In order to approach the effects of Shenmai Injection on SOD activity and MDA level in the senile patients with coronary heart disease, 48 cases, who had stenosis of over 70% in more than one branches of the coronary ...In order to approach the effects of Shenmai Injection on SOD activity and MDA level in the senile patients with coronary heart disease, 48 cases, who had stenosis of over 70% in more than one branches of the coronary arteries, were assigned randomly into a treatment group (given Shenmai Injection plus the routine treatment) and a control group (given the routine treatment only). The superoxide dismutase (SOD) activity and malondialdehyde (MDA) level were determined before treatment and at the end of a 3-week treatment. The results showed that in the treatment group, the SOD activity was significantly increased (P<0.05) and the MDA level markedly decreased (P<0.01) in the treatment group. It can be concluded that Shenmai Injection may enhance the antioxidant ability of the senile patients with coronary heart disease.展开更多
Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming ...Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg^(-1)·d^(-1)) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluorometric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days′ administration of Eb, the tissue contents of sele-(nium) in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significan-tly, compared with controls; but no significant changes of such contents were found in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in vitro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immunostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immunocompetence and specific distribution in liver, lungs, kidneys, bone, and spleen.展开更多
AIM: TO assess the safety and efficacy of antioxidant therapy for patients with chronic hepatitis C virus (HCV) infection.METHODS: One hundred chronic HCV infection patients failed in interferon treatment were enr...AIM: TO assess the safety and efficacy of antioxidant therapy for patients with chronic hepatitis C virus (HCV) infection.METHODS: One hundred chronic HCV infection patients failed in interferon treatment were enrolled and randomly assigned to receive combined intravenous and oral antioxidants or placebo, or oral treatment alone, Primary end points were liver enzymes, HCV-RNA levels and histology.RESULTS: Combined oral and intravenous antioxidant therapy was associated with a significant decline in ALT levels in 52% of patients who received antioxidant therapy vs 20% of patients who received placebo (P = 0.05). Histology activity index (HAI) score at the end of treatment was reduced in 48% of patients who received antioxidant therapy vs 26% of patients who received placebo (P = 0.21). HCV-RNA levels decreased by l-log or more in 28% of patients who received antioxidant therapy vs 12% who received placebo (P = NS). In part 11 of the trial, oral administration of antioxidants was not associated with significant alterations in any of the end points.CONCLUSION: Antioxidant therapy has a mild beneficial effect on the inflammatory response of chronic HCV infection patients who are non-responders to interferon. Combined antiviral and antioxidant therapy may be beneficial for these patients.展开更多
Electroporation creates aqueous pathways by short high-voltage pulses resulting in a transient perme- abilization of stratum corneum and an increase in the transdermal delivery rate.However the aqueous pathways will r...Electroporation creates aqueous pathways by short high-voltage pulses resulting in a transient perme- abilization of stratum corneum and an increase in the transdermal delivery rate.However the aqueous pathways will reseal after pulsing,which leads to the rapid drop of transdermal flux.In the present study,the surfactants were added to the donor solution to hinder the shrinkage and resealing of the electropore,and to prolong the lifetime of the aqueous pathways with the consideration that the surfactants could reduce the surface energy of the electropore. These effects of surfactants were demonstrated by the dynamic electrical resistance of the skin and the fluorescent imaging of the local transport regions.Piroxicam(PIX)was transported percutaneously in the presence of surfac- tants in vitro.Owing to the longer lifetime of aqueous pathways,together with the promotion of PIX availability at the barrier exterior and the improvement in the partition of PIX into the aqueous pathways,the presence of surfac- tants led to a remarkable increase in the transdermal delivery rate during electroporation and a significant growth of the accumulative transdermal amount of PIX.展开更多
