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Preparation and application of polymer composition loaded with sirolimus compound or its derivative

A technology of sirolimus and polymers, which is applied in the field of nano-medicine preparation, can solve problems such as disapproval of using the human body, inability to release smoothly, and increased side effects

Inactive Publication Date: 2013-09-11
单颖
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, CN200510105774.1, CN101532662B, US8053444B2, US6004973, US6197781, and US2003 / 000835 all adopt solid dispersion technology to prepare sirolimus preparations, but the solubility of sirolimus is only improved, and cannot be released stably, and does not solve the problem of sirolimus preparations. The problem of narrow therapeutic window of rolimus, and it is just close to the release of the reference preparation nanochip released in vitro, so its bioavailability will not exceed 27%, and the problem of low bioavailability has not been fundamentally solved
CN1919194A adopts the self-emulsification technology similar to cyclosporine soft capsules to prepare the liquid composition of sirolimus. Although the oral bioavailability is improved, the gastrointestinal discomfort caused by a large amount of surfactants cannot be ignored , its side effects are also greatly improved
CN101032463A has adopted organic solvent plus cosolvent polyvinylpyrrolidone or hydroxypropyl beta cyclodextrin, nicotinamide to prepare sirolimus injection, but clinically for polyvinylpyrrolidone or hydroxypropyl beta cyclodextrin, nicotinamide in vein The use of injections is very cautious. Due to its various safety problems such as hemolysis, it is generally not approved to be used in humans
For scar repair, CN101094650A, CN101014299A, reported the use of biodegradable polymer carrier materials, dissolved by organic solvents, the drug is dissolved in the solution of the carrier and the solvent, and then the organic solvent is volatilized, and the drug is evenly dispersed in the carrier material. The principle is the same as that of solid dispersion technology. Although the drug can be slowly released from the carrier, the drug is not easy to enter the blood and cell tissue; the effect is not ideal

Method used

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  • Preparation and application of polymer composition loaded with sirolimus compound or its derivative
  • Preparation and application of polymer composition loaded with sirolimus compound or its derivative
  • Preparation and application of polymer composition loaded with sirolimus compound or its derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] 100mg of methoxypolyethylene glycol-poly(ε-caprolactone) copolymer (MPEG 2000 -PCL 2000) and 15 mg of sirolimus were dissolved in 3 ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5 ml of preheated water for injection was added, under stirring conditions, 60 ° C into bundles, and passed through a 0.22 μm filter membrane, The filtrate was lyophilized to obtain a sample.

Embodiment 2

[0048] 100mg of methoxypolyethylene glycol-polylactic acid copolymer (MPEG 2000 -PLA 1700 ) and 15 mg of sirolimus were dissolved in 3 ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5 ml of preheated water for injection was added, under stirring conditions, 60 ° C into bundles, and passed through a 0.22 μm filter membrane, The filtrate was lyophilized to obtain a sample, see figure 1 , the transmission electron microscope spectrum of nanomicelle solution is shown in figure 2 .

[0049] Twelve SD rats were randomly divided into two groups, 6 in each group, Temsirolimus micelle and Temsirolimus injection Sirolimus injection group. The two groups of experimental animals were injected with sirolimus nanomicelle and sirolimus injection respectively through the tail vein, and the blood was collected by docking the tail at 0.083, 0.5, 1, 2, 4, 6, 8, 10, 12, and 24 hours after administration , the blood sample was centrifuged at...

Embodiment 3

[0058] 100mg of polycaprolactone-polyethylene glycol-polycaprolactone copolymer (PCL 800 -PEG 2000 -PCL 800 ) and 15 mg of sirolimus were dissolved in 3 ml of absolute ethanol, the organic solvent was quickly removed under reduced pressure, and then 5 ml of preheated water for injection was added, under stirring conditions, 60 ° C into bundles, and passed through a 0.22 μm filter membrane, The filtrate was lyophilized to obtain a sample.

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Abstract

The invention relates to a polymer composition loaded with a sirolimus compound or its derivative. The composition can have diversified forms. A necessary link includes preparing the sirolimus compound or its derivative and a polymer carrier into a micelle. Then according to needs, the micelle can be further prepared into a freeze-dried composition by a freeze-drying technology, or the micelle and other polymer and carrier can be prepared into a solid or semi-solid preparation. The polymer composition can be used for treating tumors, reducing rejection reactions after organ and tissue transplantation, promoting cell regeneration and repair, preventing excessive scar tissue growth after injury and preventing vascular restenosis and blood coagulation embolism, treating or inhibiting autoimmune diseases, and treating or inhibiting inflammation, etc.

Description

field of invention [0001] The invention relates to the preparation of a nano-medicine, and using the nano-medicine as a starting material for tumor treatment, organ transplantation anti-rejection, scar repair, prevention of vascular stenosis and coagulation embolism, treatment or inhibition of autoimmune diseases, inflammation, etc. The application of the present invention belongs to the field of pharmaceutical technology. Background technique [0002] 1. Background on Sirolimus [0003] Sirolimus is an immunosuppressive macrolide produced by Streptomyces hygroscopicus. The chemical name of sirolimus (also known as rapamycin) is (3S, 6R, 7E, 9R, 10R, 12R, 14S, 15E, 17E, 19E, 21S, 26R, 27R, 34aS)-9, 10, 12,13,14,21,22,23,24,25,26,27,32,33,34,34a-hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[( 1S, 3R, 4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-six Methyl-23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazepine-hentriacotine-1,5,11,28,29(4H,6H,31H)-5 ke...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/19A61K31/436A61K47/34A61P35/00A61P37/06A61P17/02A61P9/00A61P7/02A61P29/00
Inventor 单颖
Owner 单颖
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