Pomalidomide nanoparticle and preparation and preparation method thereof

A pomalidomide and nanoparticle technology, which is applied in the field of medicine, can solve the problems of low pomalidomide solubility, drug particle size that cannot meet the drug onset, and increased specific surface area.

Active Publication Date: 2014-12-24
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] However, pomalidomide has extremely low solubility in water and is almost insoluble in water, so the dissolution rate of pomalidomide directly determines its drug efficacy in the body
At present, solid dispersion technology, microcapsule microsphere technology, liposome technology, etc. can be used to solubilize poorly soluble drugs. However, for pomalidomide, a particularly poorly soluble drug, the drug particles obtained by the above ...

Method used

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  • Pomalidomide nanoparticle and preparation and preparation method thereof
  • Pomalidomide nanoparticle and preparation and preparation method thereof

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preparation example Construction

[0049] The present invention also provides a preparation method of pomalidomide preparation, comprising the following steps:

[0050] a) mixing pomalidomide, nanocarriers and a solvent to obtain a mixed liquid;

[0051] b) drying the mixed liquid to obtain pomalidomide nanoparticles;

[0052] c) mixing the pomalidomide nanoparticles with a diluent and a lubricant to obtain a pomalidomide preparation.

[0053] The invention mixes the pomalidomide, the nano carrier and the solvent to obtain the mixed liquid. In the present invention, the source of the pomalidomide is not particularly limited, and commercially available pomalidomide well known to those skilled in the art can be used. The pomalidomide preparation provided by the present invention includes 0.5 to 1.5 parts by weight of pomalidomide, preferably 1 part by weight.

[0054] In the present invention, the nanocarrier preferably includes lecithin, povidone, polyalkylcyanoacrylate, acrylamide, N,N-methylene diacrylate a...

Embodiment 1

[0064] (1) 45g soybean lecithin and 8g povidone K30 are dissolved in 50% ethanol aqueous solution, after adding 1g pomalidomide, place in high-speed stirring homogenizer, stir 60min with the stirring speed of 3000r / min, obtain mixed liquid;

[0065] (2) The obtained mixed liquid was spray-dried using a high-efficiency spray dryer, the spray speed was 5mL / min, the inlet air temperature was 60°C, and the outlet air temperature was 25°C to obtain pomalidomide nanoparticles.

Embodiment 2

[0067] (1) 30g soybean lecithin and 6g povidone K30 were dissolved in 50% ethanol aqueous solution, after adding 1g pomalidomide, placed in a high-speed stirring homogenizer, stirred for 60 minutes with a stirring speed of 3000r / min, get mixed liquid;

[0068] (2) The obtained mixed liquid was spray-dried using a high-efficiency spray dryer, the spray speed was 5mL / min, the inlet air temperature was 60°C, and the outlet air temperature was 25°C to obtain pomalidomide nanoparticles.

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Abstract

The invention relates to the technical field of medicines, and specifically relates to pomalidomide nanoparticle and preparation and a preparation method thereof. The pomalidomide nanoparticle comprises the following components in parts by weight: 0.5 to 1.5 parts of pomalidomide, and 10 to 100 parts of nano-carrier, wherein the nano-carrier comprises one or more of lecithin, povidone, polyalkylcyano-acrylate, acrylamide, N, N-methylene diacrylic acid amine, polysorbate, sorbitan monolaurate, lauryl alcohol polyoxyethylene, sodium dodecyl sulfate, poloxamer, polyethylene glycol, cyclodextrin and cyclodextrin derivates. The particle size of omalidomide nanoparticle is at nanometer level; on that basis, the prepared pomalidomide preparation is high in dissolution rate.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a pomalidomide nanoparticle, a preparation and a preparation method thereof. Background technique [0002] Pomalidomide, the chemical name is 3-amino-N-(2,6-dioxo-3-piperidinyl) phthalimide, the English name is pomalidomide, and the molecular formula is C 13 h 11 N 3 o 4 , the molecular weight is 273.25, and the chemical structural formula is as follows: [0003] [0004] Pomalidomide was approved by the US FDA in 2013. It is the third idomide drug after Lenalidomide (Lenalidomide) and Thalidomide (Thalidomide). Including lenalidomide (Lenalidomide) and bortezomib (Bortezomib), for patients who have failed to respond to treatment and relapsed and refractory within 60 days after the last treatment. Pomalidomide has anti-tumor activity, can inhibit the proliferation of hematopoietic tumor cells and induce apoptosis. As a new drug for the treatment of multiple myeloma, its...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/454B82Y5/00A61P35/00
Inventor 方胜张秋佳王珂赵大龙邹德超
Owner BEIJING COLLAB PHARMA
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