CN104800177A - Cefadroxil tablet and preparation method thereof - Google Patents
Cefadroxil tablet and preparation method thereof Download PDFInfo
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- CN104800177A CN104800177A CN201510238986.0A CN201510238986A CN104800177A CN 104800177 A CN104800177 A CN 104800177A CN 201510238986 A CN201510238986 A CN 201510238986A CN 104800177 A CN104800177 A CN 104800177A
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Abstract
The invention provides a cefadroxil tablet. The cefadroxil tablet is prepared by mixing and tabletting cefadroxil particles, micro-crystal cellulose and a lubricating agent. The cefadroxil particle comprises the following ingredients: 250 parts by weight of cefadroxil, 10 to 20 parts by weight of micro-crystal cellulose, 2 to 4 parts by weight of starch, and 4 to 6 parts by weight of carboxymethyl starch sodium. Compared with the prior art, the cefadroxil tablet adopts the carboxymethyl starch sodium as a disintegrating agent which is unique in swelling effect; moreover, the micro-crystal cellulose is respectively added in the granulating and tabletting process, so that the cefadroxil is more uniformly dispersed, a product tablet core has good disintegrating effect, the particles can be rapidly disintegrated, the dissolution rate of the product is high, and the disintegrating time is short. The experiment result shows that the dissolution rate of the cefadroxil tablet is 87 to 103 percent, and the disintegrating time is 4 to 6 minutes.
Description
Technical field
The present invention relates to technical field of pharmaceuticals, more particularly, relate to a kind of Cefadroxil tablets and preparation method thereof.
Background technology
Cefadroxil, English name is Cefadroxil, and molecular formula is C
16h
17n
3o
5sH
2o, molecular weight is 381.41, and chemical structural formula is as follows:
Cefadroxil is a kind of cephalosporins broad ectrum antibiotic of sterilization, effective to the infection of Gram-positive and gram negative bacteria.It is slight easily infected to moderate that oral cefadroxil preparation can be used for treatment, as because of the microbial pharyngolaryngitis of bacterial purulent hammer or streptococcus tonsillitis, urinary tract infection, reproductive tract infection and skin infection, it has good water solublity and certain fat-soluble, oral absorption is good, and not by gastric food effect, eliminate all slow in gastrointestinal tract and urine, have stronger distribution capability and antibacterial action at infection focus.Therefore, the medicinal economy of cefadroxil preparation is high, has wide market prospect.
0.25g Cefadroxil tablets is the wet granular making certain order number after being mixed with filler, disintegrating agent, binding agent by cefadroxil raw material, adds mix lubricant again, form through tabletting after drying.But, the disintegrate limited efficiency of the disintegrating agent in traditional preparation methods, and comparatively large by the impact of the other factors such as concentration, wet mixing time, dry rear moisture content of binding agent, and the conditions such as middle product moisture and hardness control slightly difference, disintegrate weak effect will be caused, cause dissolution unstable.
Summary of the invention
In view of this, the invention provides a kind of Cefadroxil tablets and preparation method thereof, the dissolution of Cefadroxil tablets provided by the invention is high and disintegration is short.
The invention provides a kind of Cefadroxil tablets, obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant;
Described cefadroxil granule comprises following component:
Cefadroxil 250 weight portion;
Microcrystalline Cellulose 10 weight portion ~ 20 weight portion;
Starch 2 weight portion ~ 4 weight portion;
Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.
Preferably, particle diameter≤20 order of described cefadroxil granule.
Preferably, described lubricant comprises one or more in magnesium stearate, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30.
Present invention also offers the preparation method of the Cefadroxil tablets described in a kind of technique scheme, comprise the following steps:
A) granulate after cefadroxil, microcrystalline Cellulose, carboxymethylstach sodium being mixed with starch, obtain cefadroxil granule;
B) by tabletting after described cefadroxil granule, microcrystalline Cellulose and mix lubricant, Cefadroxil tablets is obtained.
