Reference

Absorption of oral lornoxicam in healthy volunteers using a granular formulation in comparison with standard tablets

Absorption of oral lornoxicam in healthy volunteers using a granular formulation in comparison with standard tablets. Bareggi, Silvio R.; Gambaro, Veniero; Valenti, Mauro; Benvenuti, Claudio (Medical School, University Milan, Milan I-20129, Italy). Arzneimittel-Forschung, 47(6), 755-757 (English) 1997 Cantor. CODEN: ARZNAD. ISSN: 0004-4172. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The bioavailability of lornoxicam (CAS 70374-39-9), a novel highly potent anti-inflammatory and analgesic agent, was studied in healthy volunteers after single doses of a new oral formulation (8 mg granules) in comparison to tablets (8mg). Eighteen healthy volunteers (6 males and 12 females) with a mean age of 29.4 were given a single 8 mg dose of each formulation in an open, cross-over study, with randomized sequences. Lornoxicam plasma levels were detd. by an HPLC method. Cmax, AUC0-￥ and t1/2VFb values were similar for both the granules and tablets, but tmax and lag time values after lornoxicam granules were significantly shorter than after the tablets. No side-effects were noted with either of the formulations studied. The results show that lornoxicam granular formulation had a faster absorption than tablets even though the two formulations can be considered bioequivalent.

Preparation of benzodiazepine CGRP receptor antagonists

Some chemicals with cas registry numbers like 70374-39-9 and 88150-42-9 are also used. Preparation of benzodiazepine CGRP receptor antagonists. Burgey, Christopher S.; Stump, Craig A.; Williams, Theresa M. (Merck & Co., Inc., USA). PCT Int. Appl. WO 2005000807 A2 6 Jan 2005, 86 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D. APPLICATION: WO 2004-US20206 24 Jun 2004. PRIORITY: US 2003-PV482674 26 Jun 2003. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 Title compds. I [R1 = H, alk(en/yn)yl, etc.; R2 = H, alkyl, cycloalkyl, etc.; R7 = H, alk(en/yn)yl, etc.; W = O, amino, alkyl; X = C, S; Y = O, NCN, etc.; R3 = H, alkyl, CN, etc.; R6 = H, alkyl, cycloalkyl, etc.; G-J = N, N-alkyl, etc.] are prepd. For instance, II is prepd. from (R)-3-amino-1-ethyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine oxalate, p-nitrophenylchloroformate and 3-(piperidin-4-yl)-3,4-dihydroquinazolin-2(1H)-one hydrochloride. Compds. I exhibit affinity for the CGRP receptor with an IC50 of less than 50mM. I, alone or in combination with other agents, are useful for the treatment of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. .