Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin
The aim of this pharmacokinetic evaluation was to show the effect of the extra methyl group in simvastatin on esterase hydrolysis between lovastatin and simvastatin in male and female volunteers. This study was based on the plasma concentration-time curves and the pharmacokinetics of lovastatin and...
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| Format: | Article |
| Language: | English |
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Wiley
2003-01-01
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| Series: | The Scientific World Journal |
| Online Access: | http://dx.doi.org/10.1100/tsw.2003.121 |
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| author | Tom B. Vree Erik Dammers Ivan Ulc Stefan Horkovics-Kovats Miroslav Ryska IJsbrand Merkx |
| author_facet | Tom B. Vree Erik Dammers Ivan Ulc Stefan Horkovics-Kovats Miroslav Ryska IJsbrand Merkx |
| author_sort | Tom B. Vree |
| collection | DOAJ |
| description | The aim of this pharmacokinetic evaluation was to show the effect of the extra methyl group in simvastatin on esterase hydrolysis between lovastatin and simvastatin in male and female volunteers. This study was based on the plasma concentration-time curves and the pharmacokinetics of lovastatin and simvastatin with its respective active metabolite statin-β-hydroxy acid obtained from two different bioequivalence studies, each with 18 females and 18 males. Results were: 1-The group of female volunteers showed a higher yield of the active metabolite β-hydroxy acid than the group of males (p < 0.002) for both lovastatin and simvastatin. This difference was not related to the body weight of both groups. 2-In the male/female groups, subject-dependent yield of active metabolite β-hydroxy acid was demonstrated, which was independent of the formulation. The variation in plasma/liver hydrolysis resulted in a fan-shaped distribution of data points when the AUCt lovastatin was plotted vs. that of the β-hydroxy acid metabolite. In the fan of data points, subgroups could be distinguished, each showing a different regression line and with a different Y-intercept (AUCtβ-hydroxy acid). 3-Lovastatin hydrolysis was higher than simvastatin hydrolysis. 4-It was possible to discriminate between hydrolysis of both lovastatin and simvastatin by plasma/liver or tissue esterase activity. |
| format | Article |
| id | doaj-art-d92cef2117de40fa993808ffee6ab99d |
| institution | Kabale University |
| issn | 1537-744X |
| language | English |
| publishDate | 2003-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | The Scientific World Journal |
| spelling | doaj-art-d92cef2117de40fa993808ffee6ab99d2025-02-03T06:00:39ZengWileyThe Scientific World Journal1537-744X2003-01-0131332134310.1100/tsw.2003.121Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of SimvastatinTom B. Vree0Erik Dammers1Ivan Ulc2Stefan Horkovics-Kovats3Miroslav Ryska4IJsbrand Merkx5Institute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsInstitute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsInstitute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsInstitute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsInstitute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsInstitute for Anaesthesiology, University Medical Centre Nijmegen Sint Radboud, Nijmegen, The NetherlandsThe aim of this pharmacokinetic evaluation was to show the effect of the extra methyl group in simvastatin on esterase hydrolysis between lovastatin and simvastatin in male and female volunteers. This study was based on the plasma concentration-time curves and the pharmacokinetics of lovastatin and simvastatin with its respective active metabolite statin-β-hydroxy acid obtained from two different bioequivalence studies, each with 18 females and 18 males. Results were: 1-The group of female volunteers showed a higher yield of the active metabolite β-hydroxy acid than the group of males (p < 0.002) for both lovastatin and simvastatin. This difference was not related to the body weight of both groups. 2-In the male/female groups, subject-dependent yield of active metabolite β-hydroxy acid was demonstrated, which was independent of the formulation. The variation in plasma/liver hydrolysis resulted in a fan-shaped distribution of data points when the AUCt lovastatin was plotted vs. that of the β-hydroxy acid metabolite. In the fan of data points, subgroups could be distinguished, each showing a different regression line and with a different Y-intercept (AUCtβ-hydroxy acid). 3-Lovastatin hydrolysis was higher than simvastatin hydrolysis. 4-It was possible to discriminate between hydrolysis of both lovastatin and simvastatin by plasma/liver or tissue esterase activity.http://dx.doi.org/10.1100/tsw.2003.121 |
| spellingShingle | Tom B. Vree Erik Dammers Ivan Ulc Stefan Horkovics-Kovats Miroslav Ryska IJsbrand Merkx Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin The Scientific World Journal |
| title | Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin |
| title_full | Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin |
| title_fullStr | Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin |
| title_full_unstemmed | Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin |
| title_short | Differences Between Lovastatin and Simvastatin Hydrolysis in Healthy Male and Female Volunteers: Gut Hydrolysis of Lovastatin is Twice that of Simvastatin |
| title_sort | differences between lovastatin and simvastatin hydrolysis in healthy male and female volunteers gut hydrolysis of lovastatin is twice that of simvastatin |
| url | http://dx.doi.org/10.1100/tsw.2003.121 |
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