CN102488668A

CN102488668A - Cefuroxime axetil dispersible tablet and its preparation method

Info

Publication number: CN102488668A
Application number: CN2011104496322A
Authority: CN
Inventors: 楚春锋; 王烜; 贾法强; 梁蓓
Original assignee: XINCAT PHARMACEUTICAL CO Ltd
Current assignee: XINCAT PHARMACEUTICAL CO Ltd
Priority date: 2011-12-29
Filing date: 2011-12-29
Publication date: 2012-06-13

Abstract

The invention belongs to the medicine preparation field, more specifically relates to a Cefuroxime axetil dispersible tablet and its preparation method, the dispersible tablet comprises the following raw materials: Cefuroxime axetil, magnesium stearate, microcrystalline cellulose PH-102, aspartame, cross linked sodium carboxymethyl cellulose, essence, silica and sodium dodecyl sulfate. The method comprises the following steps: passing the above raw materials through a sieve with 40 meshes, mixing the aspartame and microcrystalline cellulose PH-102 with equal weight for 5 minutes, then adding all the cross linked sodium carboxymethyl cellulose for mixing for 5 minutes, placing the mixed powder and residual raw materials in a mixed tank, mixing for 20 minutes, tabletting by a high speed rotary tablet machine to obtain the Cefuroxime axetil dispersible tablet. The dissolution rate of the prepared Cefuroxime axetil dispersible tablet can reach more than 90% after 15 minutes, 99.5% after 45 minutes, thereby the biological availability and curative effect of the medicines can be fully enhanced.

Description

Cefuroxime axetil dispersible tablets agent and preparation method thereof

Technical field

The invention belongs to field of medicine preparations, be specifically related to a kind of cefuroxime axetil dispersible tablets agent and preparation method thereof.

Background technology

(cefuroxime axetil CXMIA) as second generation cephalosporin, has broad spectrum antibacterial to CEFUROXIME AXETIL, and gram positive bacteria and gram-negative bacteria are all had activity.It is the prodrug of cefuroxime, is discharged cefuroxime and brings into play drug effect by the nonspecific esterase hydrolysis in the gastrointestinal tract mucosa cell rapidly after oral.CEFUROXIME AXETIL is a lipophilic drugs, and poorly water-soluble is difficult to absorb, and bioavailability is low, and rate of dissolution is the limiting factor of drug absorption.After the administration, in digestive tract the dissolving and absorb relatively poor, cause bioavailability and curative effect the reduction.

CEFUROXIME AXETIL is processed dispersible tablet can effectively improve its dissolution, thereby improve bioavailability and curative effect.

Comparatively loose because of the CEFUROXIME AXETIL raw material, be unfavorable for direct powder compression, adopt wet method to process granule more, and then the production technology of tabletting.But wet granulation technology exists, and production efficiency is low, the energy consumes high shortcoming, and through wet granulation, dissolution is still on the low side.In addition, the CEFUROXIME AXETIL bitterness is bigger, is unfavorable for that the patient takes.

Summary of the invention

The purpose of this invention is to provide a kind of cefuroxime axetil dispersible tablets agent and preparation method thereof, can solve the bitterness defective of tablet, and a kind of rational and effective production technology is provided, solve the low problem of dissolution.

Cefuroxime axetil dispersible tablets agent of the present invention, process by the raw material of following parts by weight:

250 parts of CEFUROXIME AXETILs;

4～10 parts of magnesium stearate;

250～350 parts of microcrystalline Cellulose PH-102;

15～25 parts of aspartames;

28～56 parts of cross-linking sodium carboxymethyl celluloses;

10～50 parts in essence;

5～20 parts of silicon dioxide;

2～10 parts of sodium lauryl sulphates.

To produce 1000, specification is that the cefuroxime axetil dispersible tablets agent of 250mg is an example:

CEFUROXIME AXETIL 250g;

Magnesium stearate 4～10g;

Microcrystalline Cellulose PH-102 250～350g;

Aspartame 15～25g;

Cross-linking sodium carboxymethyl cellulose 28～56g;

Essence 10～50g;

Silicon dioxide 5～20g;

Sodium lauryl sulphate 2～10g.

