| US 7,465,462 B1 | ||
| Multiparticulate controlled release selective serotonin reuptake inhibitor formulations | ||
| Theresa Ann Jeary, Roscommon (Ireland); Catherine Ann Morrissey, County Westmeath (Ireland); and Paul Stark, County Westmeath (Ireland) | ||
| Assigned to Elan Pharma International Limited, Monksland Athlone County Westmeath (Israel) | ||
| Appl. No. 9/744,169 PCT Filed May 10, 2000, PCT No. PCT/IE00/00060 § 371(c)(1), (2), (4) Date Apr. 19, 2001, PCT Pub. No. WO00/71099, PCT Pub. Date Nov. 30, 2000. |
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| Claims priority of application No. 990406 (IE), filed on May 20, 1999. | ||
| Int. Cl. A61K 9/14 (2006.01) | ||
| U.S. Cl. 424—489 [424/451; 424/457; 424/459; 424/464; 424/468; 424/490; 424/493; 424/494; 424/495] | 45 Claims |
| 1. A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration
comprising two quantities of particles, each of the particles comprising
(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following
oral administration, wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity
of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of
the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine
release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution
apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 15% of the total fluvoxamine is released after 0.5 of an hour of measurement in the apparatus;
(b) no more than about 25% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(c) between about 20% and 75% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(d) not less than about 75% of the total fluvoxamine is released after 4 hours of measurement in the apparatus; and
(e) not less than about 85% of the total fluvoxamine is released after 6 hours of measurement in the apparatus.
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