Preferably, step a) described in particle diameter≤100 order of carboxymethylstach sodium.
Preferably, described step a) specifically comprises the following steps:
A1) stir after cefadroxil, microcrystalline Cellulose being mixed with carboxymethylstach sodium, obtain cefadroxil and mix powder;
A2) starch is added in solvent and steam slurry after mixing, obtain starch slurry;
A3) described cefadroxil is mixed after powder mixes with described starch slurry and stir, obtain cefadroxil soft material;
A4) after being sieved by described cefadroxil soft material, dry, granulate, obtains cefadroxil granule;
Described step a1) and a2) not order restriction.
Preferably, step a2) described in solvent comprise in water, ethanol, castor oil hydrogenated and Polyethylene Glycol one or more.
Preferably, step a2) described in the mass ratio of starch and solvent be (3 ~ 5): (90 ~ 100).
Preferably, step b) described in the mass ratio of cefadroxil granule, microcrystalline Cellulose and lubricant be (266 ~ 280): (10 ~ 20): (2 ~ 10).
Preferably, step b) described in mixing mode for stir; Described mixing speed is 2r/min ~ 5r/min, and mixing time is 30min ~ 60min.
The invention provides a kind of Cefadroxil tablets, obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant; Described cefadroxil granule comprises following component: cefadroxil 250 weight portion; Microcrystalline Cellulose 10 weight portion ~ 20 weight portion; Starch 2 weight portion ~ 4 weight portion; Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.Compared with prior art, Cefadroxil tablets provided by the invention take carboxymethylstach sodium as disintegrating agent, there is unique expansion, and in granulation and tablet forming technique, add microcrystalline Cellulose respectively, make principal agent cefadroxil disperse evenly, thus not only make product label have good disintegrate effect, and make granule also can disintegrate rapidly, product dissolution is high and disintegration is short.Experimental result shows, the dissolution of Cefadroxil tablets provided by the invention is 87% ~ 103%, and disintegration is 4min ~ 6min.
Detailed description of the invention
Below in conjunction with the embodiment of the present invention, be clearly and completely described technical scheme of the present invention, obviously, described embodiment is only the present invention's part embodiment, instead of whole embodiments.Based on the embodiment in the present invention, those of ordinary skill in the art, not making the every other embodiment obtained under creative work prerequisite, belong to the scope of protection of the invention.
The invention provides a kind of Cefadroxil tablets, obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant;
Described cefadroxil granule comprises following component:
Cefadroxil 250 weight portion;
Microcrystalline Cellulose 10 weight portion ~ 20 weight portion;
Starch 2 weight portion ~ 4 weight portion;
Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.
In the present invention, described Cefadroxil tablets is obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant.In the present invention, described cefadroxil granule comprises following component: cefadroxil 250 weight portion; Microcrystalline Cellulose 10 weight portion ~ 20 weight portion; Starch 2 weight portion ~ 4 weight portion; Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.In the present invention, described cefadroxil is the principal agent composition of Cefadroxil tablets provided by the invention; The source of the present invention to described cefadroxil is not particularly limited, and adopts the commercial goods of cefadroxil well known to those skilled in the art.In the present invention, the particle diameter of described cefadroxil is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.In the present invention, described cefadroxil granule comprises the cefadroxil of 250 weight portions.
In the present invention, described microcrystalline Cellulose is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays filling effect, has certain adhesive effect simultaneously concurrently and have certain disintegration in medication process.The source of the present invention to described microcrystalline Cellulose is not particularly limited, and adopts the commercial goods of microcrystalline Cellulose well known to those skilled in the art.In the present invention, the particle diameter of described microcrystalline Cellulose is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.In the present invention, described cefadroxil granule comprises the microcrystalline Cellulose of 10 weight portion ~ 20 weight portions, is preferably the microcrystalline Cellulose of 15 weight portions.
