Anticholinergic glycopyrrolate esters for the treatment of hyperhidrosis

A topical application, phenyl technology, applied in the direction of ointment delivery, organic active ingredients, cosmetic preparations, etc., can solve the problems of repeated injections

Pending Publication Date: 2019-02-22
BODOR LAB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The effect lasts for several months, but requires repeated injections and is usually not an appropriate option for pediatric patients

Method used

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  • Anticholinergic glycopyrrolate esters for the treatment of hyperhidrosis
  • Anticholinergic glycopyrrolate esters for the treatment of hyperhidrosis
  • Anticholinergic glycopyrrolate esters for the treatment of hyperhidrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Experiments can be performed to demonstrate that the activity of the compounds of the invention in the treatment of hyperhidrosis is unexpectedly comparable to that of equivalent doses of glycopyrronium bromide.

[0095] Comparative sweat reduction in the armpit area

[0096] A 4% solution of soft glycopyrronium bromide (eg ethyl or methyl ester) in 70% ethanol was prepared (Solution 1).

[0097] A 4% solution of glycopyrronium bromide in 70% ethanol was prepared (Solution 2).

[0098] On Day 1, baseline sweat production assessments were determined during 4 consecutive 5 minute (min) periods each under sweat stimulation conditions (92°F, 60% humidity). Average Sweat Production will calculate and take into account the Baseline-5 Minute Sweat Volume.

[0099] The reduction in sweat production can be quantified as follows:

[0100] 0.5 ml of solution 1 was applied to the axillary area on day 1 at bedtime. On Day 2, approximately 8 hours after application of Solution 1...

Embodiment 2

[0104] Preparation of compound (v), i.e. (2R,3'R)3-(2-cyclopentyl-2-phenyl-2-hydroxyacetoxy)-1-(methoxycarbonylmethyl base)-1-methylpyrrolidine bromide 5% solution and tested its efficacy in reducing sweating in human subjects.

[0105] Axillary sweat production was measured gravimetrically: filter paper was weighed and then placed in the armpit for 5 minutes, then re-weighed to determine the amount of sweat produced (weight) during this time. The weight difference (dry weight) from the final weight of the filter paper was determined as the sweat production during this period.

[0106] Four independent assessments were performed for 5 minutes each (to reduce variability) and the mean was assessed.

[0107] The baseline is the mean of a total of 8 assessments (measured over 2 days, 4 assessments per day) for each 5 minute period without treatment with a compound of the invention.

[0108] Four once-daily doses of 0.5 ml of 5% glycopyrrolate compound solution were administer...

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PUM

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Abstract

Use of a compound having the formula (I) in the preparation of a medicament composition comprising from about 1.0% to about 25% of said compound and a pharmaceutically acceptable vehicle, for topicaladministration to skin of an area of a mammalian subject suffering from hyperhidrosis, before bedtime, such that compared to untreated, baseline conditions, sweat production is reduced by at least about 25% for at least about six (6) hours.

Description

[0001] This application is a divisional application of an application with an application date of March 14, 2014, an application number of 2014800156770, and an invention title of "soft anticholinergic ester for the treatment of hyperhidrosis". Background technique [0002] Various anticholinergic compounds have been described before, none optimal. [0003] Muscarinic receptor antagonists are frequently used therapeutic agents by blocking their binding to neural effector sites on smooth muscle, cardiac muscle and gland cells as well as in peripheral ganglia and in the central nervous system (CNS) Muscarinic cholinergic receptors inhibit the effect of acetylcholine. However, their side effects (including dry mouth, photophobia, blurred vision, urinary hesitancy and retention, drowsiness, dizziness, restlessness, irritability, disorientation, hallucinations, tachycardia and arrhythmias, nausea, constipation, and severe allergic reaction) often limits its clinical use. Local ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/40A61P43/00
CPCA61K8/4913A61Q15/00A61K31/40A61K9/0014A61K47/10A61P17/00A61P25/02A61P43/00A61K8/49A61K9/00A61K31/4015A61K8/416A61K9/06A61K8/0216A61K31/14A61K31/205
Inventor N·S·博多尔D·安古洛
Owner BODOR LAB
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