CN103494783B - A kind of Azithromycin dispersible tablet and preparation method thereof - Google Patents
A kind of Azithromycin dispersible tablet and preparation method thereof Download PDFInfo
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- CN103494783B CN103494783B CN201310442662.XA CN201310442662A CN103494783B CN 103494783 B CN103494783 B CN 103494783B CN 201310442662 A CN201310442662 A CN 201310442662A CN 103494783 B CN103494783 B CN 103494783B
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Abstract
The invention discloses a kind of Azithromycin dispersible tablet and preparation method thereof, said preparation is formed by medicine-containing particle and pharmaceutically acceptable auxiliary materials and mixing tabletting, described medicine-containing particle is dissolved in dehydrated alcohol by azithromycin and Semen Maydis Ruan, add filler, rotary evaporation drying ethanol, sieve, to obtain final product.Compared with prior art, Azithromycin dispersible tablet stripping prepared by the present invention is rapid, good stability, not sticking, and preparation technology is simple, well solves existing preparation Problems existing.
Description
Technical field
The invention belongs to pharmaceutical preparations technology field, in particular to a kind of solid orally ingestible of azithromycin, particularly relate to a kind of Azithromycin dispersible tablet and preparation method thereof.
Background technology
Azithromycin belongs to macrolide antibiotics, and have unique pharmacokinetic characteristics, biological half-life is long, and tissue permeability is high, chemical and biological stability is good, has a broad antifungal spectrum, the advantages such as untoward reaction is little, better tolerance.Be widely used in respiratory tract, skin soft tissue and urogenital infections clinically.This kind dosage form of current domestic listing includes ordinary tablet, dispersible tablet, capsule, granule, dry suspension etc.
At present, the Azithromycin dispersible tablet of listing is all tablettings after wet granulation, but azithromycin is macrolide antibiotics, unstable under wet heat condition, inevitably be exposed in hygrothermal environment in wet-granulation process, principal agent can be degraded, and related substance can obviously increase, and makes medicine may there is certain potential safety hazard.If the method for powder formulation tabletting can be adopted to prepare dispersible tablet, then can solve the problem.But research finds, because the compressibility of azithromycin own is poor, and has viscosity, is easy to cause sticking, sliver, the problems such as friability is defective in the process of carrying out tabletting, this phenomenon more highlights expressively when adopting technique of direct powder compression.
CN101129398A discloses a kind of Azithromycin dispersible tablet and preparation method thereof, and its concrete grammar is: get pulverize and cross respectively the azithromycin of 120 mesh sieves and medical starch, the abundant mix homogeneously of pregelatinized Starch again with 60% ethanol for wetting agent wet granulation.But it uses 60% alcohol granulation, contained humidity is easy to the degraded causing medicine lactonic ring.
CN102973529A discloses a kind of Azithromycin dispersible tablet and preparation method thereof, selects microcrystalline Cellulose, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose, silicon dioxide, magnesium stearate.But granulate with water, be easy to the degraded causing medicine.
CN102895203A discloses a kind of preparation method of Azithromycin dispersible tablet, and Azithromycin Raw Material is carried out in the mode of external feeding the production that feeds intake by this method, inside adds adjuvant 50% alcohol granulation.Improve medicine stability to a certain extent, but Azithromycin Raw Material viscosity being large, there is the problem of easy sticking in additional mixed pressuring plate equally.
CN102648898A provides the method overcoming azithromycin tabletting and adhere to, and azithromycin and dispersant were pulverized 80 mesh sieves respectively, loads jet mill and carries out micronizing; By micronizing mixture mix with one or more in filler, disintegrating agent, lubricant, binding agent, fluidizer, correctives, tabletting.The consumption of dispersant is that azithromycin weight is in the 2-10 of base times.Dispersant dosage is large, and after azithromycin micropowder, surface area is larger, easier sticking.
Found by retrieval, prior art is solve azithromycin poor stability, the easily problem of sticking to have carried out large quantifier elimination, but still does not have a kind of method to solve the problem preferably simultaneously.
Summary of the invention
In view of the deficiencies in the prior art, the present inventor is studied by lot of experiments and explores preparation prescription and technique, be surprised to find that, azithromycin and Semen Maydis Ruan are dissolved in ethanol, add filler, rotary evaporation drying ethanol, azithromycin Semen Maydis Ruan is wrapped up, and be attached to filler surface, avoid and cause greatly sticking problem because of medicine viscosity in tableting processes; Semen Maydis Ruan is water insoluble, moist without drawing, but dissolves in buffer salt, when stripping measures, after disintegration of tablet, and Semen Maydis Ruan rapid solution, under being attached to the effect of medicine osmotic pressure inside and outside granule on filler surface, rapid stripping; In study on the stability, because of the film wrapped that medicine is formed by Semen Maydis Ruan, outside moisture is difficult to ooze people, therefore good stability.Based on this, the invention provides a kind of stripping rapid, good stability, the not Azithromycin dispersible tablet of sticking and preparation technology thereof during tabletting.
