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Pde5 inhibitor powder formulations and methods relating thereto

a technology of pde5 inhibitor and powder formulation, which is applied in the field of powder formulations of pde5 inhibitors, can solve the problems of poor and variable bioavailability, increased incidence of heart and increased incidence of failure of right ventricle of hear

Inactive Publication Date: 2016-11-03
RESPIRA THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The patent is for a method of making a powder pharmaceutical that can be inhaled. The method involves using an inhaler with a dispersion chamber and an actuator that helps to spread the powder pharmaceutical out. This way, the pharmaceutical can be easily delivered to a person through the inhaler. The technical effect of this patent is to provide a more effective and precise way of delivering powder pharmaceuticals for inhalation.

Problems solved by technology

Pulmonary arterial hypertension, a disease characterized by sustained elevations of pulmonary artery pressure, which leads to an increased incidence of failure of the right ventricle of the heart, which in turn can result in the blood vessels in the lungs become overloaded with fluid.
However, oral administration of PDE5 inhibitors results in poor and variable bioavailability and also extensive metabolism in the liver.
If oral doses are increased beyond certain levels, the incidence of systemic side effects increase which prevents the acceptable use of these drugs.

Method used

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  • Pde5 inhibitor powder formulations and methods relating thereto
  • Pde5 inhibitor powder formulations and methods relating thereto
  • Pde5 inhibitor powder formulations and methods relating thereto

Examples

Experimental program
Comparison scheme
Effect test

example 1

Identification of Vardenafil Compounds

[0112]In view of the range of vardenafil forms, including salts and hydrates, as well as the limitation of conventional chemical identification methods, it is not straightforward to identify the form of vardenafil sold commercially or described in the art. For example, both anhydrous VarHCl (vardenafil hydrochloride) and Var(HCl)2 (vardenafil dihydrochloride) can stoichiometrically obtain 1-3 bound water molecules to form hydrates. Among them, crystalline VarHCl.3H2O is the thermodynamically stable form that has been used in commercial formulations. However, VarHCl and Var(HCl)2 can be difficult to differentiate from each other by each individual analytical method such as high performance liquid chromatography (HPLC), ultraviolet spectrophotometer (UV), mass spectroscopy (MS), Infra-red (IR), elemental analysis (CHN) and chloride ion analysis. For example, the molecular weight of Var(HCl)2.xH2O (579.55 g / mol) and VarHCl.3H2O (579.12 g / mol) are n...

example 2

Intrinsic Stability Assessment of Vardenafil Compounds

[0134]The intrinsic stability of vardenifil compounds can be assessed to aid in identification of suitable conditions for preparation of pharmaceutically acceptable formulations. Characterization of the degradation pathways for vardenafil compounds provides information useful to the development of pharmaceutically acceptable formulations for long term storage. Described below are exemplary experiments relating to characterization of VarHCl.3H2O.

[0135]Materials:

[0136]VarHCl.3H2O, HPLC grade water, 36.5% HCl, NaOH pellets, 6% H2O2 were all purchased. 1N HCl and 1N NaOH were prepared in house.

[0137]Method:

[0138]VarHCl.3H2O, HPLC grade water, 36.5% HCl, NaOH pellets, 6% H2O2 were all purchased, and 1N HCl and 1N NaOH were prepared in house. Intrinsic stability testing was performed according to International Conference on Harmonization (ICH) Guidance for Industry Q1A(R2) Stability Testing of New Drug Substances and Products (November...

example 3

Excipient Compatability Assessment of Vardenafil Compounds

[0149]Studies were performed to assess the chemical compatibility / stability of vardenafil compounds with excipients. The testing of vardenafil compounds with one or more pharmaceutically acceptable excipients / carriers is an aspect of developing a pharmaceutically-acceptable, stable, carrier-based vardenafil formulation. One of the most frequently used excipients for dry powder aerosol formulation is lactose. However, lactose is a reducing sugar. Vardenafil contains amine groups that could react with lactose via the Maillard reaction. In the absence of prior studies assessing the vardenafil and reducing sugar compatibility, the following experiments were performed to assess if lactose could be used to prepare a stable vardenafil blend formulation.

[0150]A. Materials and Methods

[0151]Var(HCl)2.xH2O and VarBase were purchased, and VarHCl.3H2O was prepared in house using Var(HCl)2.xH2O. Conversion of Var(HCl)2.xH2O to VarHCl.3H2O ...

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Abstract

Novel dry powder compositions comprising and methods relating thereto are provided. The dry powder compositions comprise PDE5 inhibitors, such as vardenafil, or pharmaceutically acceptable salts or esters thereof. The dry powder compositions may optionally include an carrier / excipient. The concentration of active agent may be at least about 2% by weight. Methods of aerosolizing the dry powder compositions and using them to treat various diseases are also disclosed.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application claims priority under 35 U.S.C. 119(e) to U.S. Provisional Application Nos. 61 / 913,734 and 61 / 913,744, both filed Dec. 9, 2013, and both of which are hereby incorporated by reference in their entireties herein.FIELD[0002]The invention relates to powder formulations of PDE5 inhibitors and methods relating thereto.BACKGROUND[0003]Phosphodiesterase type 5 inhibitors (PDE5 inhibitors) block the degradative action of cGMP-specific phosphodiesterase type 5 (PDE5) on cyclic GMP in the smooth muscle cells lining the blood vessels supplying the corpus cavernosum of the penis. These drugs, including vardenafil (Levitra™), sildenafil (Viagra™), and tadalafil (Cialis™), are administered orally for the treatment of erectile dysfunction and were the first effective oral treatment available for the condition.[0004]PDE5 inhibitors have also been studied for other clinical use as well, including cardiovascular and heart diseases. F...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/53A61K47/26A61M15/00A61K9/00
CPCA61K31/53A61K9/0075A61M2202/064A61M15/0008A61K47/26A61K31/166A61K31/4985A61K31/506A61K31/519Y02A50/30
Inventor XU, ZHENSMYTH, HUGHGIBBONS, AILEENSHREENIWAS, REVATISONI, PRAVINDEATON, DANHANNON, JAMESLERMER, STEPHENCURTIS, ROBERT
Owner RESPIRA THERAPEUTICS INC
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