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Application of papaverine hydrochloride as transdermal absorption enhancer

A technology of papaverine hydrochloride and an absorption enhancer, which is applied in the application field of papaverine hydrochloride as a transdermal absorption enhancer, and can solve the problems of azone irritant, long lag time onset, poor effect and the like

Active Publication Date: 2011-11-16
YANTAI RONGCHANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A large number of documents prove that azone is a good transdermal absorption accelerator, which can effectively promote the transdermal absorption of drugs, but azone has some shortcomings such as irritation, long lag time for onset of action, and sometimes poor effect when used alone

Method used

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  • Application of papaverine hydrochloride as transdermal absorption enhancer
  • Application of papaverine hydrochloride as transdermal absorption enhancer
  • Application of papaverine hydrochloride as transdermal absorption enhancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The in vitro transdermal absorption experiment of embodiment 1 diclofenac sodium gel

[0038] Prescription: 10g of diclofenac sodium, appropriate amount of ethanol, 18g of triethanolamine, 20g of papaverine hydrochloride, 500g of carbomer-940 aqueous solution, and add distilled water to 1000g.

[0039] Process: Dissolve diclofenac sodium in an appropriate amount of ethanol, then mix Carbomer-940 aqueous solution and papaverine hydrochloride evenly, grind, add diclofenac sodium solution to Carbomer-940 matrix under stirring, slowly add three Add ethanolamine and stir to make a gel, add distilled water to the full amount, stir evenly, and pack to obtain diclofenac sodium gel containing 2% papaverine hydrochloride.

[0040] According to the above prescription and process, diclofenac sodium gel containing 5% papaverine hydrochloride and diclofenac sodium gel without papaverine hydrochloride were made respectively. Using physiological saline as the receiving solution, the i...

Embodiment 2

[0044] The in vitro transdermal absorption experiment of embodiment 2 estradiol ointment

[0045] The specification of estradiol ointment is 10g:13.3mg. Using physiological saline containing 40% polyethylene glycol 400 as the receiving solution, the in vitro transdermal absorption experiment of rat skin was carried out. Take 0.5g ointment and apply it evenly on the stratum corneum of the skin. Sampling was carried out for analysis and detection, and the experimental results are shown in Table 6:

[0046] Table 6 Cumulative penetration per unit area of ​​estradiol (μg / cm 2 , n=5)

[0047]

[0048] Note: The data in the table are the average values ​​of each group.

Embodiment 3

[0049] The in vitro transdermal absorption experiment of embodiment 3 vitamin E cream

[0050] Prescription: vitamin E 20g, glyceryl monostearate 70g, stearic acid 112.5g, glycerin 85g, white petrolatum 85g, sodium lauryl sulfate 10g, ethyl p-hydroxybenzoate 1g, distilled water added to 1000g.

[0051] Process: Dissolve glycerin, sodium lauryl sulfate, and ethyl p-hydroxybenzoate in 80°C water (water phase); separately take glyceryl monostearate, stearic acid, and white petrolatum and heat to 80°C on a water bath Melt, stop heating, add vitamin E and stir well (oil phase); slowly add oil phase to water phase, stir while adding, until condensed to obtain vitamin E cream without papaverine hydrochloride.

[0052] Make the vitamin E cream that contains 1% papaverine hydrochloride again according to above prescription and technology. Using physiological saline containing 10% polyethylene glycol 400 as the receiving solution, the in vitro transdermal absorption experiment of rat s...

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Abstract

The invention relates to application of papaverine hydrochloride in a transdermal preparation, in particular to application of the papaverine hydrochloride as a transdermal absorption enhancer in various transdermal administration preparations or functional cosmetics.

Description

technical field [0001] The invention relates to the application of papaverine hydrochloride in transdermal preparations, specifically the application of papaverine hydrochloride as a transdermal absorption accelerator in various transdermal drug delivery preparations or functional cosmetics. Background technique [0002] Transdermal drug delivery system refers to a type of drug delivery system that is administered through the skin surface, allowing the drug to pass through the skin at a constant rate (or close to a constant rate), and absorbed into the systemic circulation through capillaries to produce systemic or local therapeutic effects. Compared with traditional drug administration methods, transdermal absorption preparations have the characteristics of avoiding liver first-pass effect and gastrointestinal inactivation, maintaining constant blood drug concentration or pharmacological effects, reducing adverse drug reactions, and patients can self-administer medication. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/22A61K9/00A61K8/49
Inventor 夏丕芳熊晓滨
Owner YANTAI RONGCHANG PHARMA