Detail of "145599-86-6"

Reference

Studies on the interaction between fibrates and statins using human hepatic microsomes

Studies on the interaction between fibrates and statins using human hepatic microsomes. Fujino, Hideki; Shimada, Syunsuke; Yamada, Iwao; Hirano, Masaru; Tsunenari, Yoshihiko; Kojima, Junji (Tokyo New Drug Research Laboratories I, Kowa Company Ltd., Tokyo, Japan). Arzneimittel-Forschung, 53(10), 701-707 (English) 2003 Editio Cantor Verlag. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) To gain a better understanding of the mechanism of drug-drug interaction between fibrates and statins, several in vitro expts. were performed. On coincubation with several fibrates, pitavastatin (CAS 147526-32-7) did not displace fibrates from their protein binding in human plasma. The presence of gemfibrozil (CAS 25812-30-0) inhibited the metab. of statins (cerivastatin (CAS 145599-86-6) and atorvastatin (CAS 134523-00-5)) remarkably. However, the increase of the unchanged form was fairly small for pitavastatin. The metabolic profile of gemfibrozil was also investigated. The cytochrome P (CYP) enzyme CYP2C9 plays a major role in the metab. of gemfibrozil. Gemfibrozil showed a high affinity for CYP enzymes and a relatively high metab. velocity. Moreover, several inhibitory effects of gemfibrozil on CYP-mediated metab. were detected - in contrast to other fibrates. Although the mechanism of the drug-drug interaction was not completely clarified, it is suggested that the increase of plasma concn. caused by the coadministration of gemfibrozil and statins is at least partially due to the inhibition of the CYP-mediated metab.

Preparation of complex forms of pharmaceuticals such as statins for improved bioavailability and solubility

All Rights Reserved. Preparation of complex forms of pharmaceuticals such as statins for improved bioavailability and solubility. Krishnan, Ramu (India ). PCT Int. 145599-86-6 and 474-62-4 are also occured in this study. Appl. WO 2007004236 A2 11 Jan 2007,44pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, KE, KG, KM, KN, KP, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-IN222 29 Jun 2006. PRIORITY: IN 2005-861 4 Jul 2005. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1, 27 The administration of pharmaceuticals of drugs which are having less soly., lower bioavailability, lower bioabsorbability, less rate of absorption has become a big challenge. Therefore an attempt has been made to prep. a complex modified form of the said pharmaceutical or drug such that the modified complex drugs or pharmaceuticals exhibits the enhanced properties of soly., bioavailability, bioabsorbability and rate of absorption despite the increased complexity of the mol. Surprisingly such modification was found to enhance retentivity of the active drug ingredient in the blood. Higher amts. of the active drug ingredient has shown lower toxicity. An oil sol. form of atorvastatin was prepd. starting with atorvastatin Ca, treatment with Na EDTA, then (S)-2.6-diaminohexanoic acid, and (Z)-9-octadecenoic acid chloride. .