Abstract：
During recent years there have been shortages of certain drugs due to problems in raw material supply. These are often related to active ingredients but could also affect excipients. Lactose is one of the most used excipients in tableting and comes in two anomeric and several solid-state forms. The aim of this study was to utilize lactose from a dairy side-stream and compare it against a commercial reference in direct compression. This would be a sustainable option and would secure domestic availability during crises. Two types of lactose, spray-dried and freeze-dried, were evaluated. Lactose was mixed with microcrystalline cellulose in different ratios together with lubricant and glidant, and flowability and tabletability of the formulations was characterized. The fully amorphous and small particle-sized spray-dried lactose flowed inadequately but exhibited good tabletability. The larger particle-sized, freeze-dried lactose exhibited sufficient flow and better tabletability than the commercial reference. However, disintegration and drug release were slower when using the investigational lactose formulations. This was most likely due to remaining milk proteins, especially caseins, in the lactose. Overall, the investigational lactose provides promise for the use of such a side-stream product during crisis situations but enhancing their properties and/or purity would be needed.
摘要：
近年来，由于原料供应问题，某些药物短缺。这些通常与活性成分有关，但也可能影响赋形剂。乳糖是压片中最常用的赋形剂之一，有两种异头和几种固态形式。这项研究的目的是利用来自乳制品侧流的乳糖，并将其与直接压缩中的商业参考进行比较。这将是一个可持续的选择，并将在危机期间确保国内供应。两种乳糖,喷雾干燥和冷冻干燥，进行了评估。乳糖与微晶纤维素以不同比例混合，润滑剂和助流剂，并对制剂的流动性和压片性进行了表征。完全无定形和小颗粒大小的喷雾干燥乳糖流动不充分,但表现出良好的压片性。较大的颗粒大小，冷冻干燥的乳糖表现出足够的流动性和比商业参考更好的可压性。然而,使用研究性乳糖制剂时，崩解和药物释放较慢。这很可能是由于残留的牛奶蛋白质，尤其是酪蛋白,在乳糖中。总的来说,研究乳糖为在危机情况下使用这种侧流产品提供了希望，但需要提高其性质和/或纯度。
