Method for preparing ophthalmic preparation containing tacrolimus

A technology of tacrolimus and ophthalmic preparations, which is applied in the field of preparation of ophthalmic preparations, can solve problems such as obvious foreign matter, stinging or burning sensation, difficulty in controlling quality standards, complicated preparation process, etc., and achieves prolonged residence time, no Toxic and side effects, good solubility

Inactive Publication Date: 2009-09-02
ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
View PDF0 Cites 15 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In the prior art, tacrolimus eye drops use tacrolimus injection as a raw material. After the ethanol is removed, a solvent is added to dissolve it. The preparation process is complicated, the quality standard is difficult to control, and the stability is poor. Can be stored

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing ophthalmic preparation containing tacrolimus
  • Method for preparing ophthalmic preparation containing tacrolimus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028]The eye drops, in 100 milliliters, contain 0.01 grams of tacrolimus, 0.02 milliliters of absolute ethanol, 0.01 milliliters of Tween-800.01 milliliters, 0.03 grams of polyethylene glycol hydrogenated castor oil (10 grams of polyethylene glycol hydrogenated castor oil Sesame oil is about 10ml), glycerin 0.015ml, sodium citrate 0.05g, thimerosal 0.002g, pH value 5.5-7.5; also contains hypromellose 0.3g, or sodium hyaluronate 0.1g.

[0029] Preparation method: first dissolve 0.3 g of hypromellose or 0.1 g of sodium hyaluronate with an appropriate amount of water for injection; take 0.01 g of tacrolimus, dissolve it in 0.02 ml of absolute ethanol, add 0.03 g of polyethylene glycol hydrogenated castor oil G, Tween-800.01 ml dissolved in water for injection, add 0.015 ml of glycerin, 0.05 g of sodium citrate, 0.002 g of thimerosal, add 0.3 g of dissolved hypromellose, or 0.1 g of sodium hyaluronate , add water for injection to the required volume, and adjust the pH value to 5....

Embodiment 2

[0031] The eye drops, in 100 ml, contain 0.02 g of tacrolimus, 0.2 ml of absolute ethanol, 0.1 ml of Tween-800.1 ml, 0.3 g of polyethylene glycol hydrogenated castor oil, 0.15 ml of glycerin, and an appropriate amount of sodium hydroxide , 0.03 grams of ethyl paraben, pH value of 5.5 to 7.5; also contains 0.3 grams of hypromellose, or 0.1 grams of sodium hyaluronate.

[0032] Preparation method: first dissolve 0.3 g of hypromellose or 0.1 g of sodium hyaluronate with appropriate amount of water for injection; dissolve 0.03 g of ethylparaben with appropriate amount of hot water for injection. Take 0.02 g of tacrolimus, dissolve it in 0.2 ml of absolute ethanol, add 0.3 g of polyethylene glycol hydrogenated castor oil, Tween-800.1 ml to dissolve in water for injection, add 0.15 ml of glycerin, and add the dissolved hydroxyl 0.3 g of propyl methylcellulose, or 0.1 g of sodium hyaluronate, add water for injection to the required volume, adjust the pH value to 5.5-7.5 with an appro...

Embodiment 3

[0035] The eye drops, in 100ml, contain 0.05g of tacrolimus, 1.0ml of absolute ethanol, 0.3ml of Tween-800.3ml, 1.2g of polyethylene glycol hydrogenated castor oil, 0.5ml of glycerin, sodium citrate 2.0 grams, 0.002 grams of thimerosal, pH value of 5.5 to 7.5; also contains 0.3 grams of hypromellose, or 0.1 grams of sodium hyaluronate.

[0036] Preparation method: first dissolve 0.3 g of hypromellose or 0.1 g of sodium hyaluronate with an appropriate amount of water for injection; take 0.05 g of tacrolimus, dissolve it in 1.0 ml of absolute ethanol, add polyethylene glycol hydrogenated castor oil 1.2 G, Tween-800.3 ml dissolved in water for injection, add 0.5 ml of glycerin, 2.0 g of sodium citrate, 0.002 g of thimerosal, add 0.3 g of dissolved hypromellose, or 0.1 g of sodium hyaluronate gram, add water for injection to the required volume, and adjust the pH value to 5.5-7.5; then use a 0.2 μm microporous membrane to filter and sterilize, and pack it into 2 ml / support to obta...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses a method for preparing a preparation containing tacrolimus, which comprises the following steps of: using absolute ethyl alcohol to dissolve the tacrolimus first wherein the mass ratio range of the tacrolimus and the alcohol is 0.01-0.5g: 0.01-2ml; adding a solubilizing agent and/or a stabilizing agent which is dissolved in water for injection; then adding a thickening agent and/or a bacteriostat, and supplementing the water for injection to the needed volume; or then adding a well-dissolved eye ointment matrix to obtain the preparation containing the tacrolimus. The preparation containing the tacrolimus prepared by the method has the advantages of good solubility, small irritation, stable characteristics, no toxic side effect, and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of ophthalmic preparations containing tacrolimus. Background technique [0002] Tacrolimus (FK506) is a new type of potent immunosuppressant. It was successfully used in the treatment of liver transplantation rejection in 1989, which greatly reduced the incidence of rejection and significantly reduced the dosage of hormones, thereby reducing the related side effects of hormone therapy. dangerous. The immunosuppressive effect of FK506 is 30-100 times stronger than that of cyclosporine A, and the therapeutic dose is 100 times lower than that of cyclosporine A. At present, FK506 is used to prevent and treat immune rejection after various organ transplants and for the treatment of autoimmune diseases. It has become the first choice for treatment of refractory rejection or cyclosporine A side effects. The initial dose of treatment is 0.15mg / ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K9/06A61K31/436A61K47/44A61K47/34A61K47/38A61P37/06A61P27/02A61K47/26
Inventor 陈家祺袁进葛坚叶成添翟嘉洁
Owner ZHONGSHAN OPHTHALMIC CENT SUN YAT SEN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap