Gafiţanu E, Dumistrăcel I, Antochi S
Universitatea de Medicină şi Farmacie Iaşi.
Rev Med Chir Soc Med Nat Iasi. 1991 Jan-Jun;95(1-2):127-8.
The present work reports some facts about the preparation and release characteristics of the tablets of propiphenazone made by lyophilizing method (lyoc); they are compared with the classic tablets obtained by simple compression. Our substance, the propiphenazone, is a stable one, but we can talk about its poor solubility. Therefore, in order to obtain the lyoc tablets, we chose the method of paste. This tablets had a spongy aspect, with a desaggregation time of 1-2 min.; the latter (classic tablets) were regularly and the desaggregation time in about 9 min. The kinetics of propiphenazone absorbtion would be expected to differ in these structurally-distinct tablets types. Indeed, the concentration was really appreciable for the lyoc tablets after 30 min., with the peak at 60 min.; for the classic tablets the peak was remarkably only after 90 min. The relative bioavailability for these two types of tablets pointed out the differences, confirming the evident advantages for using the lyoc tablets in analgesic, antipyretic therapy.
本研究报告了关于通过冻干法（lyoc）制备的异丙安替比林片的一些制备及释放特性的事实；并将其与通过简单压制获得的传统片剂进行了比较。我们的物质，即异丙安替比林，是一种稳定的物质，但我们可以说它的溶解性较差。因此，为了获得冻干片，我们选择了制糊法。这种片剂呈海绵状，崩解时间为1 - 2分钟；后者（传统片剂）质地规整，崩解时间约为9分钟。预计在这些结构不同的片剂类型中，异丙安替比林的吸收动力学将有所不同。实际上，冻干片在30分钟后的浓度确实相当可观，在60分钟时达到峰值；而传统片剂的峰值明显仅在90分钟后出现。这两种片剂的相对生物利用度指出了差异，证实了在止痛、退热治疗中使用冻干片的明显优势。
