1.Pharmacokinetics of scopolamine hydrobromide oral disintegrative microencapsule tablets in Beagle dogs determined with LC-MS/MS.
Tian XIA ; Deding LIU ; Lifu SHI ; Jinhong HU
Acta Pharmaceutica Sinica 2011;46(8):951-4
The study aims to elucidate the characteristics of pharmacokinetics of scopolamine hydrobromide oral disintegrative microencapsule tablets in healthy Beagle dogs. Chromatographic separation was performed on a C18 column (100 mm x 3.0 mm, 3.5 microm) with methanol - 2 mmol x L(-1) ammonium formate (25 : 75) as the mobile phase. A trip-quadrupole tandem mass spectrum with the electrospray ionization (ESI) source was applied and positive ion multiple reaction monitoring mode was operated. Six Beagle dogs were randomly devided into two groups. They received oral single dose of scopolamine hydrobromide oral disintegrative microencapsule tablets 0.6 mg (test tablet) or scopolamine hydrobromide normal tablets (reference tablet). Plasma samples were collected at designed time. Plasma concentration of scopolamine hydrobromide was determined by LC-MS/MS and pharmacokinetic parameters were calculated. The pharmacokinetic parameters of test tablet vs reference tablet were as follows: C(max): (8.16 +/- 0.67) ng x mL(-1) vs (3.54 +/- 0.64) ng x mL(-1); t1/2: (2.83 +/- 0.45) h vs (3.85 +/- 0.82) h; t(max): (1.25 +/- 0.27) h vs (0.42 +/- 0.09) h; AUC(0-12h): (25.06 +/- 3.75) h x ng x mL(-1) vs (9.59 +/- 1.02) h x ng x mL(-1); AUC(0-infinity): (26.30 +/- 3.92) h x ng x mL(-1) vs (10.80 +/- 1.45) h x ng x mL(-1); MRT(0-12h): (3.38 +/- 0.34) h vs (3.86 +/- 0.26) h; MRT(0-infinity): (3.98 +/- 0.63) h vs (5.37 +/- 1.00) h. The absorption rate and AUC of test tablet is different from that of reference tablet. The bioavailability of test tablet is better than those of reference tablet.
2.The impact of nucleos(t)ide analogue antiviral therapy on anxiety and depression of patients with chronic hepatitis B
Shuangshuang XIE ; Qiang LI ; Xia YANG ; Wenbo FAN ; Jinhong YU ; Li LIU ; Wenwen LI ; Shijun CHEN
Chinese Journal of Infectious Diseases 2011;29(12):723-728
Objective To explore the impact of nucleos(t)ide analogue antiviral therapy on anxiety and depression of patients with chronic hepatitis B (CHB),and analyze the related factors.Methods Before nucleos(t)ide analogue antiviral therapy,1 year and 2 years after antiviral therapy,120 CHB patients were investigated with self-rating anxiety scale (SAS) and self-rating depression scale (SDS).The demography data of patients were collected.Serum levels of alanine transaminase (ALT) and hepatitis B virus (HBV) DNA and other biochemical indicators were measured regularly.Results Before nucleos(t)ide analogue antiviral therapy,1 year and 2 years after antiviral therapy,both the mean scores of SAS and SDS became lower gradually (F=12.661 and 22.395,respectively;both P<0.01).The percentage of patients with SAS and SDS scores more than 50 were 5.8%,4.2%,1.7% and 13.3%,7.5%,5.0%,respectively.After 2 years of therapy,the anxiety improvement rate of the patients obtained HBV DNA<1000 copy/mL was 69.0%,while those with HBV DNA≥1000 copy/mL was 22.2% (x2 =22.325,P<0.01).Meanwhile,after 2 years of therapy,the depression improvement rate of the patients obtained HBV DNA<1000 copy/mL was 77.4%,while those with HBV DNA≥1000 copy/mL was 22.2% (x2 =32.179,P<0.01).Multiple factors Logistic regression analysis indicated that the odds ratios (OR) of improvement of anxiety and depression in patients with HBV DNA<1000 copy/mL were 7.751 (95% CI:3.026-19.853) and 15.069(95% CI:5.309-42.770),respectively,compared with those with HBV DNA≥1000 copy/mL; and OR of improvement of depression in patients with ALT≤40 U/L waa 4.103 (95% CI: 1.376 - 12.238).Conclusions Nucleos(t) ide analogue antiviral therapy could improve the anxiety and depression of CHB patients.The HBV DNA negativity is the independent impact factor of improvement of anxiety and depression in CHB the patients.
3.Regulatory effect of catalpol from Radix Rehmanniae on M_2 receptor density in M_2 receptor transfected CHO cells
Jinhong WANG ; Qixiang SUN ; Zongqin XIA ; Yaer HU
Chinese Pharmacological Bulletin 2003;0(12):-
Aim To investigate the effect of catalpol from Radix Rehmanniae on M_2 receptor density in CHO cells transfected with gene of M_2 receptors(CHO m2).Methods Cultured CHOm2 cells were randomly divided into 4 groups:three concentrations of catalpol :10-6、10-5、10-4 mol?L-1,and saline control.After addition of catalpol and saline for 72 h,M_2 Receptor density was measured by single point 3H-NMS binding assay,the content of protein was measured with Lowry's method.Competitive binding assay using the binding system of 3H-NMS was performed to address the question about whether catalpol could occupy the M receptor binding site.Addition of catapol to brain homogenate and measuring the enzyme activity with the Ellman's colorimetric method were performed to address the question about whether catalpol could in-hibit acetylcholinesterase activity.Results Catalpol can elevate the M_2 receptor density in CHO m2 cells significantly at the doses of 10-5、10-4 mol?L-1(P

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