Lymphatic Transport of Halofantrine in the Conscious Rat When Administered as Either the Free Base or the Hydrochloride Salt: Effect of Lipid Class and Lipid Vehicle Dispersion

1996 ◽  
Vol 85 (4) ◽  
pp. 357-361 ◽  
Author(s):  
Christopher J.H. Porter ◽  
Susan A. Charman ◽  
Andrew J. Humberstone ◽  
William N. Charman



1992 ◽  
Vol 25 (1) ◽  
pp. 133-161
Author(s):  
Laurine A. LaPlanche ◽  
Robert Rothchild ◽  
Yangdong Xu


2016 ◽  
Vol 8 (4) ◽  
pp. 28 ◽  
Author(s):  
Guan Wang ◽  
Dongsheng Chen ◽  
Yuanyuan Sun ◽  
Qing Cao ◽  
Bonan Li ◽  
...  

<p>A practical method for the preparation of high-purity (<em>R, R</em>)-dexmethylphenidate free base was developed. The method involves a substitution reaction of 2-chloropyridine and phenylacetonitrile via hydrolysis followed by hydrogenation, configuration inversion, chiral resolution, methyl esterification, and salification to give high-purity dexmethylphenidate hydrochloride. The hydrochloride salt was then neutralized by powder sodium hydroxide overnight to give dexmethylphenidate free base with over 99% purity. This method can be used for the industrial production of the dexmethylphenidate patch API, which could also be further applied for the preparation of other types of amino acid ester free bases.</p>



1962 ◽  
Vol 203 (4) ◽  
pp. 641-643 ◽  
Author(s):  
R. S. Alphin ◽  
T. M. Lin

The volume output and hydrochloric acid secretion from the denervated gastric pouch of the rat in response to food and histamine were studied. Food was given at three dose levels—1.25, 2.5, and 5.0 g—and histamine (as free base) was given subcutaneously at dose levels of 0.34, 0.7, 1.4, and 2.8 mg/kg. The results show that the chronic denervated gastric pouch of the rat responds in a graded manner to both food and histamine in a certain dose range. Although rats are not as sensitive to histamine as humans and dogs, the chronic gastric pouch of the conscious rat is far more sensitive to histamine than the stomach of the pyloric-ligated or anesthetized rat. The feasibility of using this preparation for testing the effect of agents inhibiting food- or histamine-stimulated gastric secretion is discussed.



Author(s):  
Sándor L. Bekö ◽  
Silke D. Thoms ◽  
Martin U. Schmidt ◽  
Michael Bolte

A crystallization series of tizanidine hydrochloride, used as a muscle relaxant for spasticity acting centrally as an α2-adrenergic agonist, yielded single crystals of the free base and the hydrochloride salt. The crystal structures of tizanidine [systematic name: 5-chloro-N-(imidazolidin-2-ylidene)-2,1,3-benzothiadiazol-4-amine], C9H8ClN5S, (I), and tizanidine hydrochloride {systematic name: 2-[(5-chloro-2,1,3-benzothiadiazol-4-yl)amino]imidazolidinium chloride}, C9H9ClN5S+·Cl−, (II), have been determined. Tizanidine crystallizes with two almost identical molecules in the asymmetric unit (r.m.s. deviation = 0.179 Å for all non-H atoms). The molecules are connected by N—H...N hydrogen bonds forming chains running along [2\overline{1}1]. The present structure determination corrects the structure determination of tizanidine by Johnet al.[Acta Cryst.(2011), E67, o838–o839], which shows an incorrect tautomeric form. Tizanidine does not crystallize as the usually drawn 2-amino–imidazoline tautomer, but as the 2-imino–imidazolidine tautomer. This tautomer is present in solution as well, as shown by1H NMR analysis. In tizanidine hydrochloride, cations and anions are connected by N—H...Cl hydrogen bonds to form layers parallel to (100).







Drug Delivery ◽  
2014 ◽  
Vol 23 (1) ◽  
pp. 147-153 ◽  
Author(s):  
Qingqing Cai ◽  
Xinxian Deng ◽  
Zhongdong Li ◽  
Dianyun An ◽  
Teng Shen ◽  
...  


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