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Tacrolimus suspending eye drop liquid and preparation method thereof

A technology for tacrolimus and eye drops, which is used in liquid delivery, pharmaceutical formulations, emulsion delivery, etc., can solve the problems of rising impurity content, high equipment requirements, thermal instability, etc., to achieve stable product quality and preparation. The process is simple and the effect of avoiding toxic and side effects

Active Publication Date: 2015-03-04
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The particle size distribution of the gained tacrolimus microparticles prepared by this method is wide, and the particle size is too large; water is added in the organic solvent to precipitate a large number of microparticles very easily, which causes great difficulties to the later stage dispersion process; the addition speed of water has a great impact on the particle size The diameter has a great influence, and the process scale-up is not easy to realize; the freeze-drying operation is complicated and requires high equipment
Moreover, tacrolimus is unstable to heat, and dry heat, damp heat and radiation sterilization will all cause degradation, resulting in a significant increase in impurity content

Method used

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  • Tacrolimus suspending eye drop liquid and preparation method thereof
  • Tacrolimus suspending eye drop liquid and preparation method thereof
  • Tacrolimus suspending eye drop liquid and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0063] Embodiment 1, the preparation of 0.1% tacrolimus suspension eye drops (0.1% refers to 0.1g / 100mL, i.e. 1mg / mL; the same below) prescription:

[0064]

[0065] Preparation Process:

[0066] (1) Weigh the prescribed amount of tacrolimus, add it to ethanol and stir to dissolve, filter and sterilize through a 0.2μm filter membrane to obtain a sterile filtrate; in a sterile environment, add the filtrate to 200mL water for injection to precipitate tacrolimus Moss particles (particle size D 90 1.0 μm), the ethanol solvent was removed by diafiltration through a tangential flow ultrafiltration device, and 4-6 times the volume was diafiltered to obtain a sterile suspension of tacrolimus particles;

[0067] (2) Weigh the polyvinyl alcohol of the prescribed amount, add it to 700mL water for injection, heat and stir to dissolve, add benzalkonium chloride, sodium chloride, sodium dihydrogen phosphate, and disodium hydrogen phosphate, and stir to dissolve, add phosphoric acid or ...

Embodiment 2、01

[0070] Example 2, Preparation of 0.1% Tacrolimus Suspension Eye Drops

[0071]

[0072]

[0073] Preparation Process:

[0074] (1) Weigh the prescribed amount of tacrolimus and add it to ethyl acetate, stir and dissolve, filter and sterilize through a 0.2 μm filter membrane to obtain a sterile filtrate, add the filtrate to 300ml of water for injection in a sterile environment, and separate out tacrolimus Crolimus microparticles (average particle size D 90 1.3 μm), the ethyl acetate solvent was removed by washing and filtering through a tangential flow ultrafiltration device, and 4-6 times the volume was washed and filtered to obtain a sterile suspension of tacrolimus particles;

[0075] (2) Weigh 0.5 g of hypromellose in the prescribed amount, add it to 300 ml of water for injection, stir to dissolve, and sterilize by moist heat at 121 ° C for 30 min,

[0076] (3) Weigh 0.1 g of benzalkonium bromide, 3.5 g of sodium dihydrogen phosphate, and 0.85 g of disodium hydrogen...

Embodiment 3、01

[0101] Example 3, Preparation of 0.1% Tacrolimus Suspension Eye Drops

[0102] prescription:

[0103]

[0104] Preparation Process:

[0105] (1) Weigh the prescribed amount of tacrolimus, add it to ethanol and stir to dissolve, filter and sterilize through a 0.2μm filter membrane to obtain a sterile filtrate; in a sterile environment, add the filtrate to 400mL water for injection to precipitate tacrolimus Moss particles (particle size D 90 0.5 μm), remove the ethanol solvent by washing and filtering through a tangential flow ultrafiltration device, wash and filter 4-6 times the volume, and concentrate the feed solution to 200-300ml to obtain a sterile suspension of tacrolimus particles;

[0106] (2) Weigh the polyvinyl alcohol of the prescribed amount, add it to 700mL water for injection, heat and stir to dissolve, add benzalkonium chloride, sodium chloride, sodium dihydrogen phosphate, and disodium hydrogen phosphate, and stir to dissolve, add phosphoric acid or Sodium ...

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Abstract

The invention relates to a preparation method for tacrolimus suspending eye drop liquid. The preparation method comprises the following steps: dissolving the tacrolimus in an organic solvent; filtering and sterilizing the tacrolimus solution through a micropore filtration film; adding the tacrolimus organic solution after sterilization and filtration in injection water; separating out tacrolimus particles with appropriate particle diameter; displacing the solvent by adopting a tangential flow ultrafiltration device; removing organic solvent residue to obtain sterile tacrolimus particle slurry; mixing the slurry with other auxiliary solution after sterilization uniformly to obtain the tacrolimus suspending eye drop liquid. The tacrolimus suspending eye drop liquid prepared by the method meets requirements in sterility and particle diameter, and can effectively improve retention performance of the medicine in eyes; the preparation method is simple and reasonable in technology, and suitable for production on large scale.

Description

technical field [0001] The invention relates to a preparation method of suspension-type eye drops, in particular to a preparation method of tacrolimus suspension-type eye drops, and belongs to the technical field of pharmaceutical preparations. Background technique [0002] Conjunctivitis is the most common and frequently-occurring disease in ophthalmology, and it is a general term for the inflammatory reaction of conjunctival tissue under the action of external factors and the body's own factors. Although conjunctivitis itself is not serious for vision, it can lead to vision impairment when the inflammation spreads to the cornea or causes complications. A variety of eye drops are currently on the market, such as tobramycin eye drops, tacrolimus eye drops, olopatadine eye drops, ketotifen eye drops, etc.; some of these drugs are water-soluble , such as tobramycin, olopatadine, etc. Some drugs have poor water solubility, such as tacrolimus; when preparing suspension eye drop...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/436A61P27/02
Inventor 李燕刘晓旭刘禄娟李红英张明会
Owner QILU PHARMA
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