Sustained-release tacrolimus eye-drops preparation and preparation method thereof

A crolimus ophthalmic and tacrolimus technology, applied in the field of tacrolimus ophthalmic preparations and its preparation, can solve the problems of tacrolimus' poor solubility and stability, poor solubility in water, and restrictions on its wide application , to achieve the effect of simple and feasible preparation process, easy access to raw materials, and enhanced immune function

Inactive Publication Date: 2016-02-03
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The best way of topical ophthalmology is eye drops, but tacrolimus is insoluble in water and easily degraded in aqueous solution, which limits its wide application in clinical practice, especially in ophthalmology
[0005] Astragalus and / or Panax notoginseng are added as a mucoadhesive polymer drug delivery system, in which water and active molecule tacrolimus can be embedded to form a stable aqueous gel-like eye drop, which can solve the problem of tacrolimus in Poor solubility and stability in simple aqueous solution

Method used

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  • Sustained-release tacrolimus eye-drops preparation and preparation method thereof
  • Sustained-release tacrolimus eye-drops preparation and preparation method thereof
  • Sustained-release tacrolimus eye-drops preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0021] Embodiment 1-3 prepares sustained-release tacrolimus eye drops raw material components and consumption

[0022]

[0023] According to the technical scheme of the present invention, the optional auxiliary materials for preparing tacrolimus eye drops are not limited to the varieties listed in the above table, and there are also multiple choices, such as bacteriostatic agents, any bacteriostatic agents known in pharmacy can be used , and its dosage is according to the conventional dosage in pharmacy. For example, ① 0.002% ~ 0.005% thimerosal; ② quaternary ammonium salts (including benzalkonium chloride, benzalkonium bromide), dumiphene, spirityl, etc., the effective concentration is 0.002% ~ 0.01%; ③ alcohols, commonly used 0.3 ~ 0.6% chlorobutanol; ④ Parabens, commonly used 0.03-0.06% ethylparaben; ⑤ Acids, such as 0.01-0.08% tricolic acid. The concentrations of the above substances are all volume-weight percentages, that is, every 100 milliliters contains grams.

[...

Embodiment 4-6

[0025] Example 4-6 Preparation of Sustained-release Tacrolimus Ophthalmic Gel Raw Material Components and Consumption

[0026]

[0027] According to the technical solution of the present invention, the types of auxiliary materials that can be used to prepare tacrolimus ophthalmic gel are not limited to the types listed in the above table, and the following multiple options can also be selected:

[0028] Wherein, the kind selection and consumption of antibacterial agent are the same as embodiment 1~3.

[0029] The dosage ratio of the thickener to tacrolimus is 0.5-5.0:1.0.

[0030] The preparation method is as follows: dissolving the whole amount of tacrolimus with Astragalus notoginseng extract, dissolving the thickener with water for injection to disperse and let it cool, and dissolving the pH regulator and bacteriostat with water for injection, and adding the dissolved thickener The thickener and tacrolimus are supplemented with water for injection to the required volume...

Embodiment 7-9

[0031] Example 7-9 Preparation of sustained-release tacrolimus eye ointment raw material components and dosage

[0032]

[0033] Preparation method: Dissolve the whole amount of tacrolimus in astragalus notoginseng extract, add an appropriate amount of sterilized and cooled liquid paraffin, grind it into a fine paste, pass through a 200-mesh sieve, and then gradually add sterile and filtered lanolin, Yellow vaseline mixture, mix well, that is. All preparation equipment and packaging containers used must be sterilized.

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Abstract

The invention relates to a sustained-release tacrolimus eye-drops preparation. The sustained-release tacrolimus eye-drops preparation is characterized by being prepared from tacrolimus playing a pharmacological role, radix astragali and/or pseudo-ginseng serving as a mucosal adhesive polymer medicine release system, and pharmaceutically acceptable pharmaceutical adjuvants for local eyes, wherein by weight, 100 parts of sustained-release tacrolimus eye-drops preparation contains 0.01-1.0 part of tacrolimus, the weight ratio of the tacrolimus to the radix astragali and/or pseudo-ginseng is 1 to (0.5-5.0), and the weight ratio of the radix astragali to the pseudo-ginseng is 1 to 3. The sustained-release tacrolimus eye-drops preparation prepared by a preparation method has the advantages of good intraocular penetration, high intraocular bioavailability, little toxic or side effect and capabilities of treating and preventing ophthalmic immune-related diseases such as autoimmune uveal retinitis.

Description

technical field [0001] The invention belongs to the field of medicines, and more specifically relates to a tacrolimus ophthalmic preparation and a preparation method thereof. Background technique [0002] Tacrolimus, also known as FK506, is a fermentation product isolated from Streptomyces tsukubaensis, and its chemical structure is a 23-membered macrolide antibiotic. It is a powerful new type of immunosuppressant, mainly by inhibiting the release of interleukin-2 (L-2), and comprehensively inhibits the effect of T lymphocytes, which is 100 times stronger than cyclosporine (CsA). It is practically insoluble in water, freely soluble in ethanol, and readily soluble in methanol and chloroform. [0003] Tacrolimus is a macrolide compound with useful immunosuppressive activity, antimicrobial activity, and other pharmacological activities, and is useful for organ or tissue transplant rejection, graft-versus-host disease, autoimmune disease, and infection valuable in the treatmen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/46A61K31/436A61K36/481A61K36/258A61P27/02A61P37/06A61P27/14
Inventor 姚向超王海英王延东李晓纯吴绮峰曹琛
Owner GUANGDONG WHOLEWIN TECH
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