Cefuroxime axetil tablets and preparation method thereof

Abstract

The invention discloses a cefuroxime axetil tablets, which are prepared by mixing and directly tableting medicine-carrying pellets containing cefuroxime axetil, a filling agent and a lubricating agent, wherein the medicine-carrying pellets are prepared by the following steps of: weighing cefuroxime axetil and a disintegrating agent, dissolving or dispersing the cefuroxime axetil and the disintegrating agent into acetone to form a solution or suspension, spraying the solution or suspension into lactose pellets for coating in a fluidized bed, and drying to obtain the medicine-carrying pellets. According to the invention, the cefuroxime axetil raw material is coated on the outer layers of the lactose pellets, so that the medicine, namely the cefuroxime axetil can be uniformly distributed on the surfaces of the pellets, the specific surface area of the medicine is greatly increased, the raw cefuroxime axetil raw material can be rapidly released, and therefore the medicine dissolubility and the bioavailability are improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a cefuroxime axetil tablet capable of dissolving rapidly in vivo and in vitro and a preparation method thereof. Background technique [0002] Cefuroxime axetil is a semi-synthetic second-generation cephalosporin with a broad antibacterial spectrum and strong antibacterial activity against Gram-positive and Gram-negative bacteria. The active ingredient of cefuroxime axetil tablet is cefuroxime, which is absorbed into the body through the gastrointestinal tract when taken orally, and is rapidly hydrolyzed into cefuroxime under the action of esterase. By combining with one or more penicillin-binding proteins (PBPs), Inhibits the cell wall synthesis of bacterial dividing cells, thereby exerting an antibacterial effect. Cefuroxime axetil is a lipophilic drug, unstable in wet and hot environments, and bitter in taste, poor in water solubility, difficult ...

AI Technical Summary

Problems solved by technology

This technology uses a lot of disintegrants and surfactants, and the production cost is high. At the same time, the risk of discoloration of raw materials and increase of related substances is prone to occur during the wet granulation process.

CN101606914A discloses a cefuroxime axetil tablet suitable for direct powder compression. The tablet mainly achieves the powder direct compression effect of the preparation by increasing the fluidity of the auxiliary materials, but the bulk density of the required auxiliary materials is large and the flow rate is high. Good performance, the bulk density of the disintegrant is greater than 0.35g / cm 3 , the bulk density of the filler is greater than 0.38g / cm 3 , the requirements for excipients are too high, which increases the cost of excipients. At the same time, this product needs to be dispersed within 10 minutes, which fails to meet the requirements of tablets in the Pharmacopoeia.

In actual production, some drugs with unstable chemical properties are often encountered, such as easily hydrolyzed esters and amides, easily oxidized phenolic hydroxyl drugs, vitamin C, etc. In the method, hydrolysis reaction often occurs, or the particles are destroyed by heat during the drying process, or the drug is decomposed by light due to the complicated process.

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