic acid (Ⅰ),trans-p-hydroxycinnamic acid(Ⅱ),cis-p-hydroxycinnamic acid(Ⅲ),tricin(Ⅳ)and 3,4-dihydroxycinnamic acid(Ⅴ).CONCLU- SION All compounds above were isolated from the plant for the first time.

Study on chemical constitutes of {\sl Codonopsis pilosula}

Abstract: OBJECTIVE To elucidate the active component for the quality evaluation of Rdix Codonopsis.METHODS The compounds were separated with chromatography techniques and their structures were elucidated on the basis of spectroscopic evidences and physiochemical properties. RESULTS Ten compounds were isolated from the n-butanol fraction of the ethanolic extract of Codonopsis pilosula and structurally identified as lobetyolin (1),syringin (2), hexyl-β-D-glucopyrannoside (3), butyl-β-D-fructofurnanoside (4), lobetyolinin (5), geniposide (6), tryptophan (7), uracil (8),3',4',5,9,9'- pentaydroxy-5-4,7' -epoxylignan (9) and emodin (10) , respectively. CONCLUSION Compound 4-10 are isolated from genus Codonopsis for the first time and lobetyolin (Ⅰ) can be chosen for quality evaluation.

Studies on Flavonoids from Stems and Leaves of Panax notoginseng

Abstract: OBJECTIVE To separate and identify the flavonoids from the stems and leaves of Panax notoginseng(Burk.) F.H.Chen.METHODS It was decocted with water,then absorbed by macroporous adsorption resin,isolated by silica gel column chromatography and ODS column chromatography.RESULTS Six compounds were elucidated as kaempferol(Ⅰ),quercetin(Ⅱ),kaempferol 7-O-α-L-rhamnoside(Ⅲ),kaempferol 3-O-β-D-galactoside(Ⅳ),kaempferol 3-O-(2″-β-D-glucopyranosyl)-β-D-galactopyranoside(Ⅴ) and quercetin 3-O-(2″-β-D-glucopyranosyl)-β-D-galactopyranoside(Ⅵ).CONCLUSION compound Ⅲ,Ⅳ,Ⅴ and Ⅵ are isolated and identified for the first time from Panax notoginseng.

Absorption Characteristics of Baicalin and Baicalein in Rat Small Intestine

Abstract: OBJECTIVE To study the absorption characteristics of baicalin and baicalein. METHODS The model of in situ intestinal perfusion was used.A HPLC method was established to determine the drug concentration in the perfusate. RESULTS When the bile duct was not ligated, the absorption rate constant of baicalin and baicalein were (-0.004 7±0.013 4)h~ -1 and(0.496 0±0.051 2)h~ -1 , respectively; When the bile duct was ligated, the absorption rate constant of baicalin and baicalein were(0.023 9±0.026 2)h~ -1 and (0.210 6±0.073 5)h~ -1 , respectively. When baicalin or baicalein was perfused alone after the ligation of the bile duct,the concentrations of baicalein or baicalin were increased in the perfusate respectively. When baicalein was intravenous administered to rats after the ligation of the bile duct,baicalin were obtained in the perfusate.CONCLUSION Baicalin is more suitable to be administered orally than baicalin. Bile can not only excrete baicalin, but also evidently promote the absorption of baicalein. Baicalin is absorbed as baicalein formed by the intestinal bacteria, and then restored as its original form in the body.The part of the baicalin formed from the absorbed or intravenous administered baicalein can be excreted back into the gut.

Preparation of Oleanolic Acid Nanosuspension

Abstract: OBJECTIVE To study the preparation of oleanolic acid nanosuspension by means of high-pressure homogenization technique.METHODS Oleanolic acid nanosuspension was prepared with different pressure, homogenization cycles,and surfactants.Average particle size and the polydispensible index(PI) were measured to investigate the influences of these operation parameters on the nanosuspensions.The solubility and dissolution of drug nanoparticles were also investigated.RESULTS Homogenization pressure was the major factor that determined the average particle size,increased homogenization cycles led to a decreased PI,and surfactants helped to keep the system stable.Compared to crude drug powder,the solubility and dissolution of drug nanoparticles were evidently improved.CONCLUSION High-pressure homogenization technique can be used successfully to prepare oleanolic acid nanosuspensions.

