Vorinostat solid preparation

A technology of vorinostat and solid preparation, applied in the field of medicine, can solve the problems of slow disease change, low malignancy, and increased toxicity

Inactive Publication Date: 2010-11-03
PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In terms of treatment, it varies according to the different processes of the disease. Usually, the initial lesion is limited to the skin, so external ointment or phototherapy (phototherapy) can effectively control the disease; if it has invaded the lymph nodes or other internal organs, and Biological agents (such as bexarotene) combined with radiation or chemotherapy can receive a better response rate, but for more difficult relapsed cutaneous T-cell lymphoma, the above-mentioned treatment mode does not seem to be able to obtain significant curative effect
However, cutaneous T-cell lymphoma is a lymphoma with low malignancy and slow disease change. Therefore, if strong chemotherapy is used, it will not prolong the survival period of patients, but will only increase toxicity and cause discomfort

Method used

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  • Vorinostat solid preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] Vorinostat 100g, filler 90g, disintegrant 8.34g, lubricant 1.66g.

[0076] It is prepared according to the conventional methods for solid preparations.

[0077] Wherein the solid preparation is capsule, tablet, granule or pellet.

[0078] The fillers of the aforementioned pharmaceutical excipients include but are not limited to fillers commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of lactose, starch, dextrin, powdered sugar, microcrystalline cellulose, pregelatinized starch, mannitol, calcium hydrogen phosphate, calcium sulfate

[0079] The disintegrants of the above-mentioned pharmaceutical excipients include, but are not limited to, disintegrators commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of sodium carboxymethyl starch, hydroxypropyl starch, hydroxypropyl cellulose, starch, crospovidone, croscarmellose sodium, and microcrystalline cellulo...

Embodiment 2

[0082] Vorinostat 100g, filler 450g, disintegration 41.70g, lubricant 8.30g.

[0083] It is prepared according to the conventional methods for solid preparations.

[0084] Wherein the solid preparation is capsule, tablet, granule or pellet.

[0085] The fillers of the aforementioned pharmaceutical excipients include but are not limited to fillers commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of lactose, starch, dextrin, powdered sugar, microcrystalline cellulose, pregelatinized starch, mannitol, calcium hydrogen phosphate, calcium sulfate

[0086] The disintegrants of the above-mentioned pharmaceutical excipients include, but are not limited to, disintegrators commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of sodium carboxymethyl starch, hydroxypropyl starch, hydroxypropyl cellulose, starch, crospovidone, croscarmellose sodium, and microcrystalline cel...

Embodiment 3

[0089] Vorinostat 100g, filler 97g, disintegrant 8.92g, lubricant 1.94g.

[0090] It is prepared according to the conventional methods for solid preparations.

[0091] Wherein the solid preparation is capsule, tablet, granule or pellet.

[0092] The fillers of the aforementioned pharmaceutical excipients include but are not limited to fillers commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of lactose, starch, dextrin, powdered sugar, microcrystalline cellulose, pregelatinized starch, mannitol, calcium hydrogen phosphate, calcium sulfate

[0093] The disintegrants of the above-mentioned pharmaceutical excipients include, but are not limited to, disintegrators commonly used in the preparation of solid preparations in pharmacy. Including but not limited to one or more of sodium carboxymethyl starch, hydroxypropyl starch, hydroxypropyl cellulose, starch, crospovidone, croscarmellose sodium, and microcrystalline cellulo...

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PUM

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Abstract

The invention discloses a Vorinostat solid preparation which is prepared from bulk drug Vorinostat and pharmaceutical adjuvant, wherein the pharmaceutical adjuvant comprises a filling agent, a disintegrating agent and a lubricating agent. The Vorinostat solid preparation is characterized in that the weight ratio of the Vorinostat to the filling agent is 1:0.9-4.5, the weight ratio of the Vorinostat to the disintegrating agent is 1:0.0834-0.4170, and the weight ratio of the Vorinostat to the lubricating agent is 1:0.0166-0.0830. The invention determines the doses of the disintegrating agent, the filling agent and the lubricating agent in the prescription of the Vorinostat solid preparation by creative experiments, and the dissolution of the Vorinostat solid preparation reaches more than 80% in 45 minutes.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a solid preparation of vorinostat. Background technique [0002] Vorinostat, chemical name: N-hydroxy-N′-phenylsuberamide, is indicated for the treatment of cutaneous T-cell lymphoma (CTCL) that has been exacerbated, persistent, and relapsed or that has not responded to two systemic agents. Cutaneous T-cell lymphoma is a type of lymphoma that first develops lesions in the skin and then spreads to lymph nodes or other organs. Cutaneous T-cell lymphoma was first diagnosed in 1806 by Alibert, a French dermatologist. It was discovered that many fungal-like lumps would appear on the skin of patients that had nothing to do with fungal infection. There are two main phenotypes of cutaneous T-cell lymphoma, one is erythroderma (Sezary syndrome), the patient's skin is red, very itchy and sensitive to cold, and lymphoma cells enter the peripheral blood; the other is It is Mycosis fungoid...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K9/16A61K9/20A61K31/16A61P17/00A61P35/00
Inventor 顾群金治刚孙学伟徐春霞王东孙德杰
Owner PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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