Views:0 Author:Site Editor Publish Time: 2021-05-24 Origin:Site
Sulfamidine belongs to the sulfa class of antibacterial drugs. It is a white or slightly yellow crystalline powder, odorless, and slightly bitter in taste. Slightly soluble in water, slightly soluble in ethanol, soluble in boiling water, acetone, methanol and dilute inorganic acids.
Sulfamidine is one of the earlier antibacterial drugs used for intestinal infections. It can treat various bacillary dysentery and enteritis. It can also be used to prevent bacterial infections before intestinal surgery. At the same time, sulfamir is still the first choice for the treatment of leprosy. It is suitable for the treatment of various types of leprosy and can improve clinical symptoms. For general mucosal lesions, it improves faster, skin lesions improve more slowly, and neuropathy is slower. Therefore, the treatment course is long, easy to produce drug resistance, and difficult to cure. In addition, it can also be used to treat herpetiform dermatitis, lupus erythematosus, psoriasis, Podiatry and malaria, etc.
The inclusion compound formed by the inclusion of the drug sulfamidine and the sulfobutyl beta cyclodextrin sodium with different degrees of substitution, and the powder injection preparation formed by the corresponding inclusion compound, the powder injection preparation comprising the sulfa gland and different substituted sulfonidines -Β-cyclodextrin and pharmaceutical excipients. The invention improves the water solubility of sulfamidine, and realizes the expansion goal of preparing corresponding aqueous solution formulations and powder injection formulations of sulfamidine.
Sulfobutyl-β-cyclodextrin sodium is also known as sulfobutyl ether beta cyclodextrin sodium salt, sulfobutyl ether beta cyclodextrin sodium salt is the sulfonated modified sodium salt of beta cyclodextrin, and The name thiobutyl ether beta cyclodextrin sodium is an anionic, highly water-soluble cyclodextrin derivative, which can be well included with drug molecules to form non-covalent complexes, thereby improving the stability and water solubility of the drug , Safety, reduce nephrotoxicity, ease drug hemolysis, control drug release rate, mask bad odor, etc.
Accurately weigh 0.2 mol of sulfamidine raw material and dissolve it with boiling water solvent to obtain a standby solution; weigh 0.1 mol of sulfobutyl beta cyclodextrin sodium with a degree of substitution of 1 according to the inclusion molar ratio, and dissolve it with distilled water. Slowly add the aqueous solution containing the drug to the above-mentioned standby liquid, dilute with distilling water to a constant volume of 200ml; adjust the ultrasonic frequency to 25KHz, the temperature to 60℃, ultrasonically wrap the above-mentioned mixture for 45 minutes, and then cool it to -28℃ Freeze in the refrigerator for 48 hours, freeze-dry in a freeze dryer, to obtain a fluffy light yellow solid, that is, a sulfamidine-sulfobutyl beta cyclodextrin sodium inclusion compound with a molar ratio of 2:1.