Composition of dexibuprofen transdermal hydrogel

A technology of dexbuprofen and hydrogel, applied in the field of topical pharmaceutical compositions, can solve problems such as poor solubility of ibuprofen

Inactive Publication Date: 2012-09-12
SHASUN CHEM & DRUGS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

All the different forms of ibuprofen are poorly soluble in water

Method used

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  • Composition of dexibuprofen transdermal hydrogel
  • Composition of dexibuprofen transdermal hydrogel

Examples

Experimental program
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preparation example Construction

[0015] The invention relates to a locally used pharmaceutical composition containing dexibuprofen, more specifically to a non-alcoholic transdermal hydrogel of dexibuprofen and a preparation method thereof.

[0016] Topical NSAID preparations are commonly used to treat pain and inflammation associated with joints and muscles. The three main advantages of topical NSAIDs over oral treatments for pain and inflammation associated with joints and muscles are:

[0017] i) Higher concentration of NSAID delivered to the desired site;

[0018] ii) Only 1-3% of NSAIDs are absorbed systemically, reducing the likelihood of gastrointestinal upset or ulcers; and

[0019] iii) Low blood levels reduce the incidence of drug interactions.

[0020] A topical formulation of ibuprofen can be used to treat pain and inflammation associated with joints and muscles. Ibuprofen (2-(4-isobutylphenyl)propanoic acid) has one chiral center and therefore exists as two enantiomers, S(+)-ibuprofen (dexibupr...

example 1

[0050] The manufacturing procedure of example 1:

[0051] 1. Disperse Carbopol 971P in pure water with stirring for 15 minutes and allow to soak overnight.

[0052] 2. Dissolve sodium metabisulfite and sodium benzoate in pure water, and then disperse Dexibuprofen in it.

[0053] 3. Dissolve menthol in triethanolamine.

[0054] 4. With constant stirring, add step 3 to step 2 to obtain a clear solution.

[0055] 5. Mix propylene glycol with PEG 400, add this mixture to diethylene glycol monoethyl ether, then add lavender oil and mix well.

[0056] 6. Add step 5 to step 4 and mix well.

[0057] 7. Finally, with constant stirring, add step 6 to step 1 to obtain a homogeneous gel.

[0058] Example-2 (Table-2) Dexibuprofen non-alcoholic transdermal hydrogel prepared by using HPMC as gelling polymer:

[0059] Numbering

example 2

[0060] The manufacturing procedure of example 2:

[0061] 1. Under stirring, disperse HPMC K4M, HPMC E5, Lutrol F68 in pure water for 15 minutes, and let it soak overnight.

[0062] 2. Add simethicone to step 1 and mix well.

[0063] 3. Dissolve sodium metabisulfite and sodium benzoate in water, and then disperse Dexibuprofen in it.

[0064] 4. Dissolve menthol in triethanolamine.

[0065] 5. With constant stirring, add step 4 to step 3 to get a clear solution.

[0066] 6. Mix Propylene Glycol, PEG 400 and add this mixture to Diethylene Glycol Monoethyl Ether followed by Lavender Oil and mix well.

[0067] 7. Add step 6 to step 5.

[0068] 8. With constant stirring, add step 7 to step 2 to obtain a homogeneous gel.

[0069] Example-3 (Table-3) Dexibuprofen non-alcoholic transdermal hydrogel prepared by using Carbopol as gelling polymer:

[0070] Numbering

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Abstract

Stable non-alcoholic transdermal hydrogel of dexibuprofen was prepared by using a simple manufacturing process, and the experimental trials showed that the pH modifying agent, antioxidant and water miscible solvent are the essential excipients to obtain stable non-alcoholic transdermal hydrogel of dexibuprofen. The dexibuprofen hydrogel prepared using carbopol as a gelling polymer produced an opaque gel, whereas hydrogel prepared using hyroxypropyl methylcellulose (HPMC) as a gelling polymer produced a transparent gel. There was no significant changes observed with respect to physical description, pH, assay and particularly to the related substance values when the hydrogels were subjected to the stability study at accelerated condition (40 DEG C / 75% RH) for 3 months in laminated tubes.

Description

technical field [0001] The present invention relates to a topical pharmaceutical composition containing dexibuprofen [(S)-2-(4-isobutylphenyl)propionic acid] and a preparation method thereof. Background technique [0002] Ibuprofen (2-(4-isobutylphenyl)propanoic acid) has one chiral center and therefore exists as two enantiomers, S(+)-ibuprofen (dexibuprofen) and R(-)-Ibuprofen, also known as (S+)-Ibuprofen and (R-)-Ibuprofen. The racemic form consisting of equal amounts of S(+)-ibuprofen and R(-)-ibuprofen is exclusively used in currently available commercial formulations, and the water-soluble salts of ibuprofen are also used in these commercial formulations , such as lysinate (lysinate), arginate (arginate), sodium salt, potassium salt, etc. Racemic ibuprofen has a relatively high melting point (about 78°C), while two stereoisomers of ibuprofen, S(+)-ibuprofen and R(-)-ibuprofen, have a melting point of about 52°C to Melting at 54°C. All the different forms of ibuprof...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/192A61K47/36A61K47/38
CPCA61K9/0014A61K31/192A61K47/10A61K47/32A61K47/38A61P29/00A61K9/06A61K9/70A61K47/02A61K47/12A61K47/18
Inventor 斯图尔杰弗里特·伯格曼桑帕斯库马尔·德佛拉简塞沃库马尔·拉玛林格穆安娜森蒂尔威尔·帕拉尼萨米
Owner SHASUN CHEM & DRUGS LTD
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