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Trospium containing compositionsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Effervescent Or Pressurized Fluid Containing, Organic Pressurized Fluid, Powder Or Dust ContainingTrospium containing compositions description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20070041912, Trospium containing compositions. Brief Patent Description - Full Patent Description - Patent Application Claims
RELATED APPLICATIONS [0001] This application is a continuation-in-part of U.S. application Ser. No. 10/392,333, filed Mar. 19, 2003, which claims the benefit of U.S. Provisional Application Nos. 60/366,479, 60/366,449, 60/354,354, 60/366,487 and 60/366,440, filed on Mar. 20, 2002. The entire teachings of the above application(s) are incorporated herein by reference. BACKGROUND OF THE INVENTION [0002] It is known from the prior art that .beta.-mimetics and anticholinergics can successfully be used as bronchospasmolytics for the treatment of obstructive respiratory ailments, such as, e.g., asthma. Substances with ..beta..-sympathomimetic effectiveness, such as, e.g., the active substance formoterol, also known from the prior art, can, however, be associated with undesirable side-effects when administered to humans. There remains a need for formulations and methods for administering combinations of beta-mimetics and anticholingerics in a formulation that provides long lasting broncoprotection in a patient while minimizing undesireable side effects. SUMMARY OF THE INVENTION [0003] The invention relates to a method for treating a disease characterized by a constrictive airway comprising administering to a patient in need thereof via inhalation a pharmaceutical composition comprising trospium (spiro [8 azaniabicyclo[3.2.1] octane-8,1'-pyrrolidinium], 3-4[hydroxydiphenylacetyl)oxy]-chloride (1.alpha., 3.beta., 5.alpha.)) wherein said patient achieves an effective therapy for at least 10 hours. The trospium composition is preferably a particulate formulation useful for administration via a dry powder inhaler. In a preferred embodiment, the composition further comprises a second active agent, such as a beta-2 agonist. A particularly preferred second active agent is formoterol, wherein the trospium, formoterol composition is manufactured by spray drying a mixture comprising trospium and formoterol. BRIEF DESCRIPTION OF THE DRAWINGS [0004] FIGS. 1a and 1b show the percent (%) baseline PenH over time following treatment at varying doses of aqueous Ipatropium bromide (IpBr) (FIG. 1a) and aqueous Trospium Chloride (TRCl) (FIG. 1b). [0005] FIG. 2 shows the percent (%) baseline PenH over time following treatment at equal nominal doses of aqueous IpBr or aqueous TrCl. [0006] FIG. 3 shows the percent (%) baseline PenH over time following treatment with aqueous TrCl or particle formulations TrCl at a nominal dose of 1 mcg for each formulation. DETAILED DESCRIPTION OF THE INVENTION [0007] The invention is based upon the discovery that trospium, when administered via inhalation results in surprisingly long acting formulation. Thus, a single daily administration, or twice daily administration, of trospium can be used to achieve and maintain relief of such diseases as chronic pulmonary disorder. [0008] Thus, in one embodiment, the invention relates to a method for treating a disease characterized by a constrictive airway comprising administering to a patient in need thereof via inhalation a pharmaceutical composition comprising trospium, wherein said patient achieves an effective therapy for at least about 10 hours, preferably at least about 15 hours, more preferably at least about 24 hours. [0009] Diseases that can be treated by the present invention include diseases indicated for trospium. For example, patients suffering from asthma, chronic obstructive pulmonary disease (COPD), restriction of the bronchial airways, or bladder diseases, such as urinary incontinence, can be treated by practicing the invention [0010] The invention further relates to pharmaceutical compositions for use in the present methods. The compositions comprise a therapeutically effective amount of trospium. A therapeutically effective amount includes an amount which, alone or in combination with one or more other active agents, can control, decrease, inhibit, ameliorate, prevent or otherwise affect one or more symptoms of the disease(s) or condition(s) to be treated. [0011] Typically, the dose of the active agent to be delivered is related to the efficiency of the inhalation device to deliver the active agent to the patient and the bioavailability of