The in-vivo bioavailability of Qingxintong administrated by intramuscular injection, intravenous injection and gastric infusion was compared. Experimental results showed that Qingxintong was rapidly absorbed and excreted. The half-life time for absorption was 0.05 - 0.07 h and the half-life time for elimination was 0.14 - 0.29 h. The bioavailability of Qingxintong in the dose of 10 mg/kg by intramuscular injection or by intravenous injection was 94.71 %, and was 9.16% in the dose of 60 mg/kg by gastric infusion or in the dose of 10mg/kg by intramuscular injection.

The pharmacodynamic active parts of protecting liver of Peristrope japonica (thunb.) Bremek were identified. Rat acute liver injury model was induced by D-galactosamine (D-GlaN). The active parts were identified on the whole extraction and 4 fractions. The results showed that the pharmacodynamic active parts of Peristrope japonica were the n-BuOH fraction.
Acanthaceae ; Drugs, Chinese Herbal/*pharmacology ; Drugs, Chinese Herbal/therapeutic use ; Galactosamine ; Hepatitis, Toxic/etiology ; Hepatitis, Toxic/*prevention & control ; Liver Function Tests ; Phytotherapy ; Protective Agents/pharmacology ; Protective Agents/therapeutic use ; Random Allocation

AIM To study the pharmacokinetic characters of dauricine(Dau) in rats after different administration ways. METHOD RP-HPLC method was used in the study. RESULT The results indicated that the plasma C-T curve conform to two-compartment open model after iv. The plasma concentration of Dau in rats after ig Dau 150 mg*kg-1 is low, less than 1 mg*L-1 of peak concentration. The absolute bioavailibility is about 16.6 %. The plasma concentration-time profile shows a double-peak phenomenon. The time taken to reach the peak is about 15 min after ig and the trough time is 3 h. The plasma concentration increased again in 4 h to form the second peak. The studies suppose a stomach-intestine recirculation of Dau is the major reason for double-peak phenomenon. Dau has a wide distribution in rat body. It lies in all tissues and organs in both adminastration ways. The tissue Dau concentration are hundreds times higher than that in plasma concurrently. Feces is the main route whereby Dau are excreted from the rats after ig 150 mg*kg-1. The excreted percentage through feces is 26.29 %, while through urine is 4.93%. The total amount is 31.22% after 48h of oral administration of Dau. The study of the mean percentage of the dose remaining in stomach, small intestine, large intestine and whole GI tract from each rat sacrificed at different times after oral administration of Dau suggest the stomach-intestine circle. CONCLUSION　The bioavailibility of Dau is low. The plasma drug concentration versus time curve shows an innormal double-peak phenomenon. Dau can distribute abroadly to almost all kinds of the tissues in rats. The main excretion routes are through feces and urine. The pilot study suggests that stomach-intestine circle be the main reason for the innormal double-peak phenomenon.

To establish the determination method of dauricine (Dau) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dau and its internal standard,daurisoline were 9.2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70%, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0.030 to 3.000 mg/L in blood samples and 0.050 to 5.000 mg/L in other tissue samples. The intraday and interday coefficients of variation were below 10%. The results showed that the method can be used for detecting Dau in all kinds of biological samples.

To establish the determination method of dauricine (Dau) concentration in rats' blood and other biological samples, a reverse-phase HPLC method was adopted. Under the given condition, dauricine could be well separated. The retention time (tR) of Dau and its internal standard,daurisoline were 9.2 and 6.1 respectively. The detection limit was 10-2 mg/ml. The absolute recoveries of all kinds of samples were above 70%, and the relative ones were over 85%. A good liner relationship has been obtained over the entire range of 0.030 to 3.000 mg/L in blood samples and 0.050 to 5.000 mg/L in other tissue samples. The intraday and interday coefficients of variation were below 10%. The results showed that the method can be used for detecting Dau in all kinds of biological samples.