In the present invention, described starch is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays cementation.The source of the present invention to described starch is not particularly limited, and adopts the commercial goods of starch well known to those skilled in the art.In the present invention, described cefadroxil granule comprises the starch of 2 weight portion ~ 4 weight portions, is preferably the starch of 2.2 weight portion ~ 3.7 weight portions.
In the present invention, described carboxymethylstach sodium is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays disintegration.The source of the present invention to described carboxymethylstach sodium is not particularly limited, and adopts the commercial goods of carboxymethylstach sodium well known to those skilled in the art.In the present invention, the particle diameter of described carboxymethylstach sodium is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.In the present invention, described cefadroxil granule comprises the carboxymethylstach sodium of 4 weight portion ~ 6 weight portions, is preferably the carboxymethylstach sodium of 5 weight portions.
In the present invention, the particle diameter of described cefadroxil granule is preferably less than or equal to 20 orders, is more preferably and is less than or equal to 15 orders.In the present invention, described Cefadroxil tablets is preferably obtained by tabletting after the cefadroxil granule of 266 weight portion ~ 279 weight portions and microcrystalline Cellulose, mix lubricant, is more preferably 266.2 weight portion ~ 278.7 weight portions.
In the present invention, described Cefadroxil tablets is obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant.Described microcrystalline Cellulose is identical with the microcrystalline Cellulose described in above-mentioned cefadroxil granule, does not repeat them here.In the present invention, described Cefadroxil tablets is obtained by tabletting after the microcrystalline Cellulose of cefadroxil granule and 10 weight portion ~ 20 weight portions, mix lubricant, is more preferably 15 weight portions.
In the present invention, described lubricant preferably include in magnesium stearate, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30 one or more, be more preferably in magnesium stearate and micropowder silica gel one or both, most preferably be magnesium stearate and micropowder silica gel.The source of the present invention to described lubricant is not particularly limited, and adopts the commercial goods of above-mentioned magnesium stearate well known to those skilled in the art, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30.In the present invention, the particle diameter of described lubricant is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.In the present invention, described Cefadroxil tablets is obtained by tabletting after the mix lubricant of cefadroxil granule and microcrystalline Cellulose, 2 weight portion ~ 10 weight portions, is more preferably 4 weight portion ~ 8 weight portions, is more preferably 6 weight portions.In the present invention's preferred embodiment, described lubricant is the magnesium stearate of 2 weight portions and the micropowder silica gel of 4 weight portions.
Present invention also offers the preparation method of the Cefadroxil tablets described in a kind of technique scheme, comprise the following steps:
A) granulate after cefadroxil, microcrystalline Cellulose, carboxymethylstach sodium being mixed with starch, obtain cefadroxil granule;
B) by tabletting after described cefadroxil granule, microcrystalline Cellulose and mix lubricant, Cefadroxil tablets is obtained.
In the present invention, granulate after cefadroxil, microcrystalline Cellulose, carboxymethylstach sodium are mixed with starch, obtain cefadroxil granule.In the present invention, described cefadroxil is the principal agent composition of Cefadroxil tablets provided by the invention; The source of the present invention to described cefadroxil is not particularly limited, and adopts the commercial goods of cefadroxil well known to those skilled in the art.In the present invention, the particle diameter of described cefadroxil is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.
In the present invention, described microcrystalline Cellulose is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays filling effect, has certain adhesive effect simultaneously concurrently and have certain disintegration in medication process.The source of the present invention to described microcrystalline Cellulose is not particularly limited, and adopts the commercial goods of microcrystalline Cellulose well known to those skilled in the art.In the present invention, the particle diameter of described microcrystalline Cellulose is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.
In the present invention, described carboxymethylstach sodium is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays disintegration.The source of the present invention to described carboxymethylstach sodium is not particularly limited, and adopts the commercial goods of carboxymethylstach sodium well known to those skilled in the art.In the present invention, the particle diameter of described carboxymethylstach sodium is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.
