Transdermal drug delivery preparation with drug-loaded three-dimensional mesh spatial configuration and preparation method of transdermal drug delivery preparation

Abstract

The invention discloses a transdermal drug delivery preparation with a drug-loaded three-dimensional mesh spatial configuration and a preparation method of the transdermal drug delivery preparation. The transdermal drug delivery preparation with the drug-loaded three-dimensional mesh spatial configuration is composed of a transdermal drug delivery with the drug-loaded three-dimensional mesh spatial configuration, a backing layer and an anti-sticking layer, wherein the backing layer is compounded on one side of the transdermal drug delivery with the drug-loaded three-dimensional mesh spatial configuration; the anti-sticking layer is compounded on the other side of the transdermal drug delivery with the drug-loaded three-dimensional mesh spatial configuration; and an active medicine comprises the forms of oxybutynin hydrochloride or tartrate thereof, sulfate, phosphate, fumarate and a basic group. According to the transdermal drug delivery preparation, the drug loading capacity is greatly increased; the drug loading capacity can be improved; the medicine devitrification is inhibited; the medicines are sequentially and uniformly dispersed into the transdermal drug delivery system; stable release is carried out; long-term lasting transdermal permeation of the medicines can be realized; stable blood concentration is maintained; and the preparation is high in transdermal absorption rate and high in transdermal absorption amount, and has the characteristics of being stable and efficient.

Description

technical field [0001] The invention relates to a three-dimensional network three-dimensional transdermal drug delivery system containing oxybutynin with nanoporous silicon dioxide as a carrier and a preparation method thereof. Background technique [0002] Transdermal drug delivery preparation is a sustained and controlled release preparation in which the active drug is absorbed into the blood circulation of the whole body through the skin and has a therapeutic effect. The transdermal drug delivery preparation is composed of an active ingredient and a carrier. In addition to the performance of the ingredients, it is mainly determined by the carrier used to load the active ingredients. [0003] 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 sui...

AI Technical Summary

Problems solved by technology

[0004] 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

[0005] At present, the carriers of conventional transdermal drug delivery preparations, such as the pressure-sensitive adhesive matrix transdermal drug delivery systems disclosed in patents CN1269717A and CN101229144A, all have low drug loading, easy crystallization of drugs, and influence on transdermal absorption performance. The adhesive performance of the pressure-sensitive adhesive system is not ideal, the pressure-sensitive adhesive system is easy to age, and the drug stability is poor, which is difficult to meet the clinical needs.

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; Chinese patent CN101455650A discloses an oxybutynin hydrochloride patch that also uses a hydrophobic pressure-sensitive adhesive as a matrix, but it needs a small amount of water to dissolve Drugs, poor compatibility with hydrophobic pressure-sensitive adhesive matrix, difficult to mix evenly

Images