Effect of extract method on pharmacokinetics of baicalin and berberine in dogs

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1 7. J Yu LBridgers APolli Jet al. Vitamin E-TPGS increases ab- 8. sorption flux of an HIV protease inhibitor by enhancing its solubility and permeability J. J Pharm J Sci Cornaire G. Woodley JHermann P et al. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo J. Int J Pharm Wandel CKim R BStein C Met al. " Inactive" excipients such as Cremophor can affect in vivo drug disposition J. Clin Pharmacol Ther Wang ZRavula RCao Met al. Transporter-mediated multidrug resistance and its modulation by Chinese medicines and other herbal products J. Curr Drug Discov Technol Vautier SFernandez C. ABCB1the role in Parkinson's disease and pharmacokinetics of antiparkinsonian drugs J. Expert Opin Drug Metab Toxicol Haber B AMohn K LDiamond R Het al. Induction patterns of 70 genes during nine days after hepaterctomy define the temporal course of liver regeneration J. J Clin Invest Caco-2 J T S 1 S 2 Baicalin Ba Berberine Be T S 1 S 2 C max ± ng /mlt Ba ± ng /mls 1 Ba ± ng /mlt Be ± ng /mls 2 Bet max ± hT Ba ± hS 1 Ba ± hT Be ± hS 2 Be AUC 0 ~ ± ng /h ml T Ba ± 77. 3ng /h ml S 1 Ba ± ng /h ml T Be ± 8. 36ng /h ml S 2 Be R A Effect of extract method on pharmacokinetics of baicalin and berberine in dogs WANG Li 1 2 ZHAO Ying 1 1. Heilongjiang University of Traditional Chinese MedicineHarbin China2. School of Pharmacy Harbin University of Commerce Harbin China ABSTRACTAIM To investigate the effect of extract method on pharmacokinetics in dogs of baicalin Ba berberinebeby determining Ba and Be concentration of serum after administration of traditional Chinese medicine Gegen Qinlian Decoction T Scutellaria baicalensis Georgi DecoctionS 1 and Coptis chinensis Franch. DecoctionS 2. METHODS HPLC method was established to determine serum concentration of Ba Be and pharmacokinetic parameters were calculated. RESULTS The parameters in dogs after administration of T S 1 S 2. were as followsc max was ± ng /mlt Ba ± ng /mls 1 Ba ± ng /mlt Be ± LBH-Z08003 D Tel kurb@ sohu. com

2 0. 653ng /mls 2 Bet max ± hT Ba ± hS 1 Ba ± hT Be ± hS 2 Be AUC 0 ~ ± ng /h ml T Ba ± 77. 3ng /h ml S 1 Ba ± ng /h ml T Be ± 8. 36ng /h mlrespectively. CONCLUSION Extract method has significant effect on pharmacokinetic parameters of Ba and Be in dogs. KEY WORDSGegen Qinlian Decoctionbaicalinberberinedogs pharmacokinetics Ultimate TM C mm 4. 6 mm 5 μm ml /min 20μL % NaH 2 PO 4 7 ph V /V 280 nm - NaH 2 PO 4 ph V /V 346 nm Dionex P680 TCC-100 Chromeleon ASI-100 UVD-340U -25 XKG6-A 2. 3 TGL-16G 1. 5 ml μl A r /min 10 min 20 A0151 μl min min 6. 8 min T min 15 g 9 g 6 g ml 30 min2 200 ml 9 g 20 min ml S 1 S 2 45 g 60% 10 ml 30 min mg /ml ml 200 ml ± 2. 1kg 2 12 h T S 1 S ml 195 g h 5 ml 20 μl 2 min 5 ml 5 min r /min 10 min 4 ml mg mg /ml mg /ml μg /ml 100μL7 1327

3 1 2 1 Tab. 1 n = 5 Precision and method recovery of HPLC method to determine Ba in dog s serum n = 5 /% RSD /% /μg /ml Fig. 1 HPLC HPLC chromatograms of Ba Be in serum A. B C D. S 1 1. E. S 2 1. F. T A. blank serum B. blank serum spiked with Ba and internal standard 1. Ba 2. Metronidazole C. blank serum spiked with Be and internal standard 1. Be 2. Lacidipine D. serum sample after administration of decoction S 1 to dogs 1. Ba E. serum sample after administration of decoction S 2 to dogs 1. Be F. serum sample after administration of decoction T to dogs 1. Ba 2. Be 10μL μg /ml μl 1. 0μg /ml μg /ml 2. 3 min h-20 15d 3 20μg /ml RE% 12% μg /ml T S 1 S 2 Ar /Ai C W = 1 /C 2 13 Ar / Ai = C r = Ar /Ai = C r = ~ 20 μg /ml ~ Tab. 2 n = 5 Precision and method recovery of HPLC method to determine Be in dog s serum n = 5 /% RSD /% /μg /ml % ~ 105% RSD < 10% μl 3 μg /ml 2 T S Fig. 2 Mean serum concentration-time curve of Ba after μg /ml administration of decoction T and S 1 to dogs μg /ml 5 3 d 2. 6 RSD TS 1 S 2 DAS

4 Fig. 3 3 Mean serum concentration-time curve of Be after administration of decoction T and S 2 to dogs C max t max λ Z - t 1 /2 - AUC 0 ~ t AUC 0 ~ = AUC 0 ~ t + C t /λ Z SPSS Tab. 3 4 Tab. 4 n = 6 x ± s Parameters of Ba in dogs after administration of decoction T and S 1 n = 6 x ± s λ Z h ± ± C max ng ml ± ± t max h ± ± t 1 /2 h ± ± * MRT 0-36 h ± ± MAT 0-36 h ± ± AUC 0-36 ng h ml ± ± * AUC 0- ng h ml ± ± * * T P < n = 6 x ± s Parameters of Be in dogs after administration of decoction T and S 2 n = 6 x ± s J λ Z h ± ± C max ng ml ± ± * 6. 7 t max h ± ± * J t 1 /2 h ± ± MRT 0-36 h ± ± MAT 0-36 h ± ± * J AUC 0-36 ng h ml ± ± * 8. AUC 0- ng h ml ± ± * J * T P < S 1 T S 2 T S 1 T AUC T S 2 AUC 7 C max 5. 3 T S 2-1. J J J J J RP-HPLC J J

5 J J * Franz 28 h mg % mg % Franz R A Study on eugenol and cinnamaldehyde's permeative properties of Erxiekang Emplastra in vitro YIN Xing-bin 1 NI Jian 1* SHEN Xiao-chun 2 1. Beijing University of Chinese MedicineBeijing China2. Patent Examination Cooperation Center of SIPOBeijing China KEY WORDSErxiekang EmplastraeugenolcinnamaldehydeFranz diffusion cell TK-6A YP SD 180 ~ 200 g SCXK GC Franz ml 1 ml mg 1 Agilent ml Tel yxbtcm@ 163. com * njtcm@ 263. net 1330

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