It is generally accepted that eggs besides being a source of everyday diet, can also be used as raw material for special food, nutraceutical, pharmaceutical and cosmetic production. The biological activity of the majo...It is generally accepted that eggs besides being a source of everyday diet, can also be used as raw material for special food, nutraceutical, pharmaceutical and cosmetic production. The biological activity of the majority of substances presented in egg matter is related to their anti-microbial and anti-cancer properties and their immunogenic features as well. Due to the use of new generation of feed additives and techniques of immunisation of hens, the chemical composition and biological features of eggs may be modified and enriched with desired components, like n-3 fatty acids (alpha-linolenic acid (ALA), docosahexaenoic acid (DHA) phospholipids), vitamins, microelements. Egg material may also be used for the production of new biopreparations for the prophylaxis of various civilisation diseases, such as heart and cardiovascular diseases, cancers, neurogenerative disorders, metabolic bone diseases etc.. New progress in egg science allowed to discover new bioactive substances, like monomeric and dimeric cystatin and yolkin. It is necessary to develop efficient methods of isolation of biologically active substances contained in eggs, which would make it possible to produce new generation of diet supplements and biomedical products. It seems that new generation of eggs could be the best source for production of natural, high value nutraceutical supplements of diet, and also biomedical and biocosmetic preparations.展开更多
The mandatory preclinical safety evaluation is an essential prerequisite to obtain the qualitative and effective medicines. Due to the fact that drugs may reveal genotoxic properties, the investigation of their mutage...The mandatory preclinical safety evaluation is an essential prerequisite to obtain the qualitative and effective medicines. Due to the fact that drugs may reveal genotoxic properties, the investigation of their mutagenic activity is an obligatory part of the preclinical drug safety program. The aim of the research is to study mutagenic properties of a new original immunomodulator Arglabin native in tablets in the induced test of gene mutations (the Ames test) on Salmonella typhimurium strains. Materials and methods: Four strains of S. typhimurium TA98, TA100, TA1535, and TA1537 were used to assess the mutagenicity in the Ames test. Results and conclusions: No statistically reliable dose-dependent increase in the number of revertant colonies of Salmonella typhimurium has been observed in the presence of the given drug within the investigated dose ranges from 5.0 to 100.0 μg/mL for strains TA100 and TA1535, and from 5.0 to 250 μg/mL for strains TA98 and TA1537 against the baseline of spantaneous mutations. Arglabin native in tablets does not reveal a mutagenic activity within the studied dose ranges on Salmonella typhimurium strains TA98, TA100, TA1535, TA1537.展开更多
Capparis spinosa L. is a traditionally used plant in Algerian folk medicine to treat asthma, rheumatism and other free radicals related disorders such inflammatory. The present study was designated to study the antiox...Capparis spinosa L. is a traditionally used plant in Algerian folk medicine to treat asthma, rheumatism and other free radicals related disorders such inflammatory. The present study was designated to study the antioxidant activity of aerial and root parts of Capparis spinosa L.. Total polyphenol content was determined, after extraction with solvents in five subfractions; methanol (CE), Hexan (HE) chloroform (CHE), ethyl acetate (EAE) and aqueous extracts (AE), employing the "Prussian blue assay". The results showed that EAE containing the highest concentration of phenolic compounds and Flavonoids followed by those of CHE of aerial and root parts, repectively. The antioxidant protective effects of extracts were determined by measuring the erythrocyte membrane resistance to free radical-induced. The results demonstrated that all the extracts exhibited a protective effect against t-BHP induced oxidative damages in human erythrocytes, the most potents wer CEs and CHEs with 86.55%, 85.81%, 74.59%, and 68.70%, for aerial and root parts, respectively, which were more effective than used standards: Quercetin (65.46%) and rutin (59.62%). In order to more clarify the previous antioxidants activity of the extracts through other mechanisms, the iron chelating ability assays were realized. The results showed that the iron chelating ability of Aerial and root extracts were very considerable; the CE showed an excellent chelating with ICs0 of 0.197 ± 0.031 μM/quercetin equivalent, higher than that used standard EDTA, with approximately 0.34 folds. These results show that Capparis spinosa L. extracts have strong anti-oxidant effects and may have some clinical benefits.展开更多
Drug abuse is a common problem that all countries in the world face. The most distinguishing characteristic of drug abuse in |apart is that use of stimulants, mostly methamphetamine, accounts for over 80% of the arre...Drug abuse is a common problem that all countries in the world face. The most distinguishing characteristic of drug abuse in |apart is that use of stimulants, mostly methamphetamine, accounts for over 80% of the arrests. Abuse of a stimulant called Philopon was widespread after the Second World War in ]apan, but the situation was dramatically improved after 1954 because the Japanese government enacted the Stimulant Control Act and restructured the police system and Japanese society recovered from post-war unrest. The situation of drug abuse in Japan has become less serious compared to the past and to the situation in many other countries, because we are taking comprehensive and nationwide measures, including proactive disclosure of the situation, control, drug abuse prevention class, and introduction of partial suspension of sentence. On the other hand, as in many countries, the rapid spread of new psychoactive substances (NPS) in recent years became a serious social issue. The situation of NPS has been rapidly improving due to comprehensive and government-wide measures, but the means of acquisition is quickly shifting to the Internet. It is necessary to strengthen cyber patrol.展开更多
