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42-(Dimethylphosphono)rapamycin solid composition and coating method thereof

A technology of dimethyl phosphinoylidene and solid composition, applied in the field of solid pharmaceutical composition and its coating, can solve the problems of poor stability, low in vitro dissolution rate, poor solubility, etc., achieve good stability and improve solubility , the effect of better performance

Active Publication Date: 2014-10-08
FUJIAN INST OF MICROBIOLOGY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] One of the technical problems to be solved by the present invention is to provide a solid composition of 42-(dimethylphosphono)rapamycin, which solves the existing problems of poor solubility, poor stability, and low dissolution rate in vitro.

Method used

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  • 42-(Dimethylphosphono)rapamycin solid composition and coating method thereof
  • 42-(Dimethylphosphono)rapamycin solid composition and coating method thereof
  • 42-(Dimethylphosphono)rapamycin solid composition and coating method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Table 1

[0041] Category

[0042] Prepare each material according to Table 1, pass the starch, dextrin, and crospovidone through an 80-mesh sieve. Weigh the starch, dextrin, and crospovidone in a mixer according to the ratio shown in Table 1. Standby; Dissolve AP23573, poloxamer 188, ascorbyl palmitate, and starch slurry in 90% ethanol to obtain a mixed solution, and then add the mixed solution to the mixer containing the above-mentioned starch, dextrin and crospovidone Stir and mix to form a soft material. Then, the soft material is granulated with a 18-mesh granulating machine to obtain AP23573 wet granules. Then the AP23573 wet granules are dried in a drying oven or a fluidized bed dryer at 45-60℃, and then Use a 20-mesh sieve granulator to sizing to obtain AP23573 dry particles. Finally, AP23573 dry particles and micro-powder silica gel are mixed in a mixer to obtain AP23573 solid composition.

Embodiment 2

[0044] Table 2

[0045] Category

[0046] Prepare the materials according to Table 2. Pass the microcrystalline cellulose and sodium carboxymethyl starch through an 80 mesh sieve. Weigh the microcrystalline cellulose and sodium carboxymethyl starch in a mixer according to the ratio shown in Table 2. Standby; Dissolve AP23573, polyvinylpyrrolidone, and butylated hydroxytoluene in 95% ethanol to obtain a mixed solution, then add the mixed solution to a mixer containing the above-mentioned microcrystalline cellulose and sodium carboxymethyl starch, stir and mix to form The soft material is then granulated with a 18-mesh granulating machine to obtain AP23573 wet granules, and then the AP23573 wet granules are dried in a 45-60℃ drying oven or a fluidized bed dryer, and then sieved with 20 mesh The granulator granules the granules to obtain AP23573 dry granules. Finally, the AP23573 dry granules and the micro-powder silica gel are mixed in a mixer to obtain an AP23573 solid composit...

Embodiment 3

[0048] table 3

[0049] Category

[0050] Prepare each material according to Table 3, pass the lactose and hydroxypropyl cellulose through an 80-mesh sieve, weigh the lactose and hydroxypropyl cellulose according to the ratio shown in Table 3, and mix them in a mixer for use; Propyl methyl cellulose, sodium carboxymethyl cellulose, and vitamin E are dissolved in 95% ethanol to obtain a mixed liquid, and then the mixed liquid is added to the mixer containing the above lactose and hydroxypropyl cellulose to stir and mix. The soft material is formed, and then the soft material is granulated with a 18-mesh granulating machine to obtain AP23573 wet granules, and then the AP23573 wet granules are dried in a drying oven at 45-60°C or a fluidized bed dryer, and then sieved with 20 mesh The granulator is sized to obtain AP23573 dry granules. Finally, AP23573 dry granules and magnesium stearate are mixed in a mixer to obtain AP23573 solid composition.

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Abstract

The invention discloses an mTOR (mammalian target of rapamycin kinase) inhibitor 42-(dimethylphosphinate)rapamycin (i.e. AP23573) solid composition and a coating method thereof. The preparation of the 42-(dimethylphosphinate)rapamycin solid composition from AP23573, carriers, antioxidants, fillers, bonding agents, disintegrants, lubricants and the like greatly improves the solubility, in vitro dissolution and absorption of the active component AP23573. The active component AP23573 of the inventive composition is good in stability. The problems of AP23576 medicine such as insolubility and poor stability and absorption are solved. The AP23573 solid composition of the invention can be further processed into tablets, capsules, granules, film-coated tablets, enteric-coated tablets or the like, which are convenient for oral administration.

Description

【Technical Field】 [0001] The invention relates to a solid pharmaceutical composition and a coating method thereof, in particular to a 42-(dimethylphosphinyl) rapamycin solid composition and a coating method thereof. 【Background technique】 [0002] mTOR (target of rapamycin) inhibitors are recently expanded drugs for the treatment of various cancers and other diseases. 42-(dimethylphosphonyl) rapamycin or AP23573 is a derivative of rapamycin Things. AP23573 is an mTOR inhibitor, its structural formula is as follows: [0003] [0004] AP23573 binds to FKBP12 (ie FK506 binding protein 12), forms a complex and then binds to mTOR, thereby inhibiting the activity of mTOR, blocking the PI3K-Akt-TSC1 / 2-mTOR signal transduction pathway and making it difficult for tumor cells to grow and proliferate. AP23573 effectively inhibits the proliferation of various tumor cell lines such as prostate cancer, endometrial cancer, soft tissue and osteosarcoma, leukemia, lymphoma and glioblastoma. [000...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61K9/28A61P35/00A61P35/02A61P31/10A61P25/00A61P29/00A61P19/02A61P37/00A61P11/00A61P3/10A61P17/00A61P17/06A61P1/00A61P9/00A61P7/06
Inventor 陈有钟程元荣黄捷余辉杨国新金东伟陈夏琴
Owner FUJIAN INST OF MICROBIOLOGY
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