Objective To investigate the efficacy of 125I radioactive particle implantation combined with surgery and chemotherapy in the treatment of locally advanced urinary tract urothelial carcinoma (UTUC).Methods The clinical data of 128 patients of locally advanced (T3,T4) UTUC treated with surgery with radioactive particle implantation plus postoperative GC chemotherapy (experimental group) and surgery plus postoperative GC chemotherapy (control group) were retrospectively analyzed.All the patients underwent complete resection of the tumor.The postoperative pathology was urinary tract epithelium cancer.In the experimental group,there were 45 (69.2％) males and 20 (30.8％) females,with median age 56.5 years.There were 39 (60.0％) patients diagnosed with renal pelvic cancer,including 13 (33.3 ％) patients with local lymph node metastasis;26 patients (40.0％) with ureteral cancer,11 patients (42.3％) with local lymph node metastasis.In the control group,there were 46 males (73.0％) and 17 females (27.0％),with median age 57.1 years.There were 40 (63.5％) patients with renal pelvic cancer,including 12 (30％) cases of local lymph node metastasis;23 patients with ureteral carcinoma (36.5％),including 10 patients (43.4％) with local lymph node metastasis.There was no significant difference in basehne data between the two groups (P ＞ 0.05).The recurrence and distant metastasis,recurrence-free survival,distant disease free survival(DDFS),disease-specific survival(DSS),overall survival (OS) and comphcations of two groups were compared.Results The follow-up time was 50.5 months (ranged 5 to 62 months).In experimental group,there were 2 cases,5 cases,11 cases,16 cases and 21 cases occurred recurrence and distant metastasis in 6 months,1 year,2 years,3 years and 5 years respectively,and the 5-year cumulative recurrence and distant rate was 32.3％ (21/65).In control group,there were 3 cases,5 cases,17 cases,21 cases and 32 cases,occurred recurrence and distant metastasis in 6 months,1 year,2year,3 year,5 year respectively,and the 5-year cumulative recurrence and distant rate was 50.8％(32/63).There was significant difference between the two groups (P =0.034).In the experimental group and the control group,the 5-year non-metastatic survival rates were 61.5％ (40/65)and 41.3％ (26/63),respectively.There was significant difference in 5-year non-metastatic survival rate between the two groups (P =0.033).The 5-year DSS rates were 69.2％ (45/65) and 50.8％ (32/63),respectively.The 5-year DSS rate of the two groups was significantly different (P =0.033).The 5-year OS rates were 53.8％ (35/65) and 36.5％ (23/63) respectively.There was significant difference in the 5-year OS rate between the two groups (P =0.049).Condusions Compared with surgery and chemotherapy,the use of 125I radioactive particle implantation combined with surgery and chemotherapy in the treatment of locally advanced stage (T3-T4) UTUC could achieve the total survival benefit,and less adverse reactions.

The pharmacodynamic active parts of protecting liver of Peristrope japonica (thunb.) Bremek were identified. Rat acute liver injury model was induced by D-galactosamine (D-GlaN). The active parts were identified on the whole extraction and 4 fractions. The results showed that the pharmacodynamic active parts of Peristrope japonica were the n-BuOH fraction.
Acanthaceae ; Animals ; Chemical and Drug Induced Liver Injury ; etiology ; prevention & control ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Female ; Galactosamine ; Liver Function Tests ; Male ; Phytotherapy ; Protective Agents ; pharmacology ; therapeutic use ; Random Allocation ; Rats

Objective To investigate the efficacy and safety of intravesical instillation with Sufuning (SFN) lotion for prevention of postoperative recurrence of bladder cancer. Methods A total of 240 bladder cancer patients who were diagnosed as bladder cancer and accepted trans-urethral resection of bladder tumor from January 2010 to June 2016 in Shanxi Provincial Cancer Hospital were randomly divided into the experimental group (120 cases) and the control group (120 cases) according to the envelope method. The patients in the experimental group were treated with SFN lotion for immediate intravesical instillation(250 mg for once), and the patients in the control group were treated with pirarubicin (THP) for immediate intravesical instillation (30 mg for once). The patients of two groups were treated with intravesical chemotherapy once a week for 8 times, and the chemotherapy was performed once a month for 1 year. The recurrence rate, progression-free survival (PFS) rate, overall survival (OS) rate and recent side effects were compared between the two groups. Results The patients were followed up for 6 to 60 months. The median follow-up time was 36.5 months.In the experimental group,6 patients were lost and 8 patients were lost in the control group.The experimental group, the total recurrence rate was 26.3 % (30/114). The control group, the overall recurrence rate was 25.0 % (28/112) (χ2= 0.142, P = 0.781). Five years of PFS rate in the experimental group and the control group was 73.7 % (84/114) and 75.0 % (84/112) respectively, and there was no significant difference between the two groups (χ2= 2.011, P= 0.615). Five years of OS rate in the experimental group and the control group was 95.6 % and 92.9 % respectively, and there was no significant difference between the two groups (χ 2= 1.611, P= 0.425). The major side effects included chemical cystitis and hematuria. The incidence of chemical cystitis and hematuria in the experimental group was significantly lower than that in the control group(χ2=5.991,P=0.018;χ2=4.925,P=0.036).There was a statistically significant difference of the hematological side effects (blood routine changes) between the two groups (χ 2= 4.891, P= 0.032). Conclusion It is safe and effective for intravesical instillation of SFN lotion to prevent the recurrence of bladder cancer.