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Novel type nanometer particle preparation capable of reducing gastroenteritic toxicity of camptothecin medicines

A nanoparticle and camptothecin technology, applied in the field of medicine, can solve problems such as difficult to obtain effects, achieve the effect of reducing excretion and increasing anti-tumor effect

Inactive Publication Date: 2010-06-02
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In summary, it is difficult to achieve the desired effect by reducing the gastrointestinal toxicity of camptothecin drugs only by using BCRP small molecule inhibitors or functional excipients to inhibit the action of BCRP

Method used

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  • Novel type nanometer particle preparation capable of reducing gastroenteritic toxicity of camptothecin medicines
  • Novel type nanometer particle preparation capable of reducing gastroenteritic toxicity of camptothecin medicines
  • Novel type nanometer particle preparation capable of reducing gastroenteritic toxicity of camptothecin medicines

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073]

[0074] Preparation method: Take the prescription amount of hydroxycamptothecin, glyceryl monostearate, medium chain triglyceride (MCT), soybean lecithin, olive ene, add appropriate amount of ethanol to dissolve, spin evaporate to dry organic solvent, vacuum dry, 80 ℃ heating and dissolving as an oil phase. Sodium oleate was dissolved in water for injection and heated to 80°C as the water phase. Under stirring at 80°C, drop the water phase into the oil phase while hot, and pass through N 2 Colostrum was prepared in a high-shear homogenizer under the condition of 2 Under the condition of high pressure homogeneous treatment, the hydroxycamptothecin nanoparticles are obtained after cooling, and then freeze-dried to obtain the hydroxycamptothecin nanoparticles freeze-dried preparation.

[0075] Average particle size (Particle size) = 112.4 ± 31.1nm; polydispersity coefficient (PI) = 0.114

Embodiment 2

[0077]

[0078]

[0079] Preparation method: Weigh hydroxycamptothecin, limonene, soybean lecithin and stearic acid according to the prescription amount, heat to (80±5)°C under nitrogen, then add glycerol and Poloxamer- 188 aqueous solution to make coarse milk; under the condition of (80±5)°C and nitrogen flow, the milk was homogenized for 5 times under the pressure of 4114 MPa on the high-pressure homogenizer, and after filling with nitrogen, it was cooled rapidly to form hydroxycamptothecin nanoparticles, and separated After packaging, freeze-drying, the hydroxycamptothecin nano-particle freeze-drying preparation is obtained.

[0080] Particle size=201.0±15.9nm; PI=0.102

Embodiment 3

[0082]

[0083] Preparation method: Weigh the prescription amount of CPT-11, glyceryl monostearate, zedoary oil, Tween80, and egg yolk lecithin, add appropriate amount of ethanol to dissolve, spin evaporate to dryness to remove organic solvent, dry in vacuum, heat and dissolve at 80°C as the oil phase. Sodium oleate was dissolved in water for injection and heated to 80°C as the water phase. Add the water phase to the oil phase under stirring at 80°C, and pass N 2 Colostrum was prepared in a high-shear homogenizer under the condition of 2 Under the condition of high-pressure homogeneous treatment, after cooling, irinotecan nanoparticles were prepared, subpackaged, freeze-dried, and stored at 4°C to obtain irinotecan nanoparticle freeze-dried preparations.

[0084] Particle size=123.6±21.0nm; PI=0.124

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Abstract

The invention belongs to the field of medical technology and relates to a novel nano-particle preparation for reducing the gastrointestinal toxicity of camptothecin derivatives. The preparation mainlyconsists of camptothecin derivatives treating effective doses, carrier matrix, excipents with the BCRP inhibitory effect and emulsifiers. The novel nano-particle preparation of camptothecin derivatives of the invention can decrease the metabolism yield by bile, reduce the irritation to the gastrointestinal tract by medicines and reduce the gastrointestinal toxicity by medicines.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a novel nanoparticle preparation capable of reducing gastrointestinal toxicity of camptothecin drugs. Background technique [0002] Camptothecin drugs (cytotoxic drugs) currently used for tumor treatment have obvious anti-tumor activity, can prolong the survival time of patients, reduce mortality, and are more active against digestive tract tumors, leukemia, bladder cancer, etc. powerful. However, gastrointestinal toxic reactions such as nausea, vomiting, and diarrhea caused by these treatments are still the rate-limiting steps for patients to be cured. Among them, irinotecan (CPT-11) is the first-line drug for the treatment of advanced colorectal cancer. The elimination pathway of CPT-11 and its active metabolites SN-38 and SN-38G in the body is mainly through bile excretion. When different doses of CPT-11 are given to different patients, the cumulative excretion of CPT-11, SN-3...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P35/00A61K47/34A61K31/4745A61K47/44A61K9/14A61K47/06A61K47/22
Inventor 甘勇张馨欣朱春柳甘莉
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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