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Pharmacokinetic Study of NADPH Oxidase Inhibitor Ewha-18278, a Pyrazole Derivative
- Title
- Pharmacokinetic Study of NADPH Oxidase Inhibitor Ewha-18278, a Pyrazole Derivative
- Authors
- Lee, Seul Gee; Lee, Jaeok; Kim, Kyung Min; Lee, Kee-In; Bae, Yun Soo; Lee, Hwa Jeong
- Ewha Authors
- 배윤수; 이화정; 이재옥
- SCOPUS Author ID
- 배윤수; 이화정; 이재옥
- Issue Date
- 2019
- Journal Title
- PHARMACEUTICS
- ISSN
- 1999-4923
- Citation
- PHARMACEUTICS vol. 11, no. 9
- Keywords
- pharmacokinetics; human applicable formulation; pyrazole derivative; NOX1; 2; 4 inhibitor; osteoporosis
- Publisher
- MDPI
- Indexed
- SCIE; SCOPUS
- Document Type
- Article
- Abstract
- In a previous study, the specific NOX1/2/4 inhibitor Ewha-18278 was confirmed as a possible treatment for osteoporosis both in vitro and in vivo. Here, we investigated the pharmacokinetics (PK) of the compound by intravenous (IV) and oral administrations to rats. Dimethyl sulfoxide (DMSO)-based and diazepam injection-based formulations were used to dissolve the compound. In the latter formulation applicable to humans, the changes in PK parameters were monitored at two different concentrations (1 mg/mL and 2 mg/mL). The area under the plasma concentration-time curve from zero time to infinity (AUC(inf)) of Ewha-18278 was highest in the DMSO-based formulation (2 mg/mL). Also, the concentration was increased 1.6-fold at the low concentration of the diazepam injection-based formulation compared to the high concentration. There was no statistical significance in the AUC(inf) of the compound between DMSO-based formulation (2 mg/mL) and diazepam injection-based formulation (1 mg/mL). These results suggest that Ewha-18278 can be delivered to humans by both IV and oral routes. In addition, the diazepam injection-based formulation of Ewha-18278 appears to be a suitable candidate for dosage development for future toxicity test and clinical trial.
- DOI
- 10.3390/pharmaceutics11090482
- Appears in Collections:
- 자연과학대학 > 생명과학전공 > Journal papers
- Files in This Item:
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