Drug release from hydroxypropyl cellulose and polyethylene oxide capsules : In vitro and in vivo assessment

Abstract: In this study, hard capsule shells produced using a heat-melting method, which involved heating polyethylene oxide (PEO, with a molecular weight (MW) of 200,000) or hydroxypropyl cellulose (HPC, with MWs of 80,000, 100,000, and 370,000) powder in a mold, followed by inserting a suitably sized pestle in the mold in order to coat the melted shell materials (HPC or PEO) onto the pestle with a certain force. The water uptake and dissolution tests of these capsule shells were evaluated in acidic buffer, basic buffer, and water. Theophylline was selected as the model drug. The drug release rate decreased with increasing viscosity grades of HPC used as the shell material. In viva studies were conducted in rabbits with the novel capsules, and comparisons were made with gelatin capsules. It was found that the pharmacokinetic parameters, including AUC 0-∞ and T 1/2 , showed no significant differences among the various capsules. Correlations between the in vitro T D50 values and several in vivo parameters were established.

Assay of Buspirone Hydrochloride in Tablets Using Kinetic Spectrophotometry

Abstract: A simple kinetic method was developed for the determination of Buspirone hydrochloride (BUS) in pharmaceutical preparation. The method is based on kinetic investigation of the oxidation reaction of the drug with alkaline potassium permanganate at room temperature for a fixed time of 20 min. The absorbance of the green coloured manganate ion produced was measured at 610 nm. Alternatively, the decrease in the absorbance of permanganate ion after addition of the drug was measured at 525 nm. Calibration graphs in both procedures were linear over the concentration range 10-40 μg/mL. The different experimental parameters affecting the development and stability of the colours were carefully studied and optimized. The determination of BUS by rate constant method, fixed concentration method and fixed time method was also feasible with calibration equations obtained but the latter method was found to be more applicable.

Immunopharmacological Effect of Rabdosia amethystoieds(benth.) Hara in Mice

Abstract: OBJECTIVE To investigate the immunopharmacological effect of Rabdosia amethystoieds(Benth.) Hara(RAB).METHODS The immunomodulatory effect of RAB was observed by delayed-type hypersensitivity(DTH) induced by DNFB and the production of specific haemolysin antibody against sheep red blood cell(SRBC) in serum.RESULTS RAB decoction markedly inhibited delayed hypersensitivity induced by DNFB in mice,but had no significant effect on the index of thymus and spleen.The level of hemolysin induced by sheeperythrocyte immunization in the serum was increaed.CONCLUSION RAB decoction can markedly inhibit the function of cell-mediate immunity(CMI) and improve the function of humoral immunity in vivo.

Determination of Encapsulation Efficiencies of Liposomes and Nanoliposomes by Protamine Aggregation Method

Abstract: OBJECTIVE To establish the protamine aggregation method for the drug encapsulation efficiency determinations of liposomes and nanoliposomesMETHODS Protamine aggregation method was applied to separate the free drug and liposomesThe drug concentration was determined by HPLCThe encapsulation efficiency determined by the sephadex chromatography method and protamine aggregation method was comparedThe liposomes sizes and zeta potentials,protamine contents and the dissolubilities,charges and molecular weights of drugs were taken as factors to evaluate the feasibility of protamine aggregation methodRESULTS Liposomes containing drugs of different dissolubilities were well separated by protamine aggregation methodLohexol liposomes(size≥220 nm)and the free lohexol were well separated by sephadex G-50 chromatography method and protamine aggregation methodThe lohexol recovery in blank liposomes declined when the liposomes size decreased using sephadex G-50 chromatography method,especially when lohexol liposomes size was below 200 nmFree TFu and TFu liposomes were not be separated by sephadex G-50 chromatography method due to the lipophilic characteristics of TFuFree TFu and TFu liposomes(sizes between 100 to 500 nm) were separated by protamine aggregation method accuratelyThe separation efficiencies of protamine aggregation method were affected by liposomes electric chargesWhen the Zeta potentials of TFu liposomes were changed to-4407,-476 and 145 mV by adjusting the pH of the liposome suspensions,the drug recoverys of protamine aggregation method were 981%,953% and 866%,respectivelyMicromolecule drugs with different electric charges didn′t affect separation efficiency of protamine aggregation methodThe drug recovery of the dissociated oxaceprol(negative charge)was goodMacromolecule drugs with different electric charges,however,had different effects on the drug recoverys of protamine aggregation methodInsulin(positive charge,pH 2)had good method recovery,but insulin(negative charge,pH 7)had lower drug recoveryCONCLUSION Protamine aggregation method can be used to determine the drug entrapment efficiencies of the liposomes and nanoliposomes which encapsulated drugs with different dissolubilitiesIt is suitable to separate liposomes from encapluated micromolecule drugs and positive charge macromolecule drugs and to separate liposomes from neutral and negative charge drugs

