AIMTo investigate the impact of CYP2C9 * 3 on the pharmacokinetics of glibenclamide and lornoxicam.

METHODSCYP2C9 * 3 was measured in 83 non-related Chinese subjects by PCR-RFLP. The pharmacokinetics of lornoxicam and glibenclamide were investigated in 18 subjects (7 with CYP2C9 * 1/* 3 genotype and 11 with * 1/* 1 genotype). Glibenclamide and lornoxicam in plasma were determined by the sensitive liquid chromatography-tandem mass spectrometry, separately.

RESULTSAfter a single oral dose of 2.5 mg glibenclamide, C(max) was (70.0 +/- 11.5) microg x L(-1) in CYP2C9 * 1/ * 3 subjects and (51.9 +/- 12.3) microg x L(-1) in * 1/ *1 subjects. AUC(0-infinity) were (435 +/- 47) vs (287 +/- 95) microg x h x L(-1) (in * 1/ * 3 vs * 1/ *1 subjects), and CL/F were (96 +/- 9.3) vs (160 +/- 51) mL x min(-1), respectively. Statistic analysis results indicated that glibenclamide AUC(0-infinity) was significantly higher (1.5-fold) and subsequently CL/F was significantly lower (40%) in CYP2C9 * 1/ * 3 subjects than those in * 1/ * 1 subjects (P < 0.01). After a single oral dose of 8 mg lornoxicam, C(max) was (1.54 +/- 0.24) mg x L(-1) in CYP2C9 * 1/ * 3 subjects and (1.19 +/- 0.37) mg x L(-1) in * 1/ * 1 subjects. AUC(o-infinity were (14.9 +/- 2.2) vs (6.92 +/- 1.48) mg x h x L(-1) (in * 1/ *3 vs * 1/ * 1 subjects), and CL/F were (9.1 +/- 1.2) vs (20.1 +/- 4.6) mL x min(-1), respectively. Statistic analysis results indicated that lornoxicam AUC(0-infinity) was significantly higher (2. 2-fold) and subsequently CL/F was significantly lower (55% ) in CYP2C9 * 1/ * 3 subjects than those in * 1/ * 1 subjects (P < 0.001).

CONCLUSIONCYP2C9 * 3 greatly affects both the pharmacokinetic profiles of glibenclamide and lornoxicam. The elimination of these drugs significantly decreased in subjects with CYP2C9 * 1/ * 3 genotype, especially lornoxicam.

Adult ; Alleles ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacokinetics ; Area Under Curve ; Aryl Hydrocarbon Hydroxylases ; genetics ; Asian Continental Ancestry Group ; China ; Cytochrome P-450 CYP2C9 ; Genotype ; Glyburide ; pharmacokinetics ; Humans ; Hypoglycemic Agents ; pharmacokinetics ; Male ; Piroxicam ; analogs & derivatives ; pharmacokinetics ; Polymerase Chain Reaction ; Polymorphism, Genetic ; Polymorphism, Restriction Fragment Length

OBJECTIVETo study the thin layer chromatographic (TLC) fingerprint of flavonoid constituents from Polygonatum odoratum, to set up the identification protocol of the herbal and provide scientific information for its quality control.

METHODThe ethanol extracts were separated on silica gel G precoated plate with a mixture of toluene-ethylacetate-formic acid (5:4:1) as the mobile phase. The spots were visualized with ammonia vapor, then were examined under ultraviolet light (365 nm). The plate was scanned at wavelengths of lambdaR = 500 nm, lambdaS = 280 nm.

RESULTA fingerprint of flavonoids of P. odoratum, with 10 specific fluorescent spots while examined under ultraviolet light, was set up.

CONCLUSIONThe method can be used for quality control of P. odoratum.

Chromatography, Thin Layer ; methods ; Flavonoids ; analysis ; chemistry ; Plants, Medicinal ; chemistry ; Polygonatum ; chemistry ; Quality Control ; Rhizome ; chemistry

Aneurysm, Dissecting/surgery* ; Aorta, Thoracic/surgery* ; Aortic Aneurysm, Thoracic/surgery* ; Blood Vessel Prosthesis Implantation ; China ; Endovascular Procedures ; Humans ; Retrospective Studies ; Treatment Outcome

OBJECTIVETo evaluate the effect of different preparation methods on the encapsulation efficiency (EE) and drug loading (DL) of paclitaxel-loaded polybutylcyanoacrylate nanoparticles (PTX-PBCA-NPs) and optimize the preparation of PTX-PBCA-NPs.

METHODSWith DL and EE as the major indexes, the qualities of PTX-PBCA-NPs produced by the interfacial polymerization and emulsion polymerization method were compared. The optimized prescription was obtained by orthogonal design.

