Tacrolimus ophthalmic emulsion and its preparation method

A technology of tacrolimus and emulsion, applied in the field of tacrolimus ophthalmic emulsion and its preparation, can solve problems such as toxic and side effects of human body, and achieve good biocompatibility, good repeatability, good social and economic benefits. Effect

Inactive Publication Date: 2010-02-24
宋洪涛
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] The purpose of the present invention is to provide a kind of tacrolimus ophthalmic emulsion and preparation method thereof, to solve the problem that tacrolimus is oral preparation and injection in the prior art and bring relatively big toxic side effect to human body etc., tac

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  • Tacrolimus ophthalmic emulsion and its preparation method
  • Tacrolimus ophthalmic emulsion and its preparation method
  • Tacrolimus ophthalmic emulsion and its preparation method

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[0020] The preparation method of the tacrolimus ophthalmic emulsion of the present invention: it is prepared by ultrasonic shearing emulsification or shearing high-pressure homogenization process, and its operation steps are: (1) Weigh the oil phase and antioxidant and stir evenly, and use it as a solution① ;

[0021] (2) Add emulsifier and auxiliary emulsifier into the solution ①, heat to 70°C, stir until the emulsifier and auxiliary emulsifier are completely dissolved, add tacrolimus, continue heating and stirring until tacrolimus is completely dissolved, as Solution ②;

[0022] (3) Add the osmotic pressure regulator and preservative into water, heat to 70°C, stir, and make a solution ③;

[0023] (4) Slowly drip the solution ② into the solution ③ under magnetic stirring, then stir for 5-10 minutes after the dripping, transfer to a high-shear dispersing emulsifier, 10000r·min -1 High-speed dispersion to form colostrum;

[0024] (5) The colostrum is then ultrasonically shea...

Embodiment 1

[0030] Preparation Process:

[0031] Weigh castor oil, MCT, and vitamin E and stir evenly to make solution ①. Add the prescribed amount of egg yolk lecithin (S100) into ①, heat to 70°C, stir until the egg yolk lecithin is completely dissolved, then add tacrolimus, continue heating and stirring until tacrolimus is completely dissolved, and make solution ②. Add glycerin and benzalkonium bromide into an appropriate amount of water and heat to 70°C to form a solution ③. Slowly drop the solution ② into the solution ③ under magnetic stirring, then stir for 5 minutes after the dripping, transfer to a high-shear dispersing emulsifier, 10000r·min -1 Disperses at high speed to form colostrum. The colostrum was homogenized by ultrasonic shearing for 10 minutes to obtain the final milk. Dilute with water for injection and dilute to the prescribed volume, with 0.1mol L -1 Sodium hydroxide is used to adjust the pH value to 7.0-8.0. Filter the prepared emulsion with a 220-mesh si...

Embodiment 2

[0034] Preparation Process:

[0035] Weigh olive oil and vitamin E and stir well to make solution ①. Add the prescribed amount of soybean lecithin into ①, heat to 70°C, stir until the soybean lecithin is completely dissolved, then add tacrolimus, continue heating and stirring until the tacrolimus is completely dissolved, and make solution ②. Add glycerin and phenylmercury acetate into an appropriate amount of water, heat to 70°C, and make a solution ③. Slowly drop the solution ② into the solution ③ under magnetic stirring, then stir for 5 minutes after the dripping, transfer to a high-shear dispersing emulsifier, 10000r·min -1Disperses at high speed to form colostrum. The colostrum is then homogenized by a high-pressure homogenizer to obtain the final milk. Dilute with water for injection to the prescribed volume, and adjust the pH value to 8.0-8.5 with phosphate buffer. Filter the prepared emulsion with a 220-mesh sieve cloth, fill it with nitrogen, sterilize it, a...

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Abstract

The invention provides a tacrolimus ophthalmic emulsion and its preparation method, which belongs to the medicine preparation technical field and solve the problems of high toxic and side effects of tacrolimus oral preparation and injection to human body in the prior art. The emulsion is composed of tacrolimus, oil phase, an emulsifier, an auxiliary emulsifier, an osmotic pressure modifying agent,an antioxidant, a preservative, a pH modifying agent and an injection water, is prepared by an ultrasonic shearing emulsification or shearing-high pressure homogenization technology and is applied totreatment of ophthalmic corneal allograft rejection, keratoconjunctivitis sicca (KC) and ophthalmic anaphylactic disease. The invention prepares the tacrolimus into the ophthalmic emulsion for the first time, has the advantages of good biological compatibility, low stimulation to eyes and no toxic and side effects in the long-term application and can be applied clinically with wide development prospects.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a tacrolimus ophthalmic emulsion and a preparation method thereof. Background technique: [0002] Corneal disease caused by various reasons is currently the most important blinding corneal disease in China, and the number of patients is more than one million every year. Corneal transplantation is the most important method to treat such diseases, and immune rejection after corneal transplantation is The big problem right now. Glucocorticoids are the main means to prevent and treat postoperative graft rejection, but their long-term application can not only lead to many complications, but also often cannot effectively inhibit the rejection of high-risk keratoplasty. In recent years, cyclosporine A has been more and more widely used in ophthalmology, but the solvent of cyclosporine eye drops is oily, and it is very irritating to the eyes after it is instilled into the eyes. ...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/439A61K47/14A61K47/24A61K47/26A61K47/34A61P27/02A61P37/06A61K47/10
Inventor 宋洪涛王娟何仲贵唐星张晶周欣
Owner 宋洪涛
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