Absorption Mechanism of Liposoluble Components of Salvia miltiorrhiza with Caco-2 Cell Model

Abstract: OBJECTIVE To study the absorption mechanism of liposoluble components of Salvia miltiorrhiza with Caco-2 cell model . METHODS Caco-2 cell was used an drug absorption model. The transportation of tanshinon ⅡA, cryptotanshinone and tanshinone Ⅰ across Caco-2 cell were determined under various conditions, including giving tanshinone ⅡA and the ethanol extract of Salvia miltiorrhiza respectively, changing dosage and transport direction, adding some appropriate substances affecting absorption.RESULTS With the increasing of tanshinone ⅡA concentration, the apparent permeability coefficient (Papp) decresed at first then increased. The Papp of transport from AP to BL was five times more than that from BL to AP. With increasing dosages of borneol, the Papp increased obviously. Drug transport was not affected by EDTA. CONCLUSION The transport mechanism of tanshinon ⅡA in vivo is rather complex and involves carrier-mediated transport and passive transcellular diffusion, with neither paracellular route nor P-gp efflux. Borneol can promote transport ofliposoluble components across Caco-2 cell.The present study provided useful information for formulation study, oral administration and etc.

Studies on Chemical Constituents of Mangrove Plant Scyphiphora hydrophyllacea

Abstract: OBJECTIVE To study the chemical constituents of Scyphiphora hydrophyllacea.METHODS The constituents were isolated and purified by column chromatography, and their structures were identified by physicochemical and spectral data. RESULTS Six compounds were isolated from the ethanol extract of Scyphiphora hydrophyllacea, and their structures were elucidated as ursolic acid (Ⅰ), oleanic acid (Ⅱ), 5,7,4′-trihydroxy-3′-methoxy flavone (Ⅲ), 5,7-dihydroxy-3,3′,4′-trimethoxy flavone(Ⅳ), scopoletin (Ⅴ) and daucosterol (Ⅵ). CONCLUSION All the compounds are isolated from this plant for the first time. It′s reported that compound Ⅴ showed antitumor activity.

Effect of Absorption Enhancer of Borneol on Ginsenoside Rg1 and the Nasal Ciliotoxicity

Abstract: OBJECTIVE To investigate the nasal absorption of ginsenoside Rg1 and the absorption enhancen effect of borneol.METHODS The effect of ginsenoside Rg1 and borneol on cililary movement were evaluated by in situ toad palate model.Nasal circulatory perfusion test in vivo was employed to investigate the characteristics of nasal mucosa absorption ginsenoside Rg1 in rats.The electron microscope scanning technique was used to evaluate the nasal ciliotoxicity of ginsenoside Rg1 and borneol on the nasal mucosas of the rats.RESULTS When the concentrations of ginsenoside Rg1 were 100,250,500 mg·L~(-1),respectively,the corresponding values of the absorption rate were 0.000 30,0.000 40 and 0.000 7 min~(-1).However,when the concentration of ginsenoside Rg1 was 250 mg·L~(-1)in circulation liquid,the absorption rates were 0.001 9,0.001 2 and 0.001 3 min~(-1) with the aid of borneol of 10,20 and 30 g·L~(-1).CONCLUSION Ginsenoside Rg1 can be absorbed through the nasal mucous and borneol can enhance the absorption.The Ginsenoside Rg1 spray has no damage to the nasal mucosas of rats.

