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Pomalidomide compound and preparation method thereof

A technology of pomalidomide and complexes, which is applied in the field of pomalidomide fine particles and its technology, can solve the problems of decreased dissolution rate aggregation, increased surface energy, and decreased in vivo absorption of preparation bioavailability, achieving uniform good effect

Inactive Publication Date: 2015-04-22
NANJING CORE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the increased surface area and surface energy of the raw materials after micronization, the powder is in an unstable state, easy to aggregate, and has poor fluidity and dispersion. The aggregation of the dissolution rate decreases, resulting in a decrease in the bioavailability or in vivo absorption of the preparation

Method used

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  • Pomalidomide compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

10ml

[0019] Example 1 Preparation process: Dissolve 2-hydroxypropyl-β-cyclodextrin in 75% ethanol aqueous solution, add pomalidomide to uniformly disperse or dissolve, then add 1 g of mannitol, and freeze-dry.

[0020] The dried product obtained is mixed with 1 g of mannitol and hypromellose E15 and pulverized to a mesh size of 80-100 to obtain a pomalidomide complex.

Embodiment 2

[0022] prescription

[0023] Example 2 Preparation process: Mix the pomalidomide complex with microcrystalline cellulose, micropowder silica gel, and magnesium stearate evenly, and mix them in a SBH-20 three-dimensional mixer for 10-60 minutes, and mix them at 10, 20, and 30 minutes respectively. , 40, 50 and 60 minutes, take samples from the upper, middle and lower points to measure the content uniformity. After 60 minutes, add micronized silica gel and magnesium stearate, continue mixing for 10 minutes, and then fill the capsules with a loading amount of 50 mg / capsule.

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PUM

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Abstract

The invention discloses a pomalidomide compound which consists of pomalidomide, cyclodextrin and a modified substance thereof, a dispersant and a binder. The dosage of the cyclodextrin and the modified substance thereof is 2-8 times (w / w) of the pomalidomide, the dosage of the dispersant is 10-50 times (w / w) of the pomalidomide and the dosage of the binder is 1-5% of the entire compound. Solid preparations such as capsule prepared from the pomalidomide compound disclosed by the invention can be used for achieving good mixing uniformity within relatively short time; and meanwhile, even under severe conditions, the dissolution rate can be kept at good stability as well.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular, relates to a pomalidomide fine particle and a preparation method thereof, in particular to a pomalidomide fine particle prepared by solid dispersion technology and a process thereof. Background technique [0002] Pomalidomide, a thalidomide analogue, is an immunomodulator with antitumor activity. It can inhibit the proliferation of lenalidomide-resistant multiple myeloma cell lines and induce tumor cell apoptosis synergistically with dexamethasone in lenalidomide-sensitive and lenalidomide-resistant cell lines. At the same time, pomalidomide can enhance T cell- and natural killer (NK) cell-mediated immunity and inhibit the production of pro-inflammatory cytokines in monocytes, showing that it has certain anti-angiogenic activity. The U.S. Food and Drug Administration (FDA) approved it on February 8, 2013 for the treatment of multiple myeloma patients whose cond...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K47/40A61K47/26A61K47/32A61K47/38A61P35/00
Inventor 王雪根何凌云金皓洁徐烨
Owner NANJING CORE TECH CO LTD
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