Preparation process for cyclosporine A-pH sensitive nanoparticle

A preparation process and sensitive technology, applied in the field of chemistry, can solve the problems of low oral bioavailability, renal toxicity, allergic reaction B1, and large individual differences of ordinary preparations, and achieve high conversion rate, high yield, and low energy consumption Effect

Inactive Publication Date: 2015-03-25
李志刚
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Problems solved by technology

However, the irreversible nephrotoxicity of CyA affects 80% of transplant patients; its strong lipophilicity, coupled with the influence of extensive efflux mechanism and biotransformation in the body, make its oral bioavailability of common preparations low, and individual differences are large
Although Neoral, a self-microemulsi

Method used

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Embodiment Construction

[0011] The preparation process of cyclosporin A-pH sensitive nanoparticles of the present invention adopts the following steps.

[0012] Weigh F68 and dissolve it in 125mL distilled water as the water phase; take another 50mgCyA and appropriate amount of EudragitS100 and dissolve it in absolute ethanol to make the organic phase; quickly inject the organic phase into the water phase stirred at 400r min with a No. 7 bone marrow puncture needle; Afterwards, keep stirring and transfer to a 60°C water bath to evaporate the organic solvent to obtain a CyA-NP colloidal solution.

[0013] In the impact on CyA. On the basis of the investigation of formulation factors of NP encapsulation efficiency, particle size and span, three main factors were determined: drug to carrier material Eudragit S100 mass ratio (drug loading ratio) (A), oil-water ratio (B), and F68 mass concentration (C) , using an orthogonal design table L. (34) Arrange experiments and optimize the prescription pro...

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Abstract

Belonging to the field of chemical technologies, the invention relates to a preparation process for a cyclosporine A-pH sensitive nanoparticle, and more specifically relates to improvement of the preparation process of the cyclosporine A-pH sensitive nanoparticle. The preparation process for the cyclosporine A-pH sensitive nanoparticle is characterized by low cost and high synthesis rate, and the product has good intestinal absorption effect. The preparation process for the cyclosporine A-pH sensitive nanoparticle includes the steps of: weighing F68 and dissolving it in 125mL distilled water to serve as the water phase; dissolving 50mg of CyA and a proper amount of EudragitS100 in anhydrous ethanol to prepare an organic phase; injecting the organic phase into the water phase stirred at a speed of 400r.min with a No. 7 support marrow puncture needle quickly; and then conducting stirring continuously and transferring the mixture into 60DEG C water bath, and volatilizing the organic solvent completely, thus obtaining a CyA-NP colloidal solution.

Description

technical field [0001] The invention belongs to the technical field of chemistry, and more specifically, the invention relates to an improvement of a preparation process of cyclosporin A-pH sensitive nanoparticles. Background technique [0002] Cyclosporin A (CyA), as a potent immunosuppressant, has been successfully used in clinical solid organ transplantation and bone marrow transplantation, to prevent and treat rejection, and has good curative effect on various autoimmune diseases. A drug that changed the face of transplant medicine. However, the irreversible nephrotoxicity of CyA affects 80% of transplant patients; its strong lipophilicity, combined with the influence of extensive efflux mechanism and biotransformation in the recipient, makes its oral bioavailability of common preparations low and individual differences are large. Although Neoral, a self-microemulsion preparation commonly used in clinical practice, can improve the oral absorption of CyA, the solubilizer...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/08A61K38/13A61K47/32A61P37/06
Inventor 李志刚冯明煦周鹏涛
Owner 李志刚
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