New Conjugate Of Cyclodextrin Useful As Anti-Inflammatory And Anti-Tumoral Agents And For Preparation Of Medicaments With Colon Site-Specific Delivery(252 views) Rizzarelli E, Vecchio G, Puglisi A, La Mendola D, Pugliesi A
Am J Obstet Gynecol (ISSN: 0002-9378), 2015; 212(3): 413-413.
Division of Reproductive Endocrinology, Robert Wood Johnson Medical School, Rutgers University, New Brunswick, NJ, United States
Reproductive Medicine Associates of New Jersey, 140 Allen Rd., Basking Ridge, NJ, United States
Department of Obstetrics, Gynecology, and Reproductive Sciences, Robert Wood Johnson Medical School, Rutgers University, New Brunswick, NJ, United States
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New Conjugate Of Cyclodextrin Useful As Anti-Inflammatory And Anti-Tumoral Agents And For Preparation Of Medicaments With Colon Site-Specific Delivery
NOVELTY - A conjugate of cyclodextrin (I) is new. USE - For the preparation of medicaments with colon site-specific delivery (claimed). ADVANTAGE - The (S) -etodolac conjugate of beta -cyclodextrin is potent cyclooxygenase (COX) inhibitor. The beta -cyclodextrin etodolac conjugates allow to suitably target the drug. The optically pure etodolac conjugates is advantageous in terms of activity/side effects ratio. The solubility of the mixture of the diastereomers of the conjugate of cyclodextrin, markedly more water-soluble than etodolac itself, where the two isolated diastereomers show different solubilities in water, higher in the case of the R-etodolac conjugate (6. 8 g/l). The conjugate of beta -cyclodextrin shows excellent anti-inflammatory and anti-tumoral activity. DETAILED DESCRIPTION - A conjugate of cyclodextrin of formula (I), is new. Y1=acyl residue of is (R) or (S) 1, 8-diethyl-1, 3, 4, 9-tetrahydropyran (3, 4-b) indole-1-acetic acid (etodolac). An INDEPENDENT CLAIM is included for a pharmaceutical compositions containing conjugate of cyclodextrin of formula (Ib) in admixture with carriers
New Conjugate Of Cyclodextrin Useful As Anti-Inflammatory And Anti-Tumoral Agents And For Preparation Of Medicaments With Colon Site-Specific Delivery
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New Conjugate Of Cyclodextrin Useful As Anti-Inflammatory And Anti-Tumoral Agents And For Preparation Of Medicaments With Colon Site-Specific Delivery