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Oral solid pharmaceutical composition in micronized form and preparation method thereof

A composition and micronization technology, applied in the field of medicine, can solve the problems of severe side effects, poor bioavailability, incompleteness, etc.

Inactive Publication Date: 2020-03-27
广州艾格生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although HHT exhibits potent inhibitory activity against a variety of Bcr-Abl mutations including Bcr-AblT315I, there are still many problems to be improved: 1) Severe toxic side effects, including bone marrow suppression, cardiotoxicity, gastric Intestinal reactions, etc.; 2) Poor bioavailability, slow and incomplete oral absorption of HHT

Method used

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  • Oral solid pharmaceutical composition in micronized form and preparation method thereof
  • Oral solid pharmaceutical composition in micronized form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] The homoharringtonin derivatives were ultrafinely pulverized using MQP01 airflow pulverizer, and pulverized into D 90 Fine powder below 10μm, crushing conditions: low-temperature drying air temperature is 6°C, water content is 0.5%, inlet pressure is 0.8MPa, working pressure of ultrafine pulverizer is 0.8MPa, internal working temperature is 6°C, crushing times for 3 times.

Embodiment 2

[0039] Use a jet mill to ultrafinely pulverize the homoharringtonin derivative raw material, collect the pulverized raw material particles, and use a Beckman LS 13 320 XR laser diffraction particle size analyzer to measure the particle size of the fine powder, and the particle size at 95% cumulative volume The micronized homoharringtonin derivative is obtained below 10 μm.

Embodiment 3

[0040] Embodiment 3 Take the solid pharmaceutical composition prescription 1~4

[0041] Raw materials (g) / 1000 pieces Prescription 1 Prescription 2 Prescription 3 Prescription 4 Comparative example 1 Homoharringtonin derivatives 50 15 50 50 50 (not pulverized, particle size above 80μm) Hydroxypropyl Cellulose 30 30 45 15 30 lactose monohydrate 20 30 10 30 20 microcrystalline cellulose 35 60 30 40 35 Croscarmellose Sodium 10 10 10 10 10 Sodium dodecyl sulfate 3 3 3 3 3 Micropowder silica gel 2 2 2 2 2

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Abstract

The invention discloses an oral solid pharmaceutical composition in a micronized form by using a solid preparation with a micronized homoharringtonine derivative as an active component. The composition comprises a pharmacological active agent with an effective dosage, crospovidone or polyvinylpyrrolidone, and an oral solid pharmaceutical composition used for a pharmacological active agent. The oral solid pharmaceutical composition has an excellent in-vitro dissolution rate, and has good dissolution rates in a variety of pH conditions, so that good absorption of medicines in different populations can be effectively ensured, and the problems that an existing homoharringtonine derivative drug is not easily dissolved out in an in-vivo gastrointestinal environment and then in-vivo bioavailability of drugs is reduced and efficacy is influenced can be solved.

Description

technical field [0001] The invention relates to an oral solid pharmaceutical composition comprising a micronized form, belonging to the technical field of medicine. Background technique [0002] Chronic myelogenous leukemia is a malignant myeloproliferative disorder that accounts for approximately 20% of adult leukemias. According to Globocan's research data in 2012, there were 351,965 new leukemia cases and 265,461 deaths worldwide in 2012. The emergence of Bcr-Abl fusion protein is the main pathogenic mechanism of CML. With the application of Bcr-Abl inhibitors, the problem of acquired drug resistance, especially the emergence of Bcr-AblT315I mutant has become a major challenge in the treatment of CML, and there is an urgent need to develop new Bcr-Abl inhibitors or drugs with other mechanisms of action. [0003] The emergence of Bcr-Abl fusion protein is the main pathogenic mechanism of CML, and the acquired point mutation of Bcr-Abl kinase is the main cause of drug res...

Claims

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Application Information

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IPC IPC(8): A61K31/55A61K9/14A61K9/20A61K47/38A61P35/02
CPCA61K9/14A61K9/2054A61K31/55A61P35/02
Inventor 何盛江张庆文谭斌李阳平
Owner 广州艾格生物科技有限公司
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