Difluprednate suspension eye drops and preparation method thereof

Abstract

The invention discloses difluprednate suspension eye drops and a preparation method thereof. The difluprednate suspension eye drops comprise the following components in percentage by mass: 0.05-0.15% of difluprednate, 1-2.5% of modified collagen, 0.3-0.8% of medium-chain fatty glyceride, 0.2-0.8% of labrasol, 0.2-0.6% of polyoxyethylene hydrogenated castor oil, 2.2% of glycerol, 0.1% of benzalkonium chloride and the balance of deionized water. The modified collagen is prepared by putting collagen powder into a closed stirring container, introducing mixed steam of chlorine dioxide and nitrogen, continuously conducting stirring and synchronously carrying out ultraviolet irradiation. According to the eye drops, the retention time of the medicine in the eyes is remarkably prolonged by utilizing the adhesion of the modified collagen, compared with common eye drops, the administration frequency can be reduced, the medication compliance of an eye operation patient is improved, meanwhile, the eyes are always located in a high-concentration medicine microenvironment, and the treatment effect on eye infection symptoms can be enhanced.

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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