- Preparation method for pitavastatin calcium 5-oxo-impurity
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The invention belongs to the technical field of pharmaceutical synthesis, and particularly relates to a preparation method for a pitavastatin calcium 5-oxo-impurity. According to the preparation method for a pitavastatin calcium 5-oxo-impurity, pitavastat
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Paragraph 0010; 0029-0031; 0036-0044
(2018/11/03)
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- PHARMACEUTICAL PREPARATION HAVING EXCELLENT PHOTOSTABILITY
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The present invention relates to a pharmaceutical preparation of high photostability which contains pitavastatin, which is an HMG-CoA reductase inhibitor, a salt of pitavastatin, or an ester of pitavastatin. The pharmaceutical preparation contains a pitavastatin compound, titanium oxide, and a colorant having a maximum absorption wavelength of 400 nm to 500 nm.
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Page/Page column 7-9
(2008/12/06)
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- Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: Human UDP-glucuronosyltransferase enzymes involved in lactonization
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1. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes. Pitavastatin lactone, which can be converted back to the unchanged form, is the major metabolite of pitavastatin in humans. To clarify the mechanism of the lactonization of pitavastatin and the metabolic properties of the lactone, we performed experiments in vitro. 2. On addition of UDP-glucuronic acid, human hepatic microsomes produced pitavastatin lactone and an unknown metabolite (UM-2). UM-2 was converted to its unchanged form by enzymatic hydrolysis and to a lactone form non-enzymatically. Using several human UGT-expressing microsomes, UGT1A3 and UGT2B7 were principally responsible for glucuronidation of pitavastatin leading to lactonization. 3. No marked difference in intrinsic clearance between pitavastatin and its lactone form was detected in human hepatic microsomes. 4. Pitavastatin lactone showed no inhibitory effects on CYP2C9- and CYP3A4-mediated metabolism of model substrates in contrast to other HMG-CoA reductase inhibitors. 5. The mechanism of pitavastatin lactone formation has been clarified, in that glucuronidation by UGT occurs first followed by lactonization via an elimination reaction. It was also found that pitavastatin lactone demonstrates no drug - drug interactions.
- Fujino,Yamada,Shimada,Yoneda,Kojima
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