ABSTRACT
Objective To prepare nephritis dripping pills and study its pharmacodynamic effects. Methods The nephritis dripping pills were self-made, and the preparation was optimized by using orthogonal method. The model of chronic renal failure was established through resection of 5/6 kidney, the effect of nephritis dripping pills on rats was investigated by urinary protein and renal pathology analysis. Results The optimal preparation for nephritis dripping pills was as follows:taking PEG4000:PEG6000 =2:1, drug:matrix =1:3, setting temperature at 80 ℃ and dropping distance as 7 cm. The pharmacodynamic results showed that:compared with the model control groups, the nephritis dropping pills and renal failure pills significantly reduced the 24 h urine protein levels (P<0. 01),and the nephritis dripping pills were significant superior to renal failure pills (P<0. 05). The histopathological results showed that the renal tubular of treated groups remitted to normal, renal interstitial presented a small amount of inflammation cell infiltration and renal interstitial fibrosis was suppressed. Conclusion The preparation of nephritis dripping pills is relatively stable,and have good therapeutic effects on chronic renal failure,but the optimal dose should be further verified.
ABSTRACT
Objective: To evaluate the bioavallability and bioequivalence of rabeprazole sodium enteric-coated pellets capsules. Methods:A randomized crossover design was performed in 32 healthy male volunteers. A single oral dose of 20 mg rabeprazole sodium enteric-coated pellets capsules ( test preparation) or enteric-coated shell capsules ( the reference capsules) was administrated under fed conditions. The wash period was 7 days. The blood samples were collected at different time points. The concentration of rabeprazole in plasma was determined by an LC-MS/MS method. The pharmacokinetic parameters were calculated by DAS 3. 0 software and the bio-equivalence was evaluated. Results:The maln pharmacokinetic parameters of the two formulations were shown as follows:T1/2 of (2. 20 ± 0. 83)h and(1. 951 ± 0. 515)h,Tmax of (3. 88 ± 1. 11)h and(4. 64 ± 1. 504)h,Cmax of (401. 06 ± 170. 75)ng·ml-1 and(394. 63 ± 215.64)ng·ml-1,AUC0→t of (918.42 ±427.39)ng·h·ml-1 and (994.49 ±520.73)ng·h·ml-1, and AUC0→∞ of(937.30 ± 445.13)ng·h·ml-1 and(1 011.69 ±534.77)ng·h·ml-1. The analysis showed that the maln pharmacokinetic parameters of the two formulations had no significant differences(P>0. 05) except for Tmax(P<0. 05). The relative bioavallability of rabeprazole sodium enteric-coated pellets capsules was (99. 80 ± 7. 20) %. Conclusion:Compared with the reference capsules, rabeprazole sodium enter-ic-coated pellets capsules show the property of higher dispersion degree, milder influence from food, more rapid release and absorption. The enteric-coated pellets capsules and the reference capsules are bioequivalence.
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Objective: To investigate the effects of different extracts of Smilax china L on the activity of ovarian cancer cells. Methods:Solvent extraction method was used to extract the active ingredients of Smilax china L. , and CCK-8 assay method was ap-plied to detect the influence of different Smilax china L. extracts (0, 50, 100, 150 and 200μg·ml-1 ) on the survival rate of ovarian cancer cells including low invasiveness A2780 cells and high invasiveness HO-8910PM cells. At the same time, the status of the two kinds of ovarian cancer cells at different time points (24, 48 and 72 h) was observed. Results:The IC50 of N-butanol extracts (SCR-B) on HO-8910 and A2780 ovarian cancer cells was 47. 5 μg· ml-1 and 69. 2 μg· ml-1 , respectively, and that of ethyl acetate ex-tracts (SCR-E) on A2780 and HO-8910 cells was 147. 9 μg· ml-1 and 166. 0 μg· ml-1, respectively. Smilax china L. extracts had the inhibition against both A278 and HO-8910PM ovarian cells in a dose-and time-dependent manner. Conclusion:The inhibitory activity of SCR-B against ovarian cancer cells is stronger than that of SCR-E, and SCR-B has stronger inhibition against A2780 cells than against HO-8910 cells. SCR-B has better inhibition against ovarian cancer cells.