CN103040788A - Cefuroxime axetil capsule and preparation method thereof - Google Patents
Cefuroxime axetil capsule and preparation method thereof Download PDFInfo
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- CN103040788A CN103040788A CN2013100223734A CN201310022373A CN103040788A CN 103040788 A CN103040788 A CN 103040788A CN 2013100223734 A CN2013100223734 A CN 2013100223734A CN 201310022373 A CN201310022373 A CN 201310022373A CN 103040788 A CN103040788 A CN 103040788A
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- axetil
- cefuroxime axetil
- ceruroxime
- cefuroxime
- disintegrating agent
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Abstract
The invention discloses a cefuroxime axetil capsule. The cefuroxime axetil capsule is prepared by filling the uniformly mixed cefuroxime axetil-containing medicine-carrying pills and talcum powder into a capsule shell; and the medicine-carrying pills are prepared according to the following steps of: weighing the cefuroxime axetil and a disintegrating agent to be dissolved or dispersed in acetone, spraying the formed solution or injectable suspension to lactose pills in a fluidized bed, and coating and drying to obtain the medicine-carrying pills. The cefuroxime axetil raw material is coated on the outer layers of the lactose pills and is uniformly distributed on the surfaces of the pills, the specific surface area of the medicine is greatly increased, the raw material can be quickly released, and thus, the dissolubility and bioavailability of the medicine are improved.
Description
Technical field
The invention belongs to the pharmaceutical preparations technology field, in particular to Ceruroxime axetil capsules of a kind of in vivo and in vitro Fast Stripping 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 Ceruroxime axetil capsules is cefuroxime, it is oral in gastrointestinal absorption enters body, under the 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, and is 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 Ceruroxime axetil capsules, 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 is take CEFUROXIME AXETIL as the effective active composition, take microcrystalline Cellulose as filler, both share carboxymethyl starch sodium, crospolyvinylpyrrolidone and are disintegrating agent, calcium carbonate is stabilizing agent, magnesium stearate is lubricant, white carbon is fluidizer, sodium lauryl sulphate is cosolvent, polyvinylpyrrolidone is binding agent, the 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, occurs easily simultaneously the risk that crude drug variable color and related substance increase in the wet-granulation process.CN101606914A discloses a kind of cefuroxime axetil tablets that is applicable to direct pressed powder, this tablet mainly is by increasing the flowability of adjuvant, reach the direct powder compression effect of said preparation, but the bulk density of the adjuvant that requires 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 the pharmacopeia.CN101703448A discloses a kind of direct compression technique of cefuroxime axetil tablets, cross 40 mesh sieves by CEFUROXIME AXETIL, stearic acid, microcrystalline Cellulose, cross-linking sodium carboxymethyl cellulose, silicon dioxide and sodium lauryl sulphate, then mixed 30 minutes in tempering tank, mixed powder forms with high speed rotating tablet machine direct compression.The dissolution of the cefuroxime axetil dispersible tablets of this technique preparation was lower than 65% in the time of 15 minutes.
At present, the dosage form on the market mostly is capsule, granule, the tablet of CEFUROXIME AXETIL.There is multiple crystal formation in CEFUROXIME AXETIL, and is medicinal amorphous, and loose, the poor fluidity of its quality must be granulated to it, could be packed into better capsule.Because CEFUROXIME AXETIL is to damp and hot sensitivity, crystal formation easily occurs change, so wet granulation not only can affect its stability, and larger on the dissolution impact.Although dry granulation can improve the stability of raw material in preparation, supplementary material is difficult to mix homogeneously, and the granule dissolution rate of making is lower.
In sum, by researching and developing a kind of material content homogeneous, Ceruroxime axetil capsules that stripping is fast, this seems particularly necessary.
Summary of the invention
In view of the deficiencies in the prior art, the object of the invention is to study by prescription and technique to dry granulation, a kind of material content homogeneous, Ceruroxime axetil capsules that stripping is fast and preparation method thereof are provided.
In order to realize purpose of the present invention, the inventor studies by lot of experiments, has finally obtained following technical scheme:
A kind of Ceruroxime axetil capsules forms by incapsulating shell behind the medicine carrying piller that contains CEFUROXIME AXETIL and the Pulvis Talci mixing; Described medicine carrying piller prepares as follows and gets: take by weighing CEFUROXIME AXETIL and disintegrating agent and be dissolved or dispersed in acetone, solution or the suspension that forms is sprayed to coating and the dry medicine carrying piller that gets on the lactose pellet in fluid bed.
Preferably, described Ceruroxime axetil capsules, wherein the weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.07-0.12:1-5.
Further preferably, described Ceruroxime axetil capsules, wherein the weight ratio of CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.08-0.10:1.5-2.
Described disintegrating agent is selected from following one or more: polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium.
