The 34th Annual Meeting of the Academy of
Pharmaceutical Sciences and Technologies, Japan (APSTJ) was held in Toyama,
Japan, May 16–18, 2019. In this meeting, a joint
symposium was held with the Pharmaceutical Society of Japan and APSTJ.
The theme of the symposium was “Recent Advances in Research on Particulate
Formulations such as Lipoproteins, Liposomes, Extracellular Vesicles, and iPS
Derived Cells.” The four invited speakers provide their review articles in the Current Topics of this
Interactions between drugs and
pharmaceutical additives can cause problems when mixing multiple drugs in
clinical settings. One example is aggregate formation between levoﬂoxacin
hydrate tablets and lansoprazole orally disintegrating tablets. Nakagawa et al
investigated the factors involved in this aggregation, focusing on the role of
pharmaceutical additives and electrostatic interaction. Levoﬂoxacin, which is
zwitterionic, formed aggregates with methacrylic acid copolymer LD, one of the pharmaceutical
additives of lansoprazole orally disintegrating tablet. Other zwitterionic
ingredients, including ampicillin, meropenem, cefepime, and cephalexin, also formed
aggregates with methacrylic acid copolymer LD.
Sesamin is a
major lignan in sesame seeds, and a
recent meta-analysis of controlled trials showed that sesamin consumption reduces blood pressure. The
antihypertensive effect of sesamin was suggested to
be caused by suppression of cytochrome P450 4F2 (CYP4F2)-mediated 20-hydroxyeicosatetraenoic
acid production. However, the detailed mechanism underlying inhibition
of CYP4F2 function by sesamin was
unclear. The article by Watanabe et al.
characterized the in vitro inhibitory effects of sesamin on human CYP4F2 activity. The results indicated
that sesamin is a
mechanism-based inactivator of CYP4F2.
5-Aminosalicylic acid (5-ASA) is used as
first line therapy for inflammatory bowel disease (IBD). However, a very high
5-ASA dose is required for IBD treatment because 5-ASA formula is relatively
low delivery efficacy to local inflamed colonic sites. In this report, Yuri et
al. focused on an intestinal H+-coupled oligopeptide transporter
1 (PEPT1) which is induced in the colon under IBD condition, and demonstrated
that the newly synthesized dipeptide-like 5-ASA derivatives, which are coupling
glycine, glutamic acid and valine to amino group of 5-ASA, were transportable
substrates for PEPT1.