Cefuroxime axetil capsule and preparation method thereof

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 [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a cefuroxime axetil capsule which can dissolve 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 capsules 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.

There are many crystal forms of cefuroxime axetil, which is amorphous for pharmaceutical use. Its texture is loose and its fluidity is poor. It must be granulated to better fill it into capsules

Since cefuroxime axetil is sensitive to heat and humidity and is prone to crystal changes, wet granulation will not only affect its stability, but also greatly affect its dissolution rate

Although dry granulation can improve the stability of raw materials in the preparation, it is difficult to mix the raw and auxiliary materials evenly, and the dissolution rate of the prepared granules is low

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