Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects
Compared to pelubiprofen, a cyclooxygenase-2-selective inhibitor, pelubiprofen tromethamine has been reported to exhibit improved solubility and absorption. Pelubiprofen tromethamine combines the anti-inflammatory effect of pelubiprofen with the gastric protective function of tromethamine salt, maki...
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MDPI AG
2023-04-01
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| Online Access: | https://www.mdpi.com/1999-4923/15/4/1280 |
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| author | Yu-Jeong Son Min-Kyu Park Hyeon-Jeong Park Ha-Yeon Kim Ye-Lim Jang Young-Sim Choi Jun-Gi Hwang Ji-Hyung Seo Yu-Kyong Kim |
| author_facet | Yu-Jeong Son Min-Kyu Park Hyeon-Jeong Park Ha-Yeon Kim Ye-Lim Jang Young-Sim Choi Jun-Gi Hwang Ji-Hyung Seo Yu-Kyong Kim |
| author_sort | Yu-Jeong Son |
| collection | DOAJ |
| description | Compared to pelubiprofen, a cyclooxygenase-2-selective inhibitor, pelubiprofen tromethamine has been reported to exhibit improved solubility and absorption. Pelubiprofen tromethamine combines the anti-inflammatory effect of pelubiprofen with the gastric protective function of tromethamine salt, making it a relatively safe class of non-steroidal anti-inflammatory drugs with low levels of gastrointestinal side effects in addition to its original analgesic, anti-inflammatory, and antipyretic effects. This study assessed the pharmacokinetic and pharmacodynamic characteristics of pelubiprofen and pelubiprofen tromethamine in healthy subjects. Two independent clinical trials were performed in healthy subjects using a randomized, open-label, oral, single-dose, two-sequence, four-period, crossover design. In Study I and Study II, subjects received 25 mg of pelubiprofen tromethamine and 30 mg of pelubiprofen tromethamine, respectively, with 30 mg of pelubiprofen being the reference. Study I fell within the bioequivalence study criteria. A trend of increased absorption and exposure for 30 mg of pelubiprofen tromethamine vs. the reference in Study II was observed. The maximum cyclooxygenase-2 inhibitory effect of 25 mg of pelubiprofen tromethamine was approximately 98% compared to the reference, showing no significant pharmacodynamic variation. It is thus predicted that 25 mg of pelubiprofen tromethamine would show no clinically significant discrepancies in clinical analgesic and antipyretic effects from 30 mg of pelubiprofen. |
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| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:37:18Z |
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| series | Pharmaceutics |
| spelling | doaj.art-6b96856c05304457af1d61fc1c220c0a2023-11-17T20:55:14ZengMDPI AGPharmaceutics1999-49232023-04-01154128010.3390/pharmaceutics15041280Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy SubjectsYu-Jeong Son0Min-Kyu Park1Hyeon-Jeong Park2Ha-Yeon Kim3Ye-Lim Jang4Young-Sim Choi5Jun-Gi Hwang6Ji-Hyung Seo7Yu-Kyong Kim8Pharmacology Major in Department of Medicine Graduate School, Chungbuk National University, Cheongju 28644, Republic of KoreaPharmacology Major in Department of Medicine Graduate School, Chungbuk National University, Cheongju 28644, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaDaewon Pharmaceutical Co., Ltd., Seoul 04808, Republic of KoreaDepartment of Clinical Pharmacology and Therapeutics, Chungbuk National University College of Medicine and Hospital, Cheongju 28644, Republic of KoreaCompared to pelubiprofen, a cyclooxygenase-2-selective inhibitor, pelubiprofen tromethamine has been reported to exhibit improved solubility and absorption. Pelubiprofen tromethamine combines the anti-inflammatory effect of pelubiprofen with the gastric protective function of tromethamine salt, making it a relatively safe class of non-steroidal anti-inflammatory drugs with low levels of gastrointestinal side effects in addition to its original analgesic, anti-inflammatory, and antipyretic effects. This study assessed the pharmacokinetic and pharmacodynamic characteristics of pelubiprofen and pelubiprofen tromethamine in healthy subjects. Two independent clinical trials were performed in healthy subjects using a randomized, open-label, oral, single-dose, two-sequence, four-period, crossover design. In Study I and Study II, subjects received 25 mg of pelubiprofen tromethamine and 30 mg of pelubiprofen tromethamine, respectively, with 30 mg of pelubiprofen being the reference. Study I fell within the bioequivalence study criteria. A trend of increased absorption and exposure for 30 mg of pelubiprofen tromethamine vs. the reference in Study II was observed. The maximum cyclooxygenase-2 inhibitory effect of 25 mg of pelubiprofen tromethamine was approximately 98% compared to the reference, showing no significant pharmacodynamic variation. It is thus predicted that 25 mg of pelubiprofen tromethamine would show no clinically significant discrepancies in clinical analgesic and antipyretic effects from 30 mg of pelubiprofen.https://www.mdpi.com/1999-4923/15/4/1280phase Icomparative pharmacokinetics/pharmacodynamicstromethamine saltCOX-2 inhibitory effect |
| spellingShingle | Yu-Jeong Son Min-Kyu Park Hyeon-Jeong Park Ha-Yeon Kim Ye-Lim Jang Young-Sim Choi Jun-Gi Hwang Ji-Hyung Seo Yu-Kyong Kim Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects Pharmaceutics phase I comparative pharmacokinetics/pharmacodynamics tromethamine salt COX-2 inhibitory effect |
| title | Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects |
| title_full | Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects |
| title_fullStr | Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects |
| title_full_unstemmed | Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects |
| title_short | Pharmacokinetic and Pharmacodynamic Characteristics of Pelubiprofen Tromethamine vs. Pelubiprofen in Healthy Subjects |
| title_sort | pharmacokinetic and pharmacodynamic characteristics of pelubiprofen tromethamine vs pelubiprofen in healthy subjects |
| topic | phase I comparative pharmacokinetics/pharmacodynamics tromethamine salt COX-2 inhibitory effect |
| url | https://www.mdpi.com/1999-4923/15/4/1280 |
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