CN103006604B - Cefuroxime axetil tablets and preparation method thereof - Google Patents
Cefuroxime axetil tablets and preparation method thereof Download PDFInfo
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- CN103006604B CN103006604B CN201310016276.4A CN201310016276A CN103006604B CN 103006604 B CN103006604 B CN 103006604B CN 201310016276 A CN201310016276 A CN 201310016276A CN 103006604 B CN103006604 B CN 103006604B
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Abstract
The invention discloses a cefuroxime axetil tablets, which are prepared by mixing and directly tableting medicine-carrying pellets containing cefuroxime axetil, a filling agent and a lubricating agent, wherein the medicine-carrying pellets are prepared by the following steps of: weighing cefuroxime axetil and a disintegrating agent, dissolving or dispersing the cefuroxime axetil and the disintegrating agent into acetone to form a solution or suspension, spraying the solution or suspension into lactose pellets for coating in a fluidized bed, and drying to obtain the medicine-carrying pellets. According to the invention, the cefuroxime axetil raw material is coated on the outer layers of the lactose pellets, so that the medicine, namely the cefuroxime axetil can be uniformly distributed on the surfaces of the pellets, the specific surface area of the medicine is greatly increased, the raw cefuroxime axetil raw material can be rapidly released, and therefore the medicine dissolubility and the bioavailability are improved.
Description
Technical field
The invention belongs to pharmaceutical preparations technology field, in particular to cefuroxime axetil tablets of a kind of Fast Stripping in vivo and in vitro and preparation method thereof.
Background technology
CEFUROXIME AXETIL (cefuroxime axetil) is semisynthetic second generation cephalosporin, and has a broad antifungal spectrum all has stronger antibacterial activity to Gram-positive and negative bacterium.The active ingredient of cefuroxime axetil tablets is cefuroxime, it is oral in gastrointestinal absorption enters body, under esterase effect, be hydrolyzed to rapidly cefuroxime, by combining with one or more penicillin-binding proteins (PBPs), the Cell wall synthesis of anti-bacteria somatoblast, thereby performance antibacterial action.CEFUROXIME AXETIL is close ester medicine, unstable in wet, thermal environment, and bitter in the mouth, and poorly water-soluble, is difficult to absorb, and bioavailability is low, and dissolution rate is the limiting factor of drug absorption.
In order to improve the dissolution rate of cefuroxime axetil tablets, prior art has been reported a large amount of prescriptions and technical study test and technology.CN101874791A discloses a kind of raising cefuroxime axetil tablets, it take CEFUROXIME AXETIL as effective active composition, take microcrystalline Cellulose as filler, both share carboxymethyl starch sodium, crospolyvinylpyrrolidone as disintegrating agent, calcium carbonate is stabilizing agent, magnesium stearate is lubricant, white carbon is fluidizer, sodium lauryl sulphate is cosolvent, polyvinylpyrrolidone is binding agent, employing wet granulation is prepared, and wherein dissolution is more than 90% (15min), more than 95% (45min).Disintegrating agent and surface activity and more that this technology adopts, production cost is higher, easily occurs the risk that crude drug variable color and related substance increase in wet-granulation process simultaneously.CN101606914A discloses a kind of cefuroxime axetil tablets that is applicable to direct pressed powder, this tablet is mainly by increasing the mobility of adjuvant, reach the direct powder compression effect of said preparation, but the bulk density of the adjuvant requiring is large, good fluidity, wherein the bulk density of disintegrating agent is greater than 0.35g/cm
3, the bulk density of filler is greater than 0.38g/cm
3, this requires too high to adjuvant, increased cost of supplementary product, and while this product need to could be disperseed complete in 10min, fails to reach tablet requirement in pharmacopeia.CN101703448A discloses a kind of direct compression technique of cefuroxime axetil tablets, by CEFUROXIME AXETIL, stearic acid, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, silicon dioxide and sodium lauryl sulphate, cross 40 mesh sieves, then in tempering tank, mix 30 minutes, mixed powder forms with high speed rotating tablet machine direct compression.The dissolution of cefuroxime axetil dispersible tablets prepared by this technique in the time of 15 minutes lower than 65%.
