盐酸吡格列酮四种晶型的大鼠体内药动学研究 |
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引用本文: | 吴媛媛,靳桂民,杜冠华,吕扬,戴贵东. 盐酸吡格列酮四种晶型的大鼠体内药动学研究[J]. 中国药师, 2014, 0(8): 1253-1257 |
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作者姓名: | 吴媛媛 靳桂民 杜冠华 吕扬 戴贵东 |
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作者单位: | 宁夏医科大学 银川 750001;;北京协和医学院&中国医学科学院药物研究所;北京协和医学院&中国医学科学院药物研究所;北京协和医学院&中国医学科学院药物研究所;宁夏医科大学 |
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基金项目: | 重大新药创制十二五规划项目 (编号:2012ZX09301002-001-013,2013ZX09102110);卫生部行业基金(编号:200902008) |
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摘 要: | 目的: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.方法: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.结果: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Cmax分别为(40.925±18.601),(21.909±7.169),(45.064±7.842),(21.767±7.439) mg·L-1;Tmax分别为(3.417±3.787),(4.417±3.323),(1.333±0.876),(7.417±2.836) h;AUC(0-i)分别为(290.828±80.22),(208.192±96.745),(355.433±74.683),(267.243±100.584) mg·h·L-1.结论: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,Cmax存在差异,晶Ⅲ型Cmax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.
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关 键 词: | 盐酸吡格列酮 多晶型 药动学 高效液相色谱法 |
收稿时间: | 2014-03-18 |
修稿时间: | 2014-05-18 |
Study on Pharmacokinetics of Four Crystal Forms of Pioditazone Hydrochloride in Rats |
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Affiliation: | Ningxia Medical University, Yinchuan 750001, China;;Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College;Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College;Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College;Ningxia Medical University, Yinchuan 750001, China; |
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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 con- centrations were determined by HPLC. The pharmaeokinetic parameters were calculated. Results: After a single oral dose, the peak plasma concentration (Cmax) of pioditazone hydrochloride with crystal form I , Ⅱ, Ⅲ and IV was (40.925 ± 18. 601 ), (21. 909 ± 7. 169), (45. 064 ±7. 842) and (21. 767 ±7.439) mg · L-1; the peak time (t max) was (3. 417 ±3. 787), (4. 417 ±3. 323), (1. 333 ± 0. 876) and ( 7.417 ± 2. 836) h ; the area under curve ( A UC(0-1) ) was ( 290.828 ± 80.22), ( 208.192 ± 96. 745 ), ( 355. 433 ± 74.683) and (267. 243 ± 100. 584)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 In of pioditazone hydrochloride is a promising choice for medi- clne |
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Keywords: | Pioditazone hydrochloride Polymorphs Pharmacokinetics HPLC |
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