3Rd Grade Buoyancy Worksheet 3Rd Grade Buoyancy Worksheet
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Identificación Computacional De Nuevos Compuestos Líderes Con Actividad Analgésica
IDENTIFICACIÓN COMPUTACIONAL DE NUEVOS COMPUESTOS LÍDERES CON ACTIVIDAD ANALGÉSICA Autor: Earmin Shangoo. Tutores: Dr. Yovani Marrero Ponce MSc. Arelys López Sacerio Lic. Gerardo Maikel Casañola Martín “Año 49 de la Revolución Cubana” Curso 2006-2007 PENSAMIENTO “For all flesh is as grass, and all the glory of man as the flower of grass. The grass withereth, and the flower thereof falleth away: But the word of the Lord endureth for ever.” 1 Peter1:24,25. “Todo carne es como hierba y toda la gloria del hombre como flor de la hierba; la hierba se seca y la flor se cae, mas la palabra del Señor permanece para siempre.” 1 Pedro 1:24,25. DEDICATORIA For all my friends and family, especially my daughter, Naarah Melani Nerissa Athanase and my husband, Jeremiah Wayn Athanase, with love and admiration. “I have fought a good fight, I have finished my course…” 2Tim 4:7. Con mucho cariño y admiración, a todas mis amigos y mi familia en particular a mi hija, Naarah Melani Nerissa Athanase y mi esposo, Jeremiah Wayn Athanase. “He peleada la buena batalla, he acabado la carrera…” 2Ti 4:7 AGRADECIMIENTOS For me it is an enormous pleasure to be able to express my sincere gratefulness to all those people that in one way or another has helped me to successfully culminate my studies and this work. I would especially like to thank God because without him I am nothing; to my family for their faith, support, love and patience; to my tutors especially Arelys for their attention, dedication and orientation during this work; to all the professors of the career that made possible with their patient, constant and opportune help my formation as a pharmaceutical professional; to my friends, in particular to Solange and Harun; to all thank you. -
United States Patent (10) Patent No.: US 8,916,581 B2 Boyd Et Al
USOO891 6581 B2 (12) United States Patent (10) Patent No.: US 8,916,581 B2 Boyd et al. (45) Date of Patent: *Dec. 23, 2014 (54) (S)-N-METHYLNALTREXONE 4,194,045 A 3, 1980 Adelstein 4,203,920 A 5, 1980 Diamond et al. (75) Inventors: Thomas A. Boyd, Grandview, NY (US); 4,241,066 A 12, 1980 Kobylecki et al. H OW d Wagoner,goner, Warwick,s NY (US);s 4,311,833.4,277,605 A T.1/1982 1981 NamikoshiBuyniski et etal. al. Suketu P. Sanghvi, Kendall Park, NJ 4.322,426 A 3/1982 Hermann et al. (US); Christopher Verbicky, 4.326,074 A 4, 1982 Diamond et al. Broadalbin, NY (US); Stephen 4.326,075 A 4, 1982 Diamond et al. “. s 4,377.568 A 3/1983 Chopra et al. Andruski, Clifton Park, NY (US) 4.385,078 A 5/1983 Onda et al. 4.427,676 A 1/1984 White et al. (73) Assignee: Progenics Pharmaceuticals, Inc., 4,430,327 A 2, 1984 Frederickson et al. Tarrytown, NY (US) 4,452,775 A 6/1984 Kent 4,457,907 A 7/1984 Porteret al. (*) Notice: Subject to any disclaimer, the term of this 4,462.839 A 7/1984 McGinley et al. patent is extended or adjusted under 35 4,518.4334,466,968 A 5/19858, 1984 McGinleyBernstein et al. U.S.C. 154(b) by 344 days. 4,533,739 A 8/1985 Pitzele et al. This patent is Subject to a terminal dis- 4,606,9094,556,552 A 12/19858/1986 PorterBechgaard et al. -
Formulation and Evaluation of Thienorphine Hydrochloride
December 2012 Regular Article Chem. Pharm. Bull. 60(12) 1479–1486 (2012) 1479 Formulation and Evaluation of Thienorphine Hydrochloride Sublingual Delivery System Fei Liu,a,b Yumei Zhao, a Jianxu Sun,a Yongliang Gao,*,a and Zhenqing Zhang*,a a Beijing Institute of Pharmacology and Toxicology; No. 27 Taiping Road, Beijing 100850, P. R. China: and b Department of Pharmacy, The First Affiliated Hospital of PLA; No. 51 Fucheng Road, Beijing 10048, P. R. China. Received June 7, 2012; accepted September 4, 2012 Thienorphine hydrochloride (ThH) is a highly insoluble and readily metabolized partial-opioid