Ocular pharmacokinetics of methazolamide ophthalmic suspension in rabbit aqueous humor
文献类型：期刊论文
| 作者 | Liu Wen2; Gan Yong1 ; Gan Li1; Ping Qineng2; Cao Feng2; Xiao Yanyu2
|
| 刊名 | Journal of China Pharmaceutical University
 |
| 出版日期 | 2010 |
| 卷号 | 41期号:4页码:337-341 |
| 关键词 | methazolamide ophthalmic suspension ball milling microdialysis pharmacokinetics |
| ISSN号 | 1000-5048 |
| 其他题名 | 醋甲唑胺眼用混悬剂的家兔房水药动学 |
| 文献子类 | Article |
| 英文摘要 | Methazolamide (MTZ) is a carbonic anhydrase inhibitor widely used in oral administration in the treatment of glaucoma. Topical formulations of MTZ ophthalmic suspension were developed to avoid the systemic sideeffects. Micronized drug obtained by ball milling was suspended in the solutions of Carbopol 940 (Formulation 1) or Carbopol 974 (Formulation 2) of appropriate concentrations to develop uniform and stable MTZ ophthalmic suspension. The pharmacokinetic profiles of the ophthalmic suspensions in rabbit aqueous humor were investigated by the microdialysis technique using orally administered MTZ tablets as the control. It was shown in aqueous humor that the pharmacokinetic parameters (AUC,c_(max), and t_(max)) of Formulation 1 (with 0. 4% Carbopol 940) were estimated to be (109 838. 3 28 081. 26) ng· min/mL,(1 535. 60 125. 75) ng/mL, and (50 8. 66) min, respectively; those of Formulation 2 (with 0. 45% Carbopol 974) (116 803. 1 21 015. 71) ng · min/mL, (1 399. 78 136. 45) ng/mL, and (30 0. 00) min, respectively; those of MTZ tablets (59 197. 07 10 020. 72) ng· min/mL,(313. 96 6. 57) ng/mL, and (85 17. 32) min, respectively. In addition,AUCs of Formulation 1 and Formulation 2 were 1. 86 and 1. 97 times higher than that of the control group, respectively (P < 0. 05). These results indicate that the ophthalmic suspensions increased the bioavailability of MTZ in the eye aqueous humor, which is of significance in the development of topical dosage form of MTZ |
| 资助项目 | 国家"重大新药创制"科技重大专项资助项目[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:3976069 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/267942]  |
| 专题 | 药物制剂研究中心 |
| 作者单位 | 1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China. 2.Department of Pharmaceutics, China Pharmaceutical University, Nanjing, Jiangsu 210009, China.; |
| 推荐引用方式 GB/T 7714 | Liu Wen,Gan Yong,Gan Li,et al. Ocular pharmacokinetics of methazolamide ophthalmic suspension in rabbit aqueous humor[J]. Journal of China Pharmaceutical University,2010,41(4):337-341. |
| APA | Liu Wen,Gan Yong,Gan Li,Ping Qineng,Cao Feng,&Xiao Yanyu.(2010).Ocular pharmacokinetics of methazolamide ophthalmic suspension in rabbit aqueous humor.Journal of China Pharmaceutical University,41(4),337-341. |
| MLA | Liu Wen,et al."Ocular pharmacokinetics of methazolamide ophthalmic suspension in rabbit aqueous humor".Journal of China Pharmaceutical University 41.4(2010):337-341. |
入库方式： OAI收割
来源：上海药物研究所
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