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Transdermal absorption preparation of oxybutynin as well as preparation method and medication application thereof

A technology of transdermal absorption preparation and transdermal absorption agent, which is applied in the field of pharmaceutical preparations, and can solve problems such as side effects restricting patients' continued use, restricting the wide application of drugs, and reducing bioavailability

Inactive Publication Date: 2011-05-11
陕西麦科奥特生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] When oxybutynin is administered with oral preparations, it will not only produce the first-pass effect, which will reduce the bioavailability, but also patients will often have gastrointestinal reactions, which limits the wide application of the drug, and sometimes severe side effects limit the patient's continued use. use

Method used

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  • Transdermal absorption preparation of oxybutynin as well as preparation method and medication application thereof
  • Transdermal absorption preparation of oxybutynin as well as preparation method and medication application thereof
  • Transdermal absorption preparation of oxybutynin as well as preparation method and medication application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Embodiment 1: oxybutyninide gel and its preparation

[0105] Formula: Oxybutynin 10g

[0106] Glycerin 5g

[0107] Ethanol 75ml

[0108] Hydroxyethylcellulose 1g

[0109] pure water balance;

[0110]Preparation: Make a turbid liquid from water, ethanol, and glycerin as a solvent; dissolve oxybutynin into the solvent at a concentration of 0.1% to 30%; add an appropriate amount of water to the gel matrix to completely dissolve or swell the matrix, and stir , to obtain a blank gel matrix, if necessary, add a pH regulator to adjust the pH to 5-7, add preservatives and antioxidants, add a stabilizer; add the oxybutynin solution or turbid solution obtained above to the blank gel In the gel matrix, make the final concentration reach 10%, and aliquot.

Embodiment 2

[0111] Embodiment 2: oxybutyninide gel and its preparation

[0112] Formula: Oxybutynin 10g

[0113] Glyceryl monooleate 1g

[0114] Glycerin 5g

[0115] Ethanol 35ml

[0116] Propylene glycol 1g

[0117] Hydroxyethylcellulose 1g

[0118] Add pure water to 100g

[0119] Preparation: Make a turbid liquid from water, ethanol, glycerin, and glycerol monooleate as a solvent; dissolve oxybutynin into the solvent at a concentration of 0.1% to 30%; add an appropriate amount of water to the gel base to make the base Completely dissolve or swell, stir to obtain a blank gel matrix, if necessary, add a pH regulator to adjust the pH to 5-7, add preservatives and antioxidants, add stabilizers; solution was added to the obtained blank gel matrix to make the final concentration reach 10%, and then packed in aliquots.

Embodiment 3

[0120] Embodiment 3. Oxybutynin gel and preparation thereof

[0121] Formula: Oxybutynin 10g

[0122] Carbomer 1g

[0123] Sodium hydroxide 1g

[0124] Propylene glycol 10g

[0125] Glycerin 5g

[0126] Ethanol 35ml

[0127] Add pure water to 100g

[0128] Preparation: Take carbomer and add 35ml of purified water to make it fully swell, stir evenly to obtain Shangxue Bomer solution, adjust the pH value of the solution to 6.0-7.0 with sodium hydroxide, and stir well to obtain a blank gel; Dissolve Bunin in ethanol, stir well, add propylene glycol and glycerin, stir evenly, then slowly add the liquid medicine into the school pom matrix, stir evenly while adding, and finally add purified water to 100g to obtain oxyxib Ning gel, packed in a bag, each 100g, ready to use.

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Abstract

The invention provides a transdermal absorption preparation containing oxybutynin, which comprises gels, ointment and cream and aims at reducing the adverse reaction rate of the oxybutynin and lightening the serious adverse reaction degree, wherein when the content of the oxybutynin in the transdermal absorption preparation is 0.1-30 percent by weight, the content of the oxybutynin in the transdermal absorption preparation is preferentially to be 8-12 percent by weight. The invention also discloses the requirements of the transdermal absorption preparation in the aspects of formula compatibility and proportioning, as well as a preparation method and medication application of the transdermal absorption preparation.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, and relates to a transdermal absorbent containing oxybutynin, a preparation method thereof and its application in medicine. Background technique: [0002] Oxybutynin (Oxybutynin, 4-(Diethylamino)but-2-yn-1-yl cyclohexyl(hydroxy)phenylacetate), chemical name: 4-(diethylamino)but-2-yn-1-ylcyclohexyl (Hydroxy)phenylacetate, formula C 22 h 31 NO 3 , molecular weight 357.49, CAS accession number 5633-20-5, the molecular structure is as follows: [0003] [0004] Oxybutynin can selectively act on the detrusor muscle of the bladder, reduce bladder pressure, increase volume, reduce involuntary bladder contraction, have strong antispasmodic and anticholinergic effects on smooth muscle, and also have analgesic effects. Relief of urgency, frequency and incontinence, etc. It is used for the relief of symptoms related to urination in patients with non-inhibitory and reflux neurogenic bladder...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/06A61K31/216A61K47/12A61K47/20A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P13/10A61K47/26
Inventor 郝心宇王梅王大璋
Owner 陕西麦科奥特生物科技有限公司
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