Compound sulfamonomethoxine sodium multivesicular liposome and preparation method thereof

Abstract

The invention discloses a compound sulfamonomethoxine sodium multivesicular liposome and a preparation method thereof. The compound sulfamonomethoxine sodium multivesicular liposome is prepared from lipid, sulfamonomethoxine sodium as a hydrophilic medicament and trimethoprim as a lipophilic medicament, wherein the sulfamonomethoxine sodium and the trimethoprim are simultaneously packaged in the multivesicular liposome structure formed from soya bean lecithin, cholesterol and triacylglycerol; when the multivesicular liposome is synthesized, the addition ratio of the total mass of the sulfamonomethoxine sodium and the trimethoprim to the total mass of lipid is preferably 1:4; the added mass ratio of the sulfamonomethoxine sodium to the triacylglycerol is preferably 4:1; the added mass ratio of the soya bean lecithin to the cholesterol is prefertably 1:1; and the use level of the triacylglycerol is preferably 16 / mmol*L-1. During preparation, the ratio of the first emulsification time to the second emulsification time is preferably 4:1 (12 min:3 min). In the liposome, two medicaments with different dissolving characteristics of water solubility and lipid solubility are mixed together to be applied to the same multivesicular liposome; and the multivesicular liposome has the advantages of long slow releasing time, high packaging rate, good stability, can be used as a new preparation of veterinary medicine and lays foundations for clinical generalization and application.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, and in particular relates to compound sulfamethoxine sodium multivesicular liposome and a preparation method thereof. Background technique [0002] Sulfonamides are a class of synthetic antimicrobials that have played a huge role in controlling bacterial infections since their discovery in 1935. It has the advantages of wide antibacterial spectrum, stable property, convenient long-term storage and low price. Such as: sodium sulfamethoxine, N-(6-methoxy-4-pyrimidinyl)-4-aminobenzenesulfonamide sodium salt monohydrate. The acetylation rate in the body is low, so it has strong antibacterial effect in the body and less damage to the urinary tract, especially the kidney; after oral administration, it is well absorbed and has a high blood concentration, but the effective concentration maintains for a short time (5.8 hours for pigs, and 5.8 hours for goats). 7 hours, Hu sheep 2 hours); it has good cu...

AI Technical Summary

Problems solved by technology

One of the main features of multivesicular liposomes is that the sustained release time is significantly longer than that of ordinary liposomes. If the hydrophilic drug sulfamethoxine sodium and the lipophilic drug trimethoprim can be encapsulated in the same multivesicular liposome , will play a good pharmacological role; there is no research report in this area

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