Preclinical Toxicity Evaluation of Tepoxalin, a Dual Inhibitor of Cyclooxygenase and 5-Lipoxygenase, in Sprague—Dawley Rats and Beagle Dogs

1, 2, 9, 10-tetramethoxyaporphine phosphate (MDL-832) was once considered a potential human antitussive. MDL-832 was administered orally in the diets of Sprague-Dawley rats at dose levels of 0, 5, 10, 20, 40, 80 and 160 mg/kg/day for 3 and 6 months and in gelatin capsules to Beagle dogs at 0, 5, 10, 15, 30 and 60 mg/kg/day for 3, 6 and 12 months. Histopathologic examinations of hematoxylin and eosin-stained cerebellar sections revealed intracytoplasmic brown pigment accumulations in large fusiform neurons (presumably the motor type) of the pons. The pigment granules were found to be PAS-positive, non-acid fast, iron-free, Sudan B-positive and fuchsinophilic. Intraneuronal pigment accumulations were seen in rats after 3 months of treatment at 80 mg but not at 40 mg and after 6 months at 20 mg but not at 10 mg. For dogs the effect was observed after 3 months at 60 mg but not at 30 mg and after 12 months at 10 mg but not at 5 mg.

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Thirteen-Week Oral Toxicity Evaluation of Erinacine AEnriched Lion's Mane Medicinal Mushroom, Hericium erinaceus (Agaricomycetes), Mycelia in Sprague-Dawley Rats

International Journal of Medicinal Mushrooms ◽

10.1615/intjmedmushrooms.2019030320 ◽

2019 ◽

Vol 21 (4) ◽

pp. 401-411 ◽

Cited By ~ 1

Author(s):

Li-Ya Lee ◽

I-Chen Li ◽

Wan-Ping Chen ◽

Yueh-Ting Tsai ◽

Chin-Chu Chen ◽

...

Keyword(s):

Medicinal Mushroom ◽

Sprague Dawley ◽

Toxicity Evaluation ◽

Oral Toxicity ◽

Hericium Erinaceus ◽

Sprague Dawley Rats

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Acute oral toxicity evaluation of antihyperlipidemic polyherbal preparation comprising of aqueous extracts in female sprague dawley rats as per OECD 425 TG.

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2020.12.03.219 ◽

2020 ◽

Vol 12 (03) ◽

Keyword(s):

Aqueous Extracts ◽

Acute Oral Toxicity ◽

Sprague Dawley ◽

Toxicity Evaluation ◽

Oral Toxicity ◽

Sprague Dawley Rats

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Developmental toxicity evaluation of ELF magnetic fields in Sprague–Dawley rats

Bioelectromagnetics ◽

10.1002/bem.10114 ◽

2003 ◽

Vol 24 (4) ◽

pp. 231-240 ◽

Cited By ~ 21

Author(s):

Moon-Koo Chung ◽

Jong-Choon Kim ◽

Sung-Ho Myung ◽

Dong-Il Lee

Keyword(s):

Magnetic Fields ◽

Developmental Toxicity ◽

Sprague Dawley ◽

Toxicity Evaluation ◽

Sprague Dawley Rats

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Acylcarnitines: drug absorption-enhancing agents in the gastrointestinal tract

AJP Gastrointestinal and Liver Physiology ◽

10.1152/ajpgi.1986.251.3.g332 ◽

1986 ◽

Vol 251 (3) ◽

pp. G332-G340 ◽

Cited By ~ 2

Author(s):

J. A. Fix ◽

K. Engle ◽

P. A. Porter ◽

P. S. Leppert ◽

S. J. Selk ◽

...

Keyword(s):

Gastrointestinal Tract ◽

Drug Absorption ◽

Structural Integrity ◽

Somatostatin Analogue ◽

Beagle Dogs ◽

Sprague Dawley ◽

Solid Dosage Forms ◽

Intestinal Tissue ◽

Solid Dosage ◽

Sprague Dawley Rats

Acylcarnitines were tested as potential absorption-enhancing agents for drugs that are poorly absorbed from the gastrointestinal tract. Urethan-anesthetized Sprague-Dawley rats and conscious Beagle dogs were used. Palmitoyl-DL-carnitine was the most effective acylcarnitine tested, although significant increases in drug absorption were observed with acylcarnitines containing C12 through C18 fatty acid chains. Palmitoyl-DL-carnitine afforded significant increases in the absorption of cefoxitin, gentamicin, cytarabine, somatostatin analogue, and alpha-methyldopa. The response to palmitoyl-DL-carnitine was concentration dependent and reversible within 60-120 min. Histological examination of the intestinal tissue revealed no apparent change in mucosal structural integrity at doses of palmitoyl-DL-carnitine that resulted in increased drug absorption. The acylcarnitines were effective in increasing drug absorption from the small intestine and the rectal compartment of both rats and dogs. The data also demonstrated effectiveness with aqueous and solid dosage forms (Witepsol H-15 suppositories). The data suggest that acylcarnitines may be effective and safe absorption-enhancing agents for a variety of drugs.

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