Current, the tablet manufacturing of China is still extensive with common granulating tabletting process, and the application of direct compression of full-powder method is less.Direct compression of full-powder method is different from common granulating tabletting process, and its material that requires for tabletting is all pulverous fine powder, and the quality of material compressibility and mobility will determine the quality of final products.The Technology requirement that all can not meet direct compression of full-powder due to mobility and the compressibility of most drug powder, and the tablet machine of most of manufacturing enterprises does not have good powder device, dust arrester and the prepressing device of raising, be difficult to guarantee carrying out smoothly of direct compression of full-powder process, so the application of the suitability for industrialized production of direct compression of full-powder method is subject to many restrictions.Compare with common granulating tabletting process, direct compression of full-powder method has obvious technical advantage and cost advantage.First, direct compression of full-powder method has been avoided heating and the impact of moisture on tablet and technique.In actual production; often can run into the medicine of some unstable chemcial property; as the esters of facile hydrolysis, amide-type medicine; oxidizable phenolic hydroxyl group class medicine, vitamin C etc.; these medicines tend to occur hydrolysis in common wet granule compression tablet method; or it is destroyed to be heated, or because causing medicine, complex process sees photolysis etc. in particle drying process.For these problems, direct compression of full-powder method can solve.Direct compression of full-powder method is without granulation, without dry, thereby can effectively protect the quality stability of medicine, avoids it because the various unstable factors that wet granulation causes, thereby guarantees the quality of product.Meanwhile, the production technology of direct compression of full-powder method is simple, shortens the production cycle, enhance productivity, and energy-and time-economizing, thus can reduce the production cost of product.
In sum, by researching and developing the standby cefuroxime axetil tablets of direct compression of full-powder legal system that a kind of stripping is fast, stability is high, cost is low, this seems particularly necessary.
Summary of the invention
In view of the deficiencies in the prior art, the object of the invention is to, by direct compression of full-powder legal system is studied for prescription and the technique of cefuroxime axetil tablets, provides cefuroxime axetil tablets that a kind of stripping is fast, stability is high, cost is low and preparation method thereof.
In order to realize object of the present invention, inventor studies by lot of experiments, has finally obtained following technical scheme:
A cefuroxime axetil tablets, is formed by medicine carrying piller and filler, mix lubricant direct compression containing CEFUROXIME AXETIL; Described medicine carrying piller is prepared as follows and is obtained: take CEFUROXIME AXETIL and disintegrating agent and be dissolved or dispersed in acetone, the solution of formation or suspension are sprayed to coating the dry medicine carrying piller that to obtain on lactose pellet in fluid bed.
Preferably, described cefuroxime axetil tablets, wherein the weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.07-0.12:1-5.
Further preferably, described cefuroxime axetil tablets, wherein the weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.08-0.10:1.5-2.
Described filler is selected from following one or more: mannitol, microcrystalline Cellulose, pregelatinized Starch.
Described disintegrating agent is selected from following one or more: polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium.
Described lubricant is selected from following one or more: magnesium stearate, micropowder silica gel, Pulvis Talci.
A preparation method according to above-mentioned cefuroxime axetil tablets, comprises following steps: CEFUROXIME AXETIL and disintegrating agent are dissolved or dispersed in to acetone, the solution of formation or suspension are sprayed to coating the dry medicine carrying piller that to obtain on lactose pellet in fluid bed; Gained medicine carrying piller and filler, mix lubricant is even, and direct compression forms.
Preferably, the preparation method of described cefuroxime axetil tablets, is wherein 25 microns of D80 < by the particle size in the described suspension of grinding control step (1).
Here said term " D80 " refers to that particle diameter in described suspension is less than the granule of 25 microns and accounts for 80%.
