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Compound antitubercular preparation containing gatifloxacin, and preparation method thereof

A gatifloxacin and anti-tuberculosis technology, applied in the preparation and preparation of pyrazinamide and gatifloxacin, isoniazid, containing rifampicin, can solve the problem of incompatibility, incompatibility, and unseen Rifampicin compound preparations and other issues, to improve the effect, simplify treatment, and prevent incompatibility

Inactive Publication Date: 2014-05-21
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gatifloxacin mainly includes injections and tablets at present, and there are incompatibility between gatifloxacin injection and rifampicin injection, so they cannot be used at the same time
Compound preparations of rifampicin, isoniazid and gatifloxacin have not been seen so far

Method used

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  • Compound antitubercular preparation containing gatifloxacin, and preparation method thereof
  • Compound antitubercular preparation containing gatifloxacin, and preparation method thereof
  • Compound antitubercular preparation containing gatifloxacin, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Rifampicin 120g

[0038] Isoniazid 120g

[0039] Pyrazinamide 400g

[0040] Gatifloxacin 120g

[0041] Sodium carboxymethyl starch 100g

[0042] Microcrystalline Cellulose 130g

[0043] Magnesium Stearate 10g

[0044] Made into 1000 pieces

[0045] Preparation of tablet core: Rifampicin is passed through a 100-mesh sieve alone, and isoniazid, pyrazinamide and gatifloxacin are passed through a 60-mesh sieve. First, mix rifampicin, isoniazid, pyrazinamide, gatifloxacin, binder, 2 / 3 prescription amount of disintegrant (through 60 mesh sieve) and 1 / 3 prescription amount of lubricant, Dry granulation, granulation, and then mix the remaining 1 / 3 of the prescription amount of disintegrant and 2 / 3 of the prescription amount of lubricant with the above granules, and press into tablets to obtain;

[0046] Preparation of coating solution: Add appropriate amount of water into a suitable container, start the mixer, add the prescribed amoun...

Embodiment 2

[0049] Inner Tablet Prescription

[0050] Isoniazid 120g

[0051] Microcrystalline Cellulose 17.25g

[0052] Sodium carboxymethyl starch 6g

[0053] Dextrin 6g

[0054] Magnesium stearate 0.75g

[0055] Outer Tablet Prescription

[0056] Rifampicin 150g

[0057] Pyrazinamide 250g

[0058] Gatifloxacin 150g

[0059] Sodium carboxymethyl starch 93g

[0060] Microcrystalline Cellulose 192.8g

[0061] Magnesium Stearate 4.2g

[0062] Inner Tablet Coating Solution Prescription

[0063] Eudragit NE30 D 120ml

[0064] Eudragit L30D-55 480ml

[0065] PEG6000 13.5g

[0066] Talc powder 50g

[0067] water 520ml

[0068] Made into 1000 pieces

[0069] Preparation of tablet core: Grind isoniazid through an 80-mesh sieve, mix evenly with microcrystalline cellulose, sodium carboxymethyl starch, and dextrin, add water, make a soft material, pass through a 20-mesh sieve, dry, and sieve through a 20-mesh sieve Granules, adding magnesium ste...

Embodiment 3

[0074] Inner Tablet Prescription

[0075] Isoniazid 100g

[0076] Microcrystalline Cellulose 30.5g

[0077] Croscarmellose Sodium 6g

[0078] Dextrin 6g

[0079] Sucrose Fatty Acid Ester 7.5g

[0080] Outer Tablet Prescription

[0081] Rifampicin 150g

[0082] Pyrazinamide 250g

[0083] Gatifloxacin 150g

[0084] Croscarmellose Sodium 93g

[0085] Microcrystalline Cellulose 192.8g

[0086] Sucrose Fatty Acid Ester 42g

[0087] Inner Tablet Coating Solution Prescription

[0088] Eudragit NE30 D 120ml

[0089] Eudragit L30D-55 480ml

[0090] PEG6000 13.5g

[0091] Talc powder 50g

[0092] water 520ml

[0093] Made into 1000 pieces

[0094] Method is the same as embodiment 2

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Abstract

The invention relates to a new compound antitubercular preparation containing gatifloxacin, and a preparation method thereof. The compound antitubercular preparation comprises rifampicin, isoniazide, pyrazinamide and gatifloxacin. Each unit of preparation contains 100-150mg of rifampicin, 60-120mg of isoniazide, 200-400mg of pyrazinamide and 100-200mg of gatifloxacin. The addition of gatifloxacin in the preparation can shorten the course of treatment of tuberculosis and improve the treatment effect; and degradation of the rifampicin can be reduced through dry method granulating tabletting, thus improving the bioavailability of rifampicin and improving the curative effect of the medicament. The compound preparation can be prepared into common tablets, double-layer coated-core tablets or pellet-core tablets.

Description

technical field [0001] The invention relates to a medicine for treating pulmonary tuberculosis, in particular to a preparation containing rifampicin, isoniazid, pyrazinamide and gatifloxacin and a preparation method thereof. Background technique [0002] Rifampicin: Molecular formula is C 43 h 58 N 4 o 12 , Principle of antibacterial action Rifampicin firmly binds to the β subunit of RNA polymerase, inhibits the synthesis of bacterial RNA, prevents the enzyme from connecting with DNA, thereby blocking the RNA transcription process and stopping the synthesis of DNA and protein. Isoniazid: Molecular formula is C 6 h 7 N 3 O. Isoniazid is easy to penetrate into phagocytic cells and can kill intracellular conjunctive bacillus. Gatifloxacin: Molecular formula is C 19 h 22 FN 3 o 4 The antibacterial effect of gatifloxacin is through the inhibition of bacterial DNA gyrase and topoisomerase IV, thereby inhibiting the process of bacterial DNA replication, transcription...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4965A61K31/496A61K31/4409A61K9/34A61P31/06
Inventor 何仲贵孙进周雪芹王永军孙英华
Owner SHENYANG PHARMA UNIVERSITY
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