In the present invention, described starch is the adjunct ingredient of Cefadroxil tablets provided by the invention, mainly plays cementation.The source of the present invention to described starch is not particularly limited, and adopts the commercial goods of starch well known to those skilled in the art.
In the present invention, described cefadroxil, microcrystalline Cellulose, carboxymethylstach sodium are mixed with starch after granulate and preferably specifically comprise the following steps:
A1) stir after cefadroxil, microcrystalline Cellulose being mixed with carboxymethylstach sodium, obtain cefadroxil and mix powder;
A2) starch is added in solvent and steam slurry after mixing, obtain starch slurry;
A3) described cefadroxil is mixed after powder mixes with described starch slurry and stir, obtain cefadroxil soft material;
A4) after being sieved by described cefadroxil soft material, dry, granulate, obtains cefadroxil granule;
Described step a1) and a2) not order restriction.
In the present invention, stir after cefadroxil, microcrystalline Cellulose are mixed with carboxymethylstach sodium, obtain cefadroxil and mix powder.In the present invention, identical with described in technique scheme of described cefadroxil, microcrystalline Cellulose and carboxymethylstach sodium, does not repeat them here.In the present invention, the mass ratio of described cefadroxil, microcrystalline Cellulose and carboxymethylstach sodium is 250:(10 ~ 20): (4 ~ 6).The device of the present invention to described mixing and stirring is not particularly limited, and adopts wet granulator well known to those skilled in the art, is preferably HZ-250B type efficient wet granulator.In the present invention, step a1) described in stir process be preferably specially:
After mixing, cefadroxil, microcrystalline Cellulose and carboxymethylstach sodium are successively through stirring at low speed and high-speed stirred, obtain cefadroxil and mix powder.In the present invention, the speed of described stirring at low speed is preferably 4r/s ~ 8r/s, is more preferably 6r/s; The time of described stirring at low speed is preferably 480s ~ 720s, is more preferably 600s.In the present invention, described high-speed stirred, on the basis keeping stirring at low speed speed constant, is undertaken by opening cutting knife; Described cutting knife speed is preferably 8r/s ~ 12r/s, is more preferably 10r/s; The time of described high-speed stirred is preferably 40s ~ 80s, is more preferably 60s.
Meanwhile, the present invention steams slurry after starch being added in solvent mixing, obtains starch slurry.In the present invention, identical with described in technique scheme of described starch, does not repeat them here; Described solvent preferably include in water, ethanol, castor oil hydrogenated and Polyethylene Glycol one or more, be more preferably water.In the present invention, the mass ratio of described starch and solvent is preferably (3 ~ 5): (90 ~ 100), are more preferably 3:97.The method of the present invention to described mixing and steaming and decocting is not particularly limited, and adopts steaming slurry processes well known to those skilled in the art.
Obtain after cefadroxil mixes powder and starch slurry, described cefadroxil mixes after powder mixes with described starch slurry and stirs by the present invention, obtains cefadroxil soft material.In the present invention, described cefadroxil is mixed the process stirred after powder mixes with described starch slurry to be preferably specially:
Described starch slurry is evenly added cefadroxil to be mixed in powder, successively through stirring at low speed and high-speed stirred, obtains cefadroxil soft material.In the present invention, the speed of described stirring at low speed is preferably 4r/s ~ 8r/s, is more preferably 6r/s; The time of described stirring at low speed is preferably 40s ~ 80s, is more preferably 60s.In the present invention, described high-speed stirred, on the basis keeping stirring at low speed speed constant, is undertaken by opening cutting knife; Described cutting knife speed is preferably 8r/s ~ 12r/s, is more preferably 10r/s; The time of described high-speed stirred is preferably 240s ~ 300s, is more preferably 260s ~ 280s.
