CN102204910B - Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof - Google Patents
Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof Download PDFInfo
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- CN102204910B CN102204910B CN201110074385.2A CN201110074385A CN102204910B CN 102204910 B CN102204910 B CN 102204910B CN 201110074385 A CN201110074385 A CN 201110074385A CN 102204910 B CN102204910 B CN 102204910B
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Abstract
The invention provides a pharmaceutical composition of moxifloxacin hydrochloride, and a preparation method thereof. The composition mainly comprises moxifloxacin hydrochloride, a melting agent polyethylene glycol 6000 and other excipients. The preparation method mainly comprises the steps of: preparing drug particles by a hot melt granulating technology, and then tabletting or encapsulating.
Description
[technical field]
The invention belongs to technical field of medicine, more specifically, the present invention relates to a kind of pharmaceutical composition that contains moxifloxacin hydrochloride and fusing agent, also relates to the preparation method of described pharmaceutical composition.
[background technology]
Moxifloxacin hydrochloride (Moxifloxacin Hydrochloride), its chemistry 1-cyclopropyl-7-(S by name, S-2,8-diazonium-bicyclo-[4.3.0] nonane-8-yl) the fluoro-8-of-6-methoxy-1,4-dihydro-4-oxygen-3-quinoline carboxylic acid hydrochloride, is the efficient Development of Fluoroquinolone Antibacterials of New-type wide-spectrum of German Bayer company research and development, and commodity are called " visiing multiple pleasure ", in JIUYUE, 1999 is gone on the market in Germany, and the same year, December obtained FDA approval listing in the U.S..That uses clinically at present is mainly tablet.
Moxifloxacin hydrochloride raw material is crystalline powder, and mobility and compressibility are all poor, and said preparation specification is larger, needs the adjuvant limited space of interpolation, is not suitable for dry powder direct tabletting, and preparation technology is wet method granule tabletting processed.Traditional wet granulation, need to consider the addition, particle drying time of adhesive, the factors such as time of sieving of granulating, the machine quantity of need of production is many, space is large, and because some factor need to dependence experience judge, therefore may cause unstable product quality, between batch, difference is large etc.And along with the prolongation of resting period, may cause in addition the problem such as slack-off of dissolution.
And dry method granule technique processed need to be used the special installations such as dry granulating machine; also need by compressing, pulverize, sieve, the process such as granulate just can complete; operating process is loaded down with trivial details, time-consuming; artificially increased cost; and after tabletting, easily there is " taking off lid " phenomenon; or tablet friability is defective, in the coating process of postorder, easily there is fragment, make tablet quality defective.
Hot melt granule method processed is the emerging a kind of granulation technique of Abroad in Recent Years.This technology is different from hot-melt extruded granulation technique, and the latter need to use the special and expensive equipment such as hot-melt extruded granulator, and hot melt granule method processed only needs fluid bed to realize, and fluid bed is the common equipment generally using in modern pharmaceutical factory.This technology is time saving and energy saving, and quickness and high efficiency adapts to the development in modern pharmaceutical field.
[summary of the invention]
[technical problem that will solve]
Object of the present invention, to overcome the potential risk that prior art is brought to product stability in wet granule compression tablet technique, a kind of technology of preparing-hot melt granulation technique of time saving and energy saving, quickness and high efficiency is proposed, the application of this technology has not only reduced the production cost of product, has also guaranteed the quality of product simultaneously.
[technical scheme]
The present invention is achieved through the following technical solutions.
The present invention relates to a kind of pharmaceutical composition of moxifloxacin hydrochloride, it is characterized in that it by effective ingredient moxifloxacin hydrochloride with comprise fusing agent and other pharmaceutically acceptable carrier form, and the tablet of making by hot melt granulation technique, wherein fusing agent used is polyethylene glycol 6000.
The invention provides a kind of method that adopts hot melt granulation technique to prepare moxifloxacin hydrochloride medicinal composition, adopt fluid bed heat to found grain.Preparation technology is easy for this technology, time saving and energy saving, uniform particles, and good fluidity, tablet hardness is better, and friability is lower, and dissolution is obviously better than wet granulation.
Moxifloxacin hydrochloride is wide spectrum and the 8-methoxy fluoroquinolone class antimicrobial drug with antibacterial activity.Moxifloxacin hydrochloride is to gram positive bacteria, gram-negative bacteria, and anaerobe, acid fast bacteria, and atypical microorganism is as mycoplasma, chlamydia and legionella have broad spectrum antibiotic activity.Antibacterial action mechanism is for disturbing II, IV topoisomerase.Topoisomerase is to control the key enzyme of DNA topological sum at DNA replication dna, in repairing and transcribing.Its killing curve shows, Moxifloxacin is the bactericidal activity with concentration dependent.We know, the medicine with concentration dependent, refer to be blood drug level in body, so the stripping of medicine is fast, can make the absorption of medicine fast, reach very soon blood drug level effectively, bring into play rapidly drug effect, and if dissolution is slack-off, absorb slack-off accordingly, onset is slack-off, even may can not reach effective concentration because of medicine elimination and metabolic problems, thereby curative effect is very poor.