RESULTSThe ranges of EE of PTX-PBCA-NPs with the two methods were both 94.39%-99.23%. The highest DL with interfacial polymerization was (1.07-/+0.03)%, as compared to (0.86-/+0.01)% with emulsion polymerization. The optimized preparation conditions resulted in the mean size of PTX-PBCA-NPs of 235.6 nm, DL of 0.80%, and EE of 95.71%.

CONCLUSIONThe EE of PTX-PBCA-NPs prepared by the above two methods is consistent with the requirement of the Pharmacopoeia of China, and PTX-PBCA-NPs containing higher DL can be obtained via interfacial polymerization.

Delayed-Action Preparations ; chemical synthesis ; Drug Carriers ; chemistry ; Drug Delivery Systems ; Enbucrilate ; chemistry ; Nanoparticles ; chemistry ; Paclitaxel ; administration & dosage ; Polymerization

Administration of the immunosuppressive drug cyclosporine (CSA) after autologous peripheral blood stem cell transplantation (APBSCT) induces a systemic auto-immune syndrome resembling graft-versus-host disease (GVHD), this syndrome termed autologous GVHD has significant antitumor activity, it can reduce the incidence of tumor relapse after APBSCT. The antitumor effect of this auto-aggression syndrome can be enhanced by the administration of gamma-interferon (gamma-IFN). Five consecutive patients who received APBSCT received therapy inducing autologous GVHD. Intravenous administration of CSA [1 mg/(kg.d) for 28 days] was begin on the day of transplantation. gamma-interferon (0.025 mg/m(2) qod) was administered sub-cutaneously from days 7 throngh 28 after transplatation. Results showed that four of five occured autologous GVHD-skin demage, five in control didn't occur autologous GVHD. The relapse rate of the treated cases was 20% (1/5) versus 60% (3/5) of the control, and the median survival time of the treated cases was 20 (4 - 30) months versus 10 (2 - 20) months of the control. The data indicates that autologous GVHD results in low relapse rate of the patients rececving APBSCT.

OBJECTIVETo reveal the relationship between the storage time of the bark of Magnolia officinalis and the content of phenols in it, and lay a theoretical foundation for the harvest, processing, management and storage.

METHODThe contents of magnolol and honokoiol in 15 bark samples, collected from the main producing areas in China, were determined in the time of freshly harvest and 3 and 10 years after respectively by HPLC method.

RESULTIt showed that within a certain period of time, bark storage was favorable to conversion and accumulation of phenols, that the content of magnolol tended to increase from year 0 to year 3, then followed by slight decrease with years on account of volatilization of phenols, but was still higher when the bark was stored for 10 years than that that when the bark was freshly harvested, and the content of honokoiol still tended to increase when the bark had been stored for 10 years.

CONCLUSIONThe phenols in bark of M. officinalis is quite stable and the bark can be stored for 10 years or longer.

Biphenyl Compounds ; analysis ; Drug Storage ; methods ; Drugs, Chinese Herbal ; chemistry ; Lignans ; analysis ; Magnolia ; chemistry ; Plant Bark ; chemistry ; Time Factors

OBJECTIVETo describe observation of security and availability of covering left subclavian artery during thoracic endovascular aortic repair (TEVAR) in follow-up.

METHODSFrom December 2007 to December 2008, 111 consecutive patients received stent grafts to treat lesions involving thoracic aorta. According to the covering of left subclavian artery, four groups including total covering (TC), less-than 50% covering (LTC), more-than 50% covering (MTC) and non-covering (NC) were formed. Difference of blood pressure between two upper extremities was required before TEVAR and 1st, 3rd, 5th, 30th day after TEVAR. Patients were evaluated postoperatively and at follow-up for stroke as well as symptoms of paraplegia, hemiparalysis or left upper extremity claudication.

RESULTSFifty-five (49.6%), 18 (16.2%), 7 (6.3%) and 31 (27.9%) cases were divided into TC, LTC, MTC and NC groups, respectively. Difference of blood pressure between TC and the 3 latter groups were significantly different (P<0.01). Complications appeared as followed during one week after TEVAR: 13 patients in dizziness, among which 5 patients suffered from amaurosis and spotted vision, and 7 patients in left upper extremity claudication. No stroke, paraplegia or hemiparalysis in TC. Thoracic aortic lesions were successfully excluded in all patients.

CONCLUSIONSIntentional coverage of left subclavian artery to obtain an adequate proximal landing zone during TEVAR is safe and well-tolerated. But it may be managed expectantly with some exceptions for further lasting efficacy.