In the effort to prove the effectiveness of watermelon endocarp extract as a hypolipidemic, the authors have done an initial experiment of lipase inhibition with the extract. The puposes of this study are to evaluate...In the effort to prove the effectiveness of watermelon endocarp extract as a hypolipidemic, the authors have done an initial experiment of lipase inhibition with the extract. The puposes of this study are to evaluate: (1) the optimum condition of lipase in the pankreoflat tablet, (2) the effect of watermelon endocarp extract in inhibition the lipase activity, and (3) the effectiveness of watermelon endocarp extract as lipase inhibitor relative to the hypolipidemic drugs (orlistat). Watermelon endocarp was extracted by blender, squeezed and filtered. As a source of lipase has been used pankreoflat (Kimia Farina) tablet, inhibition test was performed by mixing 35 mL with substrate (olive oil) that has been coupled with one tablet (0.25 g) ofpankreoflat and extract of 50 g watermelon endocarp and then incubated at 37℃, pH 7.5 for 25 minutes. Lipase activity is indicated by the amount ofNaOH titrant which was used to neutralize the free fatty acid from hydrolysis of olive oil. The results showed that 50 g of watermelon endocarp can produce 26 mL extract and decrease the lipase activity by 70.34%, or equivalent to 85% of the effectiveness of one tablet orlistat (120 mg), one of the hypolipidemic drugs.展开更多
The susceptibility of Sogatella furcifera female adults on N22 to malathion increased as feeding time prolonged, while the day change of susceptibility to isoprocarb showed a inverse tendency. The activities of es...The susceptibility of Sogatella furcifera female adults on N22 to malathion increased as feeding time prolonged, while the day change of susceptibility to isoprocarb showed a inverse tendency. The activities of esterase and carboxylesterase were induced significantly after on N22 for one day, and then declined. The non susceptible level of adults to insecticides and enzyme activities seemed to be heightened after feeding on ASD7, a variety resistant to Nilaparvata lugens. The total phenol content in rice leaf sheath was the highest in N22, and could be regarded as one of the factors, which caused chages in susceptibility of S. furcifera to insecticide after feeding different rice varieties. It was recommended that suitable insecticides and planthopper resistant varieties should be coordinately used in practice so that they contribute more effects respectively.展开更多
In the present study, we aimed to examine the effects of Rong Shuan capsule, Xue Zhi Kang capsule, Xin Yuan capsule and Songling Xue Mai Kang capsule on the pharmacokinetics of clopidogrel active metabolite(CAM). Th...In the present study, we aimed to examine the effects of Rong Shuan capsule, Xue Zhi Kang capsule, Xin Yuan capsule and Songling Xue Mai Kang capsule on the pharmacokinetics of clopidogrel active metabolite(CAM). The traditional Chinese medicines(TCMs) Rong Shuan capsule, Xue Zhi Kang capsule, Xin Yuan capsule and Songling Xue Mai Kang capsule are widely used to treat cardiovascular disease in China. They are often prescribed in combination with clopidogrel, a common anti-platelet Western drug. We investigated the influence of the four TCMs on CAM pharmacokinetics following administration at human dose in rats. Pharmacokinetic parameters were determined following oral(PO) administration of clopidogrel(7.5 mg/kg) with or without Rong Shuan capsule(75 mg/kg, PO), Xue Zhi Kang capsule(60 mg/kg, PO), Xin Yuan capsule(120 mg/kg, PO), or Songling Xue Mai Kang capsule(150 mg/kg, PO). Compared with the animals in the control group, Xue Zhi Kang capsule significantly decreased the area under the plasma concentration-time curve(AUC_(0-t)) of the CAM derivative by 25.4%. However, the t1/2 and Vz/F of CAM derivative were significantly increased by 43.6% and 70.7%, respectively. It was also observed that the pharmacokinetic parameters were altered in groups pretreated with Rong shuan capsule, Xin yuan capsule or Songling Xue mai kang capsule compared with the control group, but not significant. This study indicated that Xue Zhi Kang capsule had an effect on the formation and metabolism of CAM. Therefore, in the beginning of co-administration of Xue Zhi Kang capsule and clopidogrel, the anti-platelet efficacy might be compromised because of the decreased formation of CAM. Otherwise, long-time co-administration might lead to side effects by the prolongation of the t1/2 and Vz/F increase of CAM.展开更多
文摘In order to approach the effects of Shenmai Injection on SOD activity and MDA level in the senile patients with coronary heart disease, 48 cases, who had stenosis of over 70% in more than one branches of the coronary arteries, were assigned randomly into a treatment group (given Shenmai Injection plus the routine treatment) and a control group (given the routine treatment only). The superoxide dismutase (SOD) activity and malondialdehyde (MDA) level were determined before treatment and at the end of a 3-week treatment. The results showed that in the treatment group, the SOD activity was significantly increased (P<0.05) and the MDA level markedly decreased (P<0.01) in the treatment group. It can be concluded that Shenmai Injection may enhance the antioxidant ability of the senile patients with coronary heart disease.
