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(12) United States Patent (10) Patent No.: US 9,101,662 B2 Tamarkin Et Al
USOO91 01662B2 (12) United States Patent (10) Patent No.: US 9,101,662 B2 Tamarkin et al. (45) Date of Patent: *Aug. 11, 2015 (54) COMPOSITIONS WITH MODULATING A61K 47/32 (2013.01); A61 K9/0014 (2013.01); AGENTS A61 K9/0031 (2013.01); A61 K9/0034 (2013.01); A61 K9/0043 (2013.01); A61 K (71) Applicant: Foamix Pharmaceuticals Ltd., Rehovot 9/0046 (2013.01); A61 K9/0048 (2013.01); (IL) A61 K9/0056 (2013.01) (72) Inventors: Dov Tamarkin, Macabim (IL); Meir (58) Field of Classification Search Eini, Ness Ziona (IL); Doron Friedman, CPC ........................................................ A61 K9/12 Karmei Yosef (IL); Tal Berman, Rishon See application file for complete search history. le Ziyyon (IL); David Schuz, Gimzu (IL) (56) References Cited (73) Assignee: Foamix Pharmaceuticals Ltd., Rehovot U.S. PATENT DOCUMENTS (IL) 1,159,250 A 11/1915 Moulton (*) Notice: Subject to any disclaimer, the term of this 1,666,684 A 4, 1928 Carstens patent is extended or adjusted under 35 1924,972 A 8, 1933 Beckert 2,085,733. A T. 1937 Bird U.S.C. 154(b) by 0 days. 2,390,921 A 12, 1945 Clark This patent is Subject to a terminal dis 2,524,590 A 10, 1950 Boe claimer. 2,586.287 A 2/1952 Apperson 2,617,754 A 1 1/1952 Neely 2,767,712 A 10, 1956 Waterman (21) Appl. No.: 14/045,528 2.968,628 A 1/1961 Reed 3,004,894 A 10/1961 Johnson et al. (22) Filed: Oct. 3, 2013 3,062,715 A 11/1962 Reese et al. -
Pharmaceutical and Veterinary Compounds and Metabolites
PHARMACEUTICAL AND VETERINARY COMPOUNDS AND METABOLITES High quality reference materials for analytical testing of pharmaceutical and veterinary compounds and metabolites. lgcstandards.com/drehrenstorfer [email protected] LGC Quality | ISO 17034 | ISO/IEC 17025 | ISO 9001 PHARMACEUTICAL AND VETERINARY COMPOUNDS AND METABOLITES What you need to know Pharmaceutical and veterinary medicines are essential for To facilitate the fair trade of food, and to ensure a consistent human and animal welfare, but their use can leave residues and evidence-based approach to consumer protection across in both the food chain and the environment. In a 2019 survey the globe, the Codex Alimentarius Commission (“Codex”) was of EU member states, the European Food Safety Authority established in 1963. Codex is a joint agency of the FAO (Food (EFSA) found that the number one food safety concern was and Agriculture Office of the United Nations) and the WHO the misuse of antibiotics, hormones and steroids in farm (World Health Organisation). It is responsible for producing animals. This is, in part, related to the issue of growing antibiotic and maintaining the Codex Alimentarius: a compendium of resistance in humans as a result of their potential overuse in standards, guidelines and codes of practice relating to food animals. This level of concern and increasing awareness of safety. The legal framework for the authorisation, distribution the risks associated with veterinary residues entering the food and control of Veterinary Medicinal Products (VMPs) varies chain has led to many regulatory bodies increasing surveillance from country to country, but certain common principles activities for pharmaceutical and veterinary residues in food and apply which are described in the Codex guidelines. -
Performance-Based Test Guideline for Stably Transfected Transactivation in Vitro Assays to Detect Estrogen Receptor Agonists and Antagonists
OECD/OCDE 455 Adopted: XXX OECD GUIDELINE FOR THE TESTING OF CHEMICALS Draft Performance-Based Test Guideline for Stably Transfected Transactivation In Vitro Assays to Detect Estrogen Receptor Agonists and Antagonists GENERAL INTRODUCTION Performance-Based Test Guideline 1. This Performance-Based Test Guideline (PBTG) describes the methodology of Stably Transfected Transactivation In Vitro Assays to detect Estrogen Receptor Agonists and Antagonists (ER TA assays). It comprises several mechanistically and functionally similar test methods for the identification of estrogen receptor (i.e, ER, and/or ER) agonists and antagonists and should facilitate the development of new similar or modified test methods in accordance with the principles for