After obtaining cefadroxil soft material, after described cefadroxil soft material sieves by the present invention, dry, granulate, obtains cefadroxil granule.The present invention is not particularly limited the described device sieved, and adopts oscillating granulator well known to those skilled in the art, is preferably YK-160B type oscillating granulator.In the present invention, described in the sieve order number of process screen cloth used be preferably 15 order ~ 25 orders, be more preferably 20 orders.
After process of sieving described in completing, the soft material after sieving is carried out drying, granulate by the present invention, obtains cefadroxil granule.The equipment of the present invention to described drying is not particularly limited, and adopts solid drying machine well known to those skilled in the art, is preferably MJ50-5 type vacuum and low temperature solid drying machine; The equipment of the present invention to described granulate is not particularly limited, and adopts pelletizing machine well known to those skilled in the art, is preferably KZL-160 type Fast granulate machine.After super-dry and granulate process, the cefadroxil pellet moisture that the present invention obtains is less than or equal to 5%, and particle diameter is less than or equal to 20 orders.
After obtaining described cefadroxil granule, the present invention, by tabletting after described cefadroxil granule, microcrystalline Cellulose and mix lubricant, obtains Cefadroxil tablets.In the present invention, identical with described in technique scheme of described microcrystalline Cellulose, does not repeat them here.
In the present invention, described lubricant preferably include in magnesium stearate, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30 one or more, be more preferably in magnesium stearate and micropowder silica gel one or both, most preferably be magnesium stearate and micropowder silica gel.The source of the present invention to described lubricant is not particularly limited, and adopts the commercial goods of above-mentioned magnesium stearate well known to those skilled in the art, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30.In the present invention, the particle diameter of described lubricant is preferably less than or equal to 100 orders, is more preferably and is less than or equal to 80 orders.In the present invention, the mass ratio of described cefadroxil granule, microcrystalline Cellulose and lubricant is preferably (260 ~ 280): (10 ~ 20): (2 ~ 10), are more preferably 272.2:15:(2 ~ 10).In the present invention's preferred embodiment, described lubricant is magnesium stearate and micropowder silica gel; The mass ratio of described cefadroxil granule, microcrystalline Cellulose, magnesium stearate and micropowder silica gel is preferably 270:15:2:4.
In the present invention, by described cefadroxil granule, microcrystalline Cellulose and mix lubricant; The mode of described mixing is preferably and stirs.The device of the present invention to described mixing and stirring is not particularly limited, and adopts mixer well known to those skilled in the art, is preferably HF-2000 side's cone mixer.In the present invention, described mixing speed is preferably 2r/min ~ 5r/min, is more preferably 3r/min ~ 4r/min; Described mixing time is preferably 30min ~ 60min, is more preferably 30min.
After completing described mixing, mixed cefadroxil granule, microcrystalline Cellulose and lubricant are carried out tabletting by the present invention.The device of the present invention to described tabletting is not particularly limited, and adopts tablet machine well known to those skilled in the art, is preferably GZPL-28C type Highspeedrotarytabletpress; Adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain Cefadroxil tablets.
The invention provides a kind of Cefadroxil tablets, obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant; Described cefadroxil granule comprises following component: cefadroxil 250 weight portion; Microcrystalline Cellulose 10 weight portion ~ 20 weight portion; Starch 2.2 weight portion ~ 3.7 weight portion; Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.Compared with prior art, Cefadroxil tablets provided by the invention take carboxymethylstach sodium as disintegrating agent, there is unique expansion, and in granulation and tablet forming technique, add microcrystalline Cellulose respectively, make principal agent cefadroxil disperse evenly, thus not only make product label have good disintegrate effect, and make granule also can disintegrate rapidly, product dissolution is high and disintegration is short.Experimental result shows, the dissolution of Cefadroxil tablets provided by the invention is 87% ~ 103%, and disintegration is 4min ~ 6min.
