Insulin carrier transdermal drug delivery preparation and preparation method thereof

A technology for transdermal drug delivery and insulin, which is applied in the directions of pharmaceutical formulation, drug combination, drug delivery, etc. It can solve the problems of weak penetrability of insulin drugs, large insulin molecules, and difficulty in absorbing the liver, etc., and achieve strong skin penetration, High encapsulation efficiency, promoting drug transdermal absorption

Active Publication Date: 2011-09-14
王义明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the problems faced by oral administration are: (1) proteolytic enzyme decomposition in the digestive tract; (2) insulin molecules are relatively large and easy to aggregate; (3) difficult to absorb and the first-pass effect of the liver
The problem with inhaled insulin is: Potentially dangerous to the lungs especially the fragile alveolar / capillary structure
But the biggest problem is that the penetration of insulin drugs into the skin is too weak

Method used

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  • Insulin carrier transdermal drug delivery preparation and preparation method thereof
  • Insulin carrier transdermal drug delivery preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Take 8.0g of soybean phosphatidylcholine, 8.0g of cholesterol, 1.0g of sodium deoxycholate and 1mL of eucalyptus oil, add ethanol, and ultrasonically dissolve; weigh 0.2g of insulin, and use 60mL of 0.01M triethanolamine-hydrochloric acid buffer ( pH=6.2) dissolve, add the obtained solution to the solution obtained above, through the micro-jet, each nozzle hits 8-10 cycles, the pressure is 10 4 pa, make it homogenized and nano-sized to obtain the insulin transfer body solution; take 1g of carbomer, add appropriate amount of water to make a gel matrix, slowly add the insulin transfer body solution to it, stir evenly, and obtain.

[0039] The physical properties of the insulin delivery body transdermal drug delivery preparation that the present embodiment makes:

[0040] According to the particle size measurement, the transdermal insulin transfer body formulation of this example has a uniform particle size (200-300nm); measured by ultracentrifugation, the encapsulation ra...

Embodiment 2

[0051] Take 30.0g of distearoylphosphatidylcholine, 30.0g of cholesterol, 5.0g of sodium cholate, 3mL of geranium oil and 2mL of L-menthol, add 30ml of ethanol, and ultrasonically dissolve it; weigh 1.0g of insulin, and use 80mL of 0.01 Dissolve M triethanolamine-hydrochloric acid buffer solution (pH=6.0), add the obtained solution to the solution obtained above, and make it homogenized and nano-sized by micro-jet to obtain the insulin transfer body solution; take 5g xanthan gum, add appropriate amount of water A gel matrix is ​​prepared, and the insulin transfer body solution is slowly added thereto, and the mixture is evenly stirred to obtain the product.

[0052] The physical properties of the insulin delivery body transdermal drug delivery preparation that the present embodiment makes:

[0053] According to the particle size measurement, the insulin transfer body transdermal drug delivery preparation of this example has a uniform particle size (200-300nm); measured by ultr...

Embodiment 3

[0064] Take 24.0g of distearoylphosphatidylethanolamine, 24.0g of cholesterol, 1.7g of sodium deoxycholate, 1.5mL of L-menthol and 0.5mL of turpentine, add 20ml of ethanol, and ultrasonically dissolve them; weigh 0.4g of insulin, and use 64mL Dissolve 0.01M triethanolamine-hydrochloric acid buffer solution (pH=6.8), add the obtained solution to the above obtained solution, and make it homogenized and nanometerized by micro-jet to obtain the insulin transfer body solution; take 2.5g of poloxamer 188, Add an appropriate amount of water to make a gel base, slowly add the insulin transfer body solution to it, and stir evenly to obtain the gel matrix.

[0065] The physical properties of the insulin delivery body transdermal drug delivery preparation that the present embodiment makes:

[0066] According to the particle size measurement, the transdermal insulin transfer body formulation of this example has a uniform particle size (200-300nm); measured by ultracentrifugation, the enca...

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Abstract

The invention discloses an insulin carrier transdermal drug delivery preparation which comprises the following components of insulin, phospholipid, cholesterol, surfactant, transdermal penetration enhancer, triethanolamine-hydrochloric acid and gel. A preparation method of the insulin carrier transdermal drug delivery preparation comprises the steps of: 1, taking the phospholipid, the cholesterol, the surfactant and the transdermal penetration enhancer and then adding into alcohol for dissolving; 2, taking insulin, dissolving the insulin with a triethanolamine-hydrochloric acid buffer solution, adding the obtained solution in the solution obtained in the step 1, homogenizing and nanometerizing liquid through micro jet to obtain an insulin carrier solution; and 3, taking the gel, adding water to enable the gel to be swelled to prepare a gel substrate, slowly adding the insulin carrier solution in the step 2 into the gel substrate, and uniformly stirring to obtain the insulin carrier transdermal drug delivery preparation. The insulin carrier transdermal drug delivery preparation prepared by adopting the preparation method disclosed by the invention has the characteristics of uniformparticle size, higher entrapment rate, good stability and convenience for medicine delivery; and at least three days of medicine delivery time can be maintained, and compliance of patients is improved while the medicine delivery interval is greatly shortened.

Description

technical field [0001] The invention relates to an insulin transfer body transdermal drug delivery preparation and a preparation method thereof. Background technique [0002] Insulin is the drug of choice for the treatment of diabetes. It is a protein composed of 51 amino acids. The end of its tertiary structure is easy to form a stable non-parallel and covalent β-fold, and forms a dimer with another molecule of insulin, and in zinc In the presence of ions, the 3 dimers can combine to form a more stable hexamer. This polymer has a large molecular weight, is difficult to pass through the absorption barrier, and is easily degraded by gastric acid and digestive enzymes in the gastrointestinal tract. Therefore, the administration method of insulin has always been injection administration, and long-term injection administration causes great pain and inconvenience to patients. There may even be adverse reactions such as allergies, induration, inflammation, etc. Research on safe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K38/28A61K47/44A61P3/10
CPCA61K38/28A61K9/0014A61K9/06A61K47/18A61P3/10
Inventor 王义明
Owner 王义明
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