A kind of difluprednate suspension eye drops and preparation method thereof

Abstract

The invention discloses a difluprednate suspension eye drop and a preparation method thereof, which comprises 0.05-0.15% of difluprednate, 1-2.5% of modified collagen, and 0.3-0.3% of medium-chain fatty acid glycerides according to mass percentage. 0.8%, caprylic capric acid macrogol glyceride 0.2-0.8%, polyoxyethylene hydrogenated castor oil 0.2-0.6%, glycerin 2.2%, benzalkonium chloride 0.1%, the balance is deionized water; modified collagen It is prepared by putting collagen powder into a closed stirring container, passing through the mixed steam of chlorine dioxide and nitrogen, stirring continuously, and synchronously irradiating ultraviolet rays. The present invention utilizes the adhesion of modified collagen to significantly prolong the residence time of the drug in the eye. Compared with ordinary eye drops, it can not only reduce the frequency of administration and improve the drug compliance of patients undergoing eye surgery, but also make the eye Consistent exposure to a higher concentration of the drug microenvironment enhances the therapeutic effect on ocular infection symptoms.

Description

technical field [0001] The invention belongs to the field of ophthalmic preparations, in particular to a difluprednate suspension eye drop and a preparation method thereof. Background technique [0002] Difluprednate is a difluorinated derivative of the corticosteroid prednisolone, which has strong anti-inflammatory and analgesic effects. In 2006, Sirion obtained the authorization of ophthalmic emulsion from Senshou Pharmaceutical Co., Ltd. of Japan. The phase III clinical trial of difluprednate ophthalmic emulsion has obtained positive results. In this trial, the drug can quickly resolve ocular inflammation after ophthalmic surgery, and is safe and effective. The unique structure of the drug enables the drug ingredients to quickly enter the steroid stratum corneum, which can quickly resolve the inflammation of the anterior chamber cells and the flash of the anterior humor. [0003] Difluprednate is a fat-soluble drug, and its solubility in water is not good. It can be made...

AI Technical Summary

Problems solved by technology

The ordinary difluprednate ophthalmic emulsion marketed abroad needs to be dripped 4 times a day at the beginning of use to ensure the maintenance of a high drug concentration in the eye. For patients with poor medication compliance, because the eyelids will be pulled during administration, more frequent administration does not take advantage of the healing of eye surgery wounds, and it also increases the risk of wound infection. Increased workload of medical staff

Patent CN200910015868.8 provides an ophthalmic or ear nose composition containing difluprednate and levofloxacin, and patent CN201210259768.1 provides a redispersible glucocorticoid ophthalmic suspension, using glucocorticoid (including difluprednate, etc.), preservatives (boric acid, benzalkonium chloride, benzethonium chloride, sorbic acid, potassium sorbate, etc.), pH regulators (sodium acetate, phosphoric acid and its salts, etc.), surface active Agents (Tween 80, carbomer, polyoxyethylene castor oil 60, polyoxyethylene hydrogenated castor oil 60, polyethylene glycol stearate), various fatty oils (castor oil, etc.), glycerin and other conventional The raw materials are mixed, however, according to the test method of the simulated clinical surgical incision of the model rabbit in the instruction manual, continuous administration is required for 7 days, 4 times / day, 2 drops / time; analogy to human patients, the frequency of administration is also very high

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