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Composite for treating myelodysplastic syndrome and preparation method thereof

A technology for myelodysplasia and composition, which is applied in the direction of drug combination, medical preparations with non-active ingredients, non-active ingredients of polymer compounds, etc., 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: 2015-07-22
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 treating myelodysplastic syndrome, which 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 placed in a grinding machine and ground to obtain a solid dispersion of 40-100 meshes;

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

[0057] (3) granulation: the premix obtained in (2) is compressed into large pieces or plates, and the granules are pulverized and granulated through an 8-30 mesh sieve to obtain drug-containing granules;

[0058] (4) Mixing: mixing the drug-contain...

Embodiment 2

[0062] A composition for treating myelodysplastic syndrome, which 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 placed in a grinder and ground to obtain a solid dispersion of 40-100 meshes;

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

[0067] (3) granulation: the premix obtained in (2) is compressed into large pieces or plates, and the granules are pulverized and granulated through an 8-30 mesh sieve to obtain drug-containing granules;

[0068] (4) total mixing: mixing the drug-containing granules of (3) ...

Embodiment 3

[0072] A composition for treating myelodysplastic syndrome, which 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 grinding machine and ground to obtain a solid dispersion of 40-100 meshes;

[0076] (2) Mixing: Mix the solid dispersion obtained in (1) with povidone, calcium carboxymethyl cellulose of 1 / 2 formula and powdered cellulose of about 2 / 3 formula, and mix with 1 / 2 formula. Amount of talc is mixed to obtain a premix;

[0077] (3) granulation: the premix obtained in (2) is compressed into large pieces or plates, and the granules are pulverized and granulated through an 8-30 mesh sieve to obtain drug-containing granules;

[0078] (4) total mixing: the medicated granules of (3) gained, the calcium carboxymethyl cellulose of surplus and powdery cellulose are mixed for 10min, and then the t...

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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 present 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. Functional failure, high risk of transformation to acute myeloid leukemia (AML). In recent years, the progress of drug therapy for the treatment of myelodysplastic syndrome is slow, and the curative effect is poor, and the current effective rate is less than 50%. Bone marrow transplantation is curative, but it is risky and expensive. [0003] Lenalidomide, chemical name is 3-(7-amino-3-oxo-1H-isoindol-2-yl) piperidine-2,6-dione, molecular formula C 13 H 13 N 3 0 3 , its molecular weight is 259.2606, it is a kind of insoluble compound in water, soluble in organic solvent and low pH value solution. It has lower solubilit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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