the active agent upon delivery. The preferred human dose of trospium is about 50 to 1200 micrograms per inhalation nominal dose delivered to lung, and even more preferably about 200-800 micrograms per inhalation nominal dose delivered to lung. [0012] The composition can be administered via a number of different pulmonary routes, which can impact the form of the composition. In one embodiment, the composition comprises an aqueous solution or suspension of trospium or a trospium salt, such as a hydrochloride. In another embodiment, the composition comprises a particulate formulation comprising trospium, such as a dry particulate formulation of trospium to be administered with a dry powder inhaler. In this context, a "dry powder" contains less than about 5% by weight of water, based on the total solids of the composition. [0013] The trospium formulations can, in one embodiment, comprises micronized trospium. However, it is preferred to administer formulations that comprise spray-dried trospium. Preferred formulations are described in, for example, U.S. Ser. No. 10/392,333, which is incorporated herein by reference. Such formulations have superior deposition properties. That is, preferred formulations are characterized by a tap density of less than 0.4 g/cm.sup.3, preferably less than 0.3 g/cm.sup.3, more preferably less than about 0.2 g/cm.sup.3, more preferably less than about 0.1 g/cm.sup.3, or even less than about 0.05 g/cm.sup.3. Further the formulation has a mass mean aerodynamic diameter of less than 5 microns. A preferred dry particulate formulation is characterized by a fine particle fraction of at least about 50%, wherein the fine particle fraction is defined as the mass of the composition that possesses an aerodynamic diameter of less than 3.4 microns as determined with an 8 Stage Anderson Cascade Impactor, used according to manufacturer's instructions. [0014] Preferred compositions further comprise an amino acid. Preferred amino acids are hydrophobic amino acids, such as leucine, isoleucine, alanine, valine and phenylalanine, for example. The preferred amino acid is leucine. The amino acid can advantageously be added in amount of at least about 10% by weight of the total composition. In one embodiment, the amino acid is at least about 40%, preferably at least about 50%, more preferably at least about 70% by weight of total composition. [0015] The compositions can further advantageously contain or comprise one or more phospholipids or combinations thereof. Suitable phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phosphatidylserines, phosphatidylinositols and combinations thereof. A particularly preferred phospholipid is dipalmitoylphosphatidylcholine (DPPC). The phospholipid can be advantageously added in an amount between about 1% and 90%, preferably between about 1 and 70%, more preferably between about 1% and 30%, such as between about 5 and 10% by weight of the total composition. The weight of the composition, as defined herein is, of course, non-inclusive of water and residula solvents or volatiles. [0016] The composition can comprise additional optional excipients, such as sugars, polysaccharides, lactose, salts, buffers, lipids, cholesterol, fatty acids, and combinations thereof. [0017] As described above, the formulation contains trospium. The formulation can consist of or consist essentially of trospium or a salt thereof. In another embodiment, the formulations can contain less than about 90%, 80%, 70%, 60%, 50%, 40%, 30% or 20% by weight trospium. In a preferred embodiment, the formulation contains less than about 10% by weight of trospium. In another preferred embodiment, the formulations contain about 1% to 25% by weight trospium and even more preferably about 4% to 16% by weight tropsium. [0018] A preferred composition consists essentially of a formulation having about 5% by weight trospium hydrochloride; between about 5 and 10% by weight of phospholipid and between about 85 and 90% by weight of leucine. [0019] In one embodiment, the method further comprises the administration of a second active agent. Preferred drugs for coadministration are described in more detail in U.S. Ser. No. 10/392,333 incorporated herein by reference. A preferred active agent is a beta-2 agonist, with formoterol and salneterol being preferred. Continue reading about Trospium containing compositions... Full patent description for Trospium containing compositions Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Trospium containing compositions 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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