agonist. It is used for the treatment of pain and heroin addiction. This study aimed to formulate and evaluate sublin- gual delivery systems containing ThH. Dimethyl-β-cyclodextrin (DM-β-CD) can enhance the solubility and permeability of hydrophobic drugs. In this paper, ThH cyclodextrin inclusion complexes were prepared and administrated sublingually with the objective of improving the drug’s aqueous solubility, in vitro permeation rate, and in vivo absorption rate. The formulation was prepared with DM-β-CD using the freeze-dried meth- od and characterized using phase solubility, differential scanning calorimetry (DSC), X-ray and NMR analy- ses. The results of each test indicated the formation of dynamic inclusion complexes between ThH and DM- β-CD. The inclusion complexes also showed significant increases in in vitro aqueous solubility and mucosal permeability. According to the pharmacokinetic study of the complex in rats, the AUC and Cmax values of the sublingual delivery group were 40 and 46 times higher than those of the gastrointestinal group, whereas tmax was shorter, which proved that in vivo absorption and metabolism had been improved. -
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Evaluation of Thienorphine-Loaded PLGA Microspheres
ORIGINAL ARTICLES Beijing Institute of Pharmacology and Toxicology, Beijing, People’s Republic of China Preparation and in vivo evaluation of thienorphine-loaded PLGA microspheres Yang Yang, Yongliang Gao Received February 24, 2010, accepted March 24, 2010 Yang Yang, Yongliang Gao, Beijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Haidian District, Beijing, 10085, People’s Republic of China [email protected]; [email protected] Pharmazie 65: 729–732 (2010) doi: 10.1691/ph.2010.0056 Thienorphine-loaded microspheres composed of poly(D,L-lactide-co-glycolide) were prepared by an O/W emulsion solvent evaporation method. HPLC was used to determine the drug loading and drug release, while a LC-MS-MS system was employed to analyze the plasma drug concentration. Results indicated that the PLGA particles obtained were spherical and of appropriate size. The formulation was stable during the test period. In vitro drug release from the microspheres was sustained for about 28 days mostly by the diffusion mechanism. The plasma drug concentration-time profiles were relatively smooth for about 28 days after subcutaneous injection of the drug-loaded microspheres to rats, compared with that for drug suspension. In vitro and in vivo correlation was established. 1. Introduction is the one most widely studied and used (Fu et al. 2005). The properties of the microspheres are sensitive to many variables The number of narcotic abusers in China is quite staggering. of preparation and conditions of the preparation and selection According to government statistics, there are estimated to be process. 0.791 million heroin abusers. Many relevant medical agencies Thienorphine [N-cyclopropylmethyl-7(-[(R)-1-hydroxy-1-me- have made continued efforts to reduce the number of narcotic thyl-3-(thien-2-yl)-propyl] -6,14-endo-ethano-tetrahydronoro- abusers, but have seldom achieved the ideal goal. -
(Ph OH N N Me O YO O YO
US 20070265293A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2007/0265293 A1 Boyd et al. (43) Pub. Date: Nov. 15, 2007 (54) (S)-N-METHYLNALTREXONE Publication Classification (76) Inventors: Thomas A. Boyd, Grandview, NY (51) Int. Cl. (US); Howard Wagoner, Warwick, NY A6II 3L/4355 (2006.01) (US); Suketu P. Sanghvi, Kendall Park, A6M II/00 (2006.01) NJ (US); Christopher Verbicky, A6M I5/08 (2006.01) Broadalbin, NY (US); Stephen 39t. 35O C Andruski, Clifton Park, NY (US) (2006.01) A6IP 3L/00 (2006.01) Correspondence Address: St. 4. CR WOLF GREENFIELD & SACKS, P.C. (2006.01) 6OO ATLANTIC AVENUE 3G (i. 308: BOSTON, MA 02210-2206 (US) A6IP 33/02 (2006.01) C07D 489/00 (2006.01) (21) Appl. No.: 11/441,452 (52) U.S. Cl. .............. 