Specifically, the present invention is achieved through the following technical solutions:
A kind of Azithromycin dispersible tablet, described Azithromycin dispersible tablet is formed by medicine-containing particle and pharmaceutically acceptable auxiliary materials and mixing tabletting, and described medicine-containing particle is dissolved in dehydrated alcohol by azithromycin and Semen Maydis Ruan, add filler, rotary evaporation drying ethanol, sieves, and to obtain final product.
Preferably, Azithromycin dispersible tablet as above, the weight consumption of azithromycin in wherein said medicine-containing particle, Semen Maydis Ruan and filler is than being 1:0.3-0.7:0.3-6.
Further preferably, Azithromycin dispersible tablet as above, the weight consumption of azithromycin in wherein said medicine-containing particle, Semen Maydis Ruan and filler is than being 1:0.4-0.5:0.8-2.
Again further preferably, Azithromycin dispersible tablet as above, wherein said filler is one or both in lactose and mannitol.
Azithromycin dispersible tablet of the present invention, wherein adopted pharmaceutically acceptable adjuvant comprises disintegrating agent and lubricant.Described disintegrating agent is one or more in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and low replacement Semen Maydis Ruan.Described lubricant is one or more in magnesium stearate, sodium stearyl fumarate and zinc stearate.
Present invention also offers a kind of preparation method of Azithromycin dispersible tablet as above, the method comprises the steps:
(1) be dissolved in dehydrated alcohol by azithromycin and Semen Maydis Ruan, add filler, rotary evaporation drying ethanol, sieves, and obtains medicine-containing particle;
(2) step (1) gained medicine-containing particle is mixed homogeneously with pharmaceutically acceptable adjuvant, direct compression.
Further preferably, the preparation method of Azithromycin dispersible tablet as above, wherein said filler is one or both in lactose and mannitol.
Further preferably, the preparation method of Azithromycin dispersible tablet as above, wherein said pharmaceutically acceptable adjuvant comprises disintegrating agent and lubricant; Described disintegrating agent is one or more in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and low replacement Semen Maydis Ruan; Described lubricant is one or more in magnesium stearate, sodium stearyl fumarate and zinc stearate.
Compared with prior art, Azithromycin dispersible tablet stripping prepared by the present invention is rapid, good stability, not sticking, and preparation technology is simple, well solves existing preparation Problems existing.
Detailed description of the invention
Following examples further describe preparation process of the present invention and beneficial effect, embodiment is only for the object of illustration, do not limit the scope of the invention, the simultaneously apparent change made according to the present invention of those of ordinary skill in the art and modification are also contained within the scope of the invention.
Embodiment 1 Azithromycin dispersible tablet and preparation method thereof
Preparation method:
(1) recipe quantity takes azithromycin, Semen Maydis Ruan, is dissolved in dehydrated alcohol, adds lactose, rotary evaporation, drying ethanol under 50 DEG C of conditions, crosses 30 sieves, obtains mixture.
(2) by said mixture and carboxymethyl starch sodium, the magnesium stearate mix homogeneously of crossing 80 mesh sieves, tabletting.
Embodiment 2 Azithromycin dispersible tablet and preparation method thereof
Preparation method:
(1) recipe quantity takes azithromycin, Semen Maydis Ruan, is dissolved in dehydrated alcohol, adds lactose, rotary evaporation, drying ethanol under 55 DEG C of conditions, crosses 40 sieves, obtains mixture.
(2) by said mixture and carboxymethyl starch sodium, the magnesium stearate mix homogeneously of crossing 80 mesh sieves, tabletting.
Embodiment 3 Azithromycin dispersible tablet and preparation method thereof
Preparation method:
(1) recipe quantity takes azithromycin, Semen Maydis Ruan, is dissolved in dehydrated alcohol, adds lactose, rotary evaporation, drying ethanol under 50 DEG C of conditions, crosses 30 sieves, obtains mixture.
(2) by said mixture and polyvinylpolypyrrolidone, the magnesium stearate mix homogeneously of crossing 80 mesh sieves, tabletting.
Comparative example 1 Azithromycin dispersible tablet and preparation method thereof
Preparation method:
Recipe quantity was taken the azithromycin of 100 mesh sieves, Semen Maydis Ruan, lactose, polyvinylpolypyrrolidone mix homogeneously, add dehydrated alcohol in right amount, granulate, 50 DEG C of dryings, granule crosses 30 mesh sieves, mixs homogeneously with magnesium stearate, tabletting.
Comparative example 2 Azithromycin dispersible tablet and preparation method thereof
Preparation method:
(1) recipe quantity takes azithromycin, Semen Maydis Ruan, is dissolved in dehydrated alcohol, rotary evaporation, drying ethanol under 50 DEG C of conditions, crosses 30 sieves, obtains mixture.
(2) by said mixture and lactose, polyvinylpolypyrrolidone, the magnesium stearate mix homogeneously of crossing 80 mesh sieves, tabletting.
