Institution
Merck Sharp & Dohme Federal Credit Union
About: Merck Sharp & Dohme Federal Credit Union is a based out in . It is known for research contribution in the topics: Receptor & Aryl. The organization has 328 authors who have published 149 publications receiving 1425 citations.
Topics: Receptor, Aryl, Alkylation, Indole test, Michael reaction
Papers published on a yearly basis
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349 citations
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TL;DR: Safety results from this study indicate that intravenous doses of montelukast sodium from 3 to 18 mg and a 10-mg oral dose are well tolerated, and remained essentially constant over the i.v. dosage range.
Abstract: Purpose. The safety, tolerability, and pharmacokinetics of intravenous (i.v.) montelukast sodium (Singulair™, MK-0476), and the oral bioavailability of montelukast sodium in healthy males and healthy females were studied.
Methods. This was a two-part study. Part I was a four-period study in males of rising i.v. doses of montelukast sodium (3, 9, and 18 mg) administered as 15-minute constant-rate i.v. infusions (Periods 1–3), followed by a 10-mg oral tablet dose of montelukast sodium (Period 4) under fasting conditions. Part II was a four-period study in females of i.v. montelukast sodium (9 mg) infused over 15 and 5 minutes (Periods 5 and 6, respectively) or injected as a bolus over 2 minutes (Period 7), followed by a 10-mg oral tablet dose of montelukast sodium (Period 8). Plasma samples were collected and analyzed by HPLC.
Results. In males (N = 6), as the i.v. dose of montelukast sodium increased from 3 to 18 mg, the area under the plasma concentration-time curve of montelukast sodium from time 0 to infinity (AUC) increased proportionately. The mean values of plasma clearance (CL), steady-state volume of distribution (Vss), plasma terminal half-life (t1/12), and mean residence time in the body (MRTi.v.) of montelukast sodium were 45.5 ml/min, 10.5 1, 5.1 hr, and 3.9 hr, respectively, and remained essentially constant over the i.v. dosage range. Following oral administration of a 10-mg tablet of montelukast sodium, the AUC, maximum plasma concentration (Cmax), time when Cmax occurred (Tmax), apparent t1/12, mean absorption time (MAT), and bioavailability (F) of montelukast sodium averaged 2441 ng · hr/ml, 385 ng/ml, 3.7 hr, 4.9 hr, 3.4 hr, and 66%, respectively. Following i.v. administration of 9 mg of montelukast sodium to females (N = 6), the values of CL, Vss, t1/2, and MRT i.v. averaged 47.6 ml/min, 9.6 1, 4.5 hr, and 3.6 hr, respectively. Following oral administration of a 10-mg tablet to females, the mean AUC, Cmax, Tmax, apparent t1/2, MAT and F were 2270 ng·hr/ml, 350 ng/ml, 3.3 hr, 4.4 hr, 2.6 hr, and 58%, respectively. These parameter values were similar to or slightly smaller than those in healthy males receiving the same i.v. and oral doses.
Conclusions. The disposition kinetics of montelukast sodium were linear. Gender had little or no effect on the kinetics of montelukast sodium. Safety results from this study indicate that intravenous doses of montelukast sodium from 3 to 18 mg and a 10-mg oral dose are well tolerated.
129 citations
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TL;DR: A method of converting self-emulsifying drug delivery systems to a pellet form has been studied and it was possible to relate the formulation variables to all the quantified pellet properties except the shape.
96 citations
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TL;DR: Results indicate that the hybrid cells have recovered the ability to assemble peroxisomes and that, although the mutant CHO cells are biochemically and morphologically very similar to cells from patients with Zellweger syndrome, the genetic lesions are distinct.
74 citations
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TL;DR: A highly diastereoselective bifunctional organocatalyst controlled Michael addition, a nitro-Mannich/lactamization cascade, a furan N-acyliminium cyclisation, a sequential alkyne RCM/syn-reduction and an alkene RCM has allowed a 19 step, highly stereoselectives synthesis of (-)-nakadomarin A.
73 citations
Authors
Showing all 328 results
Name | H-index | Papers | Citations |
---|---|---|---|
Andy Lawrence | 78 | 367 | 28286 |
Keith A. Wafford | 56 | 119 | 12011 |
Paul J. Reider | 55 | 344 | 9827 |
Margaret A. Cascieri | 52 | 168 | 9791 |
Ruth M. McKernan | 50 | 105 | 10885 |
Paul D. Leeson | 47 | 150 | 11774 |
Jonathan M. Goodman | 46 | 213 | 7904 |
John A. Kemp | 46 | 82 | 9922 |
James P. Springer | 45 | 225 | 10015 |
Ian Collins | 45 | 206 | 7564 |
Peter H. Hutson | 44 | 112 | 5993 |
Robert A. Reamer | 43 | 250 | 6446 |
Michael Rowley | 42 | 138 | 5973 |
Raymond Baker | 41 | 297 | 6037 |
Lee-Ann H. Allen | 41 | 78 | 5342 |