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Cyclosporin polymer micelle preparation and preparation method thereof

A technology of cyclosporine and polymer, applied in the field of cyclosporine polymer micelle preparation and preparation thereof, can solve the problems of high cost, weak compatibility, drug precipitation, etc., and achieves convenient storage and transportation, good stability Effect

Inactive Publication Date: 2021-09-24
科贝园(北京)医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the compatibility between general high molecular polymers and drugs is usually weak, so the stability of the formed drug-loaded micelles is also low, showing that the prepared micellar solution is prone to drug precipitation and precipitation
In addition, the general polymer micelle preparation is a freeze-dried powder injection, which has problems such as complicated preparation process, high cost, and difficulty in popularization.

Method used

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  • Cyclosporin polymer micelle preparation and preparation method thereof
  • Cyclosporin polymer micelle preparation and preparation method thereof
  • Cyclosporin polymer micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: Amphiphilic block copolymer mPEG-PLA-(LA) 4 Synthesis

[0055]

[0056] Dissolve 50g of dimethylolpropionic acid in 250mL of acetone, add 3.55g of p-toluenesulfonic acid, 69mL of dimethoxypropane and stir at room temperature for 4 hours, add 3mL of ammonia water to terminate the reaction, and remove the solvent by rotary evaporation. The product is washed with water to obtain hydroxyl-protected Dimethylolpropionic acid. Take 50g of hydroxyl-protected dimethylolpropionic acid and dissolve it in dichloromethane, add 30g of cyclohexylcarbodiimide, react at room temperature for 12 hours, remove the organic solvent by rotary evaporation, dissolve the product in n-hexane, freeze and crystallize in the refrigerator, and filter and dry Compound 1 was obtained.

[0057] 12g mPEG2000 was vacuum dehydrated at 130°C for two hours, added 4g D,L-lactide and 40mg stannous octoate, put the reactant at 130°C for vacuum polymerization for 24 hours, dissolved with appro...

Embodiment 2

[0061] Embodiment 2: Preparation of self-assembled cyclosporin polymer micelles solution

[0062] 100mg mPEG-PLA-(LA) 4 and 20 mg of cyclosporine were dissolved in 3 mL of ethanol, and the organic solvent was removed by rotary evaporation at 35° C., and then 10 mL of deionized water was added to the round bottom flask for dissolution to obtain a self-assembled cyclosporine polymer micelle solution.

Embodiment 3

[0063] Embodiment 3: the preparation of cyclosporin polymer micelle solution

[0064] 100mg mPEG-PLA-(LA) 4 Heating to 45° C. and melting to form a transparent liquid, adding 20 mg of cyclosporine and stirring to form a uniform transparent liquid, and forming a cyclosporine polymer composition after cooling. Then, 20L of ultrapure water was added for dissolution to obtain a clear and transparent solution, namely the cyclosporine polymer micelle solution. The encapsulation efficiency (HPLC method) is above 95%.

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Abstract

The invention provides a cyclosporin polymer composition. The cyclosporin polymer composition comprises cyclosporin and an amphiphilic block copolymer; the amphiphilic block copolymer comprises a hydrophobic chain segment and a hydrophilic chain segment; and the amphiphilic block copolymer has a structure represented by a formula (I). The composition is dissolved with water to form a cyclosporine polymer micelle solution, such as eye drops, which can be used for treating ophthalmic diseases such as dry eye. The composition is in a solid form, and is good in stability and convenient to store and transport; and a micelle solution formed by adding water for dissolving also has good stability, and can meet the requirements of eye medication. The invention also provides a preparation method of the composition, which comprises the following steps of heating and melting the amphiphilic block polymer, adding cyclosporin, stirring until the mixture is clear and transparent, and cooling to obtain the composition. The preparation process is simple and good in repeatability, can be used for large-scale production, and has a good industrialization prospect.

Description

technical field [0001] The invention belongs to the field of nano-medicines, and in particular relates to a cyclosporine polymer micelle preparation and a preparation method thereof. Background technique [0002] Dry eye, also known as keratoconjunctival sicca, refers to the abnormal tear quality, quantity or dynamics caused by any reason (including aging, wearing contact lenses, certain drugs, eye diseases, other diseases or environmental factors, etc.), resulting in Decreased tear film stability (destruction of the tear film and formation of dry spots on the cornea), accompanied by ocular discomfort (eye dryness, stinging, burning pain, gritty sensation, etc.) and / or various characteristics of ocular surface tissue lesions General term for disease. Dry eye is currently the most common ocular surface disease, and the main treatment is the use of artificial tears. In recent years, dry eye disease has become a global epidemic disease, and the prevalence rate (the ratio of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/13A61K9/107A61K47/34A61P27/02
CPCA61K38/13A61K9/1075A61K47/34A61K9/0048A61P27/02
Inventor 程增江满艳哲程思奇赵京华
Owner 科贝园(北京)医药科技有限公司
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