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Transdermal medicine composition and transdermal medicine kit

A drug and preparation technology, which is applied in the field of transdermal drug combination preparations, can solve the problems of complex processing process and inability to use transdermal drug delivery, and achieve the effects of good release performance, excellent drug release effect, and reduced research and production costs

Active Publication Date: 2011-04-13
BEIJING CAS MICRONEEDLE TECH LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, for the preparation of medical cross-linked polyacrylamide hydrogels (such as Chinese patents CN1068612C, CN 1058639C and CN 1450118A), water-soluble redox systems are basically used to initiate polymerization, and organic solvent extraction is used later to remove unreacted monomers. Processing is complex and the resulting polymer is primarily used for tissue filling rather than for transdermal drug delivery

Method used

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  • Transdermal medicine composition and transdermal medicine kit
  • Transdermal medicine composition and transdermal medicine kit
  • Transdermal medicine composition and transdermal medicine kit

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～8

[0050] Acrylamide and methylenebisacrylamide, acrylic acid and initiator azobisisobutyronitrile were added into a 100ml three-necked flask according to the amount described in Table 1, and 50ml of the first solvent (the first solvent used in Examples 1 to 7) was added. The first solvent is acetone, the first solvent used in Example 8 is isopropanol), a thermometer, a reflux device and a mechanical stirring device are installed, and the temperature is raised to 64° C. for reflux reaction under nitrogen protection for 30 hours. After removing the solvent by suction filtration, use Wash and purify the obtained polymer with ethanol until the content of acrylamide monomer in the cross-linked polyacrylamide obtained is lower than 0.000002% as measured by the detection method of the national standard GB / T12005.4-89, and then at 120°C Vacuum dried for 24 hours to obtain cross-linked polyacrylamide powder, and their glass transition temperature, cross-linking degree and gel skeleton por...

Embodiment 9

[0061] Take 0.038g of the cross-linked polyacrylamide powders of the above-mentioned Examples 1-8, add 1ml of aqueous solution, and after it swells into a gel, freeze-dry in a freeze-drying cold trap at -50°C for about 8 hours until the water in the sample The contents were lower than 10ppm, and the scanning electron microscope observation was carried out. The skeleton pore diameters of these gels after freeze-drying are listed in Table 1. figure 2 It shows the skeleton diagram of the gel formed by the cross-linked polyacrylamide powder in Example 2 after freeze-drying.

[0062] The results showed that the cross-linked polyacrylamide skeleton in these gels was observed to be porous when magnified 600 times, and the skeleton pore size was 5-30 μm. The cross-linked polyacrylamide powders of Examples 1-3 prepared according to the preferred conditions have a skeleton pore diameter of 12-30 μm after forming a gel.

Embodiment 10～22

[0067] The cross-linked polyacrylamide powders of the above-mentioned Examples 1 to 7 were formulated into different transdermal gel preparations according to the formula in Table 3 (the contents of each component are weight percentages based on the total amount of the gel preparation, and the remaining part is content of pure water), wherein the bovine serum albumin concentration is 2mg / g gel (bovine serum albumin molecular weight is 67kD, as can be seen from scanning electron microscope picture 2, the gel skeleton pore diameter is much larger than the size of various proteins, so It can be suitable for the release of proteins, polypeptides or gene medicines of various molecular weights), through the microneedle-assisted mode, use the microneedle array to act on the skin (484 holes) with an area of ​​1cm2 for 30s, and then inject 300mg of Example 10 ~22 The prepared hydrogel preparation was coated on the action site of the microneedle, and the classic Franz vertical jacketed d...

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Abstract

The invention provides a transdermal medicine composition which comprises a carrier and active medicine ingredients, wherein the main ingredient of the carrier is crosslinked polyacrylamide, the degree of crosslinking of the crosslinked polyacrylamide is about 0.5-1%, the glass-transition temperature is 110-130 DEG C and 170-185 DEG C, and the aperture of a gel skeleton of the crosslinked polyacrylamide is 5-30 mum. The invention also provides a transdermal medicine kit comprising a micro needle array and the transdermal medicine composition. In the transdermal medicine composition provided by the invention, the crosslinked polyacrylamide used as the main ingredient of the carrier has good swelling performance, the swelled crosslinked polyacrylamide has good skin adhesion performance, and meanwhile, the carrier has good performance to release water soluble medicines. Moreover, the transdermal medicine kit of the invention can increase the transdermal rate of the transdermal medicine composition, and thus, medicines can effectively enter bodies to take more excellent medicinal effects.

Description

technical field [0001] The invention relates to a transdermal drug combination preparation and a transdermal drug kit comprising the transdermal drug combination preparation. Background technique [0002] Transdermal drug delivery is a new type of painless drug delivery method, which can avoid the liver first-pass effect and gastrointestinal enzymatic hydrolysis of the traditional drug delivery method, achieve constant drug release for a long time, and is not prone to injection and oral administration peak plasma concentration of the drug. Gel preparations and cataplasms are commonly used preparation types for transdermal administration, but currently cataplasms are only suitable for transdermal administration of small molecular weight drugs, and the transdermal penetration enhancers added in cataplasms have certain effects on the skin. Therefore, it is of great significance to develop a drug gel formulation matrix with better transdermal efficiency, suitable for transderma...

Claims

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Application Information

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IPC IPC(8): A61K47/32A61K47/34A61K47/22A61K45/00A61M37/00A61K47/10
Inventor 高云华覃光炯
Owner BEIJING CAS MICRONEEDLE TECH LTD
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