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Transdermally delivered ursolic acid/insulin nanoscale slow-release preparation and preparation method thereof

A nano-sustained-release insulin technology, applied in the field of pharmacy, can solve the problems of low absorption and bioavailability, poor water solubility of insulin, etc., and achieve the effect of reducing the number of medications, reducing the number of medications, and improving solubility

Inactive Publication Date: 2018-07-13
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the existing technical deficiencies, to solve the problems of poor water solubility, low absorption and bioavailability of insulin, and to alleviate and reduce the physiological and psychological pain caused by injection to patients

Method used

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  • Transdermally delivered ursolic acid/insulin nanoscale slow-release preparation and preparation method thereof
  • Transdermally delivered ursolic acid/insulin nanoscale slow-release preparation and preparation method thereof
  • Transdermally delivered ursolic acid/insulin nanoscale slow-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A: Dissolve 1mg of insulin in 1ml of methanol to form a drug-containing organic solution, dissolve 9.06mg of ursolic acid in methanol, 0.1ml of glycerin, 200mg of hydroxymethylcellulose, 1g of mannitol, 0.4g of propylene glycol, and carbopol Sodium acrylate 5mg, sodium acrylate 150mg, dissolved in water to form a hydrophilic aqueous solution;

[0042] B: Mix 100 μL insulin methanol solution and 100 μL ursolic acid methanol solution evenly, add dropwise to the hydrophilic aqueous solution, and stir at room temperature for 1 hour to obtain ursolic acid / insulin nanoparticles.

[0043]C: Dissolve glycerin, hydroxymethylcellulose, mannitol, propylene glycol, carbomer, and sodium acrylate in 3ml of water as an aqueous solution of hydrophilic excipients, freeze-dry ursolic acid / insulin nanoparticles and mix with the aqueous solution of hydrophilic excipients Mix evenly to obtain the drug-loaded layer with sustained release function.

[0044] D: Apply the drug-loaded layer eve...

Embodiment 2

[0046] The ursolic acid / insulin nanometer prepared by the present invention is measured average particle diameter, PDI and electric potential by dynamic light scattering, as figure 1 and figure 2 shown.

Embodiment 3

[0048] Put 1ml of the drug-loaded layer in a dialysis bag with a molecular weight cut-off of 10,000, and at the same time place the dialysis bag in 30ml of PBS phosphate buffer solution with a pH of 7.4, then put the PBS buffer solution in a shaker at a constant temperature at 37°C, and the speed 233r / min, sample 1ml at different time points, and add 1ml of blank PBS at the same time. Adopt ultraviolet spectrophotometry to detect wavelength 276nm, calculate cumulative amount, such as image 3 Shown, show that the ursolic acid / insulin nano sustained-release transdermal drug preparation prepared by the present invention has the characteristics of sustained release.

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Abstract

The invention belongs to the technical field of biology, and particularly relates to a transdermally delivered ursolic acid / insulin nanoscale slow-release preparation and a preparation method thereof.The preparation consists of a backing layer, a medicine-carrying slow-release layer, and an anti-sticking layer, wherein the components of the medicine-carrying slow-release layer are ursolic acid, insulin, pressure-sensitive adhesive, penetration enhancer, substrate, hydrophilic excipient and freeze-drying protectant, and the medicine-carrying slow-release layer is sealed between the backing layer and the anti-sticking layer in the form of gel. The preparation can increase the bioavailability of insulin, enhance the stability of medicine, and can be slowly released to reduce blood sugar.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to a ursolic acid / insulin nano transdermal drug delivery preparation and a preparation method thereof. Background technique [0002] Insulin is a protein hormone secreted by insulin β cells, and it is currently the only hormone in the body that can lower blood sugar. Insulin has a molecular weight of 5700 and consists of two amino acid peptide chains. The A chain has 21 amino acids and the B chain has 30 amino acids. There are two disulfide bonds between the A-B chains. Insulin has a molecular weight of about 5800, an isoelectric point of 5.35-5.45, and is a white or off-white crystalline powder. Insulin is almost insoluble in water, ethanol, chloroform or ether, but easily soluble in mineral acid or sodium hydroxide solution. Insulin preparations on the market include injections, pulmonary inhalation preparations, implants, oral or oral mucosal absorption preparati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/28A61K38/28A61K31/56A61P3/10
CPCA61K9/7023A61K31/56A61K38/28A61K47/28A61K2300/00
Inventor 邵敬伟李超郭燕
Owner FUZHOU UNIV
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