Prolongation of Antipyretic Action and Reduction of Gastric Ulcerogenicity in the Rat by Controlled-Release Granules of Bermoprofen, A New Nonsteroidal Anti-inflammatory Drug

Q3 · MEDICINE

Article

Author: Hideo Nakamura ; Yasuhiko Nakamura ; Yasuhiro Seto ; Masaaki Mori ; Yoshimi Shirai ; Yu Imasato ; Hlrokazu Makita

While bermoprofen [(+-)-10,11-dihydro-alpha,8-dimethyl-11- oxodibenz[b,f]oxepin-2-acetic acid], a new nonsteroidal antiinflammatory drug (NSAID), has potent antipyretic and analgesic activities with a short biological half-life, it shows ulcerogenic activity as a side-effect like other nonsteroidal anti-inflammatory drugs. A bermoprofen preparation was specially designed to prolong its duration of action and to reduce its side effect. Immediate-release granules (IRGs) were prepared by coating particles of Nonpareil 103 with bermoprofen. The IRGs were also coated by spraying a film solution composed of ethylcellulose and hydroxypropylmethylcellulose (3:2), and, thereby, three kinds of retard-release granules (RRGs) were obtained with the coating amounts of 1.5, 2.5, and 4%. Peak plasma bermoprofen levels were seen 0.5, 1, 2, and 3 h after single oral administrations of IRG, RRG(1.5%), RRG (2.5%), and RRG(4%), respectively, in rats. The potency order in ulcerogenic activity was RRG(1.5%) greater than IRG greater than RRG(2.5%) greater than RRG(4%) after a single oral dosage in rats. Then, IRG and RRG(4%) were mixed (in the ratio 3:7, which was calculated from their simulated plasma bermoprofen profiles) in order to get fast onset and long duration of antipyretic action. These mixed granules [i.e., the sustained-release granules (SRGs)] exhibited a falt plasma bermoprofen profile, and longer lasting antipyretic and lower ulcerogenic activities in rats in comparison with IRG or bermoprofen. From these results, it is suggested that a bermoprofen SRG preparation has more durable therapeutic activity and lower side-effects as a NSAID.

01 Jan 1988·YAKUGAKU ZASSHIQ4 · MEDICINE

Mode of Anti-inflammatory Action of a Non-steroidal Anti-inflammatory Drug, AD-1590

Q4 · MEDICINE

Article

Author: Nakamura, Hideo ; Yokoyama, Yuichi ; Motoyoshi, Satoru ; Ishii, Katsumi ; Kadokawa, Toshiaki

The mode of anti-inflammatory action of AD 1590 (I) was studied in in vitro models.The findings indicated that AD-1590 has inhibitor activities on prostaglandin biosynthesis, leukocyte emigration, heat-denaturation of albumin and lymphocyte transformation, and membrane stabilizing action.From these results, it is suggested that AD-1590 shows anti-inflammatory activity through the mechanisms generally similar to indomethacin, while it has more potent inhibitory activity for prostaglandin biosynthesis than indomethacin.

01 Jan 1988·Folia Pharmacologica Japonica

A correlation between the species differences in anti-inflammatory activity of AD-1590, a non-steroidal anti-inflammatory drug, and its plasma level.

Article

Author: Nakamura, Hideo ; Motoyoshi, Satoru ; Yokoyama, Yuichi ; Seto, Yasuhiro ; Kadokawa, Toshiaki

Authors have reported that the oral potency ratio of AD-1590 to indomethacin varies with the animal models employed; the ratio is 4, 2.3 and 31 in the tests of acetic acid-induced vascular permeability (male mice), carrageenan hind paw edema (male rats) and UV-erythema (female guinea pigs), respectively. Thus, the relationship between the difference in the anti-inflammatory activity of AD-1590 among animal models and the species difference of the plasma AD-1590 level was investigated in experimental animals in order to ascertain the cause of the difference in the potency ratio. Inhibitory potency of AD-1590 on UV-erythema and increased vascular permeability induced by acetic acid in male rats was about 2.1 and 2.3 times, respectively, that of indomethacin. On the other hand, after a single oral administration of 5 mg/kg, the highest plasma AD-1590 level was seen in female guinea pigs (AUC9-8 hr = 63.1 micrograms.hr/ml); and followed by that in mice (male, 32.1; female, 36.1) greater than male dogs (11.5) greater than or equal to rats (male, 9.02; female, 12.5), male rabbits (9.17) greater than male monkeys (9.34 at 6 mg/kg). Hucker et al. have reported that the plasma level of indomethacin in rats is several times higher than that in guinea pigs, rabbits and monkeys. These results suggest that most of the species difference in the relative potency of AD-1590 to indomethacin in the anti-inflammatory activity results from the species difference in the plasma level of both drugs.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	NDA/BLA	-	Sumitomo Pharma Co., Ltd.	-
Inflammation	NDA/BLA	JP	Dainippon Pharmaceutical Co., Ltd.	-
Pain	NDA/BLA	-	Sumitomo Pharma Co., Ltd.	-
Pain	NDA/BLA	JP	Dainippon Pharmaceutical Co., Ltd.	-

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