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Trospium containing compositions

a composition and trospium technology, applied in the direction of drug compositions, biocides, dispersed delivery, etc., can solve the problems of undesirable side effects when administered to humans, and achieve the effect of effective therapy

Inactive Publication Date: 2007-02-22
ALKERMES INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[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 (1α, 3β, 5α)) wherein said patient achieves an effective therapy for at least 10 hours.

Problems solved by technology

Substances with .β.-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.

Method used

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  • Trospium containing compositions
  • Trospium containing compositions

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Trospium Chloride (TrCl) Particle Formulations

[0032] Particle formulations, as listed in Table 1, where prepared by spray drying. Pre-spray drying solutions were prepared as follows. Particle components were dissolved in appropriate solvents to assure solubility. Table 2 lists the mass of each particle component dissolved in each respective solvent. Leucine was dissolved in 300 mL of water. TrCl was subsequently dissolved in the aqueous solution. DPPC and / or DSPC were dissolved in 700 mL of ethanol, to form an organic phase. Both solutions were then heated separately to 50° C.

[0033] Phospholipids (dipalmitoyl phosphatidylcholine (DPPC) and distearoyl phosphatidylcholine (DSPC)) were obtained from Avanti Polar Lipids, Inc. (Alabaster, Ala.). TrCl was obtained from Boeringer Ingelheim and leucine was obtained from Spectrum Quality Products, Inc. (Gardena, Calif.).

[0034] The aqueous phase was then static mixed with the organic phase and then spray dried to produce dr...

example 2

[0036] The Fine Particle Fraction (FPF), volumetric median geometric diameter, and actual trospium content of the particles produced in Example 1 were determined.

[0037] The content of trospium chloride in the AIR-Trospium formulations was determined via HPLC using a Waters HPLC system equipped with a PDA detector as shown in Table 3. AIR-Trospium formulations were targeted to have a content of 5% trospium chloride.

TABLE 3AIR-Trospium content analysis parameters.ColumnAlltech Alltima C18 (250-4.6 mm)Dissolving Solvent90% MeOH, 10% 0.01 N HClDetection Wavelength265 nmInjection Volume10 uLFlow Rate1 mL / minMobile Phase60 / 40 (0.05% TFA in Water / 0.05% TFA in ACN)Run Time10 min.Relative Retention Time6.0 min.

[0038] The volumetric median geometric diameter (VMGD) of the particles was measured using a RODOS dry powder disperser (Sympatec, Princeton, N.J.) in conjunction with a HELOS laser diffractometer (Sympatec). Powder was introduced into the RODOS inlet and aerosolized by shear forces...

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Abstract

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 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.

Description

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 .β.-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 broncoprotectio...

Claims

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Application Information

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IPC IPC(8): A61K31/4747A61L9/04A61K9/00A61K9/16A61K31/167A61K31/40A61K31/439A61K31/46
CPCA61K9/0078A61K9/1617A61K31/40A61K9/0075A61K31/46A61K45/06A61K31/438A61P11/00A61P11/06
Inventor EHRICH, ELLIOTDEAVER, DANIELCLARKE, ROBERTLIPP, MICHAEL M.
Owner ALKERMES INC