文摘Aim To study the distribution pattern, antineoplastic activity and immunocompetence of a novel organoselenium compound Eb and investigate its in vivo antineoplastic potential. Methods Eb was administered to Kunming mice (dosage, 0.1 g·kg^(-1)·d^(-1)) intragastrically for 7 successive days. The contents of selenium in heart, liver, spleen, kidneys, lungs, stomach, brain, muscle, and bone were determined by fluorometric method on the eighth day. MTT assay was used to study tumor growth inhibition of Eb in vitro, and lymphocyte transformation, hemolysin formation and phagocytosis assay were used to study its immunocompetence. Results After 7 days′ administration of Eb, the tissue contents of sele-(nium) in liver, spleen, lungs, kidneys, and bone of mice increased, especially those in liver and spleen increased significan-tly, compared with controls; but no significant changes of such contents were found in muscle, heart, brain, and stomach. Eb demonstrated inhibitory effects on human Bel-7402, BGC-823, and Calu-3 cancer cell lines in vitro. Eb also showed ability to enhance lymphocyte transformation and serum hemolysin formation in vitro and increase the phagocytosis of macrophages. Conclusion The validated antitumor and immunostimulatory activities of Eb suggest a hypothesis that Eb may behave as a biological response modifier when used as an antitumor agent. Eb is worthy of further study in developing a new antineoplastic and immunity enhancing agent in the light of its antitumor activity, immunocompetence and specific distribution in liver, lungs, kidneys, bone, and spleen.
文摘AIM: TO assess the safety and efficacy of antioxidant therapy for patients with chronic hepatitis C virus (HCV) infection.METHODS: One hundred chronic HCV infection patients failed in interferon treatment were enrolled and randomly assigned to receive combined intravenous and oral antioxidants or placebo, or oral treatment alone, Primary end points were liver enzymes, HCV-RNA levels and histology.RESULTS: Combined oral and intravenous antioxidant therapy was associated with a significant decline in ALT levels in 52% of patients who received antioxidant therapy vs 20% of patients who received placebo (P = 0.05). Histology activity index (HAI) score at the end of treatment was reduced in 48% of patients who received antioxidant therapy vs 26% of patients who received placebo (P = 0.21). HCV-RNA levels decreased by l-log or more in 28% of patients who received antioxidant therapy vs 12% who received placebo (P = NS). In part 11 of the trial, oral administration of antioxidants was not associated with significant alterations in any of the end points.CONCLUSION: Antioxidant therapy has a mild beneficial effect on the inflammatory response of chronic HCV infection patients who are non-responders to interferon. Combined antiviral and antioxidant therapy may be beneficial for these patients.
基金Supported by the National Natural Science Foundation of China (No.20376038) and Tsinghua Basic Research Foundation (No.JCqn2005033).
文摘Electroporation creates aqueous pathways by short high-voltage pulses resulting in a transient perme- abilization of stratum corneum and an increase in the transdermal delivery rate.However the aqueous pathways will reseal after pulsing,which leads to the rapid drop of transdermal flux.In the present study,the surfactants were added to the donor solution to hinder the shrinkage and resealing of the electropore,and to prolong the lifetime of the aqueous pathways with the consideration that the surfactants could reduce the surface energy of the electropore. These effects of surfactants were demonstrated by the dynamic electrical resistance of the skin and the fluorescent imaging of the local transport regions.Piroxicam(PIX)was transported percutaneously in the presence of surfac- tants in vitro.Owing to the longer lifetime of aqueous pathways,together with the promotion of PIX availability at the barrier exterior and the improvement in the partition of PIX into the aqueous pathways,the presence of surfac- tants led to a remarkable increase in the transdermal delivery rate during electroporation and a significant growth of the accumulative transdermal amount of PIX.
