1.Study on Dermal Pharmacokinetic Difference of Triptolide in Normal and Diabetic Rats by Microdialysis
Ziping ZHANG ; Weidong ZENG ; Xiucai GUO ; Boxin ZHAO ; Yingguang DENG
China Pharmacy 2016;27(19):2641-2643
OBJECTIVE:To study the dermal pharmacokinetic difference of triptolide in normal and diabetic rats,and to pro-vide reference for rational drug use in the clinic. METHODS:12 Wistar rats were randomly divided into normal group and diabetic model group(0.1%streptozotocin intraperitoneally),with 6 rats in each group. Both group were given Triptolide cream 0.5 g to ab-dominal skin,and dialysate was collected by microdialysis every 30 min for consecutive 12 h. Subcutaneous concentration was de-tected by HPLC-MS,and subcutaneous concentration-time curves were analyzed and compared between two groups,and Winnon-lin 5.0.1 software was used to calculate pharmacokinetic parameters. RESULTS:The pharmacokinetic parameters of normal group and diabetic model group were that cmax were(1.54±0.37)and(5.12±1.34)μg/ml;tmax were(7.32±0.24)and(6.21±0.35)h;AUC0-12 h were (12.65 ± 4.64) and (37.43 ± 5.23)μg·h/ml,with statistical significance (P<0.05). CONCLUSIONS:The change of dermal structure caused by diabetes can increase percutaneous penetration amount of triptolide in rats,and drug dosage should be reduced according to circumstances so as to reduce side effects.
2.Determination of residual organic solvents in Apixaban bulks drug by headspace gas chromatography
Dongfang LIU ; Xiucai GUO ; Lina ZHAO ; Chaodong JIN
Drug Evaluation Research 2017;40(1):63-67
Objective To establish a method for determination of the twelve residual organic solvents,including methanol,ethanol,acetone,isopropanol,tert-Butyl methyl ether,dichloromethane,aceticether,tetrahydrofuran,triethylamine,trimethylorthofor-Mate,morpholine,N,N-Dimethylformamide in Apixaban bulks drug.Methods Gas head-space chromatography was applied to this study.The column was DB-624 silica capillary column (30.0 m × 0.53 mm × 3.00 μm) and the carrier gas was high purity nitrogen;The vial temperature was 100 ℃,and the vial time was 20 min.The Column temperature was kept at 40 ℃ for 6 min,then the temperature was raised to 220 ℃ at the rate of 20 ℃/min and subsequently sustained for 10 min.FID detector temperature and injection temperature were both 250 ℃.The N2 flow rate was 2.8 mL/min.Split ratio was 5∶1.Results Twelve kinds of solvents were completely separated and determined with a good linearity (r =0.9994-0.9999).The RSD values of precision experiments and the average recovery was in line with the requirements.Conclusion Theanalytical method is simple,accurate and sensitive,which could be used for determination of residual organic solvents in Apixaban bulks drug.
3.Tetrahydropalmatine's permeative properties of acupoint and non-acupoint transdermal administration of Baijiezi Tufang in vitro and in vivo.
Xiucai GUO ; Xia LIU ; Yuehong XU
China Journal of Chinese Materia Medica 2012;37(7):1034-1038
OBJECTIVETo study tetrahydropalmatine's permeative properties of acupoint and non-adupoint transdermal administration of baijiezi tufang in vitro and in vivo.
METHODTaking tetrahydropalmatine as an evaluative component to assess the permeative of baijiezi tufang in acupoint skin and non-acupoint skin with the modified Franz diffusion cell method and in vivo penetration studies. The content of tetrahydropalmatine was determined by a HPLC method.
RESULTThe 24 hours cumulative permeation amount through acupoint skin was (13.53 +/- 3.92) microg x cm(-2), about 4 times higher than non-acupoint skin. The steady-state infiltration rates of tetrahydropalmatine in acupoint skin was (0.659 1 microg x cm(-2) x h(-1)), 4.5 times higher than non-acupoint skin. The content in acupoint skin was signally higher than that in non-acupoint skin (P < 0.05). An accumulation of fluorescence can be clearly seen in the four layers: stratum corneum > viable epidermis > dermis > subcutaneous.
CONCLUSIONIn vitro and in vivo studies show that the permeation of baijiezi tufang in acupoint skin was better than in non-acupoint skin, following a higher cumulative amount and skin content.
Acupuncture Points ; Administration, Cutaneous ; Animals ; Berberine Alkaloids ; administration & dosage ; pharmacokinetics ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; administration & dosage ; metabolism ; Guinea Pigs ; Skin ; metabolism
4.A clinical analysis of 61 cases of protein-losing enteropathy
Liming ZHU ; Gang SUN ; Jiaming QIAN ; Xiucai FANG ; Guijun FEI ; Huijun SHU ; Tao GUO ; Yue LI
Chinese Journal of Internal Medicine 2011;50(3):209-211
Objective To increase the understanding in protein-losing enteropathy (PLE).Methods Sixty-one PLE patients were enrolled in the study and the clinical characteristics, complicated disease, diagnosis and treatment were analyzed. Results The age of the patients was 16-77 (40±15)years, and the gender ratio was 35:26 (female: male). The main clinical manifestations were bilateral lower limb edema in 51 cases, ascites in 41 cases, bilateral pleural effusion in 23 cases, pericardial effusion in 13cases, abdominal pain in 16 cases and diarrhea in 33 cases. The prominent abnormality in laboratory examinations was hypoalbuminemia. The underlying diseases include systemic lupus erythematosus (SLE) in 28 cases, intestinal lymphangiectasia in 12 cases, hepatic cirrhosis in 5 cases, heart diseases in 5 cases,Crohn's disease in 3 cases, membranous nephropathy in 2 cases, Budd-Chiari syndrome in 1 case. Four cases happened after abdominal operation and 1 case after radiation therapy of gastric cardia cancer. Thirtyseven cases were diagnosed by 99Tcm-labelled human serum albumin scintigraphy and 24 cases were diagnosed clinically. Treatment was focused on underlying diseases. The clinical manifestations in 21 cases of SLE improved after SLE was controlled. In 2 cases of intestinal lymphangiectasia and one with Crohn's disease, the clinical manifestations improved after surgery. The other patients had no improvement.Conclusions PLE was not uncommon in clinical practice. Its predominant characteristics were severe hypoalbuminemia, edema and dropsy of serous cavity. PLE can complicate other diseases such as SLE,intestinal lymphangiectasia. Treatment should be focused on primary disease.