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1 China Pharmacist 014 Vol. 17 No. 8 1 吴媛媛靳桂民杜冠华吕扬 1 戴贵东 & 通过研究盐酸吡格列酮四种晶型在 SD 大鼠体内药动学和生物利用度, 评价其优势药用晶型, 为药物晶型物质状态对临床用药影响提供科学依据 SD 大鼠灌胃给予不同晶型盐酸吡格列酮固体原料药, 采用高效液相色谱法测定盐酸吡格列酮血药浓度, 非房室模型计算其大鼠体内药动学参数并在不同晶型之间进行比对大鼠经口给予盐酸吡格列酮四种晶型 ( 晶 Ⅰ Ⅱ Ⅲ 及 Ⅳ 型 ) 后, 血液中的 C max 分别为 ( ± ),( ± ),( ± 7. 84), ( ± ) mg L - 1 ; T max 分别为 ( ± ),( ± 3. 33),( ± ),( ±. 836) h; AUC ( 0-t) 分别为 ( ± 80. ),( ± ),( ± ),( ± ) mg h L - 1 经 one-way ANO- VA 统计学分析, 大鼠口服不同晶型盐酸吡格列酮后,C max 存在差异, 晶 Ⅲ 型 C max 与晶 Ⅱ 型和晶 Ⅳ 型相比具有明显优势 ( P < 0. 05), 其 AUC ( 0-t) 也明显优于晶 Ⅱ 型 ( P < 0. 05), 血药浓度维持时间更长, 其可能为优势药用晶型盐酸吡格列酮 ; 多晶型 ; 药动学 ; 高效液相色谱法 R A X Study on Pharmacokinetics of Four Crystal Forms of Pioditazone Hydrochloride in Rats Wu Yuanyuan 1 Ji Guimin Du Guanhua Lü Yang Dai Guidong 1 1. Ningxia Medical University Yinchuan China. Institute of Materia Medica Chinese Academy of Medical Sciences & Peking Union Medical College ABSTRACT Objective To study the pharmacokinetics of four crystal forms of pioditazone hydrochloride in rats. Methods Totally 36 rats were divided into 4 groups with oral administration of four different crystal forms of pioditazone hydrochloride. The plasma concentrations were determined by HPLC. The pharmacokinetic parameters were calculated. Results After a single oral dose the peak plasma concentration C max of pioditazone hydrochloride with crystal form Ⅰ Ⅱ Ⅲ and Ⅳ was ± ± ± and ± mg L - 1 the peak time t max was ± ± ± and ±. 836 h the area under curve AUC 0 - t was ± ± ± and ± mg h L - 1 respectively. Conclusion There are significant differences in blood concentration among the different crystal forms of pioditazone hydrochloride. Compared with that of the other crystal forms the plasma concentration of crystal form Ⅲ is higher with longer maintenance time. Crystal form Ⅲ of pioditazone hydrochloride is a promising choice for medicine. KEY WORDS Pioditazone hydrochloride Polymorphs Pharmacokinetics HPLC pioditazone hydrochloride ~ γ PPAR-γ β 3 14 ~ 01ZX ZX Tel dugh@ imm. ac. cn 153

2 www. zgys. org min r min min N 100 μl 3 min r min min 50 μl HPLC μl 1. 1 试药 1. 5 ml 0 μl Ⅰ Ⅱ Ⅲ Ⅳ. 1 专属性试验 % A. 5 h B 仪器 Agilent 100 Agilent Minispin Eppendorf Backman N-EVAP-TM 实验动物 SPF SD 0 ± 0 g SCXK ~ 1 d 1. 4 血药浓度测定方法 Agilent TC-C mm 4. 6 mm 5 μm mol L - 1 ph = v /v 1 ml min nm mg ml mg l mg ml mg L μl C HPLC A. B.. 5 h + C HPLC. 标准曲线 135 μl 15 μl mg L ml EP 400 μl

3 China Pharmacist 014 Vol. 17 No. 8 Areas /Areai C Y = X r = n = 5 1 x 珋 ± s 0. 5 ~ mg L 检测限与定量限 S /N = 3 S / N = 稳定性 mg L mg L SD 精密度 1 n = 5 n = 3 mg L - 1 mg L - 1 RSD % mg L - 1 RSD % ± ± ± ± ± ± μl 15 μl SD 135 μl mg L μl mg L μl μl / 1 h / 3 d 1 d 5 x 珋 ± s n =5 mg L - 1 mg L - 1 RSD % mg L - 1 RSD % mg L - 1 RSD % ± ± ± ± ± ± ± ± ± SD 135 μl 15 μl mg L μl x 珋 ± s n =5 / mg L - 1 RSD RSD mg L - 1 % mg L - 1 % ± ± ± ± SD ± ± μl 15 μl mg L % 0 μl d /. 7 盐酸吡格列酮不同晶型大鼠口服吸收实验 SD h 80 mg kg min 回收率试验 h SD 135 μl 400 μl EP 15 μl r min min mg L μl 主要药动学参数. 6. SD 135 μl DAS μl mg L μl Ⅲ Ⅰ Ⅱ 155