文摘It is generally accepted that eggs besides being a source of everyday diet, can also be used as raw material for special food, nutraceutical, pharmaceutical and cosmetic production. The biological activity of the majority of substances presented in egg matter is related to their anti-microbial and anti-cancer properties and their immunogenic features as well. Due to the use of new generation of feed additives and techniques of immunisation of hens, the chemical composition and biological features of eggs may be modified and enriched with desired components, like n-3 fatty acids (alpha-linolenic acid (ALA), docosahexaenoic acid (DHA) phospholipids), vitamins, microelements. Egg material may also be used for the production of new biopreparations for the prophylaxis of various civilisation diseases, such as heart and cardiovascular diseases, cancers, neurogenerative disorders, metabolic bone diseases etc.. New progress in egg science allowed to discover new bioactive substances, like monomeric and dimeric cystatin and yolkin. It is necessary to develop efficient methods of isolation of biologically active substances contained in eggs, which would make it possible to produce new generation of diet supplements and biomedical products. It seems that new generation of eggs could be the best source for production of natural, high value nutraceutical supplements of diet, and also biomedical and biocosmetic preparations.
文摘The mandatory preclinical safety evaluation is an essential prerequisite to obtain the qualitative and effective medicines. Due to the fact that drugs may reveal genotoxic properties, the investigation of their mutagenic activity is an obligatory part of the preclinical drug safety program. The aim of the research is to study mutagenic properties of a new original immunomodulator Arglabin native in tablets in the induced test of gene mutations (the Ames test) on Salmonella typhimurium strains. Materials and methods: Four strains of S. typhimurium TA98, TA100, TA1535, and TA1537 were used to assess the mutagenicity in the Ames test. Results and conclusions: No statistically reliable dose-dependent increase in the number of revertant colonies of Salmonella typhimurium has been observed in the presence of the given drug within the investigated dose ranges from 5.0 to 100.0 μg/mL for strains TA100 and TA1535, and from 5.0 to 250 μg/mL for strains TA98 and TA1537 against the baseline of spantaneous mutations. Arglabin native in tablets does not reveal a mutagenic activity within the studied dose ranges on Salmonella typhimurium strains TA98, TA100, TA1535, TA1537.
文摘Capparis spinosa L. is a traditionally used plant in Algerian folk medicine to treat asthma, rheumatism and other free radicals related disorders such inflammatory. The present study was designated to study the antioxidant activity of aerial and root parts of Capparis spinosa L.. Total polyphenol content was determined, after extraction with solvents in five subfractions; methanol (CE), Hexan (HE) chloroform (CHE), ethyl acetate (EAE) and aqueous extracts (AE), employing the "Prussian blue assay". The results showed that EAE containing the highest concentration of phenolic compounds and Flavonoids followed by those of CHE of aerial and root parts, repectively. The antioxidant protective effects of extracts were determined by measuring the erythrocyte membrane resistance to free radical-induced. The results demonstrated that all the extracts exhibited a protective effect against t-BHP induced oxidative damages in human erythrocytes, the most potents wer CEs and CHEs with 86.55%, 85.81%, 74.59%, and 68.70%, for aerial and root parts, respectively, which were more effective than used standards: Quercetin (65.46%) and rutin (59.62%). In order to more clarify the previous antioxidants activity of the extracts through other mechanisms, the iron chelating ability assays were realized. The results showed that the iron chelating ability of Aerial and root extracts were very considerable; the CE showed an excellent chelating with ICs0 of 0.197 ± 0.031 μM/quercetin equivalent, higher than that used standard EDTA, with approximately 0.34 folds. These results show that Capparis spinosa L. extracts have strong anti-oxidant effects and may have some clinical benefits.