A kind of preparation method according to above-mentioned Ceruroxime axetil capsules comprises following steps: CEFUROXIME AXETIL and disintegrating agent are dissolved or dispersed in acetone, solution or the suspension that forms is sprayed to coating and the dry medicine carrying piller that gets on the lactose pellet in fluid bed; Incapsulate shell after gained contained the medicine carrying piller of CEFUROXIME AXETIL and Pulvis Talci mixing, get Ceruroxime axetil capsules.
Preferably, the preparation method of described Ceruroxime axetil capsules is D80＜25 micron by the particle size in the described suspension of grinding control wherein.
Here said term " D80 " refers to that particle diameter in the described suspension accounts for 80% less than 25 microns granule.
Compared with prior art, the present invention is outer at lactose pellet with CEFUROXIME AXETIL raw material coating, and medicine is evenly distributed on the piller surface, has greatly improved the specific surface area of medicine, raw material can be discharged rapidly, thereby improve drug dissolution and bioavailability.Simultaneously, technique of the present invention has avoided heating and moisture on the impact of raw material stability, thereby guarantees the quality of product.Find that by experimental study the Ceruroxime axetil capsules of the present invention's preparation press official method detection dissolution, 8 minutes drug dissolutions greater than 95.0%, 15 minute drug dissolution greater than 99.5%.In addition, Ceruroxime axetil capsules agent producing process of the present invention is simple, shortens the production cycle, enhance productivity, and the energy-and time-economizing, thus can reduce the production cost of product, be fit to industrialized great production.
Description of drawings
Fig. 1 is the cumulative leaching rate curve chart of the Ceruroxime axetil capsules of embodiment 1 preparation.
Fig. 2 is the cumulative leaching rate curve chart of the Ceruroxime axetil capsules of embodiment 2 preparations.
Fig. 3 is the cumulative leaching rate curve chart of the Ceruroxime axetil capsules of embodiment 3 preparations.
Fig. 4 is the cumulative leaching rate curve chart of the Ceruroxime axetil capsules of comparative example's preparation.
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 that the scope of the above-mentioned theme of the present invention only limits to following embodiment, all technology that realizes 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, adds polyvinylpolypyrrolidone, stir, ball mill grinding, control suspension particle diameter D80＜25 microns, coating gets the medicine carrying piller on the lactose pellet being sprayed in fluid bed with the suspension that forms.
(2) with step (1) gained medicine carrying piller and Pulvis Talci mix homogeneously, incapsulate shell, namely get Ceruroxime axetil capsules.Get 6 of the Ceruroxime axetil capsules of this example preparation, put into respectively sedimentation indigo plant, take 0.07mol/L hydrochloric acid solution 900mL as dissolution medium, rotating speed 55r/min, in accordance with the law operation, the 5mL that takes a sample respectively 0,2,5,8,11, during 15min measures and calculates accumulation stripping percentage rate.Take time t as abscissa, average accumulated stripping percentage rate is the vertical coordinate mapping, the results are shown in Figure 1.Testing result shows that 8 minutes, 15 minutes the dissolution of Ceruroxime axetil capsules of this example preparation reaches 95.2%, 99.8%.
Preparation technology:
(1) CEFUROXIME AXETIL is dissolved in 1 liter of acetone, adds polyvinylpolypyrrolidone, stir, ball mill grinding, control suspension particle diameter D80＜25 microns, coating gets the medicine carrying piller on the lactose pellet being sprayed in fluid bed with the suspension that forms.
(2) with step (1) gained medicine carrying piller and Pulvis Talci mix homogeneously, incapsulate shell, namely get Ceruroxime axetil capsules.Head is got 6 of the Ceruroxime axetil capsules of this example preparation, put into respectively sedimentation indigo plant, take 0.07mol/L hydrochloric acid solution 900mL as dissolution medium, rotating speed 55r/min, in accordance with the law operation, the 5mL that takes a sample respectively 0,2,5,8,11, during 15min measures and calculates accumulation stripping percentage rate.Take time t as abscissa, average accumulated stripping percentage rate is the vertical coordinate mapping, the results are shown in Figure 2.Testing result shows that 8 minutes, 15 minutes the dissolution of Ceruroxime axetil capsules of this example preparation reaches 95.5%, 99.6%.
Preparation technology:
(1) CEFUROXIME AXETIL is dissolved in 1 liter of acetone, adds cross-linking sodium carboxymethyl cellulose, stir, ball mill grinding, control suspension particle diameter D80＜25 microns, coating gets the medicine carrying piller on the lactose pellet being sprayed in fluid bed with the suspension that forms.