Hot melt granulation technique is different from hot-melt extruded granulation technique, the latter need to use the special and expensive equipment such as hot-melt extruded granulator, and hot melt granule method processed only needs fluid bed to realize, its operation principle is the material in material trough, the abundant mixed melting of adjuvant, by constant pressure and flow device, be delivered to the second-rate bromhidrosis stream nozzle at refrigerating chamber top, the compressed air atomization being produced by air compressor in refrigerating chamber becomes small droplet, fully contact with the air through cryotherapy, the exchange of conducting heat, complete solidification process, product after partly solidified is deposited in the powder cup of hothouse bottom, the tail gas of discharging from atomization refrigeration chamber completes gas solid separation in cyclone separator, product is captured down and collects in powder cup, tail gas enters atmosphere by air-introduced machine.Fluid bed is the common equipment generally using in modern pharmaceutical factory.This technology is time saving and energy saving, and quickness and high efficiency adapts to the development in modern pharmaceutical field.
In compositions of the present invention, contain moxifloxacin hydrochloride, fusing agent polyethylene glycol 6000 and other be acceptable carrier pharmaceutically.
Wherein pharmaceutically acceptable carrier should refer to the conventional medicine carrier in pharmaceutical field, such as disintegrating agent, lubricant etc., and disintegrating agent is as carboxymethyl starch sodium, hyprolose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose; Fluidizer is as silicon dioxide, gel silicon dioxide; Lubricant is as Pulvis Talci, calcium stearate, magnesium stearate, micropowder silica gel etc.
Preferably, described pharmaceutical composition is made by following raw material,
More preferably, described pharmaceutical composition is made by following raw material,
According to another kind of preferred implementation of the present invention, described preparation is tablet or capsule.
According to another kind of preferred implementation of the present invention, pharmaceutically acceptable carrier is that one or more are selected from the pharmaceutically carrier of normally used disintegrating agent, lubricant.
Described disintegrating agent is selected from carboxymethyl starch sodium, hyprolose, polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose.
Described lubricant is selected from Pulvis Talci, calcium stearate and magnesium, micropowder silica gel.
The invention still further relates to the preparation method of described pharmaceutical composition.The method step is as follows: moxifloxacin hydrochloride, polyethylene glycol 6000, disintegrating agent, fluidizer is put in fluid bed, carries out hot melt granulation.
The granule that the present invention further can obtain hot melt granulation is prepared into pharmaceutical preparation with galenic pharmacy routine techniques, as tablet, and capsule.And the moxifloxacin hydrochloride that the preparation of each unit contains 250mg, 500mg or 1000mg.
Therefore the preferred preparation method of the present invention is as follows:
Moxifloxacin hydrochloride, polyethylene glycol 6000, cross-linking sodium carboxymethyl cellulose and silicon dioxide are put in fluid bed, carry out hot melt granulation.
Particularly preferred preparation method is as follows: the moxifloxacin hydrochloride, 4-6 weight portion cross-linking sodium carboxymethyl cellulose, 40-60 weight portion polyethylene glycol 6000 and the 10 weight portion silicon dioxide that take 1000 weight portions are put in fluid bed, air intake frequency 30-40Hz, temperature of charge are set are the parameter such as 55-75 ℃ and carry out hot melt granulation, by adding magnesium stearate after the granule granulate making, mix, tabletting, film coating.
The present invention preferably fills a prescription and obtains through screening, is particularly conducive to commercial production.
In the present invention, the method and apparatus generally using that the those of ordinary skill in employing pharmaceutical technology field is known, the granule obtaining can be made to tablet with the combination of acceptable carrier pharmaceutically, these carriers that use or excipient are all easily to determine for the those of ordinary skill in pharmaceutical technology field, are also apparent.
[beneficial effect]
The present invention has following beneficial effect: the present invention adopts hot melt method of granulating pharmaceutical compositions, and its advantage is, compared to the prior art, preparation technology is easy, time saving and energy saving, uniform particles, good fluidity, the tablet hardness of compacting is better, friability is lower, also there will not be fragment in coating process, easily controls, this tablet stability is good simultaneously, and in accelerated stability test, dissolution and wet granulation relatively have a clear superiority in simultaneously.See accompanying drawing and subordinate list.
[accompanying drawing explanation]
Fig. 1 embodiment 1-4 and Dissolution of Tablet comparison wet granulation compacting
Through accelerated test, after 6 months, condition determination is: slurry method, 900ml water, 50rpm, 37 ℃.The Dissolution of Tablet of the visible wet granulation of result is considerably slower than the tablet that embodiment obtains.The Dissolution of Tablet comparison of the product of Fig. 2 embodiment and wet granulation compacting
Condition determination is: slurry method, 0.1NHCl, 50rpm, 37 ℃.Through accelerated test, after 6 months, the product dissolution of the visible wet granulation of result is slower than embodiment.
