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In-situ gel containing cyclosporin micelle as sustained-release ophthalmic drug delivery system

A technology of cyclosporine and micelles, which is applied in the field of pharmaceuticals, can solve the problems of increasing bioavailability, and achieve the effects of improving stability, increasing adhesion, and improving drug solubility

Pending Publication Date: 2021-03-19
IVEW THERAPEUTICS (ZHUHAI) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although micellar solutions increased the permeability of cyclosporine to the cornea, rapid loss after instillation in the eye prevented increased bioavailability

Method used

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  • In-situ gel containing cyclosporin micelle as sustained-release ophthalmic drug delivery system
  • In-situ gel containing cyclosporin micelle as sustained-release ophthalmic drug delivery system
  • In-situ gel containing cyclosporin micelle as sustained-release ophthalmic drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0072] Example 1: Determination of the medial concentration of the present invention

[0073] Table 2 lists samples containing 0.05% cyclosporine A:

[0074] Table 2. Sample formulation of cyclosporine A nano micelle solution

[0075]

[0076] Granularity and distribution testing

[0077] The micellar particle size and distribution or multi-dispersion index (PDI) (Table 3) prepared by the above formulations were tested using a particle size analyzer. The result is shown Figure 1-8 And confirm that the micelle particle diameter in the sample 1-8 of the preparation and test is less than or

[0078] Table 3. Samples with Comparison of particle size of the middle nanometer micelles

[0079]

[0080]

Embodiment 2

[0081] Example 2: Determination of gel matrix concentration

[0082] Samples containing 0.05% cyclosporine A solution are listed in Table 4-7:

[0083] Table 4. Concentration of gel matrix finish

[0084]

[0085] Table 5. Concentration of gel matrix yellow original gum

[0086]

[0087] Table 6. The concentration of gel matrix kale gel

[0088]

[0089]

[0090] Table 7. Concentration of sodium gel matrix alginate

[0091]

[0092] Preparation method of gel solution

[0093] Accurately weighed a certain amount of sodium chloride, and add 85 grams of ultrapure water evenly. The solution was stirred until sodium chloride was completely dissolved, and then the above gel matrix was slowly added slowly with continuous stirring. This solution was placed in a 90 ° C water bath and stirred for 1 hour. The mixture was then cooled to room temperature. 0.05 g of cyclosporin A was weighed and the slowly added to a cooled solution under stirring. Add water to the final amount of 100...

Embodiment 3

[0109] Example 3: In situ gel of the cyclosporine micelles of the present invention.

[0110] The formulation of the micellar eye containing 0.05% cyclosporine A is as follows:

[0111] Cyclosporine A 0.05% by weight, 0.25% by weight of the deacetyl batch, 1% by weight of polyethylene glycol, 0.15% by weight of sodium chloride, 3.3% by weight of mannitol, hydroxybenzoic acid 0.02% by weight of the ester, an appropriate amount of a mito-dyric alkanol hydrochloric acid buffer and an injection of water to prepare an ophthalmic gel containing 0.05% cyclosporine micelles (Table 12).

[0112] Table 12. Composition of Example 3 Nano-micelle in situ gel

[0113] Component Percentage (wt%) Cyclosporine A 0.05 wt% Decetyl tilation 0.25 wt% Polyethylene glycol 20 hexadecion 1.0 wt% Sodium chloride 0.15 wt% Mannitol 3.3 wt% Hydroxybenzoate 0.02 wt% Aminobutyl alcohol hydrochloric acid buffer A certain amount of Water for Injecti...

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Abstract

The invention provides an in-situ gel containing cyclosporin micelles as a sustained release ophthalmic drug delivery system. The in-situ gel contains 0.01 wt% to 5 wt% of an aqueous ophthalmic formulation of cyclosporin present in the form of a micelle with the particle size of no greater than 20 nm.

Description

Technical field [0001] The present invention belongs to the technical field of medicines. Background technique [0002] Dry eye, also known as dry corneal conjunctivitis, is an abnormality caused by tears or fluid dynamics caused by multi-factors and complicated reasons, causing tear stability to decrease, and accompanied by eye discomfort / or eye watch A common term of a variety of diseases of historical characteristics. The most common symptoms of dry eye is eye burning, pain and red. Other common symptoms include eye crying or silk adhesion. Dry eye disease is related to a variety of factors, with a incidence of 7.4% to 33.7%, of which the prevalence of women over 50 years old is about twice the male. See, JL Gayton, J. Clinical Ophthalmology (Auckland, NZ), 2009, 3: 405.Schaumberg Da, Sullivan Da, BURING JE, ET Al.Prevalence of Dry Eye Syn-Drome Among US Women.american Journal of Ophthalmology, 2003 , 136 (2): 318-326. [0003] Tears have three layers: oily outer, aqueous in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K38/13A61K47/36A61K47/38A61K47/44A61P27/02A61P29/00A61P37/06
CPCA61K9/0048A61K9/1075A61K38/13A61K47/36A61K47/38A61K47/44A61P27/02A61P29/00A61P37/06
Inventor 波·梁彭海洲朱婕屿袁旭东
Owner IVEW THERAPEUTICS (ZHUHAI) CO LTD
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