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Preparation method of tedizolid phosphate composition tablets

A technology of tedizolid phosphate and composition, which is applied in the field of preparation of tedizolid phosphate composition tablets, can solve the problems that the stability of drug crystal form greatly affects the curative effect and antibacterial effect, etc., so as to improve fluidity and Effects of compressibility, small difference in loading capacity, and improved antibacterial activity

Active Publication Date: 2018-01-26
SHANDONG YUXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the applicant found that the use of wet granulation can easily cause tedizolid phosphate to undergo crystal transformation, which affects its curative effect and antibacterial effect; and through further research, it is found that the choice of its binder has a great impact on the crystal stability of the drug

Method used

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  • Preparation method of tedizolid phosphate composition tablets
  • Preparation method of tedizolid phosphate composition tablets

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Experimental program
Comparison scheme
Effect test

preparation example Construction

[0029] The preparation method of tedizolid phosphate tablet:

[0030] (1) Raw material preparation: tedizolid phosphate, pregelatinized starch, sucrose, tyrosine, polacrilin potassium, mixed and pulverized, repeatedly passed through a 100 mesh sieve twice; povidone K30 was prepared into a 5% solution , as an adhesive;

[0031] (2) Granulation: Add the pulverized and sieved material into a wet granulator and mix evenly, the mixing speed is 400-600 rpm, the mixing time is 5-6 minutes, then add 5% povidone K30 solution For making soft materials, granulate with 18 mesh sieve, dry at 50°C for 40 minutes, and granulate with 20 mesh sieve;

[0032] (3) Total mixing: place the sized granules and sodium lauryl sulfate in a three-dimensional mixer and mix evenly. The mixing speed is 10-15 rpm, and the mixing time is 8-10 minutes.

[0033] (4) Tablets.

experiment example 1

[0066] The investigation of experimental example 1 tablet hardness stability

[0067] Get the prepared tablet samples of Example 1, Example 3, Comparative Example 1, Comparative Example 2, Comparative Example 3, and Comparative Example 4, under packaging (aluminum-plastic packaging, put in a carton), at 40 ° C, Place it under 75% relative humidity for 6 months, take samples at 0, 1, 2, 3, and 6 months, and measure the tablet hardness. The results are shown in Table 1.

[0068] Table 1 tablet hardness investigation result

[0069]

[0070] The accelerated test was conducted for 6 months, and the hardness measurement results showed that the hardness of the tablet of the present invention remained unchanged under long-term storage conditions, and the stability of the preparation was significantly improved.

experiment example 2

[0071] Experimental Example 2: Efficacy and Safety Evaluation of Treatment for MRSA Pneumonia

[0072] Refer to the patent CN105085570A method for detection, and the test results are shown in Table 2-4.

[0073] Table 2 Comparison of Clinical Curative Effects of Patients (Example)

[0074] group

[0075] Table 3 Comparison of Bacteriological Curative Effects of Patients (Example)

[0076] group

[0077] Table 4 Comparison of adverse reactions in two groups of patients (example)

[0078] group

[0079] The comparison difference of embodiment and comparative example all has statistical significance (P<0.05), can find out that the curative effect of tedizolid phosphate composition of the present invention and untoward reaction are all better than prior art, significantly to MRSA antibacterial activity improve.

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Abstract

The invention belongs to the field of medical preparation, and more specifically discloses a preparation method of tedizolid phosphate composition tablets. The preparation method comprise following steps: tedizolid phosphate, pregelatinized starch, sucrose, tyrosine, polacrilin potassium, and sodium lauryl sulfate are added into a 5% polyvinylpyrrolidone K30 solution, and wet granulation sodium lauryl sulfate is adopted so as to obtain the tedizolid phosphate composition tablets. The stability of the tedizolid phosphate composition tablets is improved obviously via screening on the accessory ingredients and controlling on the amount; and drug crystal transformation technical problem in wet granulation is solved via screening on the kind and the amount of a binding agent. It is found via experiments that, compared with the prior art, the preparation method possesses following advantages: the curative effect is better, the adverse reaction is reduced, and antimicrobial activity on MRSA is increased obviously.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a method for preparing a tedizolid phosphate composition tablet. Background technique [0002] The treatment of infectious diseases such as skin and soft tissue infections (SSSIs), pneumonia, sepsis, and endocarditis caused by Gram-positive bacteria is still facing severe challenges in today's advanced modern medicine. Taking methicillin-resistant Staphylococcus aureus (MRSA) as an example, MRSA appeared 2 years after the clinical application of methicillin, and after more than 50 years, the bacteria has been widely spread in hospitals all over the world. Since the early 1990s, community-acquired MRSA (CA-MRSA) appeared and spread globally, changing the old idea that MRSA infection only occurs in hospital settings. The problem of drug resistance in Gram-positive bacteria is not limited to MRSA, including challenges posed by vancomycin-resistant enterococci (VRE), macro...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/32A61K31/675A61P31/04
Inventor 刘振腾李志滨杨静李树凡
Owner SHANDONG YUXIN PHARMA CO LTD
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