Oral Bioavailability and Mass Balance Studies of a Novel Anti-arrhythmic Agent Sulcardine Sulfate in Sprague–Dawley Rats and Beagle Dogs

2016 ◽  
Vol 42 (3) ◽  
pp. 453-459
Author(s):  
You-li Lu ◽  
Shui-jun Li ◽  
Gang-yi Liu ◽  
Xiao-chuan Li ◽  
Ding Yang ◽  
...  
Keyword(s):  
Mass Balance ◽  
Oral Bioavailability ◽  
Beagle Dogs ◽  
Sprague Dawley ◽  
Sprague Dawley Rats

Intraneuronal accumulations of lysosomes in the cerebellum of rats and dogs after dosing with MDL-832

1990 ◽  
Vol 48 (3) ◽  
pp. 830-831
Author(s):  
S.D. Barnard ◽  
S.D. Warner
Keyword(s):  
Brown Pigment ◽  
Beagle Dogs ◽  
Sprague Dawley ◽  
Gelatin Capsules ◽  
Pigment Granules ◽  
Sprague Dawley Rats ◽  
Hematoxylin And Eosin ◽  
Dose Levels

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.

A 90-day oral (dietary) toxicity and mass balance study of corn starch fiber in Sprague Dawley rats

2016 ◽  
Vol 97 ◽  
pp. 57-69 ◽  
Author(s):  
Christine M. Crincoli ◽  
Andrey I. Nikiforov ◽  
Marisa O. Rihner ◽  
Elizabeth A. Lambert ◽  
Melanie A. Greeley ◽  
...  
Keyword(s):  
Mass Balance ◽  
Corn Starch ◽  
Sprague Dawley ◽  
Balance Study ◽  
Sprague Dawley Rats ◽  
Dietary Toxicity ◽  
Mass Balance Study

Acylcarnitines: drug absorption-enhancing agents in the gastrointestinal tract

1986 ◽  
Vol 251 (3) ◽  
pp. G332-G340 ◽  
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.

Non-clinical safety and pharmacokinetic evaluations of propylene glycol aerosol in Sprague-Dawley rats and Beagle dogs

Toxicology ◽  
2011 ◽  
Vol 287 (1-3) ◽  
pp. 76-90 ◽  
Author(s):  
Michael S. Werley ◽  
Paddy McDonald ◽  
Patrick Lilly ◽  
Daniel Kirkpatrick ◽  
Jeffrey Wallery ◽  
...  
Keyword(s):  
Propylene Glycol ◽  
Beagle Dogs ◽  
Sprague Dawley ◽  
Clinical Safety ◽  
Sprague Dawley Rats

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

1996 ◽  
Vol 33 (1) ◽  
pp. 38-48
Author(s):  
E. V. KNIGHT ◽  
J. P. KIMBALL ◽  
C. M. KEENAN ◽  
I. L. SMITH ◽  
F. A. WONG ◽  
...  
Keyword(s):  
Beagle Dogs ◽  
Sprague Dawley ◽  
Toxicity Evaluation ◽  
Dual Inhibitor ◽  
Sprague Dawley Rats

Pharmacokinetics in Sprague-Dawley rats and Beagle dogs andin vitrometabolism of ZJM-289, a novel nitric dioxide donor

Xenobiotica ◽  
2013 ◽  
Vol 44 (1) ◽  
pp. 59-69 ◽  
Author(s):  
Ning Li ◽  
Zhixia Qiu ◽  
Xuliang Wang ◽  
Tingting Li ◽  
Hui Ji ◽  
...  
Keyword(s):  
Beagle Dogs ◽  
Sprague Dawley ◽  
Sprague Dawley Rats

scholarly journals Toxicity Profile of Artesunate in Rats and Dogs

2021 ◽  
Author(s):  
Johanna Susanne Lang
Keyword(s):  
Clinical Pathology ◽  
Toxicity Profile ◽  
Beagle Dogs ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Respiratory Parameters ◽  
Safety Parameters ◽  
Repeated Administrations ◽  
Single Intravenous Administration ◽  
Intramuscular Artesunate

OBJECTIVES: The objectives of these studies were to investigate the toxicity, safety and toxicokinetics of single and multiple doses of artesunate for injection in rats and dogs. METHODS: Sprague-Dawley rats and Beagle dogs were treated intravenously or intramuscularly for 28 consecutive days with doses of up to 30 mg/kg artesunate, evaluating toxicity, kinetics, genotoxicity, and cardiovascular and central nervous safety parameters after single and 4-week repeated administrations. Furthermore, respiratory parameters were evaluated after a single intravenous administration in rats. RESULTS: Artesunate was well tolerated with no mortality and only minor effects on clinical pathology parameters. CONCLUSIONS: The results obtained in these studies support the safe use of intravenous and intramuscular artesunate in humans.

Biopharmaceutics and Pharmacokinetics of Timosaponin A-III by a Sensitive HPLC-MS/MS Method: Low Bioavailability Resulting from Poor Permeability and Solubility

2020 ◽  
Vol 21 ◽  
Author(s):  
Hai-Qiao Wang ◽  
Xiao-Mei Gong ◽  
Fen Lan ◽  
Yi-Han Zhang ◽  
Jin-Er Xia ◽  
...  
Keyword(s):  
Rat Liver ◽  
Oral Bioavailability ◽  
Liver Microsome ◽  
Transport Model ◽  
Control Group ◽  
Sprague Dawley ◽  
Sprague Dawley Rats ◽  
Absolute Oral Bioavailability ◽  
Rat Liver Microsome

Background: Timosaponin A-III is one of the most promising active saponins from Anemarrhena asphodeloides Bge. As an oral chemotherapeutic agent, there is an urgent need to clarify its biopharmaceutics and pharmacokinetics to improve its development potential. Objective: This research explores the bioavailability of timosaponin A-III and clarifies its absorption and metabolism mechanisms by a sensitive and specific HPLC-MS/MS method. Methods: Pharmacokinetics and bioavailability studies of timosaponin A-III were performed in Sprague-Dawley rats by oral (20 g/kg) and intravenous administration (2 mg/kg). Control group was given the same volume of normal saline. The absorption of timosaponin A-III was investigated in a rat intestinal perfusion model in situ and a Caco-2 cell transport model in vitro. The metabolic rate of timosaponin A-III was determined in a rat liver microsome incubation system. Results: After the oral administration, timosaponin A-III reached Cmax of 120.90 ± 24.97 ng/mL at 8 h, and the t1/2 was 9.94 h. The absolute oral bioavailability of timosaponin A-III is 9.18%. The permeability coefficients of timosaponin A-III in four intestinal segments ranged from 4.98 to 5.42 cm/s, indicating a difficult absorption. A strikingly high transport of timosaponin A-III was found, PappBA 3.27 ± 0.64 × 10−6 cm/s, which was abolished by a P-gp inhibitor. Rat liver microsome incubation studies showed that timosaponin A-III could hardly be metabolized, with a t1/2 of over 12 h. In addition, the solubility test showed a low solubility in PBS solution, 30.58 μg/mL. Conclusion: Timosaponin A-III exhibited low oral bioavailability by oral and intravenous admiConclusion: nistration, which was probably caused by its low permeability and solubility. This study may provide a reference for the rational clinical use and further study on the pharmacology or toxicology of timosaponin A-III.

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