Studies on Chemical Constituents of Kalimeris indica

Abstract: OBJECTIVE To study the chemical constituents in Kalimeris indica(L.) Sch-Bip.METHODS Compounds were separated and purified by column chromatography,preparative TLC silica gel and Sephadex LH-20,and their structures were elucidated by chemical and spectral analysis(NMR,IR,UV,and MS).RESULTS Six compounds were obtained.Their structures were characterized as mominine(Ⅰ),friedelan-3-ol(Ⅱ),dammaradienyl acetate(Ⅲ),lauric acid(Ⅳ),β-sitosterol(Ⅴ) and methyl phaeophorbide(Ⅵ);respectively.CONCLUSION All compounds are obtained from this plant for the first time.

Analysis of Active Components in Mailuoning Injection by Platelet Membrane Immobilized Chromatography

Abstract: OBJECTIVE To analysis the effective chemicals in Mailuoning injection by platelet membrane immobilized chromatograghy (PMIC) METHODS The effective chemicals in Mailuoning injection were combined by the platelet membrane under imitated physical environments The unattached substances were washed away by the PBS of pH 74Then the attached compounds were eluled by the PBS of pH 40 The released compounds from target were collected and analyzed by HPLCRESULTS Eight characteristic active compounds in the Mailuoning injection were found to bind to the membrane of platelets CONCLUSION PMIC can be a screening model for the preparations of anti-thromboembolic disease, it can reflect the intensity of the pharmacological action between the compounds and the biological targets in the cell membrane, such as receptors,channels and enzymes etc

A New Flavan from the Aerial Part of Erigeron annuus

Abstract: From the ethyl acetate soluble fraction of the aerial part of Erigeron annuus, a new flavan ent-3,5,7,2',5'-pentahydroxyflavan (14), was isolated together with thirteen known compounds including six triterpenes, friedela-3-one (friedelin) (1), lupeol (2), betulinic acid (3), oleanolic acid (5), ursolonic acid (6), 3β,23,28-triol olean-12-ene (7), one steroid, β-sitosterol (4), three phenolic, acetovanillone (8), 2,4-dihydroxyacetophenone (9), coniferaldehyde (10), one coumarin, umbel-liferone (11), as well as two flavonoids, kaempferol (12) and quercetin (13). These compounds were characterized and identified based on physical and spectral evidence. All compounds were isolated for the first time from this plant.

Effects of Fungal Elicitor on the Protocorms of Dendrobium candidum

Abstract: OBJECTIVE To study the effect of a fungal elicitor on the growth and the total alkaloid content of Dendrobium candidum protocorms cultured on the solid medium.METHODS D.candidum protocorms were cultured on the solid medium for 14 weeks,and respectively added fungal elicitor(E) and three comparisons which were wheat bran culture medium(M),glucose solution(G) and distilled water(W) for 6 weeks.The fresh weight and dry weight of harvest protocorms and their total alkaloid content were measured.RESULTS Compared with W,E,M and G significantly increased the dry weight of protocorms by 35.7%,34.3% and 22.7%,respectively(P0.01),and enhanced the dry weight coefficient of protocorms by 20.7%,20.7% and 16.3%,respectively((P0.05)).Compared with that of E,the total alkaloid content of protocorms which were cultured on control M and Control G decreased by 23% and 17%,respectively.CONCLUSION The growth of D.candidum protocorms can be improved when they are cultured on the solid medium added the fungal elicitor at the later stage of culture,and their total alkaloid content can also be affected.

