Moxifloxacin hydrochloride-containing pharmaceutical composition and preparation method thereof

Abstract

The invention relates to a pharmaceutical composition containing 9%-40% of mannitol moxifloxacin hydrochloride and / or other hydrates, at least one diluent, at least one disintegrating agent and at least one lubricant and a preparation method thereof. Moxifloxacin hydrochloride tablets prepared according to a formula have the advantages of bioavailability without dissolution limitation, satisfied fragility, good liquidity and production feasibility.

Description

technical field [0001] The invention relates to pharmaceutical preparations, in particular to a pharmaceutical composition containing moxifloxacin hydrochloride and a preparation method thereof. Background technique [0002] Moxifloxacin hydrochloride is the fourth generation of fluoroquinolone antibiotics, and the original manufacturer is Bayer, Germany. Because of its broad antibacterial spectrum, low drug resistance, strong antibacterial effect, long half-life, and low phototoxicity, it has become a very effective anti-infective agent. The existing moxifloxacin hydrochloride tablets and moxifloxacin hydrochloride sodium chloride injection were approved by the US FDA in 1996 and 2001 respectively. Compared with injections, tablets are more stable in properties; they are better tolerated and safe for oral absorption and utilization; they also have the advantages of accurate dosage, convenient carrying and application, low cost, and a high degree of mechanization in product...

AI Technical Summary

Problems solved by technology

Cannot meet the requirement that the bioavailability is not limited by dissolution

[0007] Chinese patent CN1672680A discloses a method of using film-forming materials to prepare moxifloxacin hydrochloride tablets to prevent discoloration during granulation and tabletting, but it is found through experiments that the friability of tablets prepared by this method can meet the requirements The dissolution rate in 0.1mol / L HCl for 15 minutes is only 60.3%, which cannot meet the requirement that the tablet bioavailability is not limited by dissolution

However, after testing, it was found that the dissolution rate of the tablets prepared by the patented formula that can meet the requirements in 0.1mol / L HCl for 15 minutes is only 71.6%, which cannot meet the requirement that the bioavailability of the tablet is not limited by dissolution.

[0009] Chinese patent CN102204911A discloses a tablet prescription composed of 500 parts by weight of moxifloxacin hydrochloride, 10-50 parts by weight of mannitol, and an appropriate amount of disintegrants, fillers and lubricants, but found through tests that if According to this prescription, dry granulation is adopted. Due to the expensive dry granulation equipment and the need to crush large tablets after dry pressing, the dust will fly, which is not conducive to the protection of workers. The granules produced by dry granulation are too small to use a conventional tablet press Tablets produce defects such as astringency and powder leakage, and it is not feasible to use dry granulation

If the patented prescription is used, the wet granulation method is used, and the angle of repose of the particles detected by the fixed funnel method is greater than 45 ° , the fluidity cannot meet the requirements, and the friability of the prepared tablet can meet the requirements. The dissolution rate in 0.1mol / L HCl for 15 minutes is less than 80%, which cannot meet the requirement that the bioavailability of the tablet is not limited by dissolution.

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