In the above-mentioned prescription, cross-linking sodium carboxymethyl cellulose is a disintegrating agent, and microcrystalline Cellulose PH-102 is a filler, and silicon dioxide is fluidizer, and sodium lauryl sulphate is solubilizing agent, and magnesium stearate is a lubricant, and aspartame and essence are correctives.

Wherein, described silicon dioxide is preferably used micropowder silica gel.

The method for preparing of cefuroxime axetil dispersible tablets agent of the present invention; Be that above-mentioned raw materials is crossed 40 mesh sieves, aspartame was mixed 5 minutes with the microcrystalline Cellulose PH-102 of equivalent weight, add whole cross-linking sodium carboxymethyl celluloses then and mixed 5 minutes; Mixed powder and surplus stock are rendered in the tempering tank; Mixed 20 minutes, and used high speed rotating tablet machine tabletting at last, promptly obtain the cefuroxime axetil dispersible tablets agent.

The invention has the advantages that: adopt suitable correctives, covered the bitterness of medicine, help the patient and take, adopt direct compression technology, improved production efficiency, reduced energy consumption.The dissolution of the cefuroxime axetil dispersible tablets that the present invention produces reached more than 90% in the time of 15 minutes, reached more than 99.5% in the time of 45 minutes, had fully improved the bioavailability and the curative effect of this medicine.

The specific embodiment

Below in conjunction with embodiment the present invention is further specified.

Embodiment 1:

CEFUROXIME AXETIL 250g;

Magnesium stearate 4g;

Microcrystalline Cellulose PH-102 250g;

Aspartame 15g;

Cross-linking sodium carboxymethyl cellulose 28g;

Essence 10g;

Silicon dioxide 5g;

Sodium lauryl sulphate 2g.

Method for preparing:

Above-mentioned raw materials is crossed 40 mesh sieves; Aspartame was mixed 5 minutes with the microcrystalline Cellulose PH-102 of equivalent weight; Add whole cross-linking sodium carboxymethyl celluloses then and mixed 5 minutes, mixed powder and surplus stock are rendered in the tempering tank, mix 20 minutes; Use high speed rotating tablet machine tabletting at last, promptly obtain the cefuroxime axetil dispersible tablets agent.

6 dissolutions to dispersible tablet of picked at random are tested:

Time

1

2

3

4

5

6

On average

15min

92.5％

93.2％

91.8％

92.2％

93.1％

92.6％

92.57％

45min

99.6％

99.4％

99.9％

100.1％

99.8％

100.2％

99.83％

Embodiment 2:

CEFUROXIME AXETIL 250g;

Magnesium stearate 10g;

Microcrystalline Cellulose PH-102 350g;

Aspartame 25g;

Cross-linking sodium carboxymethyl cellulose 56g;

Essence 50g;

Silicon dioxide 20g;

Sodium lauryl sulphate 10g.

Method for preparing:

6 dissolutions to dispersible tablet of picked at random are tested:

Time

1

2

3

4

5

6

On average

15min

92.9％

93.1％

92.8％

92.6％

93.3％

92.9％

92.93％

45min

99.4％

99.9％

99.1％

100.4％

99.3％

100.5％

99.76％

Claims

1. cefuroxime axetil dispersible tablets agent is characterized in that being processed by the raw material of following parts by weight:

250 parts of CEFUROXIME AXETILs;

4～10 parts of magnesium stearate;

250～350 parts of microcrystalline Cellulose PH-102;

15～25 parts of aspartames;

28～56 parts of cross-linking sodium carboxymethyl celluloses;

10～50 parts in essence;

5～20 parts of silicon dioxide;

2～10 parts of sodium lauryl sulphates.

2. the method for preparing of the described cefuroxime axetil dispersible tablets agent of claim 1; It is characterized in that above-mentioned raw materials crosses 40 mesh sieves, aspartame was mixed 5 minutes with the microcrystalline Cellulose PH-102 of equivalent weight, add whole cross-linking sodium carboxymethyl celluloses then and mixed 5 minutes; Mixed powder and surplus stock are rendered in the tempering tank; Mixed 20 minutes, and used high speed rotating tablet machine tabletting at last, promptly obtain the cefuroxime axetil dispersible tablets agent.