Analysis on Volatile Oils from Three Species of Meconopsis by GC-MS

Abstract: OBJECTIVE To analyze the chemical constituents of essential oils from three different varieties of Meconopsis:Meconopsis integrifoli,Meconopsis quintuplinervia Rl and Meconopsis horridula HMETHODS The oils were extracted by steam distillationThe chemical compounds were separated and identified by GC-MSThe relative content of each component was determined by area normalizationRESULTS Twenty-five,forty-two and fifty-three compounds from Mintegrifolia Mch,Mquintuplinervia R and M horridula were identified respectively in turnThe ratios of identification of total compounds were 8076%, 7334% and 7610%,respectivelyCONCLUSION There are some differences among three species of Meconopsis,but the main ingredients are esters

Study on Chemical Constituents of Herba Siegesbeckiae

Abstract: OBJECTIVE To study the chemical constituents in the ethyl acetate fraction of Herba Siegesbeckiae.METHODS Compounds were isolated and purified by silica gel columns and MPLC, and their structures were identified by the physicochemical properties and spectral analysis. RESULTS Seven compounds were isolated and elucidated as 3′, 5′,β-trihydroxy-3,4,4′,α-tetramethoxy-chalcone(1),kirenol(2),darutigenol(3),siegesbeckic acid(4),ent-16β,17-dihydroxy-19-kauranoic acid(5),ent-16αH-17-hydroxy-19-kauranoic acid(6) and stigmasterol(7).CONCLUSION Compound 1 is the new compound.

Inhibitory Effect of Hydroxysafflor Yellow A Against Rat Myocardial Mitochondrial Injury

Abstract: OBJECTIVE To investigate the inhibitory effects of hydroxysafflor yellow A(HSYA) against rat myocardial mitochondrial injury.METHODS Rat myocardial mitochondria were prepared through centrifugation procedure;mitochondrial swelling was observed by turbidity assay.Mitochondrial membrane fluidity was determined by fluorescence polarization technique.The elevated malonyldialdehyde(MDA) in mitochondria induced by lipid peroxidation was observed by colorimetry.RESULTS Rat myocardial mitochondrial swelling,mitochondrial membrane fluidity decrease and the mitochondria MDA elevation were remitted apparently(P0.05) by HSYA treatment.CONCLUSION It is suggested that HSYA is effective in inhibiting rat myocardial mitochondrial injury.

Studies on Preparation of Controlled-Release Delivery Systems with Drug Gradients Using Three Dimensional Printing Technique

Abstract: OBJECTIVE To prepare controlled-release delivery systems with drug gradients using three dimensional printing technique.METHODS With diclofenac sodium as model drug,controlled-release delivery systems with drug gradients were prepared using three dimensional printing technique.Basic performance,structure properties,and release characteristics were investigated through the routine tablet analysis,structure analysis,dissolution tests in vitro.RESULTS All parameters of drug delivery systems met the relevant standards,drug release from the axial direction was retarded completely,and drug distribution was gradient in the radial direction,98.14% drug was released at a zero-order rate.CONCLUSION Drug delivery systems with special properties of components,structure and surface texture to provide the desired release characteristics could be fabricated by three dimensional printing technique.

Establishment and Validation of Caco-2 Cell Lines for Lntestinal Epithelial Permeability

Abstract: OBJECTIVE To investigate the establishment of Caco2 cell monolayer model,and to identify Caco-2's natural growth in order to monitor the daily cultivation.METHODS Caco-2 cell was cultivated in Millicell plate inserts with 8×10~(4)cells·mL~(-1) cell density in standard procedures for 21 d.The morphological and growth characters of the monolayer were examined with optical microscope,electron microscope and cell density determination.The polarization and compactification of the monolayer was determined by the alkaline phosphatase activity,transepithelial electrical resistance(TEER) and apical-to-basolateral of sodium fluorescein across cell monolayers.RESULTS Caco-2 cell monolayer became well-proportioned and compact after 10 d growth.After 21 d,microvillus,alkaline phosphatase and tight conjunctions were asymmetrically distributed,TEER value reached 600 Ω·cm~(-2),and the transportation of sodium fluorescein was 4.16 μg·h~(-1)·cm~(-2) the transportation across non-cell membrane was more than 240 μg·h~(-1)·cm~(-2) in the same conditions.CONCLUSION In these cultivation conditions,the Caco-2 cell monolayer had become an analogy of small intestinal epithelium.The value of TEER and transportation of sodium fluorescein all reached the criterions,which meant that the monolayer became an valuable model system for intestinal epithelial permeability.In this research,Caco-2 cell monolayer model was established and evaluated.