The quality investigation of embodiment 4 Azithromycin dispersible tablet
1, dissolution.This test adopts high-efficient liquid phase color popularize law to measure potency of azithromycin, investigates the dissolving out capability of Azithromycin dispersible tablet.Concrete grammar adopts Chinese Pharmacopoeia version in 2010: get this product 6, according to dissolution method (the second method), with phosphate buffer (pH6.0) 900ml for dissolution medium, rotating speed is 50 turns per minute, operates in accordance with the law, through 5 minutes time, get solution appropriate, filter, get subsequent filtrate appropriate, with dissolution medium quantitatively dilute to make in every 1ml about containing the solution of azithromycin 0.2mg as need testing solution; Separately get azithromycin reference substance appropriate, accurately weighed, add ethanol in proper amount (every 2mg about adds ethanol 1ml) and make dissolving, add dissolution medium and quantitatively dilute the solution made about containing 0.2mg in every 1ml, product solution in contrast.By external standard method with the stripping quantity of the every sheet of calculated by peak area.Limit is 75% of labelled amount, should conform with the regulations.
2, related substance.Get this product fine powder appropriate, accurately weighed, add acetonitrile and make azithromycin dissolution and quantitatively dilute the solution made containing azithromycin lOmg in every lml, filter, get subsequent filtrate as need testing solution; Measure according to the method under Zitromax prime implicant, each impurity peak area and 2.0 times (2.0%) of contrast solution main peak area must not be greater than.
The dissolution of table 1 Azithromycin dispersible tablet, related substance and outward appearance measurement result
Experimental result according to table 1 can be found out, Azithromycin dispersible tablet prepared by embodiment of the present invention 1-3 is unilateral bright and clean, and stripping is rapid, and after study on the stability, related substance does not increase substantially.Azithromycin, Semen Maydis Ruan and lactose are not prepared mixture by comparative example 1, but granulate after mix homogeneously, tabletting, and because azithromycin is not wrapped up by Semen Maydis Ruan, therefore after accelerated test, related substance increases obviously, and unilateral have sticking.Comparative example 2 is by azithromycin Semen Maydis Ruan parcel, therefore after accelerating to investigate, related substance increases not obvious, but due to Semen Maydis Ruan and azithromycin mixture viscosity large, after dry, large, the granule of viscosity is firmly, therefore stripping is poor, unilateral not bright and clean.
Claims (7)
1. an Azithromycin dispersible tablet, it is characterized in that: described Azithromycin dispersible tablet is formed by medicine-containing particle and pharmaceutically acceptable auxiliary materials and mixing tabletting, described medicine-containing particle is dissolved in dehydrated alcohol by azithromycin and Semen Maydis Ruan, add filler, rotary evaporation drying ethanol, sieve, to obtain final product; The weight consumption of azithromycin in described medicine-containing particle, Semen Maydis Ruan and filler is than being 1:0.3-0.7:0.3-6; Described filler is one or both in lactose and mannitol.
2. Azithromycin dispersible tablet according to claim 2, is characterized in that: the weight consumption of azithromycin in described medicine-containing particle, Semen Maydis Ruan and filler is than being 1:0.4-0.5:0.8-2.
3. Azithromycin dispersible tablet according to claim 1 and 2, is characterized in that: described pharmaceutically acceptable adjuvant comprises disintegrating agent and lubricant.
4. Azithromycin dispersible tablet according to claim 3, is characterized in that: described disintegrating agent is one or more in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and low replacement Semen Maydis Ruan.
5. Azithromycin dispersible tablet according to claim 3, is characterized in that: described lubricant is one or more in magnesium stearate, sodium stearyl fumarate and zinc stearate.
6. a preparation method for Azithromycin dispersible tablet according to claim 1 and 2, is characterized in that comprising the steps:
(1) be dissolved in dehydrated alcohol by azithromycin and Semen Maydis Ruan, add filler, rotary evaporation drying ethanol, sieves, and obtains medicine-containing particle;
(2) step (1) gained medicine-containing particle is mixed homogeneously with pharmaceutically acceptable adjuvant, direct compression.
7. the preparation method of Azithromycin dispersible tablet according to claim 6, is characterized in that: described pharmaceutically acceptable adjuvant comprises disintegrating agent and lubricant; Described disintegrating agent is one or more in polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium and low replacement Semen Maydis Ruan; Described lubricant is one or more in magnesium stearate, sodium stearyl fumarate and zinc stearate.
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| CN102895203A (en) * | 2012-11-02 | 2013-01-30 | 江苏鹏鹞药业有限公司 | Method for preparing azithromycin dispersible tablets |
| CN102973529A (en) * | 2012-11-28 | 2013-03-20 | 康普药业股份有限公司 | Azithromycin dispersible tablet and preparation method thereof |
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Effective date of registration: 20160713 Address after: 051530 Hebei province Shijiazhuang Zhaoxian County Zhao Yuan No. 123 Patentee after: Hebei JamesHill Pharmaceutical Co., Ltd. Address before: 211200 Lishui Economic Development Zone, Jiangsu, Nanjing No. 1 Shandong Road Patentee before: Nanjing Zhengkuan Pharmaceutical Science and Technology Co., Ltd. |