In Vivo Evaluation of Zidovudine (AZT)-Loaded Ethylcellulose Microspheres After Oral Administration in Beagle Dogs

1997 ◽  
Vol 86 (5) ◽  
pp. 554-559 ◽  
Author(s):  
Khawla Abu-Izza ◽  
Laura Tambrallo ◽  
D. Robert Lu
2009 ◽  
Vol 12 (1) ◽  
pp. 129 ◽  
Author(s):  
Zhihong Zhang ◽  
Bo Peng ◽  
Xinggang Yang ◽  
Chao Wang ◽  
Guangmei Sun ◽  
...  

PURPOSE. Find a novel delivery system for oral administration of drugs that have absorption window in the upper part of gastrointestinal (GI) track. METHODS. Dipyridamole was chosen as the model drug. A novel system, which combined the osmotic pump controlled release system and the floating system, was designed; matrix tablets (MT) were prepared for compares. The effects of pH, temperature and hydrodynamic conditions on drug release and the floating behavior of floating osmotic pump system (FOP) were investigated. In vivo evaluation was performed by a three-crossover study in six Beagle dogs relative to the conventional tablet (CT). Cumulative percent input in vivo was compared with that of in vitro release profiles. RESULTS. Floating behavior of FOP, drug releases from FOP and MT were sensitive to pH of dissolution media but not sensitive to temperature; the release of dipyridamole from MT was influenced by stirring rate while drug release from FOP was not. AUC of FOP was larger than MT and CT. The linear correlations between fraction absorbed in vivo and fraction dissolved in vitro was established for FOP-a true zero-order release formula, whereas only a nonlinear correlation was obtained for MT. CONCLUTIONS. FOP could be a novel way for the oral administration for drugs like dipyridamole.


2017 ◽  
Vol 525 (1) ◽  
pp. 60-70 ◽  
Author(s):  
Jung Hyun Cho ◽  
Jin Cheul Kim ◽  
Hyung-Seo Kim ◽  
Dong Shik Kim ◽  
Kyeong Soo Kim ◽  
...  

2008 ◽  
Vol 18 (4) ◽  
pp. 239-243 ◽  
Author(s):  
S. Sun ◽  
F. Cui ◽  
Y. Kawashima ◽  
N. Liang ◽  
L. Zhang ◽  
...  

2015 ◽  
Vol 305 (1) ◽  
pp. 139-145 ◽  
Author(s):  
So-Young Ma ◽  
You Ree Nam ◽  
Jongho Jeon ◽  
Jong Kook Rho ◽  
Dong-Eun Lee ◽  
...  

2001 ◽  
Vol 222 (1) ◽  
pp. 1-6 ◽  
Author(s):  
Khaled A. Khaled ◽  
Yousif A. Asiri ◽  
Yousry M. El-Sayed

1984 ◽  
Vol 107 (2) ◽  
pp. 275-281 ◽  
Author(s):  
Roland De Coster ◽  
Dominiek Beerens ◽  
Jef Dom ◽  
Gustaaf Willemsens

Abstract. Some endocrinological effects of single daily oral administration of 150 mg ketoconazole for 15 days were investigated in 4 male beagle dogs. Plasma testosterone fell markedly within 3–4 h and then progressively returned to control concentrations by 10 h after drug administration. On the other hand, plasma 17α-hydroxyprogesterone, progesterone and 17α,20α-dihydroxyprogesterone increased within 3–10 h before returning to basal values after 24 h. Plasma LH did not rise significantly though some high individual levels were noted. Plasma cortisol and oestradiol-17α levels were not significantly modified by the treatment. These results confirm that a high therapeutic dose of ketoconazole, given orally once a day, transiently inhibits in vivo the 17–20 lyase enzyme of the testis, without modifying basal cortisol and oestradiol-17β plasma concentrations and that enzymatic inhibition still occurs after daily treatment for up to 2 weeks but remains transient and parallels the resorption profile of the drug so that normal plasma testosterone levels are observed from 10 to 24 h after drug intake. However, permanent inhibition of androgen biosynthesis might be obtained by the administration of high doses of ketoconazole given several times a day.


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