Studies on Chemical Constituents of Mimosa pudica

Abstract: OBJECTIVE To study chemical constituents of Mimosa pudica in Hainan province METHODS The compounds were separated by Diaion HP-20, Sephadex LH-20, Toyopearl HW-40, RP-18, and silica gel column chromatography,et al The structures were elucidated by means of ESI-MS, IR,~ 1 H-NMR,~ 13 C-NMR,~ 1 H-~ 1 H COSY, HSQC and HMBC spectral method respectively RESULTS Five compounds were isolated and identified from the plants They were established as 5,7,3′,4′-tetrahydroxyl-6-C-β-D-glucopyranosyl flavone(Ⅰ), 5,7,3′,4′-tetrahydroxyl-8-C-β-D-glucopyranosyl flavone(Ⅱ), succinic acid(Ⅲ), β-sitosterol(Ⅳ)and stigmasterol(Ⅴ) CONCLUSION These compounds are isolated from the plant for the first time

Studies on Absorption Kinetics of Sanchinoside R_(1) and Ginsenoside Rg_(1) in Rat Intestine

Abstract: OBJECTIVE To investigate the absorption kinetics of sanchinoside R_(1) and ginsenoside Rg_(1) at different intestinal segments of rats and the influence of concentration and co-administration with absorptive promoter on the absorptive kinetics.METHODS An in situ intestinal perfusion model was employed to investigate systemically the absorptive kinetics of sanchinoside R_(1) and sanchinoside Rg_1.RESULTS The absorptive rate constants(K_a) of sanchinoside R_(1) were 0.056, 0.114,0.076,0.085 h~(-1),and the ka of qinsenoside were 0.052,0.121,0.065,0.055 h~(-1) at gastric,jejunum,duodenum,ileum,respectively.The K_a of sanchinoside R_(1) at the concentrations of 0.02,0.2,2 g·L~(-1) were 0.122,0.095,0.090 h~(-1),and the K_a ginsenoside Rg_(1) were 0.117,0.113,0.109 h~(-1),respectively.The K_a,while being co-administered with carbomer and borneol,were significantly higher than that of references group.CONCLUSION Sanchinoside R_(1) and ginsenoside Rg_(1) are well absorbed at the superior segment of intestine in rats.With the decrease of sanchinoside R_(1) and ginsenoside Rg_1 concentration,the absorption rate is increased,their absorption was is first-order process,besides the passive diffusion mechanism,facilitated diffusion and active transport may also take part in the transport process.Carbomer and borneol significantly increase the absorptive rate in intestine.

Chemical Modification of Superoxide Dismutase by Low Molecular Weight Heparin and Their Physical and Chemical Properties

Abstract: OBJECTIVE To chemically modify superoxide dismutase (SOD) with low molecular weight heparin(LMWH) and study the physical and chemical properties of the modified enzyme (LMWH- SOD), in order to make the enzyme with higher stability. METHODS LMWH was activated by sodium periodate and then combined with Cu,Zn-SOD covalently. The relative molecular weight (Mr) of the modified enzyme was measured by gel filtration chromatography and SDS-PAGE, the contents of enzyme protein, aminoglucose, glucuronic acid and sul-fate group were determined by Lowry's method, Elson-Morgan's method, Bitter-Muir s method and Teho s method,respectively, and the stabilities of Cu,Zn-SOD to heat, pH and protease digestion were studied under high temperature, acidic and basic buffer, pepsin and trypsin treating conditions.RESULTS Cu,Zn-SOD was successfully modified by LMWH. The obtained LMWH-SOD had bigger Wr than Cu,Zn-SOD did and the Mr was heterogeneous. LMHW-SOD was evidently superior to unmodified SOD in terms of their tolerances to high temperature, acid, base, pepsin and trypsin.CONCLUSION LMWH can be used to modify SOD and improve the properties of the enzyme.