In order to further illustrate the present invention, be described in detail below by following examples.As shown in table 1, supplementary material used in following examples of the present invention all meets standards of pharmacopoeia, and through pulverizing 100 mesh sieve process.
The kind of supplementary material used and source in table 1 embodiment of the present invention
Embodiment 1
(1) first; 75kg cefadroxil, 4.5kg microcrystalline Cellulose and 1.5kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 21340g water meanwhile, then add 660g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 81.66kg cefadroxil granule, 4.5kg microcrystalline Cellulose, 0.6kg magnesium stearate and 1.2kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Embodiment 2
(1) first; 75kg cefadroxil, 3kg microcrystalline Cellulose and 1.2kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 21340g water meanwhile, then add 660g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 79.86kg cefadroxil granule, 3kg microcrystalline Cellulose, 0.6kg magnesium stearate and 1.2kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Embodiment 3
(1) first; 75kg cefadroxil, 6kg microcrystalline Cellulose and 1.8kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 21340g water meanwhile, then add 660g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 83.46kg cefadroxil granule, 6kg microcrystalline Cellulose, 0.6kg magnesium stearate and 1.2kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Embodiment 4
(1) first; 75kg cefadroxil, 4.5kg microcrystalline Cellulose and 1.5kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 20900g water meanwhile, then add 1100g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 82.1kg cefadroxil granule, 4.5kg microcrystalline Cellulose, 0.6kg magnesium stearate and 1.2kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Embodiment 5
(1) first; 75kg cefadroxil, 4.5kg microcrystalline Cellulose and 1.5kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 21340g water meanwhile, then add 660g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 81.66kg cefadroxil granule, 4.5kg microcrystalline Cellulose, 0.45kg magnesium stearate and 1.5kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Embodiment 6
(1) first; 75kg cefadroxil, 4.5kg microcrystalline Cellulose and 1.5kg carboxymethylstach sodium are added in HZ-250B type efficient wet granulator; stirring at low speed 600s under the rate conditions of 6r/s; open cutting knife again; cutting knife speed is that 10r/s carries out high-speed stirred 60s, obtains cefadroxil and mixes powder.
, added in pulping pan used for producing by 21340g water meanwhile, then add 660g starch, open Steam Heating, pressure is 0.2MPa, obtains starch slurry.
Then, above-mentioned starch slurry is evenly added cefadroxil and mixes in powder, stirring at low speed 60s under the rate conditions of 6r/s, then open cutting knife, cutting knife speed is that 10r/s carries out high-speed stirred 270s, obtains cefadroxil soft material.
Finally; cefadroxil soft material is added in YK-160B type oscillating granulator; granulate with 20 mesh sieves; drying is carried out again, after KZL-160 type Fast granulate machine carries out granulate by MJ50-5 type vacuum and low temperature solid drying machine; obtain moisture and be less than or equal to 5%, particle diameter is less than or equal to 20 object cefadroxil granules.
(2) 81.66kg cefadroxil granule, 4.5kg microcrystalline Cellulose, 0.75kg magnesium stearate and 0.9kg micropowder silica gel are added in HF-2000 side's cone mixer, 30min is stirred under the speed conditions of 4r/min, finally by GZPL-28C type Highspeedrotarytabletpress, adopt the flat oblique mould of φ 9.5mm to carry out tabletting, obtain 0.25g Cefadroxil tablets.
Comparative example
Commercially available prod 0.25g Cefadroxil tablets.
According to the dissolution detection method that pharmacopeia second method provides, the 0.25g Cefadroxil tablets that the 0.25g Cefadroxil tablets prepared embodiment 1 respectively and comparative example provide carries out disintegration time and dissolution detects.Detection method is as follows: with 900ml water for dissolution medium, pour in 6 stripping rotors respectively, treat that dissolution medium temperature reaches 37 DEG C ± 0.5 DEG C, get testing sample 6, drop into respectively in 6 stripping rotors, setting speed is 50 turns per minute, starts stirring paddle, after 30 minutes, get solution appropriate, filter, it is appropriate that precision measures subsequent filtrate, and add water the solution be quantitatively diluted to about containing 25ug in every 1ml, by determined by ultraviolet spectrophotometry, measure absorbance at the wavelength place of 263nm, calculate the stripping quantity of every sheet, limit is 80% (internal control) of labelled amount.
