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Acta Crystallogr C. 1989 Dec 15;45 ( Pt 12):1921-3.
Structure of 5-methoxy-2-([4-methoxy-3,5-dimethyl-2-pyridinyl) methyl]sulfinyl)-1H-benzimidazole (omeprazole).

Ohishi H, In Y, Ishida T, Inoue M, Sato F, Okitsu M, Ohno T.

Osaka University of Pharmaceutical Sciences, Japan.

C17H19N3O3S, Mr = 345.42, triclinic, P1, a = 10.686 (5), b = 10.608 (7), c = 9.666 (6) A, alpha = 119.75 (5), beta = 112.02 (5), gamma = 68.33 (4) degrees, V = 859 (1) A3, Z = 2, Dm = 1.332 (2), Dx = 1.335 g cm-3, Cu K alpha, lambda = 1.5418 A, mu = 18.04 cm-1, F(000) = 364, T = 293 K, R = 0.057 for 1962 observed reflections. The methylsulfinyl group, which adopts a trans conformation, links the pyridine and benzimidazole rings in an almost coplanar orientation. Thus the molecule, as a whole, adopts a nearly extended form. Two centrosymmetrically related molecules form a cyclic dimer by intermolecular N-H...O hydrogen bonding, and the dimers are held together by van der Waals contacts between the neighboring aromatic rings in the crystal structure.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2635607&dopt=Abstract

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Nippon Yakurigaku Zasshi. 1996 Dec;108(6):323-32.
[Effects of lansoprazole on indomethacin-induced gastric bleeding and mucosal lesions in rats]

[Article in Japanese]

Murakami I, Asano S, Yukishige K, Nagaya H, Satoh H, Inatomi N.

Pharmaceutical Research Laboratories III, Takeda Chemical Industries, Ltd., Osaka, Japan.

The effects of lansoprazole given intravenously on indomethacin-induced gastric bleeding and mucosal lesions were investigated in rats in comparison with those of omeprazole, famotidine and ranitidine. Lansoprazole inhibited gastric bleeding induced by indomethacin with an ID50 value of 0.29 mg/kg. Omeprazole and famotidine significantly inhibited gastric bleeding, but ranitidine provided negligible inhibition. A correlation was found between the inhibitory action of lansoprazole on gastric bleeding, and acid secretion, and its inhibitory action on gastric bleeding was almost completely abolished by adding 50 mM-HCl to the gastric perfusate, suggesting that lansoprazole's inhibitory action on gastric bleeding was mainly due to its antisecretory action. Lansoprazole inhibited the development of gastric lesions induced by indomethacin with an ID50 value of 0.10 mg/kg, whereas histamine H2-receptor antagonists did not display a potent inhibitory effect. ID50 values for omeprazole, famotidine and ranitidine were 0.69, 2.58 and 24.6 mg/kg, respectively. These results indicate that lansoprazole has a potent inhibitory action on indomethacin-induced gastric bleeding and mucosal lesions and that it is useful in the treatment of acute gastric mucosal lesions.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9017686&dopt=Abstract

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J Chromatogr B Biomed Sci Appl. 1997 Feb 7;689(1):239-43.
Determination of omeprazole in human plasma by high-performance liquid chromatography.

Macek J, Ptacek P, Klima J.

Pharmakl s.r.o., Prague, Czech Republic.

A new method for the determination of omeprazole in human plasma was developed. Omeprazole was extracted from plasma with toluene-isoamylalcohol (95:5, v/v), the organic phase was evaporated, dissolved in the mobile phase and injected into a reversed-phase C18 column. Flunitrazepam was used as an internal standard. The mobile phase consisted of 47% methanol and 53% of 0.1 M dipotassium hydrogenphosphate, pH 7.8. The spectrophotometric detection was performed at 302 nm. Limit of quantitation was 9.7 ng/ml and the calibration curve was linear up to 1240 ng/ml.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9061498&dopt=Abstract

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