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Sustained-release injection and preparation method thereof

A slow-release injection and slow-release microparticle technology, which is applied in the direction of pharmaceutical formulations, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., can solve problems such as poor injectability, low viscosity, and poor stability

Inactive Publication Date: 2009-03-11
孔庆忠
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some drugs cannot effectively cross the blood-brain barrier or blood-tumor barrier
Many drugs have poor gastrointestinal absorption when taken orally, and some drugs are unstable when given intravenously
Sustained-release injections can solve the above-mentioned problems caused by implants and or sustained-release implants to a certain extent, however, there are many problems in existing sustained-release injections, such as, but not limited to, poor injectability and easy blockage , poor stability, easy layering, low viscosity, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0173] Example 1. Comparison of suspending agent to the suspending effect of sustained-release microspheres

[0174] Put 80 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 20 mg of paclitaxel, re-shake, and then vacuum-dry to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make slow-release microparticles containing 20% ​​paclitaxel, and then suspended in physiological saline containing 0.0, 0.01, 0.05 and 1.5% sodium carboxymethylcellulose to prepare the corresponding Suspension-type sustained-release injection, the viscosity of the injection is 50, 15, 28cp (at 20°C-30°C). The sustained-release injection was injected subcutaneously into mice 20 times, and the success rates were 10%, 30%, 50% and 70% respectively. The results showed that its injectability improved with the increase of the suspending agent content, and the...

Embodiment 2

[0176] The method step that is processed into sustained-release injection is identical with embodiment 1, but difference is that contained suspending agent is respectively,

[0177] (A) 1.5-5% sodium carboxymethylcellulose; or

[0178] (B) 1.5-5% sodium carboxymethylcellulose and 0.1% Tween 80; or

[0179] (C) 1.5-5% sodium carboxymethylcellulose and 15% sorbitol and 0.1 Tween 80.

[0180] The above three sustained-release injections were injected into the hind leg muscles of rats 20 times, and the success rates were 30%, 50% and 70% respectively. The results showed that its injectability improved with the increase of the types of suspending agents, and the injectability of normal saline containing 1.5% sodium carboxymethylcellulose, 15% sorbitol and 0.1 Tween 80 was the best. All are percentages by weight.

Embodiment 3

[0182] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) at 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well and divide into three groups , the first group added 20mg docetaxel, the second group added 20mg docetaxel and 2mg sodium carboxymethylcellulose, the third group added 20mg docetaxel and 2mg sodium carboxymethylcellulose and 5% sorbic acid Alcohol, after re-shaking, the corresponding microspheres for injection were prepared by spray-drying method. Then suspend the microspheres in normal saline, and the order of the measured viscosity is: the first group < the second group < the third group, intramuscularly injected 20 times in the hind legs of rats, and the success rates were 30%, 40% and 60% respectively. %. The results showed that the injectability improved with the increase of the types of suspending agents, and the injectability of the microspheres containing sodium carboxymethylcellulose and sorbitol was the best. The ...

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PUM

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Abstract

A slow release injection contains bioactive components, slow release adjuvants, a suspending agent and a dissolvant, wherein, the dissolvant is a common dissolvant or a special dissolvant containing the suspending agent. The slow release adjuvants are chosen from copolymer of polylactic acid, polyglycolic acid and hydroxyacetic acid, copolymer of ethylene vinyl acetate, polifeprosan, etc. The injection can be slowly released to the local focuses of tumors, inflammation and tuberculosis during the decomposition and absorption of the slow release adjuvants, therefore, the slow release adjuvants can not only extremely reduce general toxic reactions thereof but also keep the effective drug concentration at the chronic local focuses of tumors, etc. The suspending agent is chosen from sodium carboxymethyl cellulose, mannitol, and the like, and is used for suspending the active components or suspending the slow release particles or microspheres containing anticancer active components. The slow release injection has the advantages of good injectivity, seldom blockage, strong stability, infrequent demixing, and little general toxic reaction of local injection; furthermore, the slow release injection can selectively increase the drug concentration in local focuses, and enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy, and the like.

Description

[0001] This application is a divisional application of No. 2006101260389 (1) Technical field [0002] The invention relates to a sustained-release injection and a preparation method and application thereof, belonging to the technical field of medicines. It specifically relates to the composition, preparation and application of a sustained-release microparticle and its injection. (2) Background technology [0003] Blood vessels, connective tissue, matrix proteins, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the diffusion of chemotherapy drugs around the tumor and in the tumor tissue. Infiltration and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the drug delivery in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res.2000, 60 (9 ): 2497-503). Due to the excessive expansive hyperplasia of solid tumors, the i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/08A61K45/06A61K47/34A61P35/00
Inventor 孔庆忠
Owner 孔庆忠
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