The 0.25g Cefadroxil tablets that the 0.25g Cefadroxil tablets prepared the embodiment 1 ~ 6 of 10 batches respectively according to the method described above and comparative example provide detects, and testing result is in table 2 ~ 3.
The detection data of table 2 0.25g Cefadroxil tablets disintegration time
| Batch | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Comparative example |
| 1 | 6min | 6min | 4min | 5min | 4min | 5min | 18min |
| 2 | 5min | 6min | 5min | 6min | 5min | 6min | 14min |
| 3 | 4min | 5min | 4min | 4min | 6min | 4min | 19min |
| 4 | 4min | 6min | 4min | 5min | 6min | 5min | 13min |
| 5 | 5min | 5min | 5min | 5min | 5min | 6min | 15min |
| 6 | 5min | 6min | 4min | 4min | 4min | 5min | 16min |
| 7 | 6min | 5min | 4min | 6min | 6min | 6min | 12min |
| 8 | 4min | 5min | 4min | 5min | 5min | 4min | 19min |
| 9 | 5min | 6min | 4min | 4min | 6min | 5min | 11min |
| 10 | 6min | 6min | 4min | 6min | 4min | 6min | 17min |
The detection data of table 3 0.25g Cefadroxil tablets dissolution
| Batch | Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Comparative example |
| 1 | 92％ | 92％ | 95％ | 98％ | 90％ | 91％ | 68％ |
| 2 | 90％ | 96％ | 93％ | 97％ | 95％ | 99％ | 75％ |
| 3 | 98％ | 94％ | 94％ | 89％ | 100％ | 92％ | 70％ |
| 4 | 101％ | 99％ | 99％ | 92％ | 89％ | 89％ | 81％ |
| 5 | 94％ | 100％ | 102％ | 90％ | 96％ | 93％ | 74％ |
| 6 | 95％ | 91％ | 100％ | 95％ | 94％ | 92％ | 78％ |
| 7 | 87％ | 97％ | 98％ | 101％ | 95％ | 99％ | 72％ |
| 8 | 93％ | 87％ | 93％ | 96％ | 98％ | 101％ | 79％ |
| 9 | 96％ | 92％ | 99％ | 93％ | 96％ | 95％ | 67％ |
| 10 | 102％ | 96％ | 103％ | 92％ | 101％ | 98％ | 74％ |
Testing result shows, 0.25g Cefadroxil tablets dissolution provided by the invention is high and disintegration is short, and the dissolution of 0.25g Cefadroxil tablets provided by the invention is 87% ~ 102%, and disintegration is 4min ~ 6min.
The above-mentioned explanation of the disclosed embodiments, enables professional and technical personnel in the field realize or uses the present invention.To be apparent for those skilled in the art to the multiple amendment of these embodiments, General Principle as defined herein can without departing from the spirit or scope of the present invention, realize in other embodiments.Therefore, the present invention can not be restricted to these embodiments shown in this article, but will meet the widest scope consistent with principle disclosed herein and features of novelty.
Claims (10)
1. a Cefadroxil tablets, is characterized in that, is obtained by tabletting after cefadroxil granule and microcrystalline Cellulose, mix lubricant;
Described cefadroxil granule comprises following component:
Cefadroxil 250 weight portion;
Microcrystalline Cellulose 10 weight portion ~ 20 weight portion;
Starch 2 weight portion ~ 4 weight portion;
Carboxymethylstach sodium 4 weight portion ~ 6 weight portion.