Chemical Constituents from Fruit of Garcinia cowa

Abstract: OBJECTIVE To study the chemical constituents of the fruit of Garcinia cowa.METHODS Compounds were isolated by col- umn chromatography with silica gel and LH-20,whose structures were elucidated by spectral analysis and chemical evidence.RESULTS Six compounds were obtained and identified asβ-sitisterol(Ⅰ),cirsiumaldehyde(Ⅱ),p-coumaric acid(Ⅲ),amentoflavone(Ⅳ),daucos- terol(Ⅴ)and morelloflavone(Ⅵ).CONCLUSION CompoundsⅠ～Ⅵwas isolated from the plant for the first time.

Studies on Chemical Constituents of Ranunculus ternatus(III)

Abstract: OBJECTIVE To study the constituents in the roots of Ranunculus ternatus. METHODS Column chromatography was used to separate constituents whose structures were elucidated by ESI-MS,NMR spectral data and hydrolysis method. RESULTS Five compounds were isolated and elucidated as sternbin(Ⅰ),methylparaben(Ⅱ),3-[(4-O-D-glucopyranosyl)-phenyl]-2-propenoic acid(Ⅲ),linocaffein(Ⅳ) and β-D-glucose(Ⅴ).CONCLUSION Compound Ⅰ～Ⅳ are isolated from Ranunculus genus for the first time.

Determination of Zolmitriptan in Human Plasma by HPLC-MS and Study on Bioequivalence of Domestic and Import Zolmitriptan Tablets

Abstract: OBJECTIVE To develop a HPLC-MS method for the determination of zolmitriptan in plasma and evaluate the bioequivalence of domestic and imported zolmitriptan tabletsMETHODS Samples were pre-treated by solid extraction and analyzed by a Nucleodur C_ 18 column The mobile phase consisted of CH_ 3 CN-CHCOOH(005%) = 10∶90, and the internal standard was sumatriptan A single oral dose of 5 mg domestic and imported zolmitriptan was administered to 18 healthy volunteers in a randomized crossover study Zolmitriptan concentration in plasma was determined by the developed LC-MS method, and the pharmacokinetics and bioavailability were studied RESULTS The calibration curve was linear over the range of 025～40 μg·L~ -1 (r=0999 5), the solid extraction recoveries of zolmitriptan and sumatriptan respectively were between 867%～964%(n=5)and 797%～814%(n=15), the method recovery was in the range of 1022%～1060% (n=5) , inter-day and intra-day RSDs were 23%～34%(n=5) and 34%～54%(n=5),respectively The AUC_ 0～t of the two tablets were(596±244) and (566±312) μg·h·L~ -1 ,AUC_ 0～∞ were (623±259) and (602±240) μg·h·L~ -1 ,ρ_ max were(124±42) and(127±44) μg·L~ -1 ,t_ max were (19±05) and (21±04) h, the relative bioavailability of domestic to imported tablet was (1071±257)% CONCLUSION Statistice analysis shows no significant differences between the two preparations, and bioequivalence is observed The established HPLC-MS method is accuracy and sensible for zolmitriptan determination

Studies on Flavonoids of Lysimachia christinae Hance

Abstract: OBJECTIVE To study the chemical constituents of Lysimachia christinae.METHODS Manifold chromatography methods were used to separated the chemical constituents,and the chemical structures were determined by spectral analysis.RESULTS Twelve compounds were isolated from Lysimachia christinae and identified as: isorhamnetin(1),kaempferol(2),quercetin(3),astragalin(4),trifolin(5),hyperin(6),linarin(7),hesperidin(8),isorhamnetin-robinobioside(9),kaempferol-robinobioside(10),rutin(11),vicenin-2 (12). CONCLUSION Compound 1,6,9,10 and 11 are isolated from this plant for the first time,compound 7,8 and 12 are isolated from this genus for the first time.