Melphalan sustained-release implant treating for solid tumor

A slow-release implant, melphalan technology, applied in anti-tumor drugs, pharmaceutical formulations, drug combinations, etc., can solve the problem of short release period of slow-release preparations

Inactive Publication Date: 2008-06-25
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 preparations have a short release period and obvious burst release phenomenon.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Put the weighed slow-release auxiliary material (molecular weight is 15000-25000 PLGA, 50:50) and slow-release modifier (mannitol) into different containers respectively, then add a certain amount of organic solvent to dissolve and mix well (to fully dissolve prevail) and 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:

[0081] (A) 1% melphalan, containing 1mg melphalan, 99mg PLGA

[0082] (a) 1% melphalan, containing 1mg melphalan, 95mg PLGA, 4mg mannitol;

[0083] (B) 5% melphalan, containing 5mg melphalan, 95mg PLGA;

[0084] (b) 5% melphalan, containing 5mg melphalan, 91mg PLGA, 4mg mannitol;

[0085] (C) 10% melphalan, containing 10mg melphalan, 90mg PLGA;

[0086] (c) 10% melphalan, containing 10mg melphalan, 80mg PLGA, 10mg mannitol;

[0087] (D) 15% melphalan, containing 15mg melphalan, 85mg...

Embodiment 2

[0092] 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 without a sustained-release modulator (mannitol) had obvious burst release phenomenon, and the burst release phenomenon mostly occurred on the 20th-30th day, about Accounting for 60-80% of the total drug content, while (a), (b), (c), (d) and (e) and other melphalan sustained-release implants containing a sustained-release modifier (mannitol) The burst release phenomenon is obviously not obvious, and the drug is released slowly for 3-5 weeks.

Embodiment 3

[0094] Put the weighed sustained-release auxiliary material (PLGA with a molecular weight of 20000-30000, 75:25) and the sustained-release regulator (mannitol) into different containers respectively, then add a certain amount of organic solvent to dissolve and mix (to fully Dissolution prevails) and 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:

[0095] (A) 1% melphalan, containing 1mg melphalan, 99mg PLGA

[0096] (a) 1% melphalan, containing 1 mg melphalan, 95 mg PLGA and 4 mg sorbitol;

[0097] (B) 5% melphalan, containing 5mg melphalan, 95mg PLGA;

[0098] (b) 5% melphalan, containing 5 mg melphalan, 91 mg PLGA and 4 mg sorbitol;

[0099] (C) 10% melphalan, containing 10mg melphalan, 90mg PLGA;

[0100] (c) 10% melphalan, containing 10 mg melphalan, 80 mg PLGA and 10% sorbitol;

[0101] (D) 15% melpha...

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PUM

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Abstract

The invention relates to a sustained-release implant for treating a solid tumor, which is characterized in that: the sustained-release implant contains an effective anticancer amount of Melphalan and sustained-release regulator. The sustained-release excipient is the soluble degradable absorbable macromolecular polymer of organism, and the sustained-release excipient is mainly PLA and PLGA. The release regulating agent is chosen from a combination or a plurality of combinations of mannitol, sorbic alcohol, xylitol, oligosaccharide, chitin chitosan, potassium salt, sodium salt, hyaluronic acid, collagen, chondroitin, gelatin and albumin. The sustained-release implant can release carmustine to the part of the tumor in the process of the degradation and absorption; the effect medicine concentration can be maintained in the part of the tumor while the systemic toxic reaction is decreased obviously, therefore the sustained-release implant can be used independently or used with the other non-operative treatment such as the chemotherapeutics and the radiation therapy, etc., and the invention can be used for treatment of solid tumor in each period. The medicine concentration in the part of the tumor can be selectively improved, and effect of non-operative treatment such as the chemotherapeutics and the radiation therapy can be strengthened.

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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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/198A61K47/34A61P35/00
Inventor 孙娟杨健
Owner JINAN SHUAIHUA PHARMA TECH
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