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Morphine sulfate microgranules, method for preparing same and compositions containing sameRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or Pills, Sustained Or Differential Release Type, Discrete Particles In Supporting MatrixMorphine sulfate microgranules, method for preparing same and compositions containing same description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070003620, Morphine sulfate microgranules, method for preparing same and compositions containing same. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] The present invention concerns a novel sustained-release morphine sulphate formulation for oral administration. [0002] The present invention also applies to the process for manufacturing this formulation and to the pharmaceutical preparations containing it. [0003] In the present application, "morphine sulphate" is intended to mean the sulphate salt, optionally hydrated, of (5 alpha, 6 alpha)-7,8-didehydro-4,5-epoxy-17-methylmorphinane-3,6-diol. [0004] The oral administration of morphine sulphate is the best suited treatment for relieving chronic pain. Many oral formulations of morphine sulphate have been described in the prior art. [0005] EP 205 282 (EUROCELTIQUE) relates to granules comprising morphine sulphate, an aliphatic alcohol and a water-soluble hydroxyalkylcellulose. [0006] These granules are coated with a derivative of mucoadhesive cellulose, such as hydroxypropylmethyl-cellulose, and present a release profile over 12 hours, with a plasmatic peak situated between 1 and 3 hours. [0007] EP 377 518 (FAULDING) discloses sustained-release granules containing a very water-soluble active principle such as morphine. The granules make it possible to maintain plasmatic levels higher than 75% of the maximum for at least 3 hours. [0008] These granules comprise an active core coated with a polymeric layer which allows a slow release of the active principle at a very acid pH and a constant faster release of the active principle at a pH which is less acid to basic, over an extended period of time. [0009] This polymeric layer contains three compounds: a polymeric matrix which is insoluble whatever the pH, an enteric polymer, the solubility of which is pH-dependent, and a polymer which is soluble in acid medium. [0010] The preparations described in EP 377 518 have a bioavailability requiring an administration which should be at least twice daily. [0011] A subject of EP 553 392 (EUROCELTIQUE) is a process for preparing a stable sustained-release formulation consisting of granules obtained in a fluidized air bed by spraying an aqueous solution of active principle over neutral grains, followed by a coating with HPMC, by a coating with an acrylic polymer and by a protective film required for reducing the agglomeration of the granules. [0012] EP 636 366 (EUROCELTIQUE) discloses sustained-release morphine sulphate microgranules comprising a neutral core coated with an active layer consisting of an active principle/HPMC mixture, of a sustained-release layer consisting of Eudragit.RTM. RS D and/or of Eudragit.RTM. RL D, and of an HPMC film, which represents 5% of gain in mass. [0013] In documents EP 533 392 and EP 636 366, the granules undergo a heat treatment above the glass transition temperature of the polymeric coating, in order to stabilize its structure. This heat treatment is carried out at 45.degree. C. approximately for at least 24 hours, which considerably lengthens the duration of the process. [0014] EP 647 448 (EUROCELTIQUE) discloses morphine sulphate granules, the in vitro dissolution profile of which stretches over 24 hours. The granules consist of Neutral grains coated with active principle and with lactose. The active layer is covered with a film of Opadry.RTM., and then coated with Aquacoat ECD 30.RTM., Eudragit RS 30 D.RTM. or a Eudragit RS.RTM./Eudragit RL.RTM. mixture: 97.5/2.5. The titre of the granules described in this document is quite low, of the order of 15%. [0015] U.S. Pat. No. 5,445,829 (KV Pharmaceutical) relates to a formulation which is capable of releasing the active principle exclusively between 12 and 24 hours after the administration. [0016] This formulation contains 0 to 50% of immediate particles and the complement of controlled-release particles consisting of immediate particles coated with a cellulose derivative as delaying polymer. [0017] WO 94/22431 (KAPIPHARMACIA) discloses a controlled-release formulation of a morphine salt. [0018] This formulation can be administered in a single daily dosage intake. At 32 hours, the plasma concentration is higher than Cmax/2 and the fluctuations in the release profile are very small over this period, and so the plasmatic concentration is virtually constant over 24 hours. [0019] The formulation disclosed in WO 94/22431 consists, for example, of granules containing a core of morphine salt, of lactose and of a binder, coated with a film of HPMC/EC and of triethyl citrate. [0020] This formulation uses a mixture of two polymers, one being soluble and the other being insoluble in water. [0021] WO 95/31972 (EUROCELTIQUE) discloses sustained-release morphine sulphate granules consisting of a neutral core coated with active principle and with hydrated lactose, the bulk density of which is between 0.4 and 0.9 g/ml. The delayed-release layer coating the active principle contains for example an acrylic polymer, an alkylcellulose, a hydrogenated vegetable oil or a mixture thereof. [0022] This document teaches that the binding of the morphine sulphate to the neutral cores requires the addition of the lactose as a diluent. [0023] The release profiles of the microgranules given by way of example show that these granules are suitable for one dosage intake per day. [0024] WO 96/14059 (EUROCELTIQUE) discloses a process for extruding spherical particles containing morphine sulphate, a support the melting point of which is between 35 and 150.degree. C. and a sustained-release agent. Continue reading about Morphine sulfate microgranules, method for preparing same and compositions containing same... Full patent description for Morphine sulfate microgranules, method for preparing same and compositions containing same Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Morphine sulfate microgranules, method for preparing same and compositions containing same patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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