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Tacrolimus ophthalmic preparation and preparation method thereof

A crolimus eye and preparation technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. Demand and other issues, to achieve the effect of good compliance, accurate dosing, and low eye irritation

Active Publication Date: 2018-04-20
SHENYANG XINGQI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the above two emulsions have solved the solubility problem of the drug, terminal sterilization must be used to achieve product sterility
However, in our actual research process, we found that terminal sterilization will lead to a substantial increase in the degradation products of tacrolimus in the product, which cannot meet the clinical needs of ophthalmic preparations
[0008] In conclusion, the above-mentioned products and existing technologies fail to solve the problems of uniform administration of tacrolimus ophthalmic preparation system, stable bioavailability and product sterility assurance

Method used

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  • Tacrolimus ophthalmic preparation and preparation method thereof
  • Tacrolimus ophthalmic preparation and preparation method thereof
  • Tacrolimus ophthalmic preparation and preparation method thereof

Examples

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Effect test

Embodiment 1

[0050] Prepare the ophthalmic preparation of the present invention according to the corresponding prescription proportioning in Table 1.

[0051] Preparation method: (1) Take an appropriate amount of water for injection and add the prescribed amount of sodium hyaluronate, fully swell for later use; (2) Mix the prescribed amount of MCT, Tween80 and polyethylene glycol evenly, add the prescribed amount of tacrolimus, fully dissolve, and set aside; (3) Take an appropriate amount of water for injection, and dissolve the prescribed amount of glycerin and benzalkonium chloride sequentially; (4) mix the solutions obtained from (2) and (3) and stir thoroughly to obtain a clear solution; (5) mix the sodium hyaluronate solution obtained from (1) with the solution obtained from (4) evenly; (6) Add water for injection to the solution obtained in (5) to 100ml, stir evenly, and adjust the pH value to 5.0 if necessary. (7) Filter and sterilize the obtained medicinal solution through a 0.22 μ...

Embodiment 2~ Embodiment 4

[0053] Prepare the ophthalmic preparation of the present invention according to the corresponding prescription proportioning in Table 1.

[0054] The preparation method is the same as in Example 1. Wherein, without changing the dissolving sequence of surfactant osmotic pressure regulator and osmotic pressure regulator, the type of osmotic pressure regulator and surfactant is replaced according to the preparation method of Example 1; for the prescription without adding sodium hyaluronate, omit the example 1 Step (1) in the preparation method.

[0055] Table 1 Prescription ratio

[0056]

Embodiment 5~ Embodiment 8

[0058] Prepare the ophthalmic preparation of the present invention according to the corresponding prescription proportioning in Table 2.

[0059] Preparation method: (1) Take an appropriate amount of water for injection and add the prescribed amount of sodium hyaluronate to fully swell for later use; (2) Add the prescribed amount of MCT, Solutol ® Mix HS15 and polyethylene glycol evenly, add the prescribed amount of tacrolimus, fully dissolve, and set aside; (3) take an appropriate amount of water for injection, and dissolve the prescribed amount of glycerin and benzalkonium chloride in sequence; (4) mix the solutions obtained from (2) and (3) , fully stirred to obtain a clear solution; (5) mix the sodium hyaluronate solution obtained from (1) with the solution obtained from (4) evenly; (6) add water for injection to the solution obtained from (5) to 100ml, stir evenly, and adjust the pH value to 4.8 if necessary . (7) Filter and sterilize the obtained medicinal solution thr...

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Abstract

The invention provides a tacrolimus ophthalmic preparation and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. According to the present invention, thetacrolimus ophthalmic preparation has a micro-emulsion-like structure, is clarified and transparent, has good patient compliance, is prepared from tacrolimus, oil for injection, a surfactant, a stabilizer, an osmotic pressure regulator, a preservative, a pH value regulator, a tackifier and water for injection, and is used for preventing and treating immunological rejection after corneal transplantation or immunological corneal xerosis and conjunctival xerosis. According to the present invention, with the tacrolimus ophthalmic preparation, the problem of the water insolubilization of tacrolimusis solved, the tacrolimus is firstly prepared into the clarified and transparent eye drops with the micro-emulsion-like structure, the irritation on the eyes by the existing tacrolimus-suspended ophthalmic eye drops can be substantially reduced, and the patient compliance can be improved, such that the tacrolimus ophthalmic preparation of the present invention is suitable for the long-term use byimmunological rejection after corneal transplantation, corneal xerosis and conjunctival xerosis, and other patients with indications.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically relates to a tacrolimus ophthalmic preparation suitable for long-term medication and a preparation method thereof. Background technique [0002] Tacrolimus (Tacrolimus, FK506) is a metabolite extracted from Streptomyces culture medium by Fujisawa Pharmaceutical Company of Japan. Its chemical structure is a macrolide immunosuppressant. Inhibits the action of T lymphocytes. Its immunosuppressive effect is 10 to 100 times stronger than that of cyclosporine A (CsA), thus greatly reducing the clinical dose, reducing treatment costs, and significantly reducing adverse drug reactions. In addition, tacrolimus has a strong antibacterial effect on Fusarium of Aspergillus fumigatus in fungi, but has no obvious inhibitory effect on bacteria and yeast. Tacrolimus has been used clinically as an immunosuppressant for more than 20 years. A large number of studies have proved tha...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/436A61K47/14A61K47/26A61K47/44A61K47/10A61P27/02A61P37/06A61K9/107
CPCA61K9/0048A61K9/08A61K9/1075A61K31/436A61K47/10A61K47/14A61K47/26A61K47/44
Inventor 刘继东唐海高坤
Owner SHENYANG XINGQI PHARM CO LTD
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