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Melittin pamoate capable of being continuously released and preparation agent thereof

A technology of pamolate and pamoate sodium salt, applied in the field of medicine, can solve problems such as biological activity influence, and achieve the effect of short half-life and unstable physical and chemical properties

Inactive Publication Date: 2012-06-20
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This is a traditional method of encapsulating water-soluble drugs. The organic solvents and high shear forces involved in the preparation process will have a great impact on the biological activity of solution-type free polypeptides.

Method used

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  • Melittin pamoate capable of being continuously released and preparation agent thereof
  • Melittin pamoate capable of being continuously released and preparation agent thereof
  • Melittin pamoate capable of being continuously released and preparation agent thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The separation and purification of embodiment 1 melittin

[0024] Weigh 10g of dried bee venom, put it in a centrifuge tube, add formic acid-ammonium formate (0.1M, pH4.5) buffer solution to fully dissolve it, centrifuge at 4000r / min for 5min, absorb the supernatant, pass through a 0.45um micropore Membrane filtration; wash the residue at the bottom of the centrifuge tube with buffer, centrifuge, take the supernatant, filter, combine the two filtrates, and set aside. Put the above-mentioned pretreated sample on a Sephadex G-50 column, and use formic acid-ammonium formate buffer as the eluent for elution, the flow rate is 10mL / h, and the detection wavelength is 280nm; The column was subjected to secondary chromatography under the same conditions, and the eluate from the main peak was collected and freeze-dried. The purity of melittin isolated by high performance gel permeation chromatography was 96.4%.

Embodiment 2

[0025] Example 2 Preparation of pamoic acid sodium salt solution (0.1M)

[0026] Suspend 3.88g of pamoic acid in 20ml of water for injection, add 20ml of 1.0M sodium hydroxide solution under stirring until the pamoic acid is completely dissolved, add water for injection to dilute to 100ml.

Embodiment 3

[0027] Example 3 Preparation of melittin pamolate (1:0.5 mol / mol)

[0028] Dissolve 1.42g of melittin in 20ml of water for injection, and add 10ml of pamoic acid disodium salt solution (0.1M) under stirring until crystallization occurs. The precipitate was filtered off, washed with water for injection and dried. The product contained 2:1 peptide pamolate (mol / mol).

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Abstract

The invention relates to the technical field of medicine and discloses a melittin pamoate capable of being continuously released and a preparation agent and a preparation method of the same. The melittin pamoate is used for treatment of rheumatic arthritis and scapulohumeral periarthritis, is capable of enabling effective constituent to be continuously released for one to four weeks, overcomes the shortcoming that solution type free melittin is short in plasma half-life and poor in stability and requires frequency injection, and improves adaptability of patients for pharmacy.

Description

[0001] technical field [0002] The invention relates to the technical field of medicine, and specifically provides a sustained-release melittin pamoate and its formulation and preparation method. [0003] Background technique [0004] Melittin is the most important component of bee venom with pharmacological effects and biological activity, accounting for about 50% of the dry weight of bee venom. Its primary structure consists of 26 amino acid residues: NH 2 -Gly-Ile-Gly-Ala-Val-Leu-Lys-Val-Leu-Thr-Thr-Gly [0005] -Leu-Pro-Ala-Leu-Ile-Ser-Trp-Ile-Lys-Arg-Lys-Arg-Gln-Gln-CONH 2 , formula C 131 h 229 o 31 , molecular weight 2840 Da. Among them, the amino acids at the 1st to 20th positions are hydrophobic groups, and the amino acids at the 21st to 26th positions are hydrophilic groups; the 2 amino acids at the N-terminal and the 4 amino acids at the C-terminal are all positively charged. The presence of three lysine and two arginine residues makes melittin a strongly ...

Claims

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Application Information

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IPC IPC(8): C07K14/435C07K1/113A61K38/17A61K9/19A61P29/00A61P35/00
Inventor 石凯毕洪书崔福德
Owner SHENYANG PHARMA UNIVERSITY
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