A novel j2-sodium alginate microsphere slow-release immunosuppressant for anti-graft immune rejection, preparation method and application

An immunosuppressant and sodium alginate technology, applied in the field of immunosuppressants, can solve the problems such as the inability of relatively uniform sustained release of drugs, the great individual differences in the degree of drug absorption, and the inability to effectively suppress immune rejection. Allergic reactions and various inconveniences, the effect of improving the level of treatment, and promoting development

Inactive Publication Date: 2011-11-30
BEIJING HONGYIYAO SCI & TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the clinically used immunosuppressants have the following defects: the drug cannot be released relatively uniformly; when the local perfusion drug concentration is too high, the shock wave effect of the drug may cause local tissue necrosis or damage; the absorption of the drug in the systemic application The degree varies greatly among individuals. When the dose is insufficient, immune rejection cannot be effectively suppressed, which may lead to treatment failure; when the dose is too large, it will cause many complications, such as severe infection, neurotoxicity, and microvascular thrombosis leading to important viscera. organ failure etc.
[0013] At present, there is no relevant information about using sodium alginate as a drug carrier to wrap J2 or (tacrolimus, sirolimus, mycophenolate mofetil, midazoribine, prednisone, methylprednisolone, cyclosporine A, cyclosporine Nipex, FTY720) immunosuppressants form microsphere slow-release implants, and are applied to the intervention (implantation) treatment and prevention of immune rejection of liver, kidney, lung, heart, skin and corneal transplantation patients.

Method used

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  • A novel j2-sodium alginate microsphere slow-release immunosuppressant for anti-graft immune rejection, preparation method and application

Examples

Experimental program
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Effect test

Embodiment 1

[0048] The method for preparing novel J2-sodium alginate microsphere slow-release immunosuppressant against graft immune rejection:

[0049] (1) Handling of glassware:

[0050] Air-dry the cleaned glassware, put it in a high-temperature oven and bake at 280 degrees Celsius for 3 hours (sterilize and remove heat source);

[0051] (2) Weigh the immunosuppressant J2, dissolve it with absolute ethanol or dimethyl sulfoxide at a concentration of 0.1-8.8% (mass volume percentage) of the drug, and obtain a drug solution;

[0052] (3) Weigh the sodium alginate, dissolve it with water for injection or physiological saline, and make it into a concentration of 1-6% (mass volume percentage) to obtain a sodium alginate solution;

[0053] (4) Divalent metal cation calcium is weighed, and described cation calcium is selected from calcium lactate, calcium chloride or barium chloride, is mixed with the solution of 1~15% (mass volume percent) concentration, obtains solidification liquid; Then ...

Embodiment 2

[0067] The method for preparing novel J2-sodium alginate microsphere slow-release immunosuppressant against graft immune rejection:

[0068] (1) Handling of glassware:

[0069] Air-dry the cleaned glassware, put it in a high-temperature oven and bake at 280 degrees Celsius for 3 hours (sterilize and remove heat source);

[0070] (2) Weigh the immunosuppressant J2, and dissolve it with absolute ethanol or dimethyl sulfoxide at a concentration of 0.3-8.8% (mass volume percentage) of the drug to obtain a drug solution;

[0071] (3) weigh sodium alginate, dissolve it with water for injection or physiological saline, and make it into a concentration of 1.5-6% (mass volume percentage) to obtain sodium alginate solution;

[0072] (4) Divalent metal cation calcium is weighed, and described cation calcium is selected from calcium lactate, calcium chloride or barium chloride, is mixed with the solution of 1.5~15% (mass volume percentage) concentration, obtains solidification liquid; Th...

Embodiment 3

[0084] The method for preparing novel J2-sodium alginate microsphere slow-release immunosuppressant against graft immune rejection:

[0085] (1) Handling of glassware:

[0086] Air-dry the cleaned glassware, put it in a high-temperature oven and bake at 280 degrees Celsius for 3 hours (sterilize and remove heat source);

[0087] (2) Weigh the immunosuppressant J2, dissolve it with absolute ethanol or dimethyl sulfoxide at a concentration of 0.5-8.8% (mass volume percentage) of the drug, and obtain a drug solution;

[0088] (3) Weigh the sodium alginate, dissolve it with water for injection or physiological saline, and make it into a concentration of 1.7-6% (mass volume percentage) to obtain a sodium alginate solution;

[0089] (4) Divalent metal cation calcium is weighed, and described cation calcium is selected from calcium lactate, calcium chloride or barium chloride, is mixed with the solution of 2~15% (mass volume percent) concentration, obtains solidification liquid; The...

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Abstract

The invention discloses a novel anti-transplantation immunological rejection J2-sodium alginate microsphere slow release immunosuppressive agent, a preparation method and application. The slow release immunosuppressive agent comprises a natural matrix material and is convenient for microsphere implantation. In the preparation, sodium alginate is used as a drug carrier, a J2 immunocompetent component is crosslinked, and the immunosuppressive agent is wrapped or adsorbed in microspheres through a microsphere liquid droplet generation device under the action of calcium ions. The preparation has targeting property to specific tissues and organs; the local action time of the drug can be prolonged; the bioavailability of the drug is improved; the toxic or side effect of a whole body can be reduced; and the immunosuppressive agent can be applied to immunosuppression of transplantation of heart, liver, kidney, lung, skin and cornea.

Description

technical field [0001] The invention relates to an immunosuppressant against transplantation immunity, especially a sodium alginate microsphere slow-release preparation of the compound immunosuppressant J2 against transplantation immune rejection, and also relates to a preparation method and application of the slow-release preparation. Background technique [0002] Although the historical development of immunosuppression is not long, it has achieved remarkable achievements in the field of organ transplantation. Immunotransplantation agents are used in organ transplantation to prevent rejection, ie, to interfere with recipient recognition of foreign antigens and clearance of non-self cells. The application of immune transplantation agents in organ transplantation has greatly improved the survival rate of transplant patients. At present, organ transplantation such as liver transplantation, kidney transplantation, corneal transplantation, skin transplantation, heart transplanta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/48A61K47/36A61K31/4045A61K45/00A61P37/06A61J3/00
CPCA61K9/19A61K31/404A61P37/06
Inventor 李新建洪宏
Owner BEIJING HONGYIYAO SCI & TECH DEV
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