文摘Drug abuse is a common problem that all countries in the world face. The most distinguishing characteristic of drug abuse in |apart is that use of stimulants, mostly methamphetamine, accounts for over 80% of the arrests. Abuse of a stimulant called Philopon was widespread after the Second World War in ]apan, but the situation was dramatically improved after 1954 because the Japanese government enacted the Stimulant Control Act and restructured the police system and Japanese society recovered from post-war unrest. The situation of drug abuse in Japan has become less serious compared to the past and to the situation in many other countries, because we are taking comprehensive and nationwide measures, including proactive disclosure of the situation, control, drug abuse prevention class, and introduction of partial suspension of sentence. On the other hand, as in many countries, the rapid spread of new psychoactive substances (NPS) in recent years became a serious social issue. The situation of NPS has been rapidly improving due to comprehensive and government-wide measures, but the means of acquisition is quickly shifting to the Internet. It is necessary to strengthen cyber patrol.
文摘In the effort to prove the effectiveness of watermelon endocarp extract as a hypolipidemic, the authors have done an initial experiment of lipase inhibition with the extract. The puposes of this study are to evaluate: (1) the optimum condition of lipase in the pankreoflat tablet, (2) the effect of watermelon endocarp extract in inhibition the lipase activity, and (3) the effectiveness of watermelon endocarp extract as lipase inhibitor relative to the hypolipidemic drugs (orlistat). Watermelon endocarp was extracted by blender, squeezed and filtered. As a source of lipase has been used pankreoflat (Kimia Farina) tablet, inhibition test was performed by mixing 35 mL with substrate (olive oil) that has been coupled with one tablet (0.25 g) ofpankreoflat and extract of 50 g watermelon endocarp and then incubated at 37℃, pH 7.5 for 25 minutes. Lipase activity is indicated by the amount ofNaOH titrant which was used to neutralize the free fatty acid from hydrolysis of olive oil. The results showed that 50 g of watermelon endocarp can produce 26 mL extract and decrease the lipase activity by 70.34%, or equivalent to 85% of the effectiveness of one tablet orlistat (120 mg), one of the hypolipidemic drugs.
文摘The susceptibility of Sogatella furcifera female adults on N22 to malathion increased as feeding time prolonged, while the day change of susceptibility to isoprocarb showed a inverse tendency. The activities of esterase and carboxylesterase were induced significantly after on N22 for one day, and then declined. The non susceptible level of adults to insecticides and enzyme activities seemed to be heightened after feeding on ASD7, a variety resistant to Nilaparvata lugens. The total phenol content in rice leaf sheath was the highest in N22, and could be regarded as one of the factors, which caused chages in susceptibility of S. furcifera to insecticide after feeding different rice varieties. It was recommended that suitable insecticides and planthopper resistant varieties should be coordinately used in practice so that they contribute more effects respectively.
基金Foundation of Science and Technology Department of Hebei Province(Grant No.14277747D)
文摘In the present study, we aimed to examine the effects of Rong Shuan capsule, Xue Zhi Kang capsule, Xin Yuan capsule and Songling Xue Mai Kang capsule on the pharmacokinetics of clopidogrel active metabolite(CAM). The traditional Chinese medicines(TCMs) Rong Shuan capsule, Xue Zhi Kang capsule, Xin Yuan capsule and Songling Xue Mai Kang capsule are widely used to treat cardiovascular disease in China. They are often prescribed in combination with clopidogrel, a common anti-platelet Western drug. We investigated the influence of the four TCMs on CAM pharmacokinetics following administration at human dose in rats. Pharmacokinetic parameters were determined following oral(PO) administration of clopidogrel(7.5 mg/kg) with or without Rong Shuan capsule(75 mg/kg, PO), Xue Zhi Kang capsule(60 mg/kg, PO), Xin Yuan capsule(120 mg/kg, PO), or Songling Xue Mai Kang capsule(150 mg/kg, PO). Compared with the animals in the control group, Xue Zhi Kang capsule significantly decreased the area under the plasma concentration-time curve(AUC_(0-t)) of the CAM derivative by 25.4%. However, the t1/2 and Vz/F of CAM derivative were significantly increased by 43.6% and 70.7%, respectively. It was also observed that the pharmacokinetic parameters were altered in groups pretreated with Rong shuan capsule, Xin yuan capsule or Songling Xue mai kang capsule compared with the control group, but not significant. This study indicated that Xue Zhi Kang capsule had an effect on the formation and metabolism of CAM. Therefore, in the beginning of co-administration of Xue Zhi Kang capsule and clopidogrel, the anti-platelet efficacy might be compromised because of the decreased formation of CAM. Otherwise, long-time co-administration might lead to side effects by the prolongation of the t1/2 and Vz/F increase of CAM.