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Composite for treating myelodysplastic syndrome and preparation method thereof

A technology for myelodysplasia and composition, which is applied in the directions of drug combination, medical preparations with non-active ingredients, non-active ingredients of polymer compounds, etc. It can solve the factors that affect the porosity of granulation and the reproducibility of specific surface area. , The drug dissolution stability is greatly affected, and the granulation and drying take a long time to achieve the effect of improving the bioavailability of the drug, solving the adhesion of the excipients, and improving the bioavailability.

Active Publication Date: 2014-04-09
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The above-mentioned lenalidomide pharmaceutical composition or oral solid preparations are all granulated by wet granulation, but wet granulation has the following limitations: (1) The operation steps are long, the granulation and drying take a long time, and consume a lot of energy. (2) The dissolution of the drug is slowed down due to crystal form changes or "coarsening" phenomena; (3) Factors affecting the reproducibility of properties such as granulation porosity and specific surface area are relatively More, it has a greater impact on the stability of drug dissolution

Method used

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  • Composite for treating myelodysplastic syndrome and preparation method thereof
  • Composite for treating myelodysplastic syndrome and preparation method thereof
  • Composite for treating myelodysplastic syndrome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] A composition for the treatment of myelodysplastic syndrome is a lenalidomide tablet comprising the following components (in 1000 tablets):

[0052]

[0053]

[0054] Its preparation method comprises the following steps:

[0055] (1) Grinding: Lenalidomide, polyvinyl alcohol and hydroxypropyl-β-cyclodextrin are ground in a grinder to obtain a solid dispersion of 40-100 mesh;

[0056] (2) Mixing: After mixing the solid dispersion obtained in (1) with povidone, 1 / 2 of the formula amount of low-substituted hydroxypropyl cellulose and about 2 / 3 of the formula amount of micropowder silica gel, mix with 1 / 2 of the formula amount of Polyoxyethylene monostearate is mixed to obtain a premix;

[0057] (3) Granulation: compress the premix obtained in (2) into large pieces or plates, pass through 8-30 mesh sieves, pulverize and granulate to obtain drug-containing granules;

[0058] (4) Total blending: Mix the drug-containing granules obtained in (3), the remaining amount of...

Embodiment 2

[0062] A composition for the treatment of myelodysplastic syndrome is a lenalidomide tablet comprising the following components (in 1000 tablets):

[0063]

[0064] Its preparation method is as follows:

[0065] (1) Grinding: lenalidomide, polyethylene glycol 6000, microcrystalline cellulose and sodium lauryl sulfate are ground in a grinder to obtain a solid dispersion of 40 to 100 mesh;

[0066] (2) Mixing: After mixing the solid dispersion obtained in (1) with povidone, 1 / 2 of the formula amount of low-substituted hydroxypropyl cellulose and about 2 / 3 of the formula amount of micropowder silica gel, mix with 1 / 2 of the formula amount of Talc powder is mixed to obtain a premix;

[0067] (3) Granulation: compress the premix obtained in (2) into large pieces or plates, pass through 8-30 mesh sieves, pulverize and granulate to obtain drug-containing granules;

[0068] (4) Total blending: Mix the drug-containing granules obtained in (3), the remaining amount of low-substitut...

Embodiment 3

[0072] A composition for the treatment of myelodysplastic syndrome is a lenalidomide tablet comprising the following components (in 1000 tablets):

[0073]

[0074] Its preparation method is as follows:

[0075] (1) Grinding: Lenalidomide, microcrystalline cellulose and poloxamer are placed in a grinder for grinding to obtain a solid dispersion of 40-100 mesh;

[0076] (2) Mixing: After mixing the solid dispersion obtained in (1) with povidone, 1 / 2 of the formula amount of carboxymethylcellulose calcium and about 2 / 3 of the formula amount of powdered cellulose, mix it with 1 / 2 of the formula Amount of talcum powder is mixed to obtain a premix;

[0077] (3) Granulation: compress the premix obtained in (2) into large pieces or plates, pass through 8-30 mesh sieves, pulverize and granulate to obtain drug-containing granules;

[0078] (4) Total blending: Mix the drug-containing granules obtained in (3), the remainder of carboxymethylcellulose calcium and powdered cellulose fo...

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Abstract

The invention discloses a composite for treating myelodysplastic syndrome. The composite comprises the following components: lenalidomide, a carrier, a solubilizing agent, a disintegrating agent, a lubricating agent, a flow aid and an adhesive, wherein the carrier is a mixture of any one or several of a high-molecular water-soluble polymer, a water-soluble small molecule compound, a hydrophilic auxiliary material and an inorganic carrier; the solubilizing agent is a mixture of one or several of lauryl sodium sulfate, poloxamer, beta. cyclodextrin and a derivative thereof, polysorbate and polyoxyethylene alkyl ether. The invention also provides a preparation method of the composite, and the preparation method comprises the steps of grinding, mixing, dry granulation, total mixing and tabletting or capsule filling. The preparation method disclosed by the invention effectively enhances the water solubility and bioavailability of the lenalidomide; the dry granulation preparation process simplifies the preparation steps, reduces the cost, saves the energy resources, reduces the labor expenditure and realizes the energy conservation and environment protection in production.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology, in particular to a composition for treating myelodysplastic syndrome and a preparation method thereof. Background technique [0002] Myelodysplastic syndromes (MDS) are a group of heterogeneous myeloid clonal diseases originating from hematopoietic stem cells, characterized by abnormal differentiation and development of myeloid cells, manifested as ineffective hematopoiesis, refractory blood cell reduction, Functional failure, high risk of transformation to acute myeloid leukemia (AML). In recent years, drug therapy for the treatment of myelodysplastic syndrome has made slow progress, and the curative effect is poor, and the current effective rate is less than 50%. Bone marrow transplantation is curative, but risky and expensive. [0003] Lenalidomide, chemical name 3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione, molecular formula C 13 h 13 N 3 0 3 , with a molecular weight o...

Claims

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Application Information

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IPC IPC(8): A61K9/36A61K9/20A61K9/48A61K31/454A61K47/40A61K47/34A61K47/20A61P7/00
Inventor 刘锋赖树挺
Owner AC PHARMA CO LTD
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