Preparation process for cyclosporine A-pH sensitive nanoparticle

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...

AI Technical Summary

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-microemulsion preparation commonly used in clinical practice, can improve the oral absorption of CyA, the solubilizer CremophorRH40 contained in the self-microemulsion can cause severe nephrotoxicity and allergic reaction B1, so a new type of drug without CremophorRH40 was developed. CyA preparation has become a hot topic at home and abroad