Benoxaprofen, a New Anti-Inflammatory Agent: Particle-Size Effect on Dissolution Rate and Oral Absorption in Humans

The Biosynthesis of the Benzoxazole in Nataxazole Proceeds via an Unstable Ester and has Synthetic Utility

“…Benzoxazoles are frequently found in pharmaceutically active compounds and natural products for example in plants (neosalvianen, salvianen, and salvianan); marine sponges (nakijinol, pseudopteroxazole, and ileabethoxazole) as well as bacteria (UK‐1, caboxamycin, A33853, calcimycin, nataxazole, and AJI956) . Benzoxazole compounds are prescribed as anticancers, anti‐inflammatories (flunoxaprofen, benoxaprofen), antibacterial (calcimycin, boxazomycin), and muscle relaxant (chlorzoxazone). Tafamidis (Figure a) is the only approved medicine to delay progression of transthyretin familial amyloid polyneuropathy …”

The Biosynthesis of the Benzoxazole in Nataxazole Proceeds via an Unstable Ester and has Synthetic Utility

“…Benzoxazoles are frequently found in pharmaceutically active compounds and natural products for example in plants (neosalvianen, salvianen, and salvianan); marine sponges (nakijinol, pseudopteroxazole, and ileabethoxazole) as well as bacteria (UK‐1, caboxamycin, A33853, calcimycin, nataxazole, and AJI956) . Benzoxazole compounds are prescribed as anticancers, anti‐inflammatories (flunoxaprofen, benoxaprofen), antibacterial (calcimycin, boxazomycin), and muscle relaxant (chlorzoxazone). Tafamidis (Figure a) is the only approved medicine to delay progression of transthyretin familial amyloid polyneuropathy …”

“…[1] Heterocycles are rigid molecules that can form hydrogen bonds as well as hydrophobic interactions,m oreover they can be modified to adjust lipophilicity,p olarity,a queous solubility,a nd selectivity.O xazoles (and oxazolines) are very common heterocycles and are found isolated or conjugated to aromatic rings,f or example, with benzene,k nown as benzoxazoles.B enzoxazoles are frequently found in pharmaceutically active compounds [2] and natural products for example in plants (neosalvianen, salvianen, and salvianan); [3] marine sponges (nakijinol, [4] pseudopteroxazole, [5] and ileabethoxazole) [6] as well as bacteria (UK-1, [7] caboxamycin, [8] A33853, [9] calcimycin, [10] nataxazole, [11] and AJI956). [12] Benzoxazole compounds are prescribed as anticancers,a nti-inflammatories (flunoxaprofen, [13] benoxaprofen [14] ), antibacterial (calcimycin, [15] boxazomycin [16] ), and muscle relaxant (chlorzoxazone [17] ). Tafamidis (Figure 1a)i s the only approved medicine to delay progression of transthyretin familial amyloid polyneuropathy.…”

A new approach in the prediction of the dissolution behavior of suspended particles by means of their particle size distribution

“…One of the aspects of the pharmaceutical dosage form, which may affect the effectiveness of the drug, is the particle size of the API [1,2]. The latter can readily be understood, since the dissolution rate of the API may highly depend on its particle size (distribution).…”