Frazier W F, Nuessle N O
J Pharm Sci. 1976 Dec;65(12):1823-6. doi: 10.1002/jps.2600651231.
A rotating-basket apparatus for dissolution testing of veterinary bolus tablets was designed and constructed. Sulfamethazine boluses containing different disintegrating agents were evaluated in vitro and by blood level data following administration to cattle. The dissolution t50 and various pharmacokinetic parameters showed directly compressible starch and carboxymethylstarch to be the most effective disintegrants in the concentrations employed while magnesium aluminum silicate and microcrystalline cellulose were about equal but less effective than the previous disintegrants. A bolus formulation containing no disintegrant gave even less satisfactory results. A correlation was established between the dissolution t50 and the time to peak plasma level and also between the t50 and the area under the plasma-time curve for the first 36 hr.
设计并制造了一种用于兽用大丸剂片剂溶出度测试的转篮装置。对含有不同崩解剂的磺胺二甲嘧啶大丸剂进行了体外评估,并通过给牛给药后的血药浓度数据进行评估。溶出t50和各种药代动力学参数表明,在所使用的浓度下,直接压片用淀粉和羧甲基淀粉是最有效的崩解剂,而硅酸镁铝和微晶纤维素效果相当,但不如前两种崩解剂有效。不含崩解剂的大丸剂配方效果更不理想。建立了溶出t50与血浆峰浓度时间之间的相关性,以及t50与给药后36小时血浆-时间曲线下面积之间的相关性。