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Novel dosage formulationRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Preparations Characterized By Special Physical Form, Tablets, Lozenges, Or PillsNovel dosage formulation description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070071813, Novel dosage formulation. Brief Patent Description - Full Patent Description - Patent Application Claims
PRIORITY TO RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Application No. 60/719,793, filed Sep. 23, 2005, which is hereby incorporated by reference in its entirety. BACKGROUND OF THE INVENTION [0002] Many substances obtained from modem drug discovery are problematic because of insufficient bioavailability. Such molecules often exhibit very low aqueous solubility and limited solubility in oils. Furthermore many substances exhibit significant food effects, i.e., when drugs and certain foods are taken at the same time they can interact in ways that diminish the effectiveness of the ingested drug or reduce the absorption of food nutrients. Additionally, vitamin and herbal supplements taken with prescribed medication can result in adverse reactions. [0003] Some examples of how foods and drugs can interact include: [0004] Food can speed up or slow down the action of a medication. [0005] Impaired absorption of vitamins and minerals in the body. [0006] Stimulation or suppression of the appetite. [0007] Drugs may alter how nutrients are used in the body. [0008] NK-1 receptor antagonists of formula I have been described in commonly owned EP 1,035,115 and U.S. Pat. No. 6,297,375 wherein [0009] R is lower alkyl, lower alkoxy, halogen or trifluoromethyl [0010] R.sup.1 is halogen or hydrogen; and when p is 1, R.sup.1 may in addition to the above substituents be taken together with R to form --CH.dbd.CH--CH.dbd.CH--; [0011] R.sup.2 and R.sup.2' are each independently hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; and when n is 1, R.sup.2 and R.sup.2 may in addition to the above substituents form --CH.dbd.CH--CH.dbd.CH--, unsubstituted or substituted by one or two substituents selected from lower alkyl or lower alkoxy; [0012] R.sup.3 and R.sup.3' are hydrogen, lower alkyl or taken together with the attached carbon atom form a cycloalkyl group; [0013] R.sup.4 is hydrogen, --N(R.sup.5)(CH.sub.2).sub.nOH, --N(R.sup.5)S(O).sub.2-lower alkyl, --N(R.sup.5)S(O).sub.2-phenyl, --N.dbd.CH--N(R.sup.5).sub.2, --N(R.sup.5)C(O)R.sup.5, [0014] R.sup.5 is hydrogen, C.sub.3-6-cycloalkyl, benzyl, or lower alkyl; [0015] R.sup.6 is hydrogen, hydroxy, lower alkyl, --(CH.sub.2).sub.nCOO--(R.sup.5), --N(R.sup.5)CO-lower alkyl, hydroxy-lower alkyl, --(CH.sub.2).sub.nCN, --(CH.sub.2).sub.nO(CH.sub.2).sub.nOH, --CHO or a 5- or 6-membered heterocyclic ring containing from 1 to 4 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur, and with one of the carbon atoms in said ring being unsubstituted or substituted with an oxo group, which heterocyclic ring is directly bonded or bonded via an alkylene group to the remainder of the molecule; is a cyclic tertiary amine which may contain one additional heteroatom selected from the group consisting of oxygen, nitrogen, or sulfur, wherein any sulfur present in the ring is thio or can be oxidized to sulfoxide or sulfur dioxide by which said cyclic tertiary amine is directly attached to the remainder of the molecule or is attached through the linker --(CH.sub.2).sub.nN(R.sup.5)--; [0016] x is --C(O)N(R.sup.5)--, --(CH.sub.2).sub.mO--, --(CH.sub.2).sub.mN(R.sup.5)--, --N(R.sup.5)C(O)--, or --N(R.sup.5)(CH.sub.2).sub.m--; [0017] n, p, and q are each independently 1 to 4; and [0018] m is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. [0019] These compounds exist in crystalline form, which is practically insoluble in water (for example <0.0001 mg/ml) and in simulated gastric fluid (for example 0.08 mg/ml) at 25.degree. C. They are active NK1 receptor antagonists, useful for the treatment of CNS disorders, such as depression, anxiety and emesis. SUMMARY OF THE INVENTION [0020] The bioavailability of a drug depends on several parameters, such as on the physicochemical nature of the active compound, the dosage form, and other physiological factors. Compounds of formula I are virtually insoluble in water and simulated gastric fluid, inhibiting oral bioavailability. [0021] The present invention provides new galenic compositions for oral administration of pharmaceutically active compounds and a new process for preparing such galenic compositions. In particular, the compositions and process employ a hot melt extrusion of the active pharmaceutical ingredient and a poloxamer. The invention further provides hot melt extrudates of an active pharmaceutical ingredient and a poloxamer. [0022] The oral dosage forms of the invention are suitable for delivery to human patients and are designed to enable sufficient availability of the active compound at its site of action. Such formulations may overcome the disadvantage of practical insolublility in simulated intestinal fluid for these compounds. [0023] The process of the invention, provides, in particular, a process for preparing a pharmaceutical tablet composition, wherein the active pharmaceutical ingredient of formula I or pharmaceutically acceptable acid addition salts thereof and a water soluble poloxamer are processed by hot melt extrusion before mixing with the other ingredients. The tablet composition can thereafter be coated with a composition comprising an immediate release film coating system and purified water. DETAILED DESCRIPTION OF THE INVENTION [0024] The following definitions of general terms used herein apply irrespective of whether the terms in question appear alone or in combination. It must be noted that, as used in the specification and the appended claims, the singular forms "a", "an," and "the" include plural forms unless the context clearly dictates otherwise. [0025] The term "lower alkyl" denotes a straight- or branched-chain alkyl group containing from 1 to 7 carbon atoms. Nonlimiting examples of lower alkyl include methyl, ethyl, propyl, isopropyl, n-butyl, i-butyl, t-butyl, and the like. [0026] The term "alkylene group" means a lower alkyl linker which is bound to a group at either end. Nonlimiting examples of alkylene groups include methylene, ethylene, propylene, and the like. [0027] The term "lower alkoxy" denotes a alkyl group as defined above, which is attached through an oxygen atom. Nonlimiting examples of lower alkoxy groups include methoxy, ethoxy, propoxy, and the like. [0028] The term "cycloalkyl" denotes a saturated carbocyclic group (e.g. a nonaromatic ring) containing 3 to 6 carbon atoms. Nonlimiting examples of cycloalkyl groups include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the like. [0029] The term "halogen" denotes chlorine, iodine, fluorine, and bromine. [0030] "Processing aids" are excipients that improve the manufacturability of the formulation by improving, for instance, flowability and by avoiding sticking. Continue reading about Novel dosage formulation... Full patent description for Novel dosage formulation Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Novel dosage formulation 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. 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