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Pharmaceutical composition as well as preparation method and use thereof

A composition and drug technology, applied in the field of pharmaceutical composition and its preparation, can solve the problems of adverse immune reaction, inability to target aggregation lesions, large dosage, etc., and achieve improved drug efficacy, good biocompatibility and solubility, quick release effect

Active Publication Date: 2014-11-26
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these two small-molecule drugs cannot be used at the same time to exert their medicinal effects, and they cannot be targeted and aggregated to the lesion in the living body. Not only do they need to be used in large amounts, but they will also produce a variety of adverse immune reactions, which will bring great pain to patients.

Method used

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  • Pharmaceutical composition as well as preparation method and use thereof
  • Pharmaceutical composition as well as preparation method and use thereof
  • Pharmaceutical composition as well as preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Preparation of hyaluronic acid-cystamine-polylactic acid-glycolic acid grafted polymer nanoparticles loaded with doxorubicin and cyclopamine

[0114] (a) 5g of polylactic acid-glycolic acid (75 / 25, molecular weight: 50,000, Jinan Daigang), 0.115g of 1-ethyl-(3-dimethylaminopropyl) carbodiimide (Alfar Aesar Company, 98%) and 0.081g of 1-hydroxybenzotriazole (Aladdin Reagent Shanghai Co., Ltd., 99%) were placed in a three-necked flask, and after vacuumizing for 1 hour, 10mL of chloroform was added to dissolve, and the temperature was 40°C , and reacted for 4 hours under the protection of nitrogen to obtain the crude product of polylactic acid-glycolic acid activated by 1-hydroxybenzotriazole. The crude product solution was rotary evaporated at 25°C to remove chloroform, then precipitated with 200mL ether, washed with a mixed solution of methanol / ether (5:5) (100mL×3 times), and dried in a vacuum oven at 25°C for 36 hours to obtain Solid product 1-hydroxybenzotriazole-act...

Embodiment 2

[0129] Steps (a) to (d) are carried out according to the method of Example 1, and the amounts, conditions and results of the substances involved in the method are shown in Table 1 to Table 4.

[0130] (e) 10 mg of hyaluronic acid-cystamine-polylactic acid-glycolic acid grafted polymer and 0.2 mg of cyclopamine were dissolved in 1 mL of dichloromethane, and 200 μL of 0.5 mg / mL doxorubicin aqueous solution was added, and the cells were sonicated Use 5% power in the pulverizer, ultrasonic 2 minutes, obtain the water-in-oil colostrum, then add 4mL polyvinyl alcohol (2%wt) solution in the colostrum, use 25% power in the ultrasonic cell pulverizer, Ultrasound for 5 minutes to obtain a water-in-oil-in-water complex emulsion. The resulting emulsion was removed with methylene chloride by a rotary evaporator to obtain hyaluronic acid-cystamine-polylactic acid-glycolic acid grafted polymer nanoparticles with blue light.

[0131] After testing, the weight average molecular weight of the ...

Embodiment 3

[0133] Steps (a) to (d) are carried out according to the method of Example 1, and the amounts, conditions and results of the substances involved in the method are shown in Table 1 to Table 4, respectively.

[0134] (e) Dissolve 10 mg of hyaluronic acid-cystamine-polylactic acid-glycolic acid graft polymer and 1 mg of cyclopamine in 1 mL of dichloromethane, add 200 μL of 2.5 mg / mL doxorubicin aqueous solution, and crush the cells under ultrasonic Use 5% power in the machine, ultrasonic for 2 minutes to obtain water-in-oil colostrum, then add 4mL polyvinyl alcohol (4%wt) solution to the colostrum, use 25% power in the ultrasonic cell pulverizer, ultrasonically After 5 minutes, a water-in-oil-in-water complex emulsion was obtained. The resulting emulsion was removed with methylene chloride by a rotary evaporator to obtain hyaluronic acid-cystamine-polylactic acid-glycolic acid grafted polymer nanoparticles with blue light.

[0135] After testing, the weight average molecular wei...

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Abstract

The invention provides a pharmaceutical composition and a preparation method thereof. The pharmaceutical composition comprises a carrier and an active ingredient loaded on the carrier, wherein the carrier is a nanoparticle of a hyaluronic acid-cystamine-polylactic acid-glycolic acid grafted polymer as shown in a formula (I) as shown in the specification; in the formula (I), n is an integer ranging from 16 to 30, the ratio of Y to X ranges from (1-3): 1, Y is an integer ranging from 153 to 549 and X is an integer ranging from 73-385. The pharmaceutical composition is capable of realizing directional delivery so that the medicine can be released quickly in cells and the effect of the medicine can be improved.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a medicine composition and its preparation method and application. Background technique [0002] Small molecule drugs (such as doxorubicin, cyclopamine, etc.) have no targeting and cannot recognize tumor tissues and cells, which reduces their efficacy and increases side effects. At the same time, some drugs have a good curative effect, but due to their poor water solubility (such as cyclopamine), they are difficult to be effectively absorbed by the human body, making it difficult to fully exert the drug effect, which has a certain impact on their clinical application. [0003] Cyclopamine (Cyc for short) is an isosteroid alkaloid that can inhibit the Hedgehog pathway and has therapeutic effects on a variety of tumors, especially on tumor stem cells, but has little effect on other tumor cells. Inhibition phenomenon, its water solubility is very poor. Doxorubicin (Dox for shor...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/58A61K31/704A61K9/113A61P35/00
Inventor 陈春英吴雁周会鸽胡克磊刘颖
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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