validation set forth in the OECD Guidance Document (GD) on the Validation and International Acceptance of New or Updated Test Methods for Hazard Assessment (1). The fully validated reference test methods (Annex 2 and Annex 3) that provide the basis for this PBTG are: The Stably Transfected TA (STTA) assay (2) using the (h) ERα-HeLa-9903 cell line; and The BG1Luc ER TA assay (3) using the BG1Luc-4E2 cell line which predominately expresses hERα with some contribution from hER(4) (5). Performance standards (PS) (6) (7) are available to facilitate the development and validation of similar test methods for the same hazard endpoint and allow for timely amendment of this PBTG so that new similar test methods can be added to an updated PBTG; however, similar test methods will only be added after review and agreement that performance standards are met. The test methods included in this Test Guideline can be used indiscriminately to address countries’ requirements for test results on estrogen receptor transactivation while benefiting from the Mutual Acceptance of Data. -
In Vitro Characterization of the Novel Solubilizing Excipient Soluplus
In vitro characterization of the novel solubility enhancing excipient Soluplus⃝R DISSERTATION zur Erlangung des Grades des Doktors der Naturwissenschaften der Naturwissenschaftlich-Technischen Fakultät III Chemie, Pharmazie, Bio- und Werkstoffwissenschaften der Universität des Saarlandes von Michael Linn Saarbrücken 2011 Tag des Kolloquiums: 19. Dezember 2011 Dekan: Prof. Dr. Wilhelm F. Maier Berichterstatter: Prof. Dr. Claus-Michael Lehr Prof. Dr. Rolf Hartmann Vorsitz: Prof. Dr. Ingolf Bernhardt Akad. Mitarbeiter: Dr. Matthias Engel To my offspring The important thing is not to stop questioning. Curiosity has its own reason for existing. Albert Einstein Table of Contents Table of Contents 1. Short summary V 2. Kurzzusammenfassung VII 3. General Introduction 1 3.1. Liberation and absorption of drugs after oral application ........... 1 3.1.1. Drug solubility and dissolution ...................... 2 3.1.2. Principles of drug absorption across the intestinal mucosa ..... 4 3.2. Formulation of poorly aqueous soluble drugs by micellar solubilization .. 10 3.3. Solid dispersions and hot melt extrusion ..................... 14 3.3.1. Solid dispersions for pharmaceutical applications ........... 14 3.3.2. Hot melt extrusion ............................. 15 3.4. The novel solubility enhancer Soluplus⃝R ..................... 18 3.5. The Caco-2 cell culture model ........................... 19 3.6. Aims of this thesis .................................. 21 3.6.1. The Caco-2 model as predictive tool for Soluplus⃝R formulations .. 22 3.6.2. Potential inhibition of P-glycoprotein and/or trypsin by Soluplus⃝R . 23 3.6.3. Optimization of Soluplus⃝R formulations ................ 23 4. Soluplus⃝R as an effective absorption enhancer of poorly soluble drugs in vitro and in vivo 25 4.1. -
(12) Patent Application Publication (10) Pub. No.: US 2014/0302163 A1 Sanchez Et Al
US 20140302163A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0302163 A1 Sanchez et al. (43) Pub. Date: Oct. 9, 2014 (54) WATER WITH IMPROVED TRANSDERMAL A613 L/714 (2006.01) AND CELLULAR DELIVERY PROPERTIES A 6LX3/59 (2006.01) AND METHODS OF MANUFACTURE AND A 6LX3/593 (2006.01) USE THEREOF A2.3L 2/52 (2006.01) A63/94 (2006.01) (71) Applicant: Subtech Industries, LLC, Stuart, FL (52) U.S. Cl. (US) CPC. A23L I/293 (2013.01); A23L 2/52 (2013.01); C02F I/30 (2013.01); A61 K33/00 (2013.01); (72) Inventors: David Sanchez, Port Saint Lucie, FL A6 IK3I/194 (2013.01); A61 K3I/714 (US); Len Deweerdt, Port Saint Lucie, (2013.01); A61 K3I/519 (2013.01); A61 K FL (US) 31/593 (2013.01); A61K 36/02 (2013.01) USPC ................. 424/600; 426/2: 426/66; 210/251: (73) Assignee: Subtech Industries, LLC, Stuart, FL 210/198.1; 210/201; 210/202: 514/569; 514/52: (US) 424/195.17; 514/789 (21) Appl. No.: 14/214,945 (57) ABSTRACT 1-1. A process for preparing conventional water sources for pro (22) Filed: Mar 16, 2014 viding “ideal state' cellular wellness benefits via topical Related U.S. Application Data hydrationabsorption. and The natural invention’s transdermal, process considersepithelial preconditioned O epicellular (60) Provisional application No. 61/788,206, filed on Mar. water sources that have removed solids, dissolved solids, 15, 2013. contaminants—both organic and inorganic and Subsequently the method purifies the water respective of removing patho Publication Classification gens, and structures the water for cellular uptake in the form of vicinal grade water, with improved characteristics of ideal (51) Int. -