[specific embodiment]
Further illustrate by the following examples the present invention, but not as limitation of the present invention.
embodiment 1:
The PEG-4000 and the 10 weight portion silicon dioxide that take moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 10 weight portions, 200 weight portions are put in fluid bed, it is that 30Hz, temperature of charge are 75 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add 1 weight portion magnesium stearate to mix 5 minutes, be pressed into 1000, then use
film coating.
embodiment 2:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 1 weight portion, 10 weight portion PEG-4000s and silicon dioxide 2 weight portions puts in fluid bed, it is that 40Hz, temperature of charge are 65 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.5 weight portion to mix 5 minutes, be pressed into 1000, then use
film coating.
embodiment 3:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 5 weight portions, PEG-4000 100 weight portions and silicon dioxide 5 weight portions puts in fluid bed, it is that 30Hz, temperature of charge are 55 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.1 weight portion to mix 5 minutes, be pressed into 1000, then use
film coating.
embodiment 4:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 7 weight portions, PEG-4000 50 weight portions and silicon dioxide 7 weight portions puts in fluid bed, it is that 40Hz, temperature of charge are 65 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.5 weight portion to mix 5 minutes, pack 1000 capsules into.
Below by data, further illustrate the advantage of pharmaceutical composition of the present invention.
The comparison of table 1 embodiment of the present invention and dry granulation technology result
As seen from the above table, from the character aspect comparison of operating time and labor intensity etc. and product intermediate, the present invention has obvious advantage than dry granulation technology and wet granulation technique.
Table 2 embodiment of the present invention and wet granulation technique are placed the comparison of stripping result after 6 months
Condition determination is: slurry method, 900ml water, 50rpm, 37 ℃.
As seen from the above table, from wet granulation product and accelerated test of the present invention result comparison in 6 months, the dissolution of wet granulation is considerably slower than the present invention, and the present invention and relatively there is no significant difference for 0 month.The present invention has obvious advantage in product quality than wet granulation technique.
Claims (4)
1. a preparation method for the pharmaceutical composition of moxifloxacin hydrochloride, is characterized in that, step is as follows:
The PEG-4000 and the 10 weight portion silicon dioxide that take moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 10 weight portions, 200 weight portions are put in fluid bed, it is that 30Hz, temperature of charge are 75 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add 1 weight portion magnesium stearate to mix 5 minutes, be pressed into 1000, then use Opadry film coating.
2. a preparation method for the pharmaceutical composition of moxifloxacin hydrochloride, is characterized in that, step is as follows:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 1 weight portion, 10 weight portion PEG-4000s and silicon dioxide 2 weight portions puts in fluid bed, it is that 40Hz, temperature of charge are 65 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.5 weight portion to mix 5 minutes, be pressed into 1000, then use Opadry film coating.
3. a preparation method for the pharmaceutical composition of moxifloxacin hydrochloride, is characterized in that, step is as follows:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 5 weight portions, PEG-4000 100 weight portions and silicon dioxide 5 weight portions puts in fluid bed, it is that 30Hz, temperature of charge are 55 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.1 weight portion to mix 5 minutes, be pressed into 1000, then use Opadry film coating.
4. a preparation method for the pharmaceutical composition of moxifloxacin hydrochloride, is characterized in that, step is as follows:
Taking moxifloxacin hydrochloride 1000 weight portions, cross-linking sodium carboxymethyl cellulose 7 weight portions, PEG-4000 50 weight portions and silicon dioxide 7 weight portions puts in fluid bed, it is that 40Hz, temperature of charge are 65 ℃ that air intake frequency is set, carry out hot melt granulation, by the granule making with in the rearmounted mixers of 18 mesh sieve granulate, add magnesium stearate 0.5 weight portion to mix 5 minutes, pack 1000 capsules into.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201110074385.2A CN102204910B (en) | 2011-03-25 | 2011-03-25 | Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof |
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| CN201110074385.2A CN102204910B (en) | 2011-03-25 | 2011-03-25 | Pharmaceutical composition of moxifloxacin hydrochloride, and preparation method thereof |
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| CN102204910B true CN102204910B (en) | 2014-10-29 |
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| CN108371655A (en) * | 2018-03-29 | 2018-08-07 | 重庆华邦制药有限公司 | Include the solid drugs and preparation method thereof of razaxaban |
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| CN1762357A (en) * | 2005-09-21 | 2006-04-26 | 深圳市天一时科技开发有限公司 | Oral medicinal formulation of moxifloxacin and its preparation method |
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| CN1762357A (en) * | 2005-09-21 | 2006-04-26 | 深圳市天一时科技开发有限公司 | Oral medicinal formulation of moxifloxacin and its preparation method |
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Address after: 100021 Beijing city Chaoyang District West business center boziwan Jinhai rich 402 (A) 21 storey building Applicant after: China Resources Saike Pharmaceutical Co., Ltd. Address before: 100021 Beijing city Chaoyang District West business center boziwan Jinhai rich 402 (A) 21 storey building Applicant before: Saike Pharmaceutical Co., Ltd., Beijing |
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