514/282; 128/200.23; 128/202.17; (22) Filed: May 25, 2006 546/45 Related U.S. Application Data (57) ABSTRACT This invention relates to S-MNTX, methods of producing (60) Provisional application No. 60/684,570, filed on May S-MNTX, pharmaceutical preparations comprising 25, 2005. S-MNTX and methods for their use. O G M Br Br e (pH OH N N Me O YO O YO OH OH R-MNTX S-MNTX Patent Application Publication Nov. 15, 2007 Sheet 1 of 6 US 2007/0265293 A1 Fig. 1 OH OH Me-N Me-N D / O O -----BBr, O O CHCI NMP, 3 AUTOCLAVE, 70'C OMe OH 1 2 Br OH As GE) G As 69 GOH Me-N ION Me-N -lass O SO EXCHANGE O SO OH OH 3 S-MNTX 1 - OXYCODONE 2 - OXYMORPHONE 3 - ODIDE SALT OF S-MNTX Fig. -
Patent Application Publication ( 10 ) Pub . No . : US 2019 / 0192440 A1
US 20190192440A1 (19 ) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2019 /0192440 A1 LI (43 ) Pub . Date : Jun . 27 , 2019 ( 54 ) ORAL DRUG DOSAGE FORM COMPRISING Publication Classification DRUG IN THE FORM OF NANOPARTICLES (51 ) Int . CI. A61K 9 / 20 (2006 .01 ) ( 71 ) Applicant: Triastek , Inc. , Nanjing ( CN ) A61K 9 /00 ( 2006 . 01) A61K 31/ 192 ( 2006 .01 ) (72 ) Inventor : Xiaoling LI , Dublin , CA (US ) A61K 9 / 24 ( 2006 .01 ) ( 52 ) U . S . CI. ( 21 ) Appl. No. : 16 /289 ,499 CPC . .. .. A61K 9 /2031 (2013 . 01 ) ; A61K 9 /0065 ( 22 ) Filed : Feb . 28 , 2019 (2013 .01 ) ; A61K 9 / 209 ( 2013 .01 ) ; A61K 9 /2027 ( 2013 .01 ) ; A61K 31/ 192 ( 2013. 01 ) ; Related U . S . Application Data A61K 9 /2072 ( 2013 .01 ) (63 ) Continuation of application No. 16 /028 ,305 , filed on Jul. 5 , 2018 , now Pat . No . 10 , 258 ,575 , which is a (57 ) ABSTRACT continuation of application No . 15 / 173 ,596 , filed on The present disclosure provides a stable solid pharmaceuti Jun . 3 , 2016 . cal dosage form for oral administration . The dosage form (60 ) Provisional application No . 62 /313 ,092 , filed on Mar. includes a substrate that forms at least one compartment and 24 , 2016 , provisional application No . 62 / 296 , 087 , a drug content loaded into the compartment. The dosage filed on Feb . 17 , 2016 , provisional application No . form is so designed that the active pharmaceutical ingredient 62 / 170, 645 , filed on Jun . 3 , 2015 . of the drug content is released in a controlled manner. Patent Application Publication Jun . 27 , 2019 Sheet 1 of 20 US 2019 /0192440 A1 FIG . -
Étude Comparative De Deux Protocoles D'anesthésie Par Voie Intramusculaire Lors De
ÉCOLE NATIONALE VÉTÉRINAIRE D’ALFORT Année 2015 ÉTUDE COMPARATIVE DE DEUX PROTOCOLES D'ANESTHÉSIE PAR VOIE INTRAMUSCULAIRE LORS DE L'OVARIECTOMIE CHEZ LA CHATTE THÈSE Pour le DOCTORAT VÉTÉRINAIRE Présentée et soutenue publiquement devant LA FACULTÉ DE MÉDECINE DE CRÉTEIL Le 22 octobre 2015 par Thomas, Raphaël, Benjamin DRESCO Né le 21 décembre 1990 à Paris 14ème JURY Président : Pr. Professeur à la Faculté de Médecine de CRÉTEIL Membres Directeur : Dr. ZILBERSTEIN Luca, Maître de conférences à l’École Nationale Vétérinaire d’Alfort Assesseur : Pr. TISSIER Renaud, Professeur à l’École Nationale Vétérinaire d’Alfort LISTE DU CORPS ENSEIGNANT Mai 2015 LISTE DES MEMBRES DU CORPS ENSEIGNANT Directeur : M. le Professeur GOGNY Marc Directeurs honoraires : MM. les Professeurs : COTARD Jean-Pierre, MIALOT Jean-Paul, MORAILLON Robert, PARODI André-Laurent, PILET Charles, TOMA Bernard. Professeurs honoraires : Mme et MM. : BENET Jean-Jacques, BRUGERE Henri, BRUGERE-PICOUX Jeanne, BUSSIERAS Jean, CERF Olivier, CHERMETTE René, CLERC Bernard, CRESPEAU François, M. COURREAU Jean-François, DEPUTTE Bertrand, MOUTHON Gilbert, MILHAUD Guy, POUCHELON Jean-Louis, ROZIER Jacques. DEPARTEMENT D’ELEVAGE ET DE PATHOLOGIE DES EQUIDES ET DES CARNIVORES (DEPEC) Chef du département : M. GRANDJEAN Dominique, Professeur - Adjoint : M. BLOT Stéphane, Professeur UNITE DE CARDIOLOGIE DISCIPLINE : NUTRITION-ALIMENTATION - Mme CHETBOUL Valérie, Professeur * - M. PARAGON Bernard, Professeur - Mme GKOUNI Vassiliki, Praticien hospitalier DISCIPLINE : OPHTALMOLOGIE - Mme SECHI-TREHIOU Emilie, Praticien hospitalier - Mme CHAHORY Sabine, Maître de conférences UNITE DE CLINIQUE EQUINE - M. AUDIGIE Fabrice, Professeur UNITE DE PARASITOLOGIE ET MALADIES PARASITAIRES - Mme BERTONI Lélia, Maître de conférences contractuel - M. BLAGA Radu Gheorghe, Maître de conférences (rattaché au DPASP) - Mme BOURZAC Céline, Maître de conférences contractuel - Mme COCHET-FAIVRE Noëlle, Praticien hospitalier - M. -
