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Transdermal preparation entrapping estrogen and having three-dimensional reticulate structure and preparation method thereof

A three-dimensional network and three-dimensional configuration technology, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, and sheet-like delivery, can solve the problem of unsatisfactory adhesion of pressure-sensitive adhesive systems and easy drug precipitation Problems such as the influence of crystallization and the easy aging of the pressure-sensitive adhesive system, etc., achieve the effects of fast transdermal absorption rate, reduced frequency of taking, and high bioavailability

Inactive Publication Date: 2015-04-29
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the carriers of conventional transdermal drug delivery preparations, such as the pressure-sensitive adhesive matrix transdermal drug delivery system disclosed in patents CN1269717A and CN101229144A, all have low drug loading, easy precipitation of drugs and crystallization, which affects 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.

Method used

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  • Transdermal preparation entrapping estrogen and having three-dimensional reticulate structure and preparation method thereof
  • Transdermal preparation entrapping estrogen and having three-dimensional reticulate structure and preparation method thereof
  • Transdermal preparation entrapping estrogen and having three-dimensional reticulate structure and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1-8

[0053] See Table 1 for the drug-loaded three-dimensional net-like three-dimensional configuration of the transdermal drug delivery controlled release system.

[0054] Table 1

[0055]

Embodiment 9-16

[0057] See Table 2 for the transdermal drug delivery system in the three-dimensional network configuration used for drug loading.

[0058] Table 2

[0059]

[0060]

Embodiment 9

[0061] The preparation method of embodiment 9:

[0062] (1) Dissolve the drug in a solvent to obtain A, disperse the nano-silicon dioxide in a dispersant to obtain B, then mix A and B, sonicate for 1 hour, and then soak for 24 hours to obtain a uniformly dispersed three-dimensional Drug-loading system with network three-dimensional configuration;

[0063] Described solvent is acetone, and in solvent, the weight content of medicine is 2%;

[0064] (2) Add transdermal penetration enhancer and plasticizer to the adhesive, and stir at a speed of 10,000 rpm for 0.5 hours to obtain a glue solution for later use;

[0065] (3) Add the product of step (1) to the above glue, and stir at a speed of 500rpm for 10-30min to obtain a drug-containing intermediate;

[0066] The above-mentioned drug-containing intermediate is coated on the release layer with a coating thickness of 0.5mm, dried at 80°C for 2 hours, and then covered with a backing layer to obtain the product.

[0067] The mate...

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Abstract

The invention discloses a transdermal preparation entrapping estrogen and having a three-dimensional reticulate structure and a preparation method thereof. The transdermal preparation is composed of a transdermal drug delivery system loading medicine and having a three-dimensional reticulate structure, a backing layer compounded on one side of the transdermal drug delivery system loading medicine and having the three-dimensional reticulate structure and an anti-adhesion layer compounded on the other side of the transdermal drug delivery system loading medicine and having the three-dimensional reticulate structure. The transdermal preparation comprises the following components in percentage by weight: 10-50% of transdermal drug delivery controlled release system, 30-85% of adhesive, 0.5-18% of penetration enhancer and 0.2-30% of plasticizer. The transdermal drug delivery system loading medicine and having the three-dimensional reticulate structure comprises the following components in percentage by weight: 1-40% of active medicine, 1-68% of nanoporous silica and 30-97% of dispersant, wherein the active medicine is estradiol or estradiol hemihydrate. The transdermal preparation disclosed by the invention can be used for effectively achieving long-term continuous transdermal of the medicine and maintain constant blood medicine concentration, and moreover, the preparation has the characteristics of high transdermal absorption rate, high transdermal absorption dosage, stability and high efficiency.

Description

technical field [0001] The invention relates to a three-dimensional net-shaped three-dimensional transdermal drug delivery system containing estradiol medicine 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] Traditionally, hormonal drugs, including estrogen, use a transdermal drug delivery system (TCDS), which is a type of drug delivery system in which drugs pass through the skin at a certain rate and are absorbed into the systemic circulation through capillaries to produce cur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/04A61K31/565A61K9/70A61P5/30
Inventor 罗华菲王浩侯惠民朱慧勇武余波陈纯
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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