4 www. zgys. org 4 x 珋 ± s n =6 Ⅰ Ⅱ Ⅲ Ⅳ AUC 0-t mg h L ± ± ± ± AUC 0- mg h L ± ± ± ± R_AUC t/ % ± ± ± ± AUMC 0-t h h mg L ± ± ± ± AUMC 0- h h mg L ± ± ± ± MRT 0-t h ± ± ± ± MRT 0- h ± ± ± ± VRT 0-t h^ ± ± ± ± VRT 0- h^ ± ± ± ± C_last mg L ± ± ± ± t 1 /z h ± ± ± ± T max h ± ± ± ±. 836 Vz /F L kg ± ± ± ± CLz /F L h - 1 kg ± ± ± ± C max mg L ± ± ± ± N 6 ~ 8 3 x 珋 ± s n = 6 Ⅳ one-way ANOVA Ⅲ C max Ⅱ Ⅳ P < AUC 0-t Ⅱ P < Ⅳ 4 h 3 17 ~ 1 Gillies PS. Dunn CJ. Pioglitazone J. Drugs J. 中国药师, Spiegelman BM. PPAR adipogenic regulator and thiazolidinedione re-. Diabetes J. 中国药师, 国家药品标准 S. WS1- X Z USP S. 34th ed EP S. 7. 8th ed JP S. 16th ed Threlfall TL. Analysis of organic polymorphs J. Analyst ceptor J HPLC-MS /MS 11 N 10% Ⅲ 10. J. 天然产物研究与开发, J. 天津药学, Lu J Rohani S. Polymorphism and crystallization of active pharmaceutical ingredients APIs J. Curr Med Chem J. 中国药学杂志, 晶型药物 M. 009

5 China Pharmacist 014 Vol. 17 No. 8 IgG IgM 苏慧刘松涛张淼朱鸿哲苏云明研究仙蓟化斑胶囊抗变态反应的作用机制通过豚鼠血清中 IgG IgM 免疫复合物 ( IC) 及红细胞免疫复合物花结试验, 观察仙蓟化斑胶囊对免疫系统的影响仙蓟化斑胶囊能降低血清中 IgG IgM 含量其中高剂量组与模型对照组比较差异具有统计学意义 ( P < 0. 05) ; 能降低血清中 IC, 其中高中剂量组差异具统计学意义 ( P < 或 0. 05) ; 并能增加红细胞免疫复合物花结的形成, 其中高中剂量组差异均有统计学意义 ( P < 0. 01) 仙蓟化斑胶囊具有一定的抗变态反应作用仙蓟化斑胶囊 ; 过敏性紫癜 ; IgG; IgM R85. 5 A X Effect of Xianji Huaban Capsules on IgG and IgM in Serum of Guinea Pigs Su Hui Liu Songtao Zhang Miao Zhu Hongzhe Su Yunming Helongjiang University of Chinese Medicine Harbin China ABSTRACT Objective To study the mechanism of Xianji Huaban capsules for anti-allergy. Methods By detecting IgG IgM and immune complex IC in serum of guinea pigs and rosette test of erythrocyte immune complex the effect of Xianji Huaban capsules on the immune system was studied. Results Xianji Huaban capsules could reduce IgG and IgM in serum and the difference between the high dose group and the model control group was statistically significant P < The capsules also could reduce IC in serum and the difference between the high or medium dose group and the model control group was statistically significant P < or P < The capsules could enhance the rosette formation of red blood cell immune complex and the high and medium dose groups were with statistically significant difference P < Conclusion Xianji Huaban capsules have certain anti-allergy effect. KEY WORDS Xianji Huaban capsules Allergic purpura IgG IgM ~ 3 / ~ 3 /d mg / IgG IgM 1. 动物 IC 350 ~ 400 g SYXK [1] 1. 1 药物 1. 3 豚鼠模型建立及给药 8 ~ GC03C5 Tel suhui1979@ 16. com g / 1. 9 g mg / 櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊櫊 15. J. 中国新 J. 中国医院药学杂志, 药与临床杂志, J. J. 中国药学杂志, 四川理工学院学报 ( 自然科学版 ), J. 中国药理学通报, J. 中国临床药理学杂志, HPLC J. 中国药物化学杂志, J. 中国药师, J. 中国医药工业杂志, J. 天津药学, Tawashi R. Aspirin dissolution rates of two polymorphic forms J. 7. Science J. 西北药学杂志, Tawashi R. Gastrointestinal absorption of two polymorphic forms of aspirin J. J Pharm Pharmacol 国药学杂志, J. 中

2016 Jun % μl 5 min ESI mg / 120 μl 1. 5 ml 15 μl A min 500 μl B = 8 2

2016 Jun % μl 5 min ESI mg / 120 μl 1. 5 ml 15 μl A min 500 μl B = 8 2 646 CN 34-1206 /R ISSN 1009-2501 http / /www. cjcpt. com 2016 Jun 21 6 646-652 1 2 3 1 1 1 3 2 1 1 2 3 100050 pravastatin sodium 1S- 1α βs * δs * 2α SD 15 mg /kg6α8β R * 8aα -1 2 6 7 8 8a- -β δ 6- -2-