(2) with step (1) gained medicine carrying piller and Pulvis Talci mix homogeneously, incapsulate shell, namely get Ceruroxime axetil capsules.Get 6 of the Ceruroxime axetil capsules of this example preparation, put into respectively sedimentation indigo plant, take 0.07mol/L hydrochloric acid solution 900mL as dissolution medium, rotating speed 55r/min, in accordance with the law operation, the 5mL that takes a sample respectively 0,2,5,8,11, during 15min measures and calculates accumulation stripping percentage rate.Take time t as abscissa, average accumulated stripping percentage rate is the vertical coordinate mapping, the results are shown in Figure 3.Testing result shows that 8 minutes, 15 minutes the dissolution of Ceruroxime axetil capsules of this example preparation reaches 96.1%, 99.9%.
The comparative example
Take the CEFUROXIME AXETIL specification as 125mg, the stock and adjunct of producing 1000 dispersible tablets consists of:
Preparation technology:
CEFUROXIME AXETIL is crossed 200 mesh sieves, and all the other adjuvants are crossed 80 mesh sieves, and mix homogeneously adopts roll-in method to carry out dry granulation, is packed into Capsules No. 2, and specification is 0.125 gram/grain.Get 6 of the Ceruroxime axetil capsules of this example preparation, put into respectively sedimentation indigo plant, take 0.07mol/L hydrochloric acid solution 900mL as dissolution medium, rotating speed 55r/min, in accordance with the law operation, the 5mL that takes a sample respectively 0,2,5,8,11, during 15min measures and calculates accumulation stripping percentage rate.Take time t as abscissa, average accumulated stripping percentage rate is the vertical coordinate mapping, the results are shown in Figure 4.Testing result shows that 8 minutes, 15 minutes the dissolution of Ceruroxime axetil capsules of this example preparation only is 76.8%, 91.0%.
Claims (5)
1. a Ceruroxime axetil capsules is characterized in that: form by incapsulating shell behind the medicine carrying piller that contains CEFUROXIME AXETIL and the Pulvis Talci mixing; Described medicine carrying piller prepares as follows and gets: take by weighing CEFUROXIME AXETIL and disintegrating agent and be dissolved or dispersed in acetone, solution or the suspension that forms is sprayed to coating and the dry medicine carrying piller that gets on the lactose pellet in fluid bed.
2. Ceruroxime axetil capsules according to claim 1, it is characterized in that: the weight ratio of described CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.07-0.12:1-5.
3. Ceruroxime axetil capsules according to claim 2, it is characterized in that: the weight ratio of described CEFUROXIME AXETIL, disintegrating agent and lactose pellet is 1:0.08-0.10:1.5-2.
4. each described Ceruroxime axetil capsules according to claim 1-3 is characterized in that: described disintegrating agent is selected from following one or more: polyvinylpolypyrrolidone, cross-linking sodium carboxymethyl cellulose, carboxymethyl starch sodium.
5. the preparation method of a Ceruroxime axetil capsules according to claim 1, it is characterized in that comprising following steps: CEFUROXIME AXETIL and disintegrating agent are dissolved or dispersed in acetone, solution or the suspension that forms is sprayed to coating and the dry medicine carrying piller that gets on the lactose pellet in fluid bed; Incapsulate shell after gained contained the medicine carrying piller of CEFUROXIME AXETIL and Pulvis Talci mixing, get Ceruroxime axetil capsules.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103349654A (en) * | 2013-07-05 | 2013-10-16 | 浙江瑞新药业股份有限公司 | Cefuroxime axetil pharmaceutical composition |
| CN105343011A (en) * | 2015-11-13 | 2016-02-24 | 青岛市海慈医疗集团 | Preparation method of cefuroxime axetil granules |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6569463B2 (en) * | 1999-11-23 | 2003-05-27 | Lipocine, Inc. | Solid carriers for improved delivery of hydrophobic active ingredients in pharmaceutical compositions |
-
2013
- 2013-01-19 CN CN2013100223734A patent/CN103040788A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6569463B2 (en) * | 1999-11-23 | 2003-05-27 | Lipocine, Inc. | Solid carriers for improved delivery of hydrophobic active ingredients in pharmaceutical compositions |
Non-Patent Citations (1)
| Title |
|---|
| 张树生等: "头孢呋辛酯胶囊的制备工艺", 《河北化工》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103349654A (en) * | 2013-07-05 | 2013-10-16 | 浙江瑞新药业股份有限公司 | Cefuroxime axetil pharmaceutical composition |
| CN103349654B (en) * | 2013-07-05 | 2014-12-03 | 浙江瑞新药业股份有限公司 | Cefuroxime axetil pharmaceutical composition |
| CN105343011A (en) * | 2015-11-13 | 2016-02-24 | 青岛市海慈医疗集团 | Preparation method of cefuroxime axetil granules |
| CN105343011B (en) * | 2015-11-13 | 2019-03-15 | 青岛市海慈医疗集团 | A kind of preparation method of cefuroxime axetil granule agent |
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Application publication date: 20130417 |