Compared with prior art, the present invention is outer at lactose pellet by CEFUROXIME AXETIL raw material coating, and medicine is evenly distributed on to piller surface, has greatly improved the specific surface area of medicine, raw material can be discharged rapidly, thereby improve drug dissolution and bioavailability.By experimental study, find, cefuroxime axetil tablets prepared by the present invention detects dissolution according to method under < < Chinese Pharmacopoeia > > version cefuroxime axetil tablets item in 2010, within 15 minutes, drug dissolution is greater than 98%, in temperature, it is 40 ℃ ± 2 ℃, humidity is to carry out accelerated test under 75% ± 5% condition, place highly stablely after 6 months, be significantly better than prior art.In addition, cefuroxime axetil tablet preparation process of the present invention is fairly simple, easy to operate, and production cost is low, is applicable to industrialized great production.
Accompanying drawing explanation
Fig. 1 is the cumulative leaching rate curve chart of the cefuroxime axetil tablets of embodiment 1 preparation.
Fig. 2 is the cumulative leaching rate curve chart of the cefuroxime axetil tablets of embodiment 2 preparations.
Fig. 3 is the cumulative leaching rate curve chart of the cefuroxime axetil tablets of embodiment 3 preparations.
The cumulative leaching rate curve chart of the cefuroxime axetil tablets that Fig. 4 is prepared for comparative example.
The specific embodiment
Form is described in further detail foregoing of the present invention again by the following examples, but this should be interpreted as to the scope of the above-mentioned theme of the present invention only limits to following embodiment, all technology realizing based on foregoing of the present invention all belong to scope of the present invention.
Preparation technology:
(1) CEFUROXIME AXETIL is dissolved in 1 liter of acetone, add polyvinylpolypyrrolidone, stir ball mill grinding, control 25 microns of suspension particle diameter D80 <, the suspension of formation is obtained to medicine carrying piller being sprayed to coating on lactose pellet in fluid bed.
(2) step (1) gained medicine carrying piller is mixed homogeneously with mannitol and magnesium stearate, direct compression, obtains cefuroxime axetil tablets.The dissolution of cefuroxime axetil tablets detects according to method under < < Chinese Pharmacopoeia > > version cefuroxime axetil tablets item in 2010, calculate accumulation stripping percentage rate, take time t as abscissa, average accumulated stripping percentage rate is vertical coordinate mapping, the results are shown in Figure before 1(accelerated test).Testing result demonstration, the cefuroxime axetil tablets dissolution of 15 minutes prepared by this example reaches 99.5%, and content is 99.8%, and dispersed homogeneous degree has all disperseed complete at 1 minute.In temperature, be 40 ℃ ± 2 ℃, carry out accelerated test under the condition that humidity is 75% ± 5%, place 6 months, the dissolution of 15 minutes is 98.3%, and content is 99.4%, and dispersed homogeneous degree has all disperseed complete in 1 minute 30 seconds.
Preparation technology:
(1) CEFUROXIME AXETIL is dissolved in 1 liter of acetone, add polyvinylpolypyrrolidone, stir ball mill grinding, control 25 microns of suspension particle diameter D80 <, the suspension of formation is obtained to medicine carrying piller being sprayed to coating on lactose pellet in fluid bed.
(2) step (1) gained medicine carrying piller is mixed homogeneously with pregelatinized Starch and magnesium stearate, direct compression, obtains cefuroxime axetil tablets.The dissolution of cefuroxime axetil tablets detects according to method under < < Chinese Pharmacopoeia > > version cefuroxime axetil tablets item in 2010, calculate accumulation stripping percentage rate, take time t as abscissa, average accumulated stripping percentage rate is vertical coordinate mapping, the results are shown in Figure before 2(accelerated test).Testing result demonstration, the cefuroxime axetil tablets dissolution of 15 minutes prepared by this example reaches 98.6%, and content is 99.9%, and dispersed homogeneous degree has all disperseed complete at 1 minute.In temperature, be 40 ℃ ± 2 ℃, carry out accelerated test under the condition that humidity is 75% ± 5%, place 6 months, the dissolution of 15 minutes is 98.1%, and content is 99.2%, and dispersed homogeneous degree has all disperseed complete in 1 minute 30 seconds.
Preparation technology:
(1) CEFUROXIME AXETIL is dissolved in 1 liter of acetone, add cross-linking sodium carboxymethyl cellulose, stir ball mill grinding, control 25 microns of suspension particle diameter D80 <, the suspension of formation is obtained to medicine carrying piller being sprayed to coating on lactose pellet in fluid bed.
