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Compositions and methods for transdermal oxybutynin therapy

A chloride, topical application technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problem of patient interruption of treatment

Inactive Publication Date: 2005-12-14
WATSON LAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In some cases, these adverse feelings are even severe enough to cause patients to discontinue treatment

Method used

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  • Compositions and methods for transdermal oxybutynin therapy
  • Compositions and methods for transdermal oxybutynin therapy
  • Compositions and methods for transdermal oxybutynin therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0153] Embodiment 1: preparation oxybutynin sticky matrix patch

[0154] The parenteral oxybutynin delivery devices used in the above clinical studies were 13 and / or 39 cm 2 transdermal adhesive matrix patch. General methods for making transdermal adhesive matrix patches are described in US Patent Nos. 5,227,169 and 5,212,199, which are incorporated herein by reference in their entirety. According to this general method, the preparation of the oxybutynin patch of the present invention is as follows:

[0155] Oxybutynin free base, triacetin (Eastman Chemical Co., Kingsport, NY) and 87-2888 acryl copolymer binder (National Starch and Chemical Co., Bridgewater, NJ) were mixed into a homogeneous solvent , and using a two-zone coating / drying / lamination oven (Kraemer Koating, Lakewood, NJ) at 6 mg / cm 2 (dry weight) coating rates were coated onto a silicone-treated polyester spunbond substrate (Rexham Release, Chicago, IL) to obtain a final oxybutynin adhesive matrix containing ...

Embodiment 2

[0156] Example 2: Preparation of biodegradable microsphere storage injections of oxybutynin

[0157] According to the method of the present invention, biodegradable microspheres capable of sustained release depot injection can be used to deliver oxybutynin. Microspheres were prepared by the following method:

[0158] Poly-d,l-lactic acid ("PLA", Birmingham Polymers, Birmingham, Alabama) having a molecular weight of 12,000 was dissolved in methylene chloride to a final concentration of 20 wt%. Oxybutynin free base was dissolved in PLA solution to a final concentration of 4 wt%. Deionized water containing 0.1% Tween 80 was charged into a reaction vessel equipped with a water jacket (the temperature was controlled at 5° C.), and the reactor was equipped with a true boring stirrer and a Teflon turbine impeller (Teflon turbine impeller). ).

[0159] Add the oxybutynin / PLA / dichloromethane solution dropwise into the reaction vessel, and disperse the organic polymer phase into fi...

Embodiment 3

[0160] Example 3: Preparation of Topical Oxybutynin Formulations

[0161] According to the methods of the present invention, oxybutynin may be delivered using a topically applied oxybutynin-containing gel. General methods of preparing topical gels are well known in the art. According to this general approach, topical gels containing oxybutynin are prepared as follows:

[0162] Dilute 95% ethanol (USP) with water (USP, United States Pharmacopoeia), glycerin (USP) and glyceryl monooleate (Eastman Chemical, Kingsport NY) to obtain a percentage of ethanol / water / glycerin / glyceryl monooleate of 35 / Final solution on 59 / 5 / 1. Oxybutynin free base was then dissolved in the above solution to a concentration of 10 mg / g (mg / gram). The resulting solution was then gelled with 1% hydroxypropylcellulose (Aqualon, Wilmington, Delaware) to obtain the final oxybutynin gel. Apply 1-2g of the above gel topically to approximately 200cm of the chest, torso and / or arms 2 on the body surface ar...

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Abstract

The present invention provides compositions and methods for administering oxybutynin while minimizing the incidence and or severity of adverse drug experiences associated with oxybutynin therapy. In one aspect, these compositions and methods provide a lower plasma concentration of oxybutynin metabolites, such as N-desethyloxybutynin, which is presumed to be contributing at least in part to some of the adverse drug experiences, while maintaining sufficient oxybutynin plasma concentration to benefit a subject with oxybutynin therapy. The invention also provides isomers of oxybutynin and its metabolites that meet these characteristics of minimized incidence and / or severity of adverse drug experiences, and maintenance of beneficial and effective therapy for overactive bladder. In some aspects, the composition may be presented in the form of an unoccluded or free form topically administered gel.

Description

[0001] priority information [0002] This application claims priority based on U.S. Patent Application Serial No. 10 / 286,381, filed November 1, 2002, which was filed March 15, 2002, with Application Serial No. 10 / 098,752, which is a continuation-in-part of U.S. Patent Application Serial No. 09 / 559,711, filed April 26, 2000, which is incorporated herein by reference All of the above applications are incorporated herein. field of invention [0003] The present invention relates to compositions and methods for minimizing adverse drug sensations associated with oxybutynin therapy. Thus, the present invention covers the fields of pharmaceutical sciences, medicine and other health sciences. Background of the invention [0004] Oral oxybutynin therapy is commonly used to treat various forms of overactive bladder and urinary incontinence. In particular, oxybutynin is effective in treating bladder disorders of neuropathic origin. The reduction of these disorders is attributed to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/195A61F13/00A61KA61K9/00A61K9/06A61K9/10A61K9/16A61K9/70A61K31/216A61K47/10A61K47/14A61K47/38
CPCA61F2013/00646A61K9/0019A61K9/1647A61K31/216A61K9/0024A61K47/38A61K47/10A61K9/0014A61K47/14A61K9/7061A61P13/00A61P13/10A61P43/00Y02A50/30A61K2300/00A61F13/00
Inventor S·W·桑德斯C·D·艾伯特
Owner WATSON LAB INC
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