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Dissolution Profiles of Oral Disintegrating Tablet with Taste Masking Granule Polymer Coating in Biorelevant Bicarbonate Buffer
Chem Pharm Bull (Tokyo). 2024;72(3):298-302. doi: 10.1248/cpb.c23-00783.ABSTRACTThe current study aimed to explore the impact of buffer species on the dissolution behavior of orally disintegrating tablets (ODT) containing a basic polymer and its influence on bioequivalence (BE) prediction. Fexofenadine hydrochloride ODT formulations were used as the model formulations, Allegra® as the reference formulation, and generic formulations A and B as the test formulations. Allegra®, generic A, and generic B are ODT formulations that contain aminoalkyl methacrylate copolymers E (Eudragit® E, EUD-E), a basic polymer commonly used...
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Masaki Higashino Kiyohiko Sugano Source Type: research

Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor
Chem Pharm Bull (Tokyo). 2024;72(3):309-310. doi: 10.1248/cpb.c23-00879.ABSTRACTThe inhibition mode of a retro-inverso (RI) inhibitor containing a hydroxyethylamine dipeptide isostere against the human T-cell leukemia virus type-1 (HTLV-1) protease was examined. Enzymatic evaluation of the RI-modified inhibitor containing a D-allo-Ile residue revealed that HTLV-1 was competitively inhibited. IC50 values of the RI-modified inhibitor and pepstatin A, a standard inhibitor of aspartic proteases, were nearly equivalent.PMID:38479891 | DOI:10.1248/cpb.c23-00879 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Chiyuki Awahara Daiki Oku Kazuya Kobayashi Yasunao Hattori Source Type: research

Organocatalyzed Amine-Free O-Phosphorylation of Alcohols with 4-Methylpyridine N-Oxide
Chem Pharm Bull (Tokyo). 2024;72(3):303-308. doi: 10.1248/cpb.c24-00029.ABSTRACTAmine-free phosphorylation of various alcohols was developed with 4-methylpyridine N-oxide in the presence of 4 Å molecular sieves at room temperature. This mild method gave various phosphorylated products in high yield and could be applied to acid- or base-sensitive substrates. Furthermore, this method was also effective for the chemoselective phosphorylation of diols or polyols.PMID:38479853 | DOI:10.1248/cpb.c24-00029 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - March 13, 2024 Category: Drugs & Pharmacology Authors: Keisuke Yoshida Wataru Hirano Ryuuki Ota Shinji Kitagaki Source Type: research

Synthesis of a Cyclic Hexaamide Consisting of a Brominated m-Phenylene Repeating Unit
Chem Pharm Bull (Tokyo). 2024;72(3):294-297. doi: 10.1248/cpb.c24-00023.ABSTRACTAiming to synthesize a cyclic hexaamide, 4-bromo-3-(isobutylamino)benzoic acid was subjected to self-condensation reactions in the presence of either dichlorotriphenylphosphorane in 1,1,2,2-tetrachloroethane or tetrachlorosilane in pyridine. However, instead of the targeted cyclic hexaamide, the cyclic triamide and the cyclic tetraamide were obtained. The cyclic hexaamide was successfully synthesized via the self-condensation of the dimer, which was synthesized in five steps from 4-bromo-3-(isobutylamino)benzoic acid. A thorough screening of th...
Source: Chemical and Pharmaceutical Bulletin - March 10, 2024 Category: Drugs & Pharmacology Authors: Akihiro Yokoyama Ayaka Chino Kenta Rakumitsu Source Type: research

Effect of Concomitant Drugs on Sodium Zirconium Cyclosilicate Hydrate in Artificial Intestinal Juice
Chem Pharm Bull (Tokyo). 2024;72(3):286-293. doi: 10.1248/cpb.c23-00687.ABSTRACTTo explore drug interactions involving sodium zirconium cyclosilicate hydrate (SZC) and concomitant drugs like calcium antagonists (amlodipine and nifedipine) and β-blockers (carvedilol and bisoprolol), we investigate how these concomitant drugs influenced the administration of SZC in an artificial intestinal juice. Initially, we assessed the potassium ion adsorption capacity, ranking it as follows: calcium polystyrene sulfonate (CPS, 54.9 mg/g) < sodium polystyrene sulfonate (SPS, 62.1 mg/g) < SZC (90.8 mg/g). However, the adsorption eq...
Source: Chemical and Pharmaceutical Bulletin - March 6, 2024 Category: Drugs & Pharmacology Authors: Yuri Mizuno Fumihiko Ogata Yugo Uematsu Naohito Kawasaki Source Type: research

Unusual Enzymatic C-C Bond Formation and Cleavage Reactions during Natural Product Biosynthesis
Chem Pharm Bull (Tokyo). 2024;72(3):241-247. doi: 10.1248/cpb.c23-00889.ABSTRACTNatural products from plants and microorganisms provide a valuable reservoir of pharmaceutical compounds. C-C bond formation and cleavage are crucial events during natural product biosynthesis, playing pivotal roles in generating diverse and intricate chemical structures that are essential for biological functions. This review summarizes our recent findings regarding biosynthetic enzymes that catalyze unconventional C-C bond formation and cleavage reactions during natural product biosynthesis.PMID:38432903 | DOI:10.1248/cpb.c23-00889 (Source: C...
Source: Chemical and Pharmaceutical Bulletin - March 3, 2024 Category: Drugs & Pharmacology Authors: Richiro Ushimaru Source Type: research

Foreword
Chem Pharm Bull (Tokyo). 2024;72(3):248. doi: 10.1248/cpb.c24-ctf7203.NO ABSTRACTPMID:38432904 | DOI:10.1248/cpb.c24-ctf7203 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - March 3, 2024 Category: Drugs & Pharmacology Authors: Akira Kotani Source Type: research

Electrochemical Characterization of a Novel Organoelectrocatalyst, 7-Azabicyclo[2.2.1]heptan-7-ol (ABHOL), and Its Application to Electrochemical Sensors
Chem Pharm Bull (Tokyo). 2024;72(3):249-252. doi: 10.1248/cpb.c23-00710.ABSTRACTElectrochemical enzyme sensors are suitable for simple monitoring methods, for example, as glucose sensors for diabetic patients; however, they have several disadvantages arising from the properties of the enzyme. Therefore, non-enzymatic electrochemical sensors using functional molecules are being developed. In this paper, we report the electrochemical characterization of a new hydroxylamine compound, 7-azabicyclo[2.2.1]heptan-7-ol (ABHOL), and its application to glucose sensing. Although the cyclic voltammogram for the first cycle was unstabl...
Source: Chemical and Pharmaceutical Bulletin - March 3, 2024 Category: Drugs & Pharmacology Authors: Masaki Toda Kyoko Sugiyama Fumiya Sato Yusuke Sasano Tsutomu Fujimura Yoshiharu Iwabuchi Katsuhiko Sato Source Type: research