Direct compression process for cefuroxime axetil dispersible tablets

Abstract

The invention relates to a direct compression process for cefuroxime axetil dispersible tablets, which is characterized in that: the following raw materials and auxiliary materials are sieved through a 40 mesh sieve and are mixed for thirty minutes in a mixing tank, and then the mixed powder materials are directly compressed by a high speed rotary tablet press to form the cefuroxime axetil dispersible tablets; and based on 125 grams of cefuroxime axetil, the raw materials and the auxiliary materials for producing 1000 dispersible tablets comprise 25 grams of cefuroxime axetil, 4 to 10 grams of stearic acid, 210 to 250 grams of microcrystalline cellulose, 28 to 35 grams of croscarmellose sodium, 2 to 4 grams of silicon dioxide and 2 to 4 grams of sodium dodecyl sulfate. The direct compression process for the cefuroxime axetil dispersible tablets improves the dissolution rate of the cefuroxime axetil dispersible tablets and improves the bioavailability and the healing effect of the medicament, wherein the dissolution rate reaches 99.5 percent at the time when the tablets dissolve for 45 minutes. The direct compression process simplifies the production process, shortens the production period and saves energy.

Description

technical field [0001] The invention relates to a production process of cefuroxime axetil dispersible tablets. Background technique [0002] Cefuroxime axetil (CXMA), as a second-generation cephalosporin, has broad-spectrum antibacterial properties and is active against both Gram-positive and Gram-negative bacteria. It is the prodrug of cefuroxime, and after oral administration, it is rapidly hydrolyzed by non-specific esterase in the mucosal cells of the gastrointestinal tract to release cefuroxime to exert its drug effect. CXM A is a lipophilic drug with poor water solubility, difficult to absorb, and low bioavailability. The dissolution rate is the limiting factor for drug absorption. After administration, the dissolution and absorption in the digestive tract are poor, resulting in reduced bioavailability and curative effect. [0003] Currently, cefuroxime axetil dispersible tablets mostly adopt the process of making wet granules. The raw materials of cefuroxime axetil ...

AI Technical Summary

Problems solved by technology

CXM A is lipophilic drug, poor water solubility, difficult to absorb, low bioavailability, dissolution rate is the limiting factor for drug absorption

After administration, the dissolution and absorption in the digestive tract are poor, resulting in reduced bioavailability and curative effect

[0003] Currently, cefuroxime axetil dispersible tablets mostly adopt the process of making wet granules. The raw materials of cefuroxime axetil and auxiliary materials are mixed to make granules. The octyl ester raw material, the raw material is further dissolved, so the dissolution time of the cefuroxime axetil dispersible tablet produced by wet granulation is long, resulting in a low dissolution rate within the specified time (45 minutes)

At the same time, wet granulation needs to add a binder to make granules, and the granules need to be dried, which consumes steam, and there is an additional process for granulation, resulting in waste of manpower and material resources

[0004] The existing production process of cefuroxime axetil dispersible tablets is wet granulation and tabletting, but the energy consumption and production cost of this process are high, and the dissolution rate is low. The quality standard requires that the dissolution rate is greater than 75% in 45 minutes. The actual wet granulation process The dissolution rate of cefuroxime axetil dispersible tablets produced is between 80% and 85% in 45 minutes