(12) Patent Application Publication (10) Pub. No.: US 2014/0144429 A1 Wensley Et Al
US 2014O144429A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0144429 A1 Wensley et al. (43) Pub. Date: May 29, 2014 (54) METHODS AND DEVICES FOR COMPOUND (60) Provisional application No. 61/887,045, filed on Oct. DELIVERY 4, 2013, provisional application No. 61/831,992, filed on Jun. 6, 2013, provisional application No. 61/794, (71) Applicant: E-NICOTINE TECHNOLOGY, INC., 601, filed on Mar. 15, 2013, provisional application Draper, UT (US) No. 61/730,738, filed on Nov. 28, 2012. (72) Inventors: Martin Wensley, Los Gatos, CA (US); Publication Classification Michael Hufford, Chapel Hill, NC (US); Jeffrey Williams, Draper, UT (51) Int. Cl. (US); Peter Lloyd, Walnut Creek, CA A6M II/04 (2006.01) (US) (52) U.S. Cl. CPC ................................... A6M II/04 (2013.O1 (73) Assignee: E-NICOTINE TECHNOLOGY, INC., ( ) Draper, UT (US) USPC ..................................................... 128/200.14 (21) Appl. No.: 14/168,338 (57) ABSTRACT 1-1. Provided herein are methods, devices, systems, and computer (22) Filed: Jan. 30, 2014 readable medium for delivering one or more compounds to a O O Subject. Also described herein are methods, devices, systems, Related U.S. Application Data and computer readable medium for transitioning a Smoker to (63) Continuation of application No. PCT/US 13/72426, an electronic nicotine delivery device and for Smoking or filed on Nov. 27, 2013. nicotine cessation. Patent Application Publication May 29, 2014 Sheet 1 of 26 US 2014/O144429 A1 FIG. 2A 204 -1 2O6 Patent Application Publication May 29, 2014 Sheet 2 of 26 US 2014/O144429 A1 Area liquid is vaporized Electrical Connection Agent O s 2. -
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ATP, 489 Absolute Configuration Benzomotphans, 204 Levotphanol
Index AIDA, 495 Affinity labeling, analogs of (Cont.) cAMP, 409, 489 motphine,448 ATP, 409, 489 naltrexone, 449 [3H] ATP, 489 norlevotphanol,449 Absolute configuration normetazocine, 181 benzomotphans, 204 norpethidine, 232 levotphanol, 115 oripavine, 453 methadone and analogs, 316 oxymotphone, 449 motphine, 86 K-Agonists, 179,405,434 phenoperidine, 234 Aid in Interactive Drug Analysis, 495 piperazine derivatives, 399 [L-Ala2] dermotphin, 363 prodines and analogs, 272 [D-Ala, D-Leu] enkephalin (DADL), 68, 344 sinomenine, 28, 115 [D-Ala2 , Bugs] enkephalinamide, 347, 447 viminol, 400 [D-Ala2, Met'] enkephalinamide, 337, 346, Ac 61-91,360 371,489 Acetylcholine, 5, 407 [D-Ala2]leu-enkephalin, 344, 346, 348 Acetylcholine analogs, 186, 191 [D-Ala2] met-enkephalin, 348 l-Acetylcodeine, 32 [D-Ala2] enkephalins, 347 Acetylmethadols (a and (3) Alfentanil, 296 maintenance of addicts by a-isomer, 304, 309 (±)-I1(3-Alkylbenzomotphans, 167, 170 metabolism, 309 11(3-Alkylbenzomotphans, 204 N-allyl and N-CPM analogs, 310, 431 7-Alkylisomotphinans, 146 stereochemistry, 323 N-Alkylnorketobemidones, 431 synthesis, 309 N-Alkylnorpethidines, 233 X-ray crystallography, 327 N-Allylnormetazocine, 420 6-Acetylmotphine, receptor binding, 27 N-Allylnormotphine, 405 Acetylnormethadol, 323 N-Allylnorpethidine, 233 8(3-Acyldihydrocodeinones, 52 3-Allylprodines (a and (3), 256 14-Acyl-4,5-epoxymotphinans, 58 'H-NMR and stereochemistry, 256 7-Acylhydromotphones, 128 X-ray crystallography, 256 Addiction, 4 N-Allylnormetazocine, 420 Adenylate cyclase, 6, 409, 413, 424,