2. Cefadroxil tablets according to claim 1, is characterized in that, particle diameter≤20 order of described cefadroxil granule.
3. Cefadroxil tablets according to claim 1, it is characterized in that, described lubricant comprise in magnesium stearate, micropowder silica gel, stearic acid, calcium stearate, sodium stearyl fumarate, paraffin oil, paraffin, glyceryl monostearate, monopalmitin, sodium acetate, sodium chloride, DL-LEUCINE, sodium laurylsulfate, magnesium laurylsulfate, Polyethylene Glycol, polyoxyethylene monostearate and Brij30 one or more.
4. a preparation method for the Cefadroxil tablets described in any one of claims 1 to 3, is characterized in that, comprises the following steps:
A) granulate after cefadroxil, microcrystalline Cellulose, carboxymethylstach sodium being mixed with starch, obtain cefadroxil granule;
B) by tabletting after described cefadroxil granule, microcrystalline Cellulose and mix lubricant, Cefadroxil tablets is obtained.
5. preparation method according to claim 4, is characterized in that, step a) described in particle diameter≤100 order of carboxymethylstach sodium.
6. preparation method according to claim 4, is characterized in that, described step a) specifically comprises the following steps:
A1) stir after cefadroxil, microcrystalline Cellulose being mixed with carboxymethylstach sodium, obtain cefadroxil and mix powder;
A2) starch is added in solvent and steam slurry after mixing, obtain starch slurry;
A3) described cefadroxil is mixed after powder mixes with described starch slurry and stir, obtain cefadroxil soft material;
A4) after being sieved by described cefadroxil soft material, dry, granulate, obtains cefadroxil granule;
Described step a1) and a2) not order restriction.
7. preparation method according to claim 6, is characterized in that, step a2) described in solvent comprise in water, ethanol, castor oil hydrogenated and Polyethylene Glycol one or more.
8. preparation method according to claim 6, is characterized in that, step a2) described in the mass ratio of starch and solvent be (3 ~ 5): (90 ~ 100).
9. preparation method according to claim 4, is characterized in that, step b) described in the mass ratio of cefadroxil granule, microcrystalline Cellulose and lubricant be (260 ~ 280): (10 ~ 20): (2 ~ 10).
10. preparation method according to claim 4, is characterized in that, step b) described in mixing mode for stir; Described mixing speed is 2r/min ~ 5r/min, and mixing time is 30min ~ 60min.
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| CN105640895A (en) * | 2016-01-15 | 2016-06-08 | 石药集团欧意药业有限公司 | Cefadroxil granular preparation and preparation method thereof |
| CN106390094A (en) * | 2016-11-11 | 2017-02-15 | 上海雅本化学有限公司 | Trandolapril-containing pharmaceutical composition and preparation method thereof |
| CN106588954A (en) * | 2016-11-08 | 2017-04-26 | 山东裕欣药业有限公司 | Anti-infective drug such as cefadroxil crystal compound and composition thereof |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105640895A (en) * | 2016-01-15 | 2016-06-08 | 石药集团欧意药业有限公司 | Cefadroxil granular preparation and preparation method thereof |
| CN105640895B (en) * | 2016-01-15 | 2019-03-01 | 石药集团欧意药业有限公司 | A kind of cefadroxil granular preparation and preparation method thereof |
| CN106588954A (en) * | 2016-11-08 | 2017-04-26 | 山东裕欣药业有限公司 | Anti-infective drug such as cefadroxil crystal compound and composition thereof |
| CN106588954B (en) * | 2016-11-08 | 2018-11-27 | 山东罗欣药业集团恒欣药业有限公司 | A kind of anti-infectives amoxycillin crystalline compounds and combinations thereof |
| CN106390094A (en) * | 2016-11-11 | 2017-02-15 | 上海雅本化学有限公司 | Trandolapril-containing pharmaceutical composition and preparation method thereof |
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