Treatment process of cyclosporine eye gel

Abstract

The invention relates to the field of medicines, and discloses a treatment process of cyclosporine eye gel. The treatment process comprises the following steps: adding water into carbomer for full stirring and homogenization, swelling a prepared carbomer matrix, and performing stirring and homogenization; performing moist heat sterilization on the matrix, then cooling the matrix, and performing vacuumizing debubbling treatment; adjusting the pH of the matrix to 5.0 to 9.0 through a filtered sodium hydroxide solution; fully mixing castor oil polyoxyhydrocarbon ester (35), ciclosporin A raw material, 1,2-propylene glycol and water to prepare a clarified solution under a water bath condition at 35 to 45 DEG C; filtering the clarified solution, uniformly mixing filtrate with the matrix, and performing vacuumizing debubbling; performing filtration again and sterile filling. According to the process disclosed by the invention, before the carbomer is added, sterilization and filtration are performed, so that industrial production is facilitated; only partial germfree treatment is required; purchasing is facilitated, and the cost can be reduced; furthermore, thermal degradation of ciclosporin is avoided, and product impurities are reduced; all indexes are qualified through detection; the treatment process has a good industrial application prospect.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a treatment process for cyclosporine eye gel. Background technique [0002] Cyclosporin A is a cyclic polypeptide containing 11 amino acids extracted from fungi, and is a third-generation highly effective immunosuppressant that can be used to treat dry eye disease. [0003] For ophthalmic preparations, the state requires that they be managed as injections, so the sterility of the preparations is very important. At present, there are three main aspects of sterility assurance: sterilization and filtration process, aseptic process and terminal sterilization process. Cyclosporin is poorly soluble and thermally unstable, so the sterile preparation of cyclosporine is a difficult problem. [0004] At present, the following three methods are mainly used for aseptic treatment: purchasing aseptic raw materials and operating in a sterile environment; moist heat sterilization of the final product; ...

AI Technical Summary

Problems solved by technology

The first type is difficult to purchase qualified sterile raw and auxiliary materials, and the preparation process and workshop environment are all aseptic, the production cost is high and difficult; It is also better, but cyclosporine itself is not resistant to high temperature, which leads to more degradation impurities of cyclosporine, increases the safety risk of preparations, and produces side effects; the third terminal sterilization process for final products can only be used for small-scale process, It is difficult to produce commercially, because the viscosity of the emulsion gel is high, it is easy to block the filter membrane with small pore size, and the filtration is very slow, so the production efficiency is difficult to guarantee

[0005] Patent No. CN201410033737.3 "A Cyclosporine Eye Gel and Its Preparation Method", which disclosed the use of moist heat sterilization to ensure sterility, reproducible detection found that damp heat sterilization caused cyclosporine to produce degradation impurities

[0006] The patent No. CN201510785005.4 is "A Cyclosporine Ophthalmic Emulsion Composition", which uses sterile raw materials and excipients to prepare preparations. This process is very difficult to apply in industry

The patent number is CN201610172271.4 "Cyclosporin Ophthalmic Emulsion", which adopts the terminal sterilization and filtration of the prepared emulsion. For viscous emulsion, it is difficult to pass through a 0.22 micron sterile filter, so it does not have Operability

In summary, the various aseptic processes currently disclosed do not have the value and feasibility of commercial production

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