Naoto Suzuki

Nihon University | Nichidai · Laboratory of Pharmaceutics

Neuroinflammation is a fundamental feature in the pathogenesis of amyotrophic lateral sclerosis (ALS) and arises from the activation of astrocytes and microglial cells. Previously, we reported that Miyako Bidens pilosa extract (MBP) inhibited microglial activation and prolonged the life span in a human ALS-linked mutant superoxide dismutase-1 (SOD1...

1H-14N internuclear distances are readily and accurately measured using the symmetry-based phase-modulated resonance-echo saturation-pulse double-resonance (PM-S-RESPDOR) method in rigid solids. The fraction curve, (S0 - S')/S0, is represented by a single variable of a 1H-14N heteronuclear dipolar coupling, where S0 and S' are the PM-S-RESPDOR sign...

Cocrystallization is a crystallization technique for drugs that are difficult to crystallize as single components. In this study, we found a novel cocrystal hydrate consisting of captopril (CPL), which is an amino acid-derived drug and has a thiol group, and l-proline (LPR), although a CPL-LPR cocrystal anhydrate has been previously reported. Nano-...

The purpose of this study was to enhance the delivery of Etodolac (ETD) to the brain through intranasal administration using an ionic liquid (IL) consisting of ETD and proline ethyl ester. The IL of ETD was prepared by mixing ETD with proline ethyl ester as a counterion in a molar ratio of 1:2.The formation of the IL was confirmed by differential s...

Clobetasol propionate ointment (CLPO) formulations have been classified as members of the "strongest" steroidal efficacy group, with eight of these formulations currently marketed in Japan. Evaluations of pharmaceutical properties of each formulation revealed three classification types: droplet dispersion type containing propylene glycol (PG) and s...

The aim of this study was to evaluate the effect of three coformers and five disintegrants in the granulation formulation on the dissociation of cocrystal during the granulation process by monitoring wet granulation with probe-type low-frequency Raman (LF-Raman) spectroscopy. As model cocrystals, paracetamol (APAP)-oxalic acid (OXA), APAP-maleic ac...

This study aimed to determine the effect of intranasal dosing speed and administrating volume of nose-to-brain delivery on candidates for peptide drugs (molecular weight ca. 1–10 kDa). Using inulin as the model molecule of a peptide drug, intranasal administration by cannulation from the airway side through the esophagus was tested in mice. This wa...

The purpose of the present study was to establish a novel method to evaluate water penetration rates by combining the local dynamic contact angle and thermographic approach to characterize water conduction properties in orally disintegrating (OD) tablets. The OD tablet tester OD-mate was used to measure the disintegration times of OD tablets. Other...

Recently, nasal administration has attracted attention as the administration method which could delivery various modalities to not only local and systemic circulation but also the central nervous system bypassing the blood-brainbarrier. However, there are also the biological barrier in the nasal cavity against the exgenous substances like other muc...

The blood-brain barrier (BBB) is limited to deliver drugs to the brain after systemic administration. Intranasal route offers several advantages over the oral and parenteral route and has shown potential for targeting drugs to the brain for treatment of various central nervous system (CNS) disor ders. Drug delivery via the intranasal route bypasses...

Recently, nasal administration has attracted attention as the administration method which could delivery various modalities to not only local and systemic circulation but also the central nervous system bypassing the blood-brainbarrier. However, there are also the biological barrier in the nasal cavity against the exgenous substances like other muc...

In this study, we coground physical mixtures of paracetamol (APAP), a neutral active pharmaceutical ingredient (API), and sulfonic acids, namely, 1,2-ethanedisulfonic acid dehydrate (EDSA), p-toluenesulfonic acid hydrate (TOSA) and 2-naphthalenesulfonic acid monohydrate (NASA), to prepare crystalline complexes. As a result of cogrinding, we identif...

We demonstrated the difference in the distribution state of pharmaceutical ingredients between tacrolimus (TCR) original ointment and six kinds of generic medicines. Two-dimensional imaging and depth analysis using attenuated total reflection Fourier transform infrared (ATR FT-IR) spectroscopy and confocal Raman microscopy were used, in addition to...

To clarify the volume of water required to paste pediatric powders, we herein established a standard for the powder paste state by measuring yield values when water was added to powders. The powders used in the present study were selected from 8 types including original and generic drugs. Tipepidine hibenzate is prescribed in the pediatric field in...

Intranasal administration has been reported to be a potential pathway for nose-to-brain delivery of therapeutic agents that circumvents the blood-brain barrier. However, there have been few reports regarding not only the quantitative analysis but also optimal administration conditions and dosing regimens for investigations of nose-to-brain delivery...

The molecular states of ketoprofen and the interaction between ketoprofen and other pharmaceutical excipients in the matrix layer were examined to determine their effect on the pharmaceutical properties of original and generic ketoprofen dermal patches (generic patches A and B). Molecular states of ketoprofen were evaluated using polarized light mi...

Betamethasone butyrate propionate ointment (BBPO) is mainly used for adult patients in dermatology and is often prescribed as a mixture containing a base or moisturizing cream for various reasons. However, in the case of a moisturizing cream, since this formulation is composed of various ingredients, a physical change is expected to occur by mixing...

Objective: The aim of this study is to evaluated evaluated the relative stability of pharmaceutical cocrystals consisting of paracetamol (APAP) and oxalic acid (OXA) or maleic acid (MLA). Significance: These observations of cocrystal stability under various conditions are useful coformer criteria when cocrystals are selected as the API in drug deve...

The blood-to-brain transport of amantadine, a weak N-methyl-D-aspartate (NMDA) antagonist, has been previously shown to participate in the cationic drug-sensitive transport system across the mouse blood-brain barrier (BBB). The purpose of the present study was to characterize the influx transport system by means of both an in situ mouse brain perfu...

Drug nanoparticles were prepared by cogrinding three components: a drug, a methacrylic copolymer, and sucrose fatty acid ester (SE). A high nanoparticle yield was obtained when cholesterol-lowering probucol (PBC), a poorly water–soluble drug, was used in the cogrinding process with D-1811, an SE with stearic acid as the fatty acid and the hydrophil...

High cholesterol levels (or hypercholesterolemia) are linked with many diseases, particularly with the risk of coronary heart diseases. Probucol is commonly used to reduce cholesterol in blood. While the effectiveness of this drug highly depends on its solubility, unfortunately, it is nearly insoluble (solubility is 5 ng/mL in water). Therefore, it...