(2) by step (1) gained medicine carrying piller and pregelatinized Starch, magnesium stearate mix homogeneously, direct compression, obtains cefuroxime axetil tablets.The dissolution of cefuroxime axetil tablets detects according to method under < < Chinese Pharmacopoeia > > version cefuroxime axetil tablets item in 2010, calculate accumulation stripping percentage rate, take time t as abscissa, average accumulated stripping percentage rate is vertical coordinate mapping, the results are shown in Figure before 3(accelerated test).Testing result demonstration, the cefuroxime axetil tablets dissolution of 15 minutes prepared by this example reaches 99.4%, and content is 99.7%, and dispersed homogeneous degree has all disperseed complete at 1 minute.In temperature, be 40 ℃ ± 2 ℃, carry out accelerated test under the condition that humidity is 75% ± 5%, place 6 months, the dissolution of 15 minutes is 98.6%, and content is 99.5%, and dispersed homogeneous degree has all disperseed complete in 1 minute 30 seconds.
Comparative example
Take CEFUROXIME AXETIL specification as 125mg, and the stock and adjunct of producing 1000 dispersible tablets consists of:
Preparation technology:
Take the stock and adjunct of above-mentioned recipe quantity, cross 40 mesh sieves, then in tempering tank, mix 30 minutes, high speed rotating tablet machine direct compression for mixed powder.The dissolution of cefuroxime axetil tablets detects according to method under < < Chinese Pharmacopoeia > > version cefuroxime axetil tablets item in 2010, calculate accumulation stripping percentage rate, take time t as abscissa, average accumulated stripping percentage rate is vertical coordinate mapping, the results are shown in Figure before 4(accelerated test).Testing result demonstration, the cefuroxime axetil tablets dissolution of 15 minutes prepared by this example reaches 62.9%, and content is 99.6%, and dispersed homogeneous degree all can not disperse complete at 2 minutes.In temperature, be 40 ℃ ± 2 ℃, carry out accelerated test under the condition that humidity is 75% ± 5%, place 6 months, the dissolution of 15 minutes is 54.3%, and content is 99.2%.
Claims (6)
1. a cefuroxime axetil tablets, is characterized in that: by medicine carrying piller and filler, mix lubricant direct compression containing CEFUROXIME AXETIL, formed; Described medicine carrying piller is prepared as follows and is obtained: take CEFUROXIME AXETIL and disintegrating agent and be dissolved or dispersed in acetone, the solution of formation or suspension are sprayed to coating the dry medicine carrying piller that to obtain on lactose pellet in fluid bed; The weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.07-0.12:1-5.
2. cefuroxime axetil tablets according to claim 1, is characterized in that: the weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.08-0.10:1.5-2.
3. cefuroxime axetil tablets according to claim 1 and 2, is characterized in that: described filler is selected from following one or more: mannitol, microcrystalline Cellulose, pregelatinized Starch.
4. cefuroxime axetil tablets according to claim 1 and 2, is characterized in that: described disintegrating agent is selected from following one or more: polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium.
5. cefuroxime axetil tablets according to claim 1 and 2, is characterized in that: described lubricant is selected from following one or more: magnesium stearate, micropowder silica gel, Pulvis Talci.
6. the preparation method of cefuroxime axetil tablets according to claim 1, it is characterized in that comprising following steps: CEFUROXIME AXETIL and disintegrating agent are dissolved or dispersed in to acetone, the solution of formation or suspension are sprayed to coating the dry medicine carrying piller that to obtain on lactose pellet in fluid bed; Gained medicine carrying piller and filler, mix lubricant is even, and direct compression forms.
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| CN103505434A (en) * | 2013-09-16 | 2014-01-15 | 江苏正大清江制药有限公司 | Cefuroxime axetil tablet and preparation method thereof |
| CN107569466A (en) * | 2017-09-17 | 2018-01-12 | 石家庄四药有限公司 | Cefuroxime axetil pharmaceutical composition prepared by a kind of direct compression method |
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