Andrographolide polymer micelle, preparation method and medicinal application thereof

A technology of andrographolide and polymer glue is applied in the directions of pharmaceutical formulations, antitumor drugs, drug combinations, etc., to achieve the effects of masking severe bitterness, stable product quality, and simple preparation process

Inactive Publication Date: 2015-03-18
CHANGZHOU TARGET MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, most of these drug delivery systems are in the academic research stage, and the research on andrographolide drug delivery systems with clinical application and development value is still a challenge

Method used

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  • Andrographolide polymer micelle, preparation method and medicinal application thereof
  • Andrographolide polymer micelle, preparation method and medicinal application thereof
  • Andrographolide polymer micelle, preparation method and medicinal application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 amphiphilic block copolymer

[0037] (1) Methoxy polyethylene glycol-polylactide block copolymer (mPEG 3400 -PLA 1800 ): Add 50g mPEG (number average molecular weight 3400) into a polymerization bottle, heat to 100°C, vacuum dehydrate for 2 hours, add 36mg stannous octoate and 36g D,L-lactide (D,L-LA), vacuum seal Reaction vial, react at 125°C for 15h. Dissolve the reactants with dichloromethane, add a large amount of ether to fully precipitate the polymer, filter and dry in vacuum.

[0038] (2) Benzoyl-terminated methoxypolyethylene glycol-polylactide block copolymer (mPEG 3400 -PLA 1800 -Bz): take 38g mPEG 3400 -PLA 1800 Add 190ml of ethyl acetate to dissolve, add 2.8ml of triethylamine, add 2.3ml of benzoyl chloride dropwise under stirring, heat the above solution to boiling after the dropwise addition, continue the reflux reaction for 6h, filter to remove insoluble matter, add a large amount of ether to precipitate The polymer ...

Embodiment 2

[0043] Embodiment 2 andrographolide polymer micelles lyophilized preparation preparation

[0044] (1) mPEG 5000 -PCL 4000 -Preparation of Ac / andrographolide polymer micelles and its lyophilized preparation

[0045] Get the mPEG prepared in 150mg embodiment 1 (4) 5000 -PCL 4000 -Ac and 30mg of andrographolide were dissolved in 2ml of tetrahydrofuran, and 5ml of ultrapure water was slowly added dropwise under stirring. After the dropwise addition, the solution was stirred at room temperature overnight to remove the organic solvent to obtain clear paclitaxel micelles with obvious blue opalescence 120 mg of mannitol was added to the solution, and the resulting solution was filtered through a 0.22 μm sterile membrane and freeze-dried to obtain a freeze-dried powder of andrographolide polymer micelles. According to HPLC analysis, the drug encapsulation rate is 96.5%, the drug loading capacity is greater than 15.4%, the average particle size is 18.7nm, and the dispersion coeffici...

Embodiment 3

[0050] The pharmacokinetics of embodiment 3 andrographolide polymer micelles in rat body

[0051] (1) Plasma drug-time curve of andrographolide polymer micelles rat tail vein injection

[0052] Test drug: andrographolide polymer micelle lyophilized preparation was prepared according to Example 2 (1), and was dissolved with physiological saline before use to make a solution containing 10 mg of andrographolide per 1 ml. In addition, DMSO was used as a solvent to dissolve andrographolide to make an andrographolide injection containing 10 mg of andrographolide per 1 ml as a reference preparation.

[0053] Dosing and blood collection scheme: 12 SD rats, weighing 200-220g, were randomly divided into two groups, with 6 rats in each group, half male and half male, and were injected with andrographolide polymer micelle solution and DMSO solution through tail vein respectively. , the dosage is 20mg / kg in terms of andrographolide. At different time points after the administration, 0.5 ...

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Abstract

The invention relates to a novel micelle drug delivery system formed by an amphipathic segmented copolymer and andrographolide. The amphipathic segmented copolymer includes a hydrophilic chain segment and a hydrophobic chain segment, wherein the hydrophobic chain segment is terminated by a hydrophobic group being one of an acetyl group, a tert-butyryl group, a tert-butyl acetyl group, a benzoyl group, an amino acid residual group or an amino acid derivative residual group. Not only is compatibility between a medicine molecule and the hydrophobic chain segment in the segmented copolymer improved and an acting force therebetween enhanced, but also a larger space is provided for accommodating the molecular molecule. The micelle can limit the medicine molecule within a core of the micelle more effectively so that the medicine molecule is not liable to dissolve out, thereby obtaining the drug delivery micelle being high in stability.

Description

technical field [0001] The invention relates to a stable polymer micelle drug-carrying system formed by andrographolide and an amphiphilic block copolymer, a preparation method and a medical application thereof, and belongs to the field of nano-pharmaceutical preparations. Background technique [0002] Andrographolide (Andrographolide) is a diterpene lactone compound with a half-helican skeleton extracted from the plant Andrographis Paniculata (bunn.f.) Nees of the family Acanthaceae. The chemical name is 3,19-dihydroxy- 8(17),13-laboiadien-16,15-olide, the chemical structure is as follows: [0003] [0004] Studies have shown that andrographolide has a wide range of physiological activities such as anti-inflammatory, antibacterial, and antiviral, and can inhibit the infiltration of leukocytes into the peritoneal cavity in peritonitis models induced by TNF-α, IL-1β, and LPS, and inhibit the endotoxin shock caused by LPS , and allergic airway inflammation mediated by eosi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K9/19A61K47/34A61P31/00A61P35/00
CPCY02A50/30
Inventor 许卉郎跃武刘西曼刘珂
Owner CHANGZHOU TARGET MEDICINE TECH CO LTD
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