Tedizolid phosphate oral solid preparation

A technology of tedizolid phosphate and solid preparations, which is applied in the direction of pill delivery, medical preparations containing no active ingredients, and medical preparations containing active ingredients, etc. It can solve problems such as poor dissolution effect and poor fluidity of tedizolid phosphate , to achieve the effect of ensuring product quality and process smoothness

Pending Publication Date: 2021-08-03
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The invention provides an oral solid preparation of tedizolid phosphate, which aims to overcome the problems of poor fluidity and poor dissolution effect of tedizolid phosphate
The oral solid preparation of tedizolid phosphate prepared by the present invention has better dissolution rate, overcomes the problem of poor fluidity of tedizolid phosphate, and ensures smooth process of the preparation in the preparation process

Method used

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  • Tedizolid phosphate oral solid preparation
  • Tedizolid phosphate oral solid preparation
  • Tedizolid phosphate oral solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] composition Dosage (g) Tedizolid Phosphate 200 Maltodextrin 120 Calcium hydrogen phosphate 10 Croscarmellose Sodium 20

[0031] Tedizolid phosphate d0.9 = 18 μm, calcium hydrogen phosphate d0.9 = 15 μm

[0032] Preparation:

[0033] (1) uniformly mixing tedizolid phosphate, maltodextrin, calcium hydrogen phosphate, and croscarmellose sodium to prepare a mixture;

[0034] (2) Add 50% ethanol aqueous solution to the mixture in step (1), granulate, granulate, and obtain drug granules;

[0035] (3) Compressing the drug granules into tablets.

Embodiment 2

[0037] composition Dosage (g) Tedizolid Phosphate 153 Maltodextrin 120 Calcium hydrogen phosphate 15 Low-substituted hydroxypropyl cellulose 8 Crospovidone 4

[0038] Tedizolid phosphate d0.9 = 25 μm, calcium hydrogen phosphate d0.9 = 20 μm

[0039] Preparation:

[0040] (1) uniformly mixing tedizolid phosphate, maltodextrin, calcium hydrogen phosphate, low-substituted hydroxypropyl cellulose, and crospovidone to prepare a mixture;

[0041] (2) Add 75% ethanol aqueous solution to the mixture in step (1), granulate and granulate to obtain drug granules;

[0042] (3) Compressing the drug granules into tablets.

Embodiment 3

[0044] composition Dosage (g) Tedizolid Phosphate 100 Maltodextrin 75 pregelatinized starch 30 Calcium hydrogen phosphate 15 Croscarmellose Sodium 20 povidone 10

[0045] Tedizolid phosphate d0.9 = 16 μm, calcium hydrogen phosphate d0.9 = 8 μm

[0046] Preparation:

[0047] (1) uniformly mixing tedizolid phosphate, maltodextrin, pregelatinized starch, calcium hydrogen phosphate, croscarmellose sodium and povidone to prepare a mixture;

[0048] (2) Add 60% ethanol aqueous solution to the mixture in step (1), granulate, granulate, and obtain drug granules;

[0049] (3) Compressing the drug granules into tablets.

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Abstract

The present invention relates to a tedizolid phosphate oral solid preparation, the oral solid preparation specifically comprises tedizolid phosphate, maltodextrin, calcium hydrogen phosphate and a disintegrating agent, and the particle size d0.9 of tedizolid phosphate is not more than 30 [mu] m. The tedizolid phosphate oral solid preparation prepared by the invention has better dissolution rate, overcomes the problem of poor flowability of tedizolid phosphate, and ensures the process smoothness of the preparation in the preparation process.

Description

technical field [0001] The invention relates to a novel oral solid preparation of oxazolidinone antibiotics, specifically tedizolid phosphate oral solid preparation, and a preparation method of the preparation. Background technique [0002] Tedizolid Phosphate, developed by Trius Therapeutics, is a new type of oxazolidinone antibiotic approved for marketing in the United States in 2014, and is clinically used for the treatment of acute bacterial skin and skin structure infections (ABSSSI). Tedizolid phosphate is a prodrug that can be rapidly converted into biologically active tedizolid by phosphatase in vivo, which can bind to the ribosomal 50S subunit of bacteria to inhibit protein synthesis. Its mechanism of action is different from that of other antibacterial drugs (such as chloramphenicol and lincomycin), and there will be no cross-resistance with other antibacterial drugs. Tedizolid phosphate is effective against Gram-positive bacteria such as Staphylococcus, Enterococ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/675A61K47/36A61K47/02A61P31/04
CPCA61K9/205A61K9/2095A61K9/2009A61K31/675A61K9/0053A61P31/04
Inventor 刘贺黄玉锋梅喆孙敏哲
Owner BEIJING WINSUNNY PHARMA CO LTD
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