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Pharmaceutical formulations of potassium ATP channel openers and uses thereof

a technology of potassium atp and pharmaceutical formulations, which is applied in the direction of drug compositions, biocides, metabolic disorders, etc., can solve the problems of reduced sodium excretion rate, range of adverse side effects, nausea, diarrhea, etc., and achieve the effect of easing the symptoms of nausea and vomiting

Inactive Publication Date: 2006-03-09
ESSENTIALIS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0089] As used herein, an erodable matrix is the core of a tablet formulation that, upon exposure to an aqueous environment, begins a process of disintegration which facilitates the release of drug from the matrix. The rate of release of drug from the tablet is controlled both by the solubility of the drug and the rate of disintegration of the matrix.
[0157] Leptin: Product (16 kD) of the ob (obesity) locus. It is found in plasma of mammals and exerts a hormonal action, which reduces food uptake and increases energy expenditure.

Problems solved by technology

Current oral formulations of diazoxide in therapeutic use result in a range of adverse side effects including dyspepsia, nausea, diarrhea, fluid retention, edema, reduced rates of excretion of sodium, chloride, and uric acid, hyperglycemia, vomiting, abdominal pain, ileus, tachycardia, palpitations, and headache (see current packaging insert for the Proglycem).
Oral treatment with diazoxide is used in individuals experiencing serious disease where failing to treat results in significant morbidity and mortality.
The adverse side effects profile of oral diazoxide limit the utility of the drug in treating obese patients at doses within the labeled range of 3 to 8 mg / kg per day.

Method used

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  • Pharmaceutical formulations of potassium ATP channel openers and uses thereof
  • Pharmaceutical formulations of potassium ATP channel openers and uses thereof
  • Pharmaceutical formulations of potassium ATP channel openers and uses thereof

Examples

Experimental program
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examples

A. Potassium ATP Channel Activator Containing Formulations:

[0399] 1. Compressed Tablet Formulations

[0400] Diazoxide or a derivative thereof at about 15-30% by weight is mixed with hydroxypropyl methylcellulose at about 55-80% by weight, ethylcellulose at about 3-10 wt / vol % and magnesium stearate (as lubricant) and talc (as glidant) each at less than 3% by weight. The mixture is used to produce a compressed tablet as described in Reddy et al., AAPS Pharm Sci Tech 4(4):1-9 (2003). The tablet may be coated with a thin film as discussed below for microparticles.

[0401] A tablet containing 100 mg of diazoxide or a derivative thereof will also contain approximately 400 mg of hydroxypropyl cellulose and 10 mg of ethylcellulose. A tablet containing 50 mg of diazoxide or a derivative thereof will also contain approximately 200 mg of hydroxypropyl cellulose and 5 mg of ethylcellulose. A tablet containing 25 mg of diazoxide or a derivative thereof will also contain approximately 100 mg of ...

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Abstract

Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering KATP channel openers with other drugs to treat diseases of humans and animals.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority to U.S. Ser. No. 60 / 604,085 filed Aug. 25, 2004, U.S. Ser. No. 60 / 654,571 filed Feb. 22, 2005, U.S. Ser. No. 60 / 668,912 filed Apr. 6, 2005, and U.S. Ser. No. 60 / 624,219 filed Nov. 3, 2004, each of which is incorporated herein in its entirety. Also incorporated herein by reference is PCT International application serial no. ______ (attorney docket no. 059599-0203) filed Aug. 25, 2005 and titled “Pharmaceutical formulations of potassium ATP channel Openers and uses thereof.”FIELD OF THE INVENTION[0002] The present invention relates to pharmaceutical formulations of potassium ATP (KATP) channel openers and their use for treatment of various diseases and conditions such as diabetes and obesity. BACKGROUND OF THE INVENTION [0003] The following description of the background of the invention is provided simply as an aid in understanding the invention and is not admitted to describe or constitute prior art to th...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/22A61K31/655
CPCA61K9/0004A61K9/2054A61K9/2853A61K31/549A61K9/5047A61K31/655A61K9/5026A61P1/00A61P3/00A61P3/04A61P3/06A61P3/10
Inventor COWEN, NEIL MADISONKASHKIN, KENNETH B.
Owner ESSENTIALIS INC
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