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Positively charged drug nanocrystal preparation and preparation method thereof

A nano-crystal, positively charged technology, applied in pharmaceutical formulations, aerosol delivery, medical preparations with non-active ingredients, etc., can solve the problems of insufficient stability of nano-crystals, lack of bioadhesion, etc., and improve drugs. The effect of dissolution, prolongation of residence time and good stability

Inactive Publication Date: 2019-02-15
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The present invention aims to provide a bioadhesive positively charged drug nanocrystal preparation that can be used for mucosal administration and its preparation method, so as to solve the problems of insufficient stability of nanocrystals and lack of bioadhesion in the prior art.

Method used

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  • Positively charged drug nanocrystal preparation and preparation method thereof
  • Positively charged drug nanocrystal preparation and preparation method thereof
  • Positively charged drug nanocrystal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Preparation and characterization of imatinib cationized nanocrystals

[0036] Preparation

[0037] Step 1: Accurately weigh imatinib (3.35 mg), polyethylene glycol α-tocopheryl succinate (3.7 mg) and citric acid (7.6 mg), add 2 mL of acetonitrile and stir to dissolve, and place in a pear-shaped bottle film formation by rotary evaporation at room temperature. Add 5mL sodium bicarbonate aqueous solution (3mg / mL), shake and hydrate to obtain imatinib nano-crystal suspension;

[0038] Step 2: adjust the pH to 7.5 with dilute hydrochloric acid, add an appropriate amount of dopamine hydrochloride (5 mg), stir electromagnetically at room temperature, react for 30 minutes, centrifuge at 10,000 rpm for 5 minutes, discard the supernatant, and disperse the precipitate with pure water to obtain the cationic ima Tiny nano crystal suspension;

[0039] Step 3: Put in 10 μL of N-(tert-butoxycarbonyl)-1,2-diaminoethane, stir electromagnetically at room temperature, react ...

Embodiment 2

[0047] Example 2 Preparation and Characterization of Imatinib Cationic Nanocrystalline / Temperature Sensitive Gel Preparation

[0048] Preparation

[0049] Step 1: Same as Example 1.

[0050] Step 2: Same as Example 1.

[0051] Step 3: Put in 10 μL of N-(tert-butoxycarbonyl)-1,2-diaminoethane, stir electromagnetically at room temperature, react for 4 hours, add an appropriate amount of hydrochloric acid to adjust the pH to 2, terminate the reaction and remove the protecting group on the amino group , centrifuged at 10,000rpm for 5 minutes, discarded the supernatant, dispersed the precipitate with 0.77mL acetate buffer (pH 5.5, 100mM), then added 0.13g poloxamer 407, and stirred electromagnetically under ice bath until the solid was completely Dissolve, that is.

[0052] Finished product test

[0053] The gelation temperature of the obtained imatinib cationized nano-crystal / temperature-sensitive gel preparation is 28-30° C., it is liquid when the gelation temperature is ...

Embodiment 3

[0056] Example 3 Preparation of Curcumin / Imatinib Composite Cationic Nanocrystalline Preparation / Temperature Sensitive Gel Preparation

[0057] Preparation

[0058] Step 1: Accurately weigh curcumin (1.25mg), imatinib (1.65mg), polyethylene glycol α-tocopheryl succinate (3.7mg) and citric acid (7.6mg), add 2mL of acetonitrile and stir Dissolved, placed in a pear-shaped bottle, and rotatively evaporated at room temperature to form a film. Add 5mL sodium bicarbonate aqueous solution (3mg / mL), shake and hydrate to obtain curcumin / imatinib composite nanocrystal suspension;

[0059] Step 2: adjust the pH to 7.5 with dilute hydrochloric acid, add an appropriate amount of dopamine hydrochloride (5 mg), stir electromagnetically at room temperature, react for 30 minutes, centrifuge at 10,000 rpm for 5 minutes, discard the supernatant, and disperse the precipitate with pure water;

[0060] Step 3: Put in 10 μL of N-(tert-butoxycarbonyl)-1,2-diaminoethane, stir electromagnetically at...

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Abstract

The invention belongs to the field of drug preparations and relates to a positively charged drug nanocrystal preparation capable of being used for mucosal drug delivery and featured with bioadhensionand a preparation method thereof. According to the positively charged drug nanocrystal preparation capable of being used for mucosal drug delivery and featured with bioadhension, by using a polydopamine coating technique, surface coating and positively charging of drug nanocrystals are realized, so that polydopamine coating layers adhere to the surfaces of the drug nanocrystals and amination modification is carried out on the surfaces of the drug nanocrystals; and therefore, the surfaces of the drug nanocrystals are rich in positive charges, and better adhesion and better stability to biological tissues are given to the drug nanocrystals. The positively charged drug nanocrystal preparation capable of being used for mucosal drug delivery and featured with bioadhension, provided by the invention, has the advantages that problems of insufficient stability, lack of bioadhension and the like of the nanocrystals in the prior art can be solved, the preparation can be used for multiple routesof mucosal drug delivery and can also be used for intravesical or surgical margin medication. Positive charges adhering to the surfaces of the drug nanocrystals in the positively charged drug nanocrystal preparation capable of being used for mucosal drug delivery and featured with bioadhension are beneficial for interaction between the nanocrystals and a biological mucosa or other tissues.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a bioadhesive positively charged drug nano crystal preparation which can be used for mucosal administration and a preparation method thereof. Background technique [0002] The prior art discloses that bioadhesion refers to the ability of synthetic or natural macromolecular substances to adhere to mucus in the cavity or the surface of epithelial cells. Since the 1980s, this research field has used this bioadhesive polymer for drug delivery systems, known as bioadhesive drug delivery systems; after the delivery system is used in the human body, it can be adhered to an accessible The target site (administration site, absorption site or lesion site), prolongs the retention time of the drug in the lesion site, and improves its effect on treating local diseases; at the same time, the higher local drug concentration and the close contact between the drug and the surface of the a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/06A61K31/506A61K31/12
CPCA61K9/06A61K31/12A61K31/506A61K47/34A61K2300/00
Inventor 刘瑜次丽倩黄志刚魏刚陆伟跃
Owner FUDAN UNIV
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