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Degradable apisin microballoons injection and preparation thereof

A biodegradable injection technology, applied in the field of medicine, can solve the problems of insufficient purity of bee venom, poor oral absorption, allergies, etc., and achieve the effects of improving compliance and quality of life, saving manpower and material resources, and stabilizing blood drug concentration

Inactive Publication Date: 2003-09-03
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although bee venom has withstood thousands of years of long-term tests, ancient and modern Chinese and foreign countries have accumulated rich experience in the medical application of bee venom, and bee venom resources are abundant, and modern basic and clinical research on bee venom is also quite active. The application is still very limited, and the reasons are mainly the following aspects: on the one hand, the purity of bee venom is not enough, which can easily cause allergies; on the other hand, because of its large molecular weight (about 3000), poor stability, oral absorption is very poor and It is easy to be destroyed. At present, bee venom injection is generally used clinically, mainly including bee venom water injection, oil injection and freeze-dried powder injection. The clinical usage of treating arthritis is generally intra-articular injection once a day, once a day, A course of treatment for 20 to 30 consecutive days, several courses of treatment need to be applied repeatedly
Such frequent injections undoubtedly brought great pain to the patient's body and mind, and due to poor compliance, it is very easy to lead to the failure of midway treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0007] Embodiment 1. Preparation of bee venom polylactic acid microspheres

[0008] Dissolve 120mg of bee venom (Jilin Taonan Pharmaceutical Factory) with 2ml of distilled water, dissolve 1.6g of PLA (molecular weight 10627) in 35ml of dichloromethane, emulsify into a water-in-oil emulsion with a cell ultrasonic pulverizer, cool down with an ice-water bath, drop Add it to 800ml of 1% polyvinyl alcohol (Japanese Wako Pure Chemical Industry Co., Ltd.) solution, and stir at a speed of 800 rpm to form double emulsion. Stirring was continued as the dichloromethane evaporated. The PLA solidifies from the emulsion droplets to form PLA microspheres encapsulating the bee venom. The encapsulation rate of bee venom can reach more than 80%.

[0009] Place 20 mg of polylactic acid microspheres of mee venom after vacuum drying in 4 ml of acetate buffer, vibrate in a SHA-B type constant temperature horizontal shaker (37 ° C, 100 rpm), and compare with the first day, third day, and Samples...

Embodiment 2

[0010] Embodiment 2. Preparation of bee venom lactic acid-glycolic acid copolymer microspheres

[0011] Dissolve 20mg of bee venom (Jilin Taonan Pharmaceutical Factory) with 0.3ml of distilled water, dissolve 200g of PLGA (molecular weight 10627) in 6ml of dichloromethane, emulsify into a water-in-oil emulsion with a cell ultrasonic pulverizer, cool down with an ice-water bath, drop Add it to 100ml of 1% polyvinyl alcohol (Japanese Wako Pure Chemical Industry Co., Ltd.) solution, and stir at a speed of 800 rpm to form a double emulsion. Stirring was continued as the dichloromethane evaporated. The PLA solidifies from the emulsion droplets to form PLGA microspheres encapsulating the bee venom. The encapsulation rate of bee venom can reach more than 85%.

[0012] Place 20 mg of polylactic acid microspheres of mee venom after vacuum drying in 4 ml of acetate buffer, vibrate in a SHA-B type constant temperature horizontal shaker (37 ° C, 100 rpm), and compare with the first day,...

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Abstract

A biodegradable aptoxin microsphere as injection is prepared through dissolving the biodegradable high-molecular material in dichloromethane or ethyl acetate, ultrasonic dispersion of the aqueous solution of aptoxin in it to obtain water-in-oil emulsion, cooling to 5 deg.C, dropping it to the aqueous solution of polyvinyl alcohol, stirring to obtain water-in-oil-in-water emulsion, continuous stirring to volatilize the dichloromethane or ethyl acetate and solidify the microspheres, filtering, washing and vacuum drying.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to a biodegradable microsphere injection of bee venom and a preparation method thereof. Background technique: [0002] The invention relates to spherical microparticles made by wrapping or absorbing bee venom with degradable macromolecule material as carrier. Bee Venom (bee venom, referred to as bee venom) is produced by the bee venom and stored in the poison sac. When the bee is stimulated, it is a kind of venom discharged from the sting needle of its tail. It can be obtained from three ways: chemical synthesis, genetic engineering Expression and extraction and purification from bee venom. Among them are melittin, melittin, MCD peptide, histamine, phospholipase A 2 Hyaluronidase and hyaluronidase are biologically active substances containing a variety of chemical components, and have a long history of clinical application in my country. The chance that bee venom can cure disea...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K35/644A61P19/02A61P29/00A61P31/04
Inventor 崔福德寸冬梅
Owner SHENYANG PHARMA UNIVERSITY
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