Transdermal preparation containing silodosin, preparation method and medicinal application thereof

A technology of sirodosin and transdermal enhancer, which is applied in the field of pharmaceutical preparations and can solve problems such as reduced bioavailability

Active Publication Date: 2013-01-30
SHAANXI MICOT TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] When silodosin is administered in an oral formulation, not only will it produce a first-pass effect, which will reduce the bioavailability, but patients will often have insomnia, increased PSA, sinusitis, abdominal pain, weakness, rhinorrhea, fainting, skin toxicity Outbreak, purpura, jaundice, transaminase and other side effects, sometimes serious side effects limit the patient's continued use

Method used

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  • Transdermal preparation containing silodosin, preparation method and medicinal application thereof
  • Transdermal preparation containing silodosin, preparation method and medicinal application thereof
  • Transdermal preparation containing silodosin, preparation method and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Embodiment 1: Sirodoxin gel and its preparation

[0106] Formula: Sirodosin 10g

[0107] Glycerin 5g

[0108] Ethanol 75ml

[0109] Hydroxyethylcellulose 1g

[0110] pure water balance;

[0111]Preparation: make turbid liquid from water, ethanol, and glycerin as a solvent; dissolve sirodosin 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 silodosin solution or turbid solution obtained above to the blank gel matrix obtained In the gel matrix, make the final concentration reach 10%, and aliquot.

Embodiment 2

[0112] Embodiment 2: Sirodoxin gel and its preparation

[0113] Formula: Sirodosin 10g

[0114] Glyceryl monooleate 1g

[0115] Glycerin 5g

[0116] Ethanol 35ml

[0117] Propylene glycol 1g

[0118] Hydroxyethylcellulose 1g

[0119] Add pure water to 100g

[0120] Preparation: make a turbid liquid from water, ethanol, glycerin, and glycerol monooleate as a solvent; dissolve silodosin into the solvent at a concentration of 0.1% to 30%; add an appropriate amount of water to the gel matrix to make the matrix 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; the silodosin solution obtained above or turbid solution was added to the obtained blank gel matrix to make the final concentration reach 10%, and then packed in aliquots.

Embodiment 3

[0121] Embodiment 3. Silodosin gel and preparation thereof

[0122] Formula: Sirodosin 10g

[0123] Carbomer 1g

[0124] Sodium hydroxide 1g

[0125] Propylene glycol 10g

[0126] Glycerin 5g

[0127] Ethanol 35ml

[0128] Add pure water to 100g

[0129] 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 Duoxin 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 get Xiluoduo Xin gel, packed in bags, each 100g, ready to use.

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PUM

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Abstract

The invention relates to transdermal preparation containing silodosin, which comprises gels, ointments and creams to reduce bad reaction rate of silodosin and reduce seriously bad reaction degree. When the content of the silodosin by mass percentage in the transdermal preparation is 1-35, the content of the silodosin by mass percentage in the transdermal preparation is 9-11 preferably. The utility model discloses requirements of the transdermal preparation in aspects of formula compatibility and proportioning and a preparation method and medicinal application of the transdermal preparation.

Description

Technical field: [0001] The invention relates to the field of pharmaceutical preparations, in particular to a transdermal absorption agent containing sirodosin, a preparation method thereof and its application in medicine. Background technique: [0002] Silodosin (Silodosin), chemical name: 1-(3-hydroxypropyl)-5[(2R)-2-({2-[2-(2,2,2-difluoroether)phenoxy ]Ethyl}amino)propanyl]-2,3-dihydroxy-1H-indolyl-7-carbamoyl, molecular formula C 25 h 32 f 3 N 3 o 4 , molecular weight 582.65, CAS accession number 160970-54-7, molecular structural formula: [0003] Silodosin can selectively antagonize α1-adrenergic receptors, and can significantly inhibit the contraction of the human prostate caused by norepinephrine; it has a dose-dependent inhibitory effect on the hyperactivity of the bladder in the benign prostatic hypertrophy model, and can improve bladder function. Systolic pressure threshold for voiding dysfunction associated with benign prostatic hyperplasia. After 0.5-6 hou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/06A61K31/4045A61K47/12A61K47/20A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P13/10A61K47/10
Inventor 郝心宇王梅王大璋
Owner SHAANXI MICOT TECH LTD
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