Vitamin E succinate-chitosan graft and preparation method and application thereof

A technology of succinate and vitamin, applied in the application of stable drug nanosuspension, vitamin E succinate-chitosan graft and its preparation, new surfactant and its preparation field, can solve the problem of easy Aggregation or crystallization growth, poor physical stability of nanocrystal suspensions, affecting the stability of preparations and drug efficacy, etc., to achieve the effect of facilitating transportation and storage, improving safety and good stability

Inactive Publication Date: 2012-07-11
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the physical stability of the nanocrystal suspension is poor, and it is easy to aggregate or crystallize and grow, thus affecting the stability of the preparation and the efficacy of the drug.

Method used

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  • Vitamin E succinate-chitosan graft and preparation method and application thereof
  • Vitamin E succinate-chitosan graft and preparation method and application thereof
  • Vitamin E succinate-chitosan graft and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 0.2 g of chitosan (95% degree of deacetylation) with a molecular weight of 34 kDa, 0.25 g of carbodiimide and 0.15 g of N-hydroxysuccinimide to prepare an aqueous solution, and weigh 0.3 g of vitamin E succinate to dissolve In 30 ml of N,N-dimethylformamide. Under the condition of stirring, the aqueous solution containing chitosan was slowly added to the N,N-dimethylformamide solution of vitamin E succinate within 3 hours. React at 30°C for 48 hours, pour a mixed solution of 270ml of methanol and 30ml of ammonia water (9:1) into the final reaction solution, filter the precipitate to obtain a yellow gel, wash it repeatedly with absolute ethanol, and place it in a dialysis bag ( MWCO3500), distilled water dialysis for 24 hours to remove residual carbodiimide, N-hydroxysuccinimide and reaction by-products. The dialysate was freeze-dried to obtain a vitamin E succinate-chitosan graft, and the graft ratio (amino substitution degree) was determined to be 20%.

Embodiment 2

[0044] Weigh 0.2 g of chitosan (90% degree of deacetylation) with a molecular weight of 34 kDa, 0.4 g of carbodiimide and 0.4 g of N-hydroxysuccinimide to prepare an aqueous solution, and weigh 0.2 g of vitamin E succinate to dissolve In 40 ml of N,N-dimethylformamide. Under the condition of stirring, the aqueous solution containing chitosan was slowly added to the N,N-dimethylformamide solution of vitamin E succinate within 3 hours. React at 30°C for 24 hours, pour a mixed solution of 300ml of methanol and 20ml of ammonia water (15:1) into the final reaction solution, filter the precipitate to obtain a yellow gel, wash it repeatedly with absolute ethanol, and place it in a dialysis bag ( MWCO7000), distilled water dialysis for 48 hours to remove residual carbodiimide, N-hydroxysuccinimide and reaction by-products. The dialysate is freeze-dried to obtain the vitamin E succinate-chitosan graft. After determination, its grafting rate is 14%.

Embodiment 3

[0046] Weigh 1 g of chitosan (deacetylation degree 97%) with a molecular weight of 100 kDa, 0.2 g of carbodiimide and 0.2 g of N-hydroxysuccinimide to make an aqueous solution, and weigh 0.5 g of vitamin E succinate to dissolve In 30 ml of N,N-dimethylformamide. Under the condition of stirring, the aqueous solution containing chitosan was slowly added to the N,N-dimethylformamide solution of vitamin E succinate within 3 hours. React at 40°C for 48 hours, pour a mixed solution of 180ml methanol and 120ml ammonia water (6:4) into the final reaction solution, filter the precipitate to obtain a yellow gel, wash it repeatedly with absolute ethanol, and place it in a dialysis bag ( MWCO7000), distilled water dialysis for 48 hours to remove residual carbodiimide, N-hydroxysuccinimide and reaction by-products. The dialysate is freeze-dried to obtain the vitamin E succinate-chitosan graft. After determination, its grafting rate is 8%.

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Abstract

The invention provides a vitamin E succinate-chitosan graft (I), a preparation method and application thereof in paclitaxel and homolog nanosuspensions. The graft has amphipathy, can play the role of a surfactant and is used for stabilizing the drug nanosuspensions. The prepared nanosuspensions have the characteristics of high drug loading, stability, safety, low toxicity, no hemolysis or vein vascular irritation and the like, and the preparation process is simple and is easy for industrialization.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a novel surfactant and a preparation method thereof, in particular to a vitamin E succinate-chitosan graft, a preparation method thereof and its application in stabilizing drug nanosuspensions . Background technique [0002] Nanosuspension is a new drug delivery form, which disperses the drug in water at the nanometer scale by crushing or controlling crystal growth to form a dispersion system. The system does not contain matrix materials and only contains a small amount of surfactant as a stabilizer. Compared with microspheres, liposomes, and solid lipid nanoparticles, it has the characteristics of simple prescription, convenient preparation, and high drug loading. The stimulation and toxic side effects caused by additional ingredients are reduced, and the compliance of patients is greatly improved; in addition, the nanosuspension significantly increases the sp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08A61K47/36A61K9/10A61K31/337A61P35/00
Inventor 崔福德李雪丰梁娜朴洪宇
Owner SHENYANG PHARMA UNIVERSITY
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