Graduate School of Industrial Technology, Nihon University, Narashino, Japan.
Drug Dev Ind Pharm. 2012 Nov;38(11):1390-3. doi: 10.3109/03639045.2011.652637. Epub 2012 Feb 22.
In some of drug developments, the amount of bulk drug powder to use in early stages is limited and it is not easy to supply a sufficient drug amount for conventional preparation methods. Therefore, an ultra-small-scale high-shear granulator (less than 5 g) (USG) was developed and applied to small-scale granulation as a pre-formulation.
The sample powder consisted of 66.5% lactose, 28.5% microcrystalline cellulose and 5.0% hydroxypropylcellulose. The granules were obtained to agitate 5 g of the sample powder with 1.0 mL of water at 300 rpm for 5 min after pre-powder mixing for 3 min by the USG and the manual hand (HM) methods.
The granules were evaluated by the 10% and 90% accumulated particle size and the recoveries of the granules and the powder solid. Median particle size for the USG and the HM methods was 159.2 ± 2.3 and 270.9 ± 14.9 µm, respectively. The USG method had a narrower particle size distribution than those by the HM method. The recovery of the granules by USG was significantly larger than that by the HM method.
Characteristics of all of the granules indicated that the USG method could produce higher quality granules within a shorter time than the HM methods.
在某些药物开发中，用于早期阶段的散装药物粉末的量是有限的，并且不容易提供用于常规制备方法的足够药物量。因此，开发了一种超小型高剪切制粒机（小于 5 克）（USG），并将其作为预配方应用于小规模制粒。
样品粉末由 66.5%乳糖、28.5%微晶纤维素和 5.0%羟丙基纤维素组成。通过 USG 和手动手（HM）方法，在预粉混合 3 分钟后，将 5 g 样品粉末用 1.0 mL 水在 300 rpm 下搅拌 5 分钟，获得颗粒。
通过 10%和 90%累积粒径以及颗粒和粉末固体的回收率对颗粒进行评估。USG 和 HM 方法的中值粒径分别为 159.2 ± 2.3 µm 和 270.9 ± 14.9 µm。USG 方法的粒径分布比 HM 方法更窄。USG 法得到的颗粒回收率明显大于 HM 法。
所有颗粒的特性表明，与 HM 方法相比，USG 方法可以在更短的时间内生产出更高质量的颗粒。