Nutraceutical Potential of Carica Papaya in Metabolic Syndrome
nutrients Review Nutraceutical Potential of Carica papaya in Metabolic Syndrome Lidiani F. Santana 1, Aline C. Inada 1 , Bruna Larissa Spontoni do Espirito Santo 1, Wander F. O. Filiú 2, Arnildo Pott 3, Flávio M. Alves 3 , Rita de Cássia A. Guimarães 1, Karine de Cássia Freitas 1,* and Priscila A. Hiane 1 1 Graduate Program in Health and Development in the Central-West Region of Brazil, Federal University of Mato Grosso do Sul-UFMS, MS 79079-900 Campo Grande, Brazil 2 Faculdade de Ciências Farmacêuticas, Alimentos e Nutrição, Federal University of Mato Grosso do Sul-UFMS, MS 79079-900 Campo Grande, Brazil 3 Institute of Biosciences, Federal University of Mato Grosso do Sul-UFMS, MS 79079-900 Campo Grande, Brazil * Correspondence: [email protected]; Tel.: +55-67-3345-7445 Received: 21 June 2019; Accepted: 10 July 2019; Published: 16 July 2019 Abstract: Carica papaya L. is a well-known fruit worldwide, and its highest production occurs in tropical and subtropical regions. The pulp contains vitamins A, C, and E, B complex vitamins, such as pantothenic acid and folate, and minerals, such as magnesium and potassium, as well as food fibers. Phenolic compounds, such as benzyl isothiocyanate, glucosinolates, tocopherols (α and δ), β-cryptoxanthin, β-carotene and carotenoids, are found in the seeds. The oil extracted from the seed principally presents oleic fatty acid followed by palmitic, linoleic and stearic acids, whereas the leaves have high contents of food fibers and polyphenolic compounds, flavonoids, saponins, pro-anthocyanins, tocopherol, and benzyl isothiocyanate. Studies demonstrated that the nutrients present in its composition have beneficial effects on the cardiovascular system, protecting it against cardiovascular illnesses and preventing harm caused by free radicals. -
WO 2014/145352 Al 18 September 2014 (18.09.2014) P O P C T
(12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2014/145352 Al 18 September 2014 (18.09.2014) P O P C T (51) International Patent Classification: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, C02F 3/06 (2006.01) C02F 9/12 (2006.01) DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, C02F 9/08 (2006.01) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, (21) International Application Number: MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, PCT/US20 14/030094 OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (22) International Filing Date: SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, 16 March 2014 (16.03.2014) TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (25) Filing Language: English (84) Designated States (unless otherwise indicated, for every (26) Publication Language: English kind of regional protection available): ARIPO (BW, GH, (30) Priority Data: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, 61/788,206 15 March 2013 (15.03.2013) US UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (71) Applicant: SUBTECH INDUSTRIES LLC [FJ/US]; PO EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, Box 1226, Stuart, FL 34995 (US). -
Cumulative Cross Index to Iarc Monographs
PERSONAL HABITS AND INDOOR COMBUSTIONS volume 100 e A review of humAn cArcinogens This publication represents the views and expert opinions of an IARC Working Group on the Evaluation of Carcinogenic Risks to Humans, which met in Lyon, 29 September-6 October 2009 LYON, FRANCE - 2012 iArc monogrAphs on the evAluAtion of cArcinogenic risks to humAns CUMULATIVE CROSS INDEX TO IARC MONOGRAPHS The volume, page and year of publication are given. References to corrigenda are given in parentheses. A A-α-C .............................................................40, 245 (1986); Suppl. 