Recombinant hirudin eye drop and preparation method thereof

Abstract

The invention discloses a recombinant hirudin eye drop. The recombinant hirudin eye drop takes recombinant hirudin as an effective component and sodium hyaluronate as a thickening agent, and also contains an isoosmotic adjusting agent, a metal complexing agent, a preservative and a pharmaceutically acceptable carrier; and the mass ratio of the sodium hyaluronate to the recombinant hirudin to the isoosmotic adjusting agent to the metal complexing agent to the preservative in the eye drop is 10 to 2 to 15.27 to 50 to 3. The preparation method comprises the following steps: dissolving the sodium hyaluronate, the isoosmotic adjusting agent, the metal complexing agent and the preservative into the pharmaceutically acceptable carrier to prepare a blank matrix of the eye drop, dissolving the recombinant hirudin into the blank matrix of the eye drop, mixing evenly, filtering, degerming and sub-packaging to prepare the recombinant hirudin eye drop. According to the eye drop disclosed by the invention, on one hand, the recombinant hirudin can be retainedin a focal zone for a long period of time; on the other hand, irritation is not generated to sensitive eye tissues; and meanwhile, the storage stability of the recombinant hirudin eye drop can also be ensured.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to a recombinant hirudin eye drop and a preparation method thereof. Background technique [0002] Hirudin is a kind of polypeptide substance composed of 65-66 amino acids that was originally isolated from the salivary glands of medical leeches. There are mainly three isomers with high homology (HV1, HV2, and HV3). Hirudin can effectively inhibit the formation of arterial and venous thrombosis and disseminated intravascular coagulation (DIC) by directly inhibiting the activity of thrombin. Therefore, hirudin is effective in preventing and treating deep venous thrombosis, coronary artery thrombosis, and angina pectoris. It has high application value. [0003] At present, there are two recombinant hirudin products approved for marketing abroad: 1. Desirudin (trade name: Revasc, product of Novartis, Switzerland); 2. Lepirudin (trade name: Refludan, product of British Pharmion and Ame...

AI Technical Summary

Problems solved by technology

Additionally, some of these thickeners are Newtonian, painful to blink, and sensitive to pH and / or temperature, while others have more incompatibility issues

For example, poloxamer temperature-sensitive gel, although it can change from liquid phase to semi-solid above 25 ° C, but when it returns to low temperature, the semi-solid gel is difficult to return to liquid state, so it is used for mass production of other gels. Process is difficult to control

In addition, carbomer gel can reduce its viscosity due to salt electrolytes, alkaline earth metal ions and cationic polymers can also be combined with it to form insoluble salts, and strong acids can also make it lose its viscosity. Multiple incompatibility

Cellulose derivatives such as hypromellose, polyvinyl alcohol, and polyvinylpyrrolidone are used as thickeners for eye drops. The main disadvantage is that they belong to Newtonian fluids, and their viscosity increases with the increase of concentration but is not subject to shear. Influenced by force (such as shear force when blinking), sometimes in order to produce obvious thickening effect, it must be added to a certain concentration, but when the viscosity reaches a certain level, it will make the eyelids difficult to blink and sensitive to the eye tissue Irritating, unbearable to the user

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