Bijanzadeh M, Mahmoudian M, Salehian P, Khazainia T, Eshghi L, Khosravy A
Pharmaceutical Research Center, Tehran, Iran.
Indian J Physiol Pharmacol. 1990 Jul;34(3):157-61.
Tablets of either microsized or ultramicrosized griseofulvin (2 x 125 mg), were administered to 6 healthy volunteers of either sex just before a breakfast containing 4o g. of butter. The plasma concentration of griseofulvin were determined 1, 3, 5, 7, 9, 24, and 32 h. after dosing using a spectrofluorometric method, and pharmacokinetic parameters (Cp max, t max, AUC 0 - greater than 32) were calculated. These parameters were found to be; Cp max = 0.0.681 +/- 0.1 mu/ml, t max. = 2.51 +/- 0.33 h. and AUC = 14.14 +/- 2.33 micrograms h/ml for microsized tablets and Cp max = 0.80 +/- 0.08 +/- g/ml, t max = 2.44 +/- 0.54 and AUC = 16.25 +/- 1.16 microgram h/ml for ultramicrosized tablets. Our results show that mean peak plasma level and AUC (0 - greater than 32) are only slightly higher for the ultramicrosized preparation and the time to peak plasma level is similar in two preparations. Therefore, it is concluded that coadministration of griseofulvin with food will tend to reduce the difference between the bioavailability of the two type of preparations.
在6名健康志愿者(男女不限)早餐前给予含40克黄油的早餐,同时给予微粒型或超微粒型灰黄霉素片(2×125毫克)。给药后1、3、5、7、9、24和32小时,采用荧光分光光度法测定血浆中灰黄霉素浓度,并计算药代动力学参数(Cmax、tmax、AUC0-大于32)。这些参数分别为:微粒型片剂的Cmax=0.681±0.1微克/毫升,tmax=2.51±0.33小时,AUC=14.14±2.33微克·小时/毫升;超微粒型片剂的Cmax=0.80±0.08微克/毫升,tmax=2.44±0.54小时,AUC=16.25±1.16微克·小时/毫升。我们的结果表明,超微粒型制剂的平均血浆峰值水平和AUC(0-大于32)仅略高,且两种制剂达到血浆峰值水平的时间相似。因此,可以得出结论,灰黄霉素与食物同时给药往往会减少两种制剂生物利用度之间的差异。