7, 56 (1987) Acenaphthene ........................................................................92, 35 (2010) Acepyrene ............................................................................92, 35 (2010) Acetaldehyde ........................36, 101 (1985) (corr. 42, 263); Suppl. 7, 77 (1987); 71, 319 (1999) Acetaldehyde associated with the consumption of alcoholic beverages ..............100E, 377 (2012) Acetaldehyde formylmethylhydrazone (see Gyromitrin) Acetamide .................................... 7, 197 (1974); Suppl. 7, 56, 389 (1987); 71, 1211 (1999) Acetaminophen (see Paracetamol) Aciclovir ..............................................................................76, 47 (2000) Acid mists (see Sulfuric acid and other strong inorganic acids, occupational exposures to mists and vapours from) Acridine orange ...................................................16, 145 (1978); Suppl. 7, 56 (1987) Acriflavinium chloride ..............................................13, -
YMC HPLC Columns Applications Notebook
WA30000 HPLC Columns Applications Notebook Table of Contents Click on the items below to go directly to that section of the notebook. To Start a new search, click on Table of Contents Bookmark to the left YMC™ HPLC Column Quality Assurance............................................................2 Guide to YMC™ Part Numbering System ...........................................................3 YMC™ Column Selection Guide ....................................................................4-7 HPLC Troubleshooting and Reference Guide..................................................8-14 List of Applications..................................................................................15-20 1. Vitamins .....................................................................................21 2. Carbohydrates ............................................................................32 3. Nucleic Acids .............................................................................43 4. Amino Acids, Peptides, Proteins......................................................48 5. Organic Acids, Fatty Acid Derivatives .............................................60 6. Food Additives ............................................................................62 7. Natural Products ..........................................................................68 8. Steroids......................................................................................77 9. Drugs, Metabolites .......................................................................87 -
Kaempferol As a Dietary Anti-Inflammatory Agent
molecules Review Kaempferol as a Dietary Anti-Inflammatory Agent: Current Therapeutic Standing Waqas Alam 1, Haroon Khan 1,* , Muhammad Ajmal Shah 2 , Omar Cauli 3 and Luciano Saso 4,* 1 Department of Pharmacy, Abdul Wali Khan University Mardan, Mardan 23200, Pakistan; [email protected] 2 Department of Pharmacognosy, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad 38000, Pakistan; [email protected] 3 Department of Nursing, University of Valencia, 46010 Valencia, Spain; [email protected] 4 Department of Physiology and Pharmacology “Vittorio Erspamer”, Sapienza University, P.le Aldo Moro 5, 00185 Rome, Italy * Correspondence: [email protected](H.K.); [email protected] (L.S.) Academic Editor: Derek J. McPhee Received: 19 July 2020; Accepted: 19 August 2020; Published: 7 September 2020 Abstract: Inflammation is a physiological response to different pathological, cellular or vascular damages due to physical, chemical or mechanical trauma. It is characterized by pain, redness, heat and swelling. Current natural drugs are carefully chosen as a novel therapeutic strategy for the management of inflammatory diseases. Different phytochemical constituents are present in natural products. These phytochemicals have high efficacy both in vivo and in vitro. Among them, flavonoids occur in many foods, vegetables and herbal medicines and are considered as the most active constituent, having the ability to attenuate inflammation. Kaempferol is a polyphenol that is richly found in fruits, vegetables and herbal medicines. It is also found in plant-derived beverages. Kaempferol is used in the management of various ailments but there is no available review article that can summarize all the natural