Treating smooth muscle hyperactivity with (R)-oxybutynin and (R)-desethyloxybutynin

An ethylamino, dysfunctional technology, applied in the direction of applications, organic chemistry, organic active ingredients, etc., can solve problems that are not chemically stable, etc.

Inactive Publication Date: 2003-11-05
WATSON PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

N-Oxybutynin is a therapeutically active compound bu

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Oral Unit Dosage Formulations

[0036] tablet:

[0037] Composition Per tablet 10,000 tablets per batch

[0038] R-OXY or R-DEO 5mg 50g

[0039] Microcrystalline Cellulose 30mg 300g

[0040] Lactose 70mg 700g

[0041] Calcium Stearate 2mg 20g

[0042] FD&C Blue #1Lake 0.03mg 300mg

[0043] Selected compounds of the present invention are mixed with lactose and cellulose until a homogeneous mixture is formed. Add the lake and mix further. Calcium stearate was finally blended in and the resulting blend was compressed into tablets using 9 / 32 inch (7 mm) dimple punches. Tablets of other strengths may be prepared by varying the ratio of active ingredient to excipients or to the final weight of the tablet.

[0044] The unexpected utility of the compounds of the present invention was confirmed by the following studies.

example 2

[0046] Pharmacological Research Materials and Methods 1. Acute Toxicity in Rats

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PUM

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Abstract

The optically pure R(-)-isomer of oxybutynin and the optically pure R(-)-isomer of desethyloxybutynin, substantially free of the corresponding S(+)-isomer, are Potent anticholinergic antispasmodics, effective in reducing symptoms associated with bladder smooth muscle hyperactivity, such as urinary incontinence, and gastrointestinal smooth muscle hyperactivity, such as irritable bowel syndrome. Disclosed is the use of optically pure oxybutynin and the R(-)-isomer of desethyloxybutynin for the treatment of cholinergic-mediated smooth muscle hyperactivity and the reduction of hyperactivity associated with administration of racemic oxybutynin or A method for racemizing side effects associated with ethyloxybutynin.

Description

technical field [0001] The present invention relates to the optically active R(-)-isomer of 4-diethylamino-2-butynylcyclohexylphenyl glycolate and its name R(-)-4-ethylamino-2-butan Optically active metabolite of alkynylcyclohexylphenylglycolate. The compound 4-diethylamino-2-butynylcyclohexylphenyl glycolate, whose common name is oxybutynin (OXY), is an approved drug for the treatment of urinary incontinence and the treatment of gastrointestinal smooth muscle function Hyperactivity is also effective. [0002] The oxybutynin (OXY) compound 4-ethylamino-2-butynylcyclohexylphenyl glycolate is known as desethyloxybutynin (DEO) and has the following chemical structure: [0003] Desethyloxybutynin (DEO) Background technique [0004] Racemic oxybutynin (OXY) is used therapeutically for the treatment of smooth muscle hyperactivity, such as urinary incontinence. OXY exerts its antispasmodic effect by inhibiting the ...

Claims

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Application Information

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IPC IPC(8): A61P1/00A61K31/21A61K31/216A61P13/12
CPCA61K31/216A61P1/00A61P1/06A61P11/00A61P13/00A61P13/02A61P13/12A61P31/14A61P37/08
Inventor A·K·G·阿伯格
Owner WATSON PHARMA INC
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