Application of penetration-enhancing composition in percutaneous penetration enhancement of external preparation

Abstract

The invention discloses application of a penetration-enhancing composition in percutaneous penetration enhancement of an external preparation. The application comprises adding the penetration-enhancing composition to the external preparation which is a nonsteroidal anti-inflammatory drug; the penetration-enhancing composition contains an organic acid and a penetration enhancer; by mass, the mixture of the penetration-enhancing composition and the external preparation comprises 0.1-5% of the nonsteroidal anti-inflammatory drug, 0.05-10% of the organic acid, and 0.05-30% of the penetration enhancer. In combination with an ion-pairing agent and a common penetration enhancer, the penetration-enhancing composition helps increase the percutaneous penetration quantity of the nonsteroidal anti-inflammatory drug to be increased by 5-10 times and relieve the damage to the skin structure due to the nonsteroidal anti-inflammatory drug.

Description

technical field

[0001] The invention relates to the field of transdermal drug delivery, in particular to the application of a penetration-enhancing composition in the transdermal enhancement of external preparations. Background technique

[0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are currently the most commonly used and most widely used drugs for the treatment of arthritis, frozen shoulder, acute upper respiratory inflammation and various pains. NSAIDs work by inhibiting cyclooxygenase (COX), the enzyme involved in the conversion of arachidonic acid to prostaglandins. Most NSAIDs are non-selective COX inhibitors that inhibit both COX-1 and COX-2. However, non-selective NSAIDs may cause severe upper gastrointestinal complications, including abdominal distension, cramping, pain, diarrhea, constipation, acid reflux, and even perforation, infarction, and gastrointestinal bleeding. COX-2 selective inhibitors can significantly reduce gastrointestinal risk compared w...

Examples

Embodiment 1

[0043] (1) Measure 30mL of purified water into a wide-mouth beaker, pour 1g of carbomer into it, swell until it is completely dispersed, adjust its pH to 6.0-6.5 with triethanolamine, and prepare solution a;

[0044] (2) Measure 20 mL of purified water and add 0.5 g of CMC-Na (sodium carboxymethyl cellulose) to obtain solution b;

[0045] (3) Mix 1g of loxoprofen sodium, 1g of malic acid and 1g of menthol with an appropriate amount of purified water, add 10mL of ethanol to dissolve, add to the mixed system of solution a and solution b, and add purified water to the total weight of the mixture 100g, adjust pH to 6.5 with triethanolamine, fully stir to obtain transparent loxoprofen sodium gel.

Embodiment 2

[0047] (1) Measure 30mL of purified water into a wide-mouth beaker, pour 1g of carbomer into it, swell until it is completely dispersed, adjust its pH to 6.0-6.5 with triethanolamine, and prepare solution a;

[0048] (2) Measure 20 mL of purified water and add 0.5 g of CMC-Na (sodium carboxymethyl cellulose) to obtain solution b;

[0049] (3) Mix 1g of loxoprofen sodium with 1g of malic acid and 1g of SDS-Na (sodium dodecyl sulfate) in an appropriate amount of purified water, add 10mL of ethanol to dissolve it, and add it to the mixed system of solution a and solution b , add purified water until the total weight of the mixed solution is 100g, adjust the pH to 6.5 with triethanolamine, and fully stir to obtain a transparent loxoprofen sodium gel.

Embodiment 3

[0065] (1) Measure 30mL of purified water into a large-mouth beaker, pour 1g of carbomer and 1g of HPMC (hydroxypropyl methylcellulose), swell until fully dispersed, adjust its pH to about 6.5 with triethanolamine, and prepare solution a;

[0066] (2) Mix 1 g of diclofenac sodium and 1 g of lactic acid with an appropriate amount of purified water, adjust the pH to about 6.5 with 2M (mol / L) NaOH, then add 10 mL of ethanol and 1 g of oleic acid to dissolve to obtain solution b;

[0067] (3) Mix solution a and solution b evenly, add purified water until the total weight of the mixed solution is 100 g, adjust the pH to 6.5 with triethanolamine, and stir thoroughly to obtain a transparent diclofenac sodium gel.

technical field

[0001] The invention relates to the field of transdermal drug delivery, in particular to the application of a penetration-enhancing composition in the transdermal enhancement of external preparations. Background technique

[0002] Non-steroidal anti-inflammatory drugs (NSAIDs) are currently the most commonly used and most widely used drugs for the treatment of arthritis, frozen shoulder, acute upper respiratory inflammation and various pains. NSAIDs work by inhibiting cyclooxygenase (COX), the enzyme involved in the conversion of arachidonic acid to prostaglandins. Most NSAIDs are non-selective COX inhibitors that inhibit both COX-1 and COX-2. However, non-selective NSAIDs may cause severe upper gastrointestinal complications, including abdominal distension, cramping, pain, diarrhea, constipation, acid reflux, and even perforation, infarction, and gastrointestinal bleeding. COX-2 selective inhibitors can significantly reduce gastrointestinal risk compared w...

Examples

Embodiment 1

[0043] (1) Measure 30mL of purified water into a wide-mouth beaker, pour 1g of carbomer into it, swell until it is completely dispersed, adjust its pH to 6.0-6.5 with triethanolamine, and prepare solution a;

[0044] (2) Measure 20 mL of purified water and add 0.5 g of CMC-Na (sodium carboxymethyl cellulose) to obtain solution b;

[0045] (3) Mix 1g of loxoprofen sodium, 1g of malic acid and 1g of menthol with an appropriate amount of purified water, add 10mL of ethanol to dissolve, add to the mixed system of solution a and solution b, and add purified water to the total weight of the mixture 100g, adjust pH to 6.5 with triethanolamine, fully stir to obtain transparent loxoprofen sodium gel.

Embodiment 2

[0047] (1) Measure 30mL of purified water into a wide-mouth beaker, pour 1g of carbomer into it, swell until it is completely dispersed, adjust its pH to 6.0-6.5 with triethanolamine, and prepare solution a;

[0048] (2) Measure 20 mL of purified water and add 0.5 g of CMC-Na (sodium carboxymethyl cellulose) to obtain solution b;

[0049] (3) Mix 1g of loxoprofen sodium with 1g of malic acid and 1g of SDS-Na (sodium dodecyl sulfate) in an appropriate amount of purified water, add 10mL of ethanol to dissolve it, and add it to the mixed system of solution a and solution b , add purified water until the total weight of the mixed solution is 100g, adjust the pH to 6.5 with triethanolamine, and fully stir to obtain a transparent loxoprofen sodium gel.

Embodiment 3

[0065] (1) Measure 30mL of purified water into a large-mouth beaker, pour 1g of carbomer and 1g of HPMC (hydroxypropyl methylcellulose), swell until fully dispersed, adjust its pH to about 6.5 with triethanolamine, and prepare solution a;

[0066] (2) Mix 1 g of diclofenac sodium and 1 g of lactic acid with an appropriate amount of purified water, adjust the pH to about 6.5 with 2M (mol / L) NaOH, then add 10 mL of ethanol and 1 g of oleic acid to dissolve to obtain solution b;

[0067] (3) Mix solution a and solution b evenly, add purified water until the total weight of the mixed solution is 100 g, adjust the pH to 6.5 with triethanolamine, and stir thoroughly to obtain a transparent diclofenac sodium gel.

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