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Kidney-targeted medicine vector and the formed prodrug, preparation method and uses

A kidney-targeted and drug-based technology, applied in the field of new kidney-targeted prodrugs and preparations, can solve problems such as preparation methods and applications that have not been proposed

Inactive Publication Date: 2006-12-20
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no suggestion that low molecular weight chitosan can be used as a good kidney-targeting drug carrier and the preparation method and application of prodrugs.

Method used

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  • Kidney-targeted medicine vector and the formed prodrug, preparation method and uses
  • Kidney-targeted medicine vector and the formed prodrug, preparation method and uses
  • Kidney-targeted medicine vector and the formed prodrug, preparation method and uses

Examples

Experimental program
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Effect test

Embodiment 1

[0059] Preparation of low molecular weight water-soluble chitosan

[0060] Dissolve 3g of chitosan in 150ml of 0.45% (w / v) hydrochloric acid aqueous solution, after completely dissolving, filter, add 1.88ml of hydrogen peroxide, and stir and react at 40-70°C for 2 hours. Adjust the pH value to 13 with sodium hydroxide, precipitate out, centrifuge at 4000 r / c to obtain a low molecular weight chitosan precipitate, wash with water until neutral, and then vacuum dry.

[0061] Take 1g of the dry product and dissolve it in 170ml of 3% acetic acid solution. After completely dissolving, add 6ml of acetic anhydride, stir and react at room temperature for 4 hours, adjust the pH value to 13 with sodium hydroxide, add 500ml of acetone, and centrifuge to obtain a precipitate , the precipitate was treated with 1 mol / L potassium hydroxide in methanol for 5 hours, washed with methanol to neutrality, dissolved in water, and further purified by gel permeation chromatography (GPC). After freeze...

Embodiment 2

[0063] Preparation and in vivo distribution of fluorescently labeled chitosan

[0064] Accurately weigh 300mg of chitosan (Mw=20000, deacetylation degree is about 50%, water-soluble) and dissolve in 10ml of 1mol / L HCl solution, then adjust the pH value to 6.9 with NaOH. Add 21 mg FITC (fluorescein isothiocyanate), mix well, react at room temperature for 24 hours, and dialyze. The dialyzed sample was freeze-dried (chitosan itself is a good scaffold base, so there is no need to add other scaffold bases). The fluorescein content was determined to be 6.56% (w / w). Take 20 Kunming mice, male, weighing between 25-30 grams, each group of 5 mice, a total of 4 groups. Calculated according to the injection dose of 40mg / kg, inject FITC-chitosan into the tail vein, kill the mice at 15min, 30min, 60min, and 120min respectively, take the heart, liver, spleen, lung, and kidney, weigh them, and prepare a tissue homogenate. After the protein was precipitated, the content was measured with a ...

Embodiment 3

[0066]Preparation of prednisolone succinate-chitosan prodrug

[0067] Precisely weighed 115mg of prednisolone succinate monoester, 28.8mg of N-hydroxysuccinimide, dissolved in 20ml ethanol; accurately weighed 100mg of chitosan (Mw=10000 Dalton, deacetylation degree is 50% left and right, water-soluble) dissolved in 30ml of distilled water, after complete dissolution, the ethanol mixture was slowly added dropwise to the water phase under stirring conditions, and finally 120mg of 1-(3-dimethylaminopropyl)-3-ethylcarbadiene was added Imine hydrochloride was used as a condensation agent, reacted overnight at 4°C, precipitated the conjugate with 150ml of acetone, washed the precipitate several times, and dried to obtain the prodrug. Sealed and stored at low temperature.

[0068] Accurately weighed 115mg of prednisolone succinate, 28.8mg of N-hydroxysuccinimide, dissolved in 20ml of ethanol; accurately weighed 100mg of chitosan (Mw=20000 Daltons, water insoluble), added 10ml After...

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Abstract

The invention relates to a new kidney target medicine carrier and relative precursor medicine, relative preparation method and application, wherein it comprises: degrading and deriving the natural chitose to obtain the chitose or its derivant with low molecule weight, with better kidney target proerpty; said medicine carier via chemical bond is linked to the anti-cancer medicine or glucocorticoids, or immunosuppressant, to obtain the precursor medicine; the medicine molecule is connected to the carrier via chemical bond. The experiments have proved that: said medicine can release the active component at kidney. And the invention has simple process, stable property and the application for batch production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and particularly relates to low-molecular-weight chitosan or its derivatives, a drug carrier with good kidney-targeting efficiency, and a novel kidney-targeted prodrug formed as a drug carrier, as well as a preparation method and application thereof. Background technique [0002] The kidney is one of the vital organs of the human body. If the physiological function of the kidney deviates, it often leads to serious diseases. Kidney-related diseases mainly include various infection inflammations, diabetes, high blood pressure, tumors, etc., such as acute and chronic nephritis, acute and chronic renal failure, urinary tract infection, kidney cancer , Wilms tumor, renal pelvis tumors, etc. In recent years, the incidence and prevalence of end-stage renal disease are increasing year by year. According to statistics, in 1989, there were 187,000 patients with end-stage renal diseas...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/36A61K45/08A61K31/365A61K9/02A61K9/08A61K9/10A61K9/12A61K9/19A61K9/20A61K9/48A61P13/12A61P35/00A61P37/06A61K47/61
Inventor 张志荣龚涛孙逊袁志翔
Owner SICHUAN UNIV
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