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1.
China Pharmacy ; (12): 601-607, 2021.
Article in Chinese | WPRIM | ID: wpr-873676

ABSTRACT

OBJECTIVE:To investigate the effects of rabepr azole on the pharmacokinetic characteristics of clopidogrel and its active metabolite in healthy volunteers with different CYP2C19 genotypes. METHODS :Healthy volunteers were selected as subjects,and then randomly divided into extensive metabolizer (EM)group,intermediate metabolizer (IM)group,and poor metabolizer(PM)group with 8 subjects in each group ,according to their CYP2C19 genotypes by random number table. In single-dose,randomized,open,two-cycle-crossover design ,each group was given Clopidogrel bisulfate tablets 300 mg or Clopidogrel bisulfate tablets 300 mg+Rabeprazole sodium enteric-coated tablets 20 mg. UPLC-MS/MS method was adopted to detect the concentration of clopidogrel and its active metabolite derivative (MP-H4). The pharmacokinetic parameters were calculated and compared by DAS 2.0 software. RESULTS :There was no statistical significance in clinical data as age ,height, body weight ,liver enzymes and serum creatinine among 3 kinds of metabolism subjects (P>0.05). Compared with subjects receiving clopidogrel alone ,cmax and AUC 0-t of clopidogrel of subjects combined with rabeprazole in EM group were increased by 36% and 27%,while those of MP-H 4 were decreased by 34% and 28%(P<0.01);cmax and AUC 0-t of clopidogrel of subjects combined with rabeprazole in IM group were increased by 19% and 18%,while those of MP-H 4 were decreased by 19% and 16% (P<0.05 or P<0.01);there was no statistical significance in cmax and AUC 0-t of clopidogrel and MP-H 4 in PM group after receiving rabeprazole additionally as well as tmax of clopidogrel and MP-H 4 in all metablism subjects ,compared with clopidogrel alone(P>0.05). CONCLUSIONS :Among CYP2C19 EM and IM subjects ,combined use of rabeprazole can significantly increase the exposure of clopidogrel and decrease the exposure of its active metabolite MP-H 4,but has no significant impact on clopidogrel and its active metabolite in CYP2C19 PM subjects.

2.
Article in Chinese | WPRIM | ID: wpr-882596

ABSTRACT

Objective:To explore the effect of Gubi Decoction on serum related inflammatory factors and PI3K/Akt/mTOR signaling pathway in osteoarthritis model rats. Methods:Seventy SPF rats were randomly divided into the blank group, sham operation group, Glucosamine sulfate group, and the low, medium and high dose Gubi Decoction groups. Except the blank group and sham operation group, knee osteoarthritis animal models were prepared by the modified Hulth method in each group. On the 28th day after successful model preparation, the high, medium and low dose Gubi Decoction groups were given Gubi Decoction 24, 12 and 6 g/kg by gavage respectively; glucosamine sulfate group was given glucosamine sulfate tablet suspension 3 g/L by gavage, once a day for 28 days. The levels of TNF-α and IL-1β in serum were detected by ELISA. The gene expressions of PI3K, Akt and mTOR in cartilage tissue were detected by Real-PCR. The protein expressions of PI3K, Akt, p-PI3K, p-Akt and mTOR were detected by Western blot. Results:Compared with the model group, the knee joint diameter[(11.17 ± 1.81) mm, (11.60 ± 1.38) mm, (10.80 ± 1.17) mm vs. (12.57 ± 0.98) mm] of the rats in the glucosamine sulfate group and the medium and high dose Gubi Decoction groups significantly decreased ( P<0.05). The content of TNF-α [(111.43 ± 21.98) ng/L, (53.42 ± 13.25) ng/L vs. (157.89 ± 23.60) ng/L], IL-1β [(67.50 ± 18.44) ng/L, (48.22 ± 9.63) ng/L vs. (96.11 ± 14.85) ng/L] in the medium and high dose Gubi Decoction groups significantly decreased ( P<0.05), and the expression of PI3K (1.87 ± 0.17, 1.24 ± 0.49 vs. 2.19 ± 0.47), Akt (1.50 ± 0.51, 1.10 ± 0.32 vs. 2.68 ± 0.63), and mTOR (1.32 ± 0.54, 1.10 ± 0.33 vs. 2.94 ± 0.55) mRNA in the medium and high dose Gubi Decoction groups significantly decreased ( P<0.05). The expression of PI3K, Akt, p-PI3K, p-Akt in the low, medium and high dose Gubi Decoction groups significantly decreased ( P<0.05), and the expression of mTOR in the medium dose Gubi Decoction group significantly decreased ( P<0.05). Conclusion:Gubi Decoction can significantly reduce the level of inflammatory factors in the serum of osteoarthritis model rats, and its anti-inflammatory and analgesic effects may be related to PI3K/Akt/mTOR signaling pathway.

3.
Article in Chinese | WPRIM | ID: wpr-582111

ABSTRACT

Objective To evaluate the clinical significance of peripheral atheral atherosclerosis after treatment by folicacid in combination with mecobalarain in uremia patient using vascular ultrasound.Methods 99 cases of uremia patients with carotid atherosclerosis were treated with folie acid tablets and mecobalamin tablets for six months.The carotid intimia-media thiclmess(IMT),total plaque area,numbers and ultrasound types of carotid atherosclerotic before and after treatment were observed.Results After six months,carotid IMT became tinner significantly,and the totsl plaque area decreased(P<0.05).The ultrasound types of carotid atherosclerotic plagues have changed after six montha.and the plaque numbers decreased significantly(P<0.05).Conclusion Threatment by folie acid combination with mecobalamin in uremia patients maybe helpful to the progression of carotid athereaclerotie disease.

4.
China Pharmacy ; (12)2005.
Article in Chinese | WPRIM | ID: wpr-534194

ABSTRACT

OBJECTIVE: To prepare Kuijieyu enemas and establish its quality standard.METHODS: Most of traditional Chinese medicines in prescription were decocted using water and some were crushed.Then they were concentrated to prepare enemas.Pueraria lobata,Rhizoma Coptidis,Scutellaria baicalensis in Kuijieyu enemas were qualitatively identified by TLC.The content of baicalin in Kuijieyu enemas was determined by HPLC.RESULTS: The TLC spots were clear,well-separated and specific.The linear range of baicalin were 210~1 750 ?g(r=0.999 9) with an average recovery of 99.13% (RSD=1.1%,n=6).CONCLUSION: The preparation process is simple and convenient.The quality control method is simple,reliable,specific and reproducible.

5.
China Pharmacy ; (12)2001.
Article in Chinese | WPRIM | ID: wpr-524749

ABSTRACT

OBJECTIVE:To study the plasma total homocysteine(tHcy)level in the uremia patients and to study the therapeutic effects of folic acid combined with methylcobalamin in the intervention treatment of uremia patients with homo-cysteinemia.METHODS:Levels of plasma tHcy of60uremia patients(treatment group)and40normal subjects(control group)were determined both before treatment and8weeks after intervention treatment with folic acid combined with methylcobal-amin.RESULTS:The plasma level of tHcy in uremia patients were significantly higher than that in the normal subjects(P

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