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Pharmaceutical composition containing gambogic acid medicament and preparation method thereof

A composition and technology of gambogic acid, applied in the field of pharmaceutical preparations, can solve the requirements of high gambogic acid liposome preparation process and quality control process, large particle size of gambogic acid liposome, poor physical and chemical stability and other problems, to achieve good anti-tumor effect, increase tumor targeting, and no vascular stimulation effect

Inactive Publication Date: 2011-07-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But gambogic acid liposome has the following defects: poor physical and chemical stability, and the medicine that is wrapped after storage for a certain period of time leaks easily; Encapsulation efficiency is low, and the highest encapsulation efficiency is only about 80%; Large particle size, lack of vascular permeability, difficult to pass through the intercellular space of liver blood vessels, and easy to be swallowed by the reticuloendothelial system; the preparation process and quality control process of gambogic acid liposomes have high requirements, and it is difficult to achieve large-scale industrialization Production

Method used

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  • Pharmaceutical composition containing gambogic acid medicament and preparation method thereof
  • Pharmaceutical composition containing gambogic acid medicament and preparation method thereof
  • Pharmaceutical composition containing gambogic acid medicament and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Synthesis of all-trans retinoic acid-hyaluronic acid conjugates

[0035] Take 10mmol all-trans retinoic acid, 12mmol dicyclohexylcarbodiimide (DCC), 15mmol hydroxysuccinimide (NHS), dissolve in 30ml N,N-dimethylformamide, protect from light and nitrogen , reacted in ice bath for 30min, and then rose to room temperature for 24h. After the reaction, the precipitate was filtered off, and a large amount of ethyl acetate was added to wash the precipitate. The filtrate was extracted, the ethyl acetate layers were combined, and the solvent was removed by rotary evaporation to obtain the activated intermediate ester of all-trans retinoic acid. Dissolve 1mmol of all-trans retinoic acid activated intermediate ester in 10ml of dichloromethane, slowly drop into 3mmol / ml of ethylenediamine in dichloromethane solution under ice-bath conditions, and monitor the reaction by thin layer chromatography (TLC method) After completion, the reaction liquid is extracted, the organ...

Embodiment 2

[0036] Embodiment 2: the synthesis of gambogic acid-hyaluronic acid conjugate

[0037] Take 10mmol gambogic acid, 12mmol dicyclohexylcarbodiimide (DCC), and 15mmol hydroxysuccinimide (NHS), dissolve them in 30ml N, N-dimethylformamide, keep away from light, under the protection of nitrogen, and place in an ice bath Reacted for 30min, then rose to room temperature for 24h. After the reaction, the precipitate was filtered off, and a large amount of ethyl acetate was added to wash the precipitate. The filtrate was extracted, the ethyl acetate layers were combined, and the solvent was removed by rotary evaporation to obtain the activated intermediate ester of gambogic acid. Dissolve 1mmol of gambogic acid activated intermediate ester in 10ml of dichloromethane, slowly drop into 3mmol / ml of ethylenediamine in dichloromethane solution under ice-bath conditions, and monitor the reaction until complete by thin-layer chromatography (TLC method) Afterwards, the reaction solution is ex...

Embodiment 3

[0038] Example 3: Preparation of self-assembled nanomicelle composition containing gambogic acid and gambogic acid-hyaluronic acid conjugate

[0039] (1) Dialysis

[0040] Gambogic acid-hyaluronic acid conjugate 18mg, dissolved in 3ml of water and stirred for 1h. Gambogic acid 9 mg was dissolved in ethanol (methanol). Then the two were mixed, after the probe was ultrasonicated for 30 minutes, it was dialyzed overnight in double distilled water, centrifuged (3000 rpm) for 15 minutes, filtered with a 0.45 μm filter membrane, and freeze-dried.

[0041] (2) Emulsion solvent evaporation method

[0042] Gambogic acid-hyaluronic acid conjugate 18mg, dissolved in 3ml of water and stirred for 1h. Gambogic acid 9 mg was dissolved in dichloromethane. Then the two were mixed, the probe was sonicated for 30 minutes, and stirred overnight at room temperature to volatilize the dichloromethane, centrifuged (3000 rpm) for 15 minutes, filtered with a 0.45 μm filter membrane, and freeze-drie...

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Abstract

The invention discloses a pharmaceutical composition containing a gambogic acid medicament and a preparation method thereof. The pharmaceutical composition containing the gambogic acid medicament is characterized by containing the gambogic acid medicament which forms micelle with an amphipathic high polymeric conjugate. In the invention, the gambogic acid medicament is coated in the amphipathic high polymeric conjugate by physical embedding and chemical conjugation, thus greatly improving the solubility of the gambogic acid medicament, notably improving the storage stability and antitumor activity and improving the safety of the medicament. Compared with gambogic acid medicaments, the pharmaceutical composition has improved curative effects and reduced irritation on treating liver cancer,cervical cancer and other cancers. The invention also provides preparation methods of the amphipathic high polymeric conjugate and the pharmaceutical composition containing the gambogic acid medicament. The preparation method is simple, has a mature process and high yield, and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a pharmaceutical composition containing gambogic acid drugs and a preparation method of the pharmaceutical composition. The pharmaceutical composition is characterized in that the amphiphilic high-polymer conjugate encapsulates gambogic acid drugs in the form of micelles. Background technique [0002] Cancer has become a common disease that seriously threatens human life and health around the world. Clinical treatments such as surgery and chemotherapy are effective means to remove tumors, but surgery can only remove tumors that are visible to the naked eye, but cannot remove invisible subclinical lesions and tumor cells that have metastasized or infiltrated into normal tissues; while conventional Due to the fact that the existing anticancer drugs have almost no selectivity for tumor tissues and cells, there are common problems such as low clinical curative effect, high t...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K47/34A61P35/00A61K47/36
Inventor 周建平姚静孙晓晶侯琳张莉
Owner CHINA PHARM UNIV
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