Rapamycin self-microemulsion injection as well as preparation method and application thereof

A technology of rapamycin and self-microemulsion, which is applied in the application field of rapamycin self-microemulsion injection, can solve the problems of low solubility and poor stability, and achieve improved solubility, stability, safety and stability Excellent effect

Pending Publication Date: 2022-04-19
严鹏科
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The first purpose of the present invention is to provide a self-microemulsion injection of rapamycin, which sol...

Method used

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  • Rapamycin self-microemulsion injection as well as preparation method and application thereof
  • Rapamycin self-microemulsion injection as well as preparation method and application thereof
  • Rapamycin self-microemulsion injection as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A self-microemulsion injection of rapamycin is composed of a drug mother solution and a diluent; the drug mother solution and the diluent respectively include the following formula components:

[0038] a. Drug mother solution

[0039]

[0040]

[0041] b. Thinner

[0042]

[0043] The above-mentioned rapamycin self-microemulsion injection, specific preparation steps:

[0044] (1) Mix 0.5 ml of absolute ethanol and 0.5 ml of polyethylene glycol 400 solution to obtain a mixed solution, add rapamycin to the mixed solution, then add 0.5 μg of antioxidant and 2.5 μg of anhydrous citric acid, Obtain the drug mother solution of 20mg / ml;

[0045] (2) Configure diluent: Measure 0.8ml of polyethylene glycol-15 hydroxystearate, 0.2ml of absolute ethanol, 1.0ml of water for injection, mix well and add 0.008g metal chelating agent, mix well to obtain diluent .

[0046] (3) Separately filter and sterilize the mother liquor of the medicine and the diluent, and then seal a...

Embodiment 2

[0048] A self-microemulsion injection of rapamycin is composed of a drug mother solution and a diluent; the drug mother solution and the diluent respectively include the following formula components:

[0049] a. Drug mother solution

[0050]

[0051]

[0052] b. Thinner

[0053]

[0054] The above-mentioned rapamycin self-microemulsion injection, specific preparation steps:

[0055] (1) Mix 0.5ml of absolute ethanol and 0.5ml of polyethylene glycol 300 solution to obtain a mixed solution, add rapamycin to the mixed solution, then add 0.5 μg of antioxidant, 2.5 μg of anhydrous citric acid, Obtain the drug mother solution of 20mg / ml;

[0056] (2) Configure diluent: Measure 0.8ml of polyethylene glycol-10 hydroxystearate, 0.2ml of absolute ethanol, 1.0ml of water for injection, mix well and add 0.004g metal chelating agent, mix well to obtain diluent .

[0057] (3) Separately filter and sterilize the mother liquor of the medicine and the diluent, and then seal and stor...

Embodiment 3

[0059] A self-microemulsion injection of rapamycin is composed of a drug mother solution and a diluent; the drug mother solution and the diluent respectively include the following formula components:

[0060] a. Drug mother solution

[0061]

[0062]

[0063] b. Thinner

[0064]

[0065] The above-mentioned rapamycin self-microemulsion injection, specific preparation steps:

[0066] (1) Mix 0.5ml of absolute ethanol and 0.5ml of polyethylene glycol 400 solution to obtain a mixed solution, add rapamycin to the mixed solution, then add 0.1 μg of antioxidant and 5 μg of anhydrous citric acid to obtain 10mg / ml drug mother solution;

[0067] (2) Configure diluent: Measure 0.8ml of polyethylene glycol-15 hydroxystearate, 0.2ml of absolute ethanol, 1.0ml of water for injection, mix well and add 0.005g metal chelating agent, mix well to obtain diluent .

[0068] (3) Separately filter and sterilize the mother liquor of the medicine and the diluent, and then seal and store ...

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PUM

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Abstract

The invention provides a rapamycin self-microemulsion injection. The rapamycin self-microemulsion injection consists of a medicine mother solution and a diluent, the medicine mother liquor comprises a medicine solvent, an antioxidant and rapamycin; the diluent comprises a surfactant and water. The rapamycin self-microemulsion injection provided by the invention consists of a medicine mother solution and a diluent, the rapamycin is dissolved in the drug solvent, after the diluent and the mother liquor are mixed and diluted, the liquid is self-assembled to form the micro-emulsion under the action of the surfactant, and meanwhile, the rapamycin is encapsulated in the micro-emulsion, so that the solubility of the rapamycin is improved, and the stability of the rapamycin is also improved.

Description

technical field [0001] The present invention specifically relates to a rapamycin self-microemulsion injection, a preparation method of the rapamycin self-microemulsion injection, and an application of the rapamycin self-microemulsion injection. Background technique [0002] Rapamycin (molecular weight: 914.2), also known as sirolimus, is a macrolide compound with immunosuppressive activity and is used as an inhibitor of transplant rejection in organ transplant patients. Moreover, it has been reported that rapamycin not only has the function of immunosuppressant, but also has the function of inducing cell death and destroying cancer cells. It has been confirmed that rapamycin has anti-tumor activity, and the compound has high anti-tumor activity in vitro, but the in vivo experimental results of oral use are usually not ideal, which may be related to the fact that rapamycin is insoluble in water, and its bioavailability low correlation. Based on this, there are a large numbe...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/436A61K47/10A61K47/14A61K47/12A61K47/20A61K47/22A61P37/06A61P35/00
CPCA61K9/0019A61K9/1075A61K31/436A61K47/10A61K47/14A61K47/12A61K47/20A61K47/22A61P37/06A61P35/00
Inventor 严鹏科
Owner 严鹏科
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