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Carmustine sustained-release implant for treating solid tumor and preparation method thereof

A slow-release implant, carmustine technology, applied in the field of medicine, can solve the problems of short release period and instability, and achieve the effects of enhanced sensitivity, enhanced effect, and enhanced anti-cancer effect.

Inactive Publication Date: 2015-04-22
SHANDONG LANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the sustained-release implants made of polyphenylpropanol as auxiliary materials have many defects, such as but not limited to: instability, need to be stored below -20°C, short release period (about 5 days), and obvious burst release ( Over 60% within 2 days)

Method used

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  • Carmustine sustained-release implant for treating solid tumor and preparation method thereof
  • Carmustine sustained-release implant for treating solid tumor and preparation method thereof
  • Carmustine sustained-release implant for treating solid tumor and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0100] Embodiment 1, compared the difference of the selected adjuvant of the present invention and polyphenylene

[0101] Mix 9.0g PLGA (the mass ratio of lactide to glycolide is 50:50, the viscosity range is 0.30dl / g) and 9.0g polyphenylene propane (p-CPP): sebacic acid ( SA) copolymer, 80:20) into containers "A" and "B", respectively, add 100ml of dichloromethane to dissolve and mix well, then add 1.0g carmustine, re-shake well, pour into the tray to heat and dry Remove organic solvents. Freeze and pulverize the dried solid composition, put the powder into a tablet machine to form after the organic residue is qualified, make sustained-release tablets at room temperature, sterilize with cobalt 60 after sub-packaging, and the obtained product is "implantation agent" No. 1", is a slow-release implant, with a diameter of 1.4 cm and a thickness of 1.0 mm, wherein,

[0102] Implant No. 1 A is: 10% carmustine, the excipient is PLGA (the ratio of lactide to glycolide is 50:50, the...

Embodiment 2

[0107] Embodiment 2, the impact of different molecular weight copolymers on BCNU release

[0108] The sustained-release implant tablet was prepared according to the preparation process of Example 1, except that the PLGA used was a copolymer of lactide and glycolide with a mass ratio of 50:50, and the weight average molecular weight was 15K, 45K and 75K respectively, and the resulting product was Implant No. 2 (A, B, C) has a diameter of 1.35-1.45 cm and a thickness of 0.8-1.2 mm, all containing 10% carmustine. The drug release results of implant No. 2 in pure water are shown in Table 2:

[0109] Table 2

[0110]

[0111] The above results show that, in the case of the same drug loading (10%), the release characteristics of carmustine implants made of lactide-glycolide copolymers are related to the molecular weight of the carrier, and the implants with a weight average molecular weight of 15K The implant (implant No. 2 A) releases too fast, and releases 76.98% on ...

Embodiment 3

[0112] Embodiment 3, compare the impact of different molecular weight copolymers on BCNU release

[0113] Sustained-release implant tablets were prepared according to the preparation process of Example 1, except that PLGA was a lactide-glycolide copolymer with a mass ratio of 50:50, and the weight-average molecular weights were 25K, 40K and 65K respectively, and the resulting product The No. 3 implant (A, B, C) has a diameter of 1.35-1.45 centimeters and a thickness of 0.8-1.2 millimeters, all containing 10% carmustine. Its release time in pure water see

[0114] table 3:

[0115] table 3

[0116]

2 days release percentage (%)

12-day release percentage (%)

28-day release percentage (%)

Implant No. 3 A

9.20

58.98

100

Implant No. 3 B

9.48

46.1

94.31

Implant No. 3 C

12.61

40.92

84.52

[0117] The above results show that, under the same drug loading (10%), the release characteristics of carmu...

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Abstract

The invention relates to a carmustine sustained-release implant for treating solid tumor and a preparation method thereof. The implant is characterized in that the sustained-release implant comprises a sustained-release auxiliary material and an effective anti-tumor component carmustine, wherein the sustained-release auxiliary material is a lactide-glycolide copolymer, the viscosity range of the copolymer is 0.3-0.6, the weight percentage of carmustine is 7.5-30% and the mass proportion of lactide to glycolide is 50: 50. The invention further relates to a method for preparing the sustained-release implant and an application of the implant for treating solid tumors such as pancreatic cancer, lung cancer, liver cancer, breast cancer, brain tumor, esophagus cancer, renal carcinoma, colorectal cancer and the like, liver and brain metastatic tumors. The sustained-release period of the implant is 3-4 weeks, wherein the accumulated release in previous two days is 5-12% of the total drug loading capacity and the accumulated release in previous 12 days is greater than 40% of the total drug loading capacity but less than 60% of the total drug loading capacity.

Description

technical field [0001] The invention relates to a carmustine sustained-release implant for treating solid tumors and its preparation, belonging to the technical field of medicines. Background technique [0002] In 2013, there were 3.5 million new cancer patients in China, of which 2.5 million died. It is estimated that 4 million people will die of cancer every year in China by 2020. The incidence of cancer in the United States and other western countries is also increasing year by year. Therefore, exploring an effective method or drug for treating cancer has become a research hotspot. [0003] At present, the main methods of treating cancer are surgery, radiotherapy and chemotherapy. Since most patients are already at an advanced stage when they go to the doctor, they lose the opportunity for surgery, and the recurrence after surgery is often the main reason for treatment failure. Therefore, effective radiotherapy and chemotherapy are particularly important. [0004] Cur...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/175A61K47/34A61P35/00
CPCA61K9/00A61K31/175A61K47/34
Inventor 孔庆忠魏明星苏红清吴松芝俞建江姜俊敏
Owner SHANDONG LANJIN PHARMA
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