Cubic water quality liquid crystal gel transdermic absorption preparation containing oxybutynin chloride and preparing method thereof

Abstract

The invention discloses a cubic water quality liquid crystal gel transdermic absorption preparation containing oxybutynin chloride and a preparing method thereof. The preparation contains the following components by weight percentage with the total weight of the preparation as standard: 1%-30% of oxybutynin hydrochloride or basic group of oxybutynin hydrochloride, 13%-90% of solvent, 0.1%-20% of gel host material, 23%-90% of solvent, 0.2%-30% of oily permeating skin penetration enhancer, 0.1%-35% of liquid crystal gel emulsifier, 1%-60% of water and 0.01%-15% of potential of hydrogen (pH) regulator. The preparation has better efficiency performance, can reduce medicine taking frequency, improves adaptability of users, simultaneously avoids first-pass effect when medicine is orally takenand passes through gastrointestinal tract and liver due to skin permeating method, and has higher bioavailability.

Description

technical field [0001] The invention relates to a preparation containing oxybutynin hydrochloride or its base. Background technique [0002] Active drugs for the treatment of overactive bladder, such as oxybutynin hydrochloride and its base form, as the third-generation drug of choice for urinary incontinence in the treatment of overactive bladder, have both anticholinergic and anti-smooth muscle spasm effects, and are suitable for the treatment of various Urinary urgency, frequent urination, urinary incontinence, enuresis, etc. [0003] Oxybutynin is rapidly metabolized by the liver when taken orally, with a bioavailability of only 6%, and is accompanied by side effects such as dry mouth, astringent mouth, constipation, and blurred vision. Therefore, the patient's compliance is poor. [0004] Chinese patent CN1134254C discloses a plaster-type transdermal preparation containing oxybutynin based on an ammonium-containing acrylate or methacrylate copolymer. The area is large...

AI Technical Summary

Problems solved by technology

[0003] Oxybutynin is rapidly metabolized by the liver when taken orally, with a bioavailability of only 6%, and it is accompanied by side effects such as dry mouth, astringent mouth, constipation, and blurred vision. Therefore, patients’ compliance is poor

[0004] Chinese patent CN1134254C discloses a plaster-type transdermal preparation containing oxybutynin based on an ammonium-containing acrylate or methacrylate copolymer. The area is large, the skin tolerance is poor, and the drug is easy to precipitate in the pressure-sensitive adhesive;

[0005] Chinese patent CN101455650A discloses the same oxybutynin hydrochloride patch with hydrophobic pressure-sensitive adhesive as the matrix, but a small amount of water is needed to dissolve the drug during preparation, and the compatibility with the hydrophobic pressure-sensitive adhesive matrix is ​​not good, and it is not easy to mix evenly

[0006] Chinese patent CN1708269A discloses a kind of oxybutynin gel preparation, this patent adopts the non-occlusive topical administration form, although the medicine can permeate through the skin, but the transdermal rate is low, and the administration area is relatively large, it needs 150~ 200cm 2 The drug effect can only be achieved by applying the area, so the tolerance of the skin is poor

At the same time, because the hydrogel system of this patent contains a lot of water, the appearance and color of the preparation will change significantly as the storage time prolongs, and the drug is easily oxidized, which greatly affects the stability.

[0007] Studies have shown that the arrangement of traditional emulsified creams or ordinary hydrogels will create a porous structure in the skin barrier, so it will damage the skin's sebum barrier, increase the rate of transepidermal water loss, and make the skin vulnerable to external attacks

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