Pharmaceutical production of tableting granules in an ultra-small-scale high-shear granulator as a pre-formulation study.

OBJECTIVE: 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. METHOD: 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. RESULTS: 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. CONCLUSION: Characteristics of all of the granules indicated that the USG method could produce higher quality granules within a shorter time than the HM methods.

Synthesis and spectroscopic properties of a series of beta-blocked long oligothiophenes up to the 96-mer: revaluation of effective conjugation length.

A series of extraordinarily long oligothiophenes up to the 96-mer has been developed by iterative oxidative coupling of the completely beta-blocked sexithiophene. They are highly conjugated like nonsubstituted oligothiophenes, and the effective conjugation of this system is extended to 96 thiophene units and much longer than that previously speculated for polythiophenes.