Aorta, Thoracic ; surgery ; Aortic Aneurysm, Thoracic ; surgery ; Blood Vessel Prosthesis Implantation ; Female ; Humans ; Male ; Middle Aged ; Prospective Studies ; Stents ; Subclavian Artery ; surgery ; Treatment Outcome

Objective To discuss characteristics of height growth such as Peak Height Velocity (PHV) and Age at Peak Height Velocity (PHA) during adolescence,and to compare the results with other research findings.Methods Primary and middle school students' annual physical examination data of Zhongshan in 2005-2010 was used.The height velocity by age,PHV,PHA,height velocity by PHA were calculated.Results The average peak height velocity boys was ( 10.03 ± 1.67 ) cm/yr.and that of the girls was ( 8.39 ± 1.05 ) cm/yr.Both findings were close to the results from previous similar findings.The average age at which peak height velocity reached 12.28± 1.30 years for boys and 10.78 ± 1.04 years for girls,both lower than the previous findings.The correlation coefficients,between height level and PHA were -0.357 (P＜0.001) for boys and -0.338 (P＜0.001) for girls.Conclusion The height levels were positively related to the height velocity before PHA.The Zhongshan students' PHA was lower than the Beijing,Shanghai and Shenyang students,also lower than American and Britain students',but their PHVs were similar.

Objective To evaluate the clinical efficacy and safety of Shaohuang laxative mixture in the treatment of intestinal gas stagnation constipation.Methods A total of 144 patients with intestinal gas stagnation constipation were randomly divided into treatment group and control group,each group 72 cases.Patients in treatment group were orally administration Shaohuang laxative mixture,20 mL each time,tid.Patients in control group were orally given Muxiang Binlang pill 6 g each time,tid.Once the defecate free,stopping the medication,and followed up for 7 d to observe the defecating awareness,frequency,stool shape (according to Bristol stool from scale),time,amount,accompanying symptoms (including defecation pain,abdominal distension,defecation difficulties,exhaust,etc.),the main related signs,physical and chemical indicators.Besides,the adverse drug reactions were recorded during the treatment.Results After treatment,the total effective rate in treatment group was 91.94％ (57/62 cases),had no significant difference with that in control group,which was 90.16％ (55/61 cases,P ＞ 0.05).After treatment,the scores of desire to defecate,defecation frequency,defecation quality,defecation time,defecation volume,defecation difficulty level,abdominal distension and pain,belching,Xiongxie fullness and borborygrmi in treatment group were 4.81 ±0.80,4.19 ±0.78,4.91 ±0.76,5.11 ±0.92,4.25 ±0.61,4.20 ±0.77,5.11 ±0.68,5.06 ±0.79,3.73 ±0.61,4.40 ±0.64 in treatment group,had no significant difference with those in control group,which were 4.65 ± 0.74,4.26 ± 0.84,4.81 ± 0.88,5.02 ± 0.99,4.12 ± 0.54,4.19 ± 0.81,5.02 ±0.76,5.00 ±0.75,3.87 ±0.66,4.33 ±0.51 (P ＞0.05),but had significant difference with those before treatment (P ＜ 0.05).The adverse reactions in treatment group and control group were nausea and diarrhea,and the incidences of adverse drug reactions in treatment group and control group were 3.23％ (2/62 cases) and 4.92％ (3/61 cases),with no significant difference (P ＞ 0.05).Conclusion Shaohuang laxative mixture and aplotaxis auriculata compound pill have similar efficacy in treatment of intestinal gas stagnation constipation.Shaohuang laxative mixture is safe and effective in the treatment of intestinal gas stagnation.

Objective:To explore the effects and mechanisms of chidamide on the osteogenic differentiation of bone marrow mesenchymal stromal cells(MSC)from myelodysplastic syndromes(MDS).Methods:MSC were isolated and cultured from bone marrow of MDS patients and healthy donors.CCK-8 assay was used to detect the effects of chidamide on the proliferation of MSC.The effects of chidamide on the activity of histone deacetylase(HD AC)in MSC was measured by a fluorescence assay kit and Western blot.Alkaline phosphatase(ALP)activity was detected on day 3 and calcium nodule formation was observed by Alizarin Red staining on day 21 after osteogenic differentiation.The expression of early and late osteogenic genes was detected on day 7 and day 21,respectively.RT-PCR and Western blot were used to detect the effects of chidamide on mRNA and protein expression of RUNX2 which is the key transcription factor during osteogenesis.Results:As the concentration of chidamide increased,the proliferation of MSC was inhibited.However,at a low concentration(1 μmol/L),chidamide had no significant inhibitory effect on MSC proliferation but significantly inhibited HD AC activity.In MSC from both MDS patients and healthy donors,chidamide(1 μmol/L)significantly increased ALP activity,calcium nodule formation,thereby mRNA expression of osteogenic genes,and restored the reduced osteogenic differentiation ability of MDS-MSC compared to normal MSC.Mechanistic studies showed that the osteogenic-promoting effect of chidamide may be related to the upregulation of RUNX2.Conclusion:Chidamide can inhibit HD AC activity in MSC,upregulate the expression of the osteogenic transcription factor RUNX2,and promote the osteogenic differentiation of MDS-MSC.