Meifaron sustained-release implantation agent for curing entity tumour

A slow-release implant, tumor technology, applied in the field of medicine, can solve the problems of short drug release cycle, poor tumor cell effect, poor effect of residual tumor cells, etc.

Inactive Publication Date: 2008-05-14
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing sustained-release agents use polyesters (polyesters) such as PLA and PLGA as sustained-release carriers, which have a short drug release cycle and have poor effects on tumor cells entering the dormant phase. Therefore, the effect on residual tumor cells Poor effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] The weighed sustained-release excipient (the PLGA with a molecular weight of 15000-25000, 75:25) or the poly(L-lactide-co-ethyl phosphate) with a molecular weight of 15000-25000 were put into different containers respectively, and then Add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add different weights of melphalan, re-shake, and then vacuum dry to remove the organic solvent. The dried solid sustained-release implant was immediately shaped to obtain the following sustained-release implant:

[0078] (A) 1% melphalan, containing 1mg melphalan, 99mg PLGA

[0079] (a) 1% melphalan, containing 1 mg melphalan, poly(L-lactide-co-ethyl phosphate);

[0080] (B) 5% melphalan, containing 5mg melphalan, 95mg PLGA;

[0081] (b) 5% melphalan, containing 5 mg melphalan, poly(L-lactide-co-ethyl phosphate);

[0082] (C) 10% melphalan, containing 10mg melphalan, 90mg PLGA;

[0083] (c) 10% melphalan, containing 10 mg melphalan, poly(L...

Embodiment 2

[0089] 10 sustained-release implants in Example 1 were put into the dissolution apparatus respectively to measure the drug cumulative release amount (%) at different times, and it was found that in the sustained-release implants (A), (B), (C ), (D) and (E) five melphalan sustained-release implants with PLGA as the auxiliary material have a fast release rate, 30-40 days, while (a), (b), (c), (d) And (e) etc., the drug slow release rate of the melphalan sustained-release implant with poly(L-lactide-co-ethyl phosphate) as auxiliary material is relatively slow, which is 40-60 days.

Embodiment 3

[0091] The weighed sustained-release excipient (the PLGA with a molecular weight of 20000-30000, 75:25) or the poly(L-lactide-co-propyl phosphate) with a molecular weight of 15000-25000 were put into different containers respectively, and then Add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add different weights of melphalan, re-shake, and then vacuum dry to remove the organic solvent. The dried solid sustained-release implant was immediately shaped to obtain the following sustained-release implant:

[0092] (A) 1% melphalan, containing 1mg melphalan, 99mg PLGA

[0093] (a) 1% melphalan, containing 1 mg melphalan, 95 mg poly(L-lactide-co-propyl phosphate);

[0094] (B) 5% melphalan, containing 5mg melphalan, 95mg PLGA;

[0095] (b) 5% melphalan, containing 5 mg melphalan, 91 mg poly(L-lactide-co-propyl phosphate);

[0096] (C) 10% melphalan, containing 10mg melphalan, 90mg PLGA;

[0097] (c) 10% melphalan, containing 10 mg melp...

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Abstract

The invention relates to a slow-release implant agent of Memphalan, which is characterized by effective amounts of Memphalan, slow-release excipients and releasing regulatory agents in the slow-release implant agent. The excipients comprise macromolecules which are biologically compatible and degradable, mainly PLA and PLGA. The releasing regulatory agents are selected from one or more items from mannitol, sorbitol, xylitol, oligosaccharide, chitin, potassium salt, sodium salt, hyaluronic acid, collagen, chondroitin, gelatin and albumin. The slow-release implant agent slowly releases Memphalanon the local tumor in the process of degradation and absorption, so the argent can evidently reduce the systemic toxicity and simultaneously apply to the effective drug concentration control on the local tumor. Therefore, the argent can be applied separately or combined with the non-surgical treatments such as chemotherapy drug and radiotherapy, which can be also widely used for tumor treatment of different phases, not only selectively improving the drug concentration on local tumor but also reinforcing the therapeutic effect of non-surgical treatments such as chemotherapy drug and radiotherapy.

Description

(1) Technical field [0001] The invention relates to a slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Although the research on cancer has made great progress, its mortality rate is still in the forefront of various common causes of death. In my country, about 1.6 million people suffer from cancer every year, and nearly 1.3 million people die of cancer, accounting for one-fifth of the total death toll. The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 million. Therefore, exploring an effective method or drug for treating cancer has become a h...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/198A61K47/34A61P35/00
Inventor 孙娟孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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