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Method of preparing polymer electrospinning fiber and application in transdermal drug delivery patch

An electrospinning fiber and polymer technology, applied in the application of transdermal drug patch, the field of polymer electrospinning fiber preparation, can solve the problems of improving, not using, not involving the compatibility of pressure-sensitive adhesives, etc., to promote the Effects of drug release, improved stability, improved performance and scope of application

Inactive Publication Date: 2012-07-11
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, some literatures have mentioned the application of electrospun fiber technology in transdermal drug delivery (Taepaiboon P., Nanotechnology, 2006, 17: 2317; Taepaiboon P., European Journal of Pharmaceutics and Biopharmaceutics 2007, 67: 387; Im J.S., Biomaterials, 2010, 31: 1414; Ngawhirunpat T., Pharmaceutical Development and Technology, 2009, 14(1): 73; Shen D., European Polymer Journal 2009, 45: 2767; Suwantong O., Polymer 2008, 49: 4239), It is limited to loading drugs with electrospun fibers, simply evaluating the drug release or transdermal penetration properties of electrospun fiber membranes, or used in dressings such as skin burns, but does not use electrospun fiber technology to increase drug loading and inhibit drug crystallization Precipitation, no use of electrospun fibers to load penetration enhancers, and no issues related to compatibility with pressure-sensitive adhesives

Method used

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  • Method of preparing polymer electrospinning fiber and application in transdermal drug delivery patch
  • Method of preparing polymer electrospinning fiber and application in transdermal drug delivery patch
  • Method of preparing polymer electrospinning fiber and application in transdermal drug delivery patch

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation of polymer electrospinning fiber solution: N,N-dimethylacetamide / acetone (V:V =2:1, volume ratio) solution, then add 20% ibuprofen and 20% azone (accounting for the mass fraction of the electrospun polymer), dissolve evenly, and then spin. The electrospinning conditions were as follows: needle No. 8, voltage 13KV, spray speed 0.5ml / h, curing distance 20cm; aluminum foil was used to receive and spin the drug-loaded electrospun fiber membrane, and the prepared electrospun fiber membrane was dried in vacuum for 24 hours. The prepared electrospun fiber membrane was vacuum dried for 24 h. A non-woven fabric coated with polyacrylate pressure-sensitive adhesive (thickness 0.1-1mm) is used as a backing film, and then a quantitative amount of the drug-loaded electrospun fiber membrane prepared above is attached to the backing film, and then coated with 2.5 The release paper protective film of the PSA2 pressure-sensitive adhesive layer (thickness 0.1-2mm) of % ibupro...

Embodiment 2

[0038] According to the method of Example 1, only the pressure-sensitive adhesive layer is changed to PSA1 pressure-sensitive adhesive layer to obtain patch I-2.

[0039] The PSA1 pressure-sensitive adhesive containing 5% ibuprofen and 5% azone was directly coated on the release paper to form the pressure-sensitive adhesive monolithic patch M-2 as a control.

[0040] Ibuprofen and azone are dissolved into the N,N-dimethylacetamide / acetone (V: V=2:1, volume ratio) solution, cast to form a film, use it to replace the electrospun film in I-2, and combine it with PSA1 pressure-sensitive adhesive to form patch F-2, as a control.

[0041] For the characterization of the dispersion state of the drug in patch I-2, see image 3 and 4 , no drug crystallization; see Tables 4, 5 and 6 for the adhesiveness, storage stability and transdermal penetration rate of patches I-2, F-2 and M-2.

Embodiment 3

[0043] Prepare an ethanol solution of 15% polyvinylpyrrolidone (PVPK90) containing 20% ​​methyl nicotinate (accounting for the mass fraction of PVP, the same below), and carry out spinning. The electrospinning conditions are: needle No. 8, voltage 10KV, The spray speed was 0.5ml / h, and the curing distance was 20cm; aluminum foil was used to receive and spin to form drug-loaded electrospun fiber membranes, and the prepared electrospun fiber membranes were vacuum-dried for 24 hours. The non-woven fabric is used as the backing film, and a layer of polyacrylate pressure-sensitive adhesive (thickness 0.1-1mm) is coated on the top, the drug-loaded electrospun fiber membrane prepared above is attached to the pressure-sensitive adhesive, and then coated with PSA2 A release paper protective film with a pressure-sensitive adhesive layer (thickness 0.1-2mm), rolled to form an I-type patch I-3. The adhesiveness of the patch is shown in Table 4.

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Abstract

The invention relates to a method of preparing polymer electrospinning fiber and application in a transdermal drug delivery patch. At least one drug or transdermal enhancer is loaded on polymer electrospinning fiber to form a polymer electrospinning fibrous membrane which is then combined with a backing membrane, pressure-sensitive adhesive and a protective membrane, thus forming a patch which can be adhered on the skin and used for transdermal penetration and drug delivery. The polymer electrospinning fiber transdermal drug delivery patch is combined by the polymer electrospinning fibrous membrane, the pressure-sensitive adhesive, the backing membrane and the protecting membrane; matters such as the patch, drug, transdermal enhancer and crystallization inhibitor can be dissolved or diffused into the polymer solution, and loaded on the fiber during the polymer fibration process, thus achieving the effects high loading amount of the drug, the transdermal enhancer and the like and crystallization inhibition effect, overcoming the problem of low loading amount of pressure-sensitive adhesive (or transdermal enhancer), and reducing the influence of components such as the drug and the transdermal enhancer on the adhesion of the pressure-sensitive adhesive.

Description

technical field [0001] The invention relates to the application of polymer electrospun fiber, which belongs to the preparation method of polymer electrospun fiber and its application in transdermal drug delivery patch. Background technique [0002] Transdermal administration can avoid the first-pass effect of the liver and the inactivation of the stomach and intestines that may occur during oral administration, and has a series of advantages such as maintaining a constant blood drug concentration, prolonging the action time, enhancing patient compliance with medication, and medication safety and convenience. , transdermal drug delivery preparation (abbreviated as TDDS) has obtained rapid development in recent years. TDDS, which is commonly used at present, is mainly a patch dosage form in which drugs and penetration enhancers are mixed in pressure-sensitive adhesives or hydrogels, and coated with a film to form an adhesive patch. The polymer pressure-sensitive adhesive laye...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K47/32A61K47/34A61K47/36A61K47/38A61K8/02A61K8/73A61K8/81A61K8/84A61K8/85A61K8/86A61L15/24A61L15/26A61L15/28
Inventor 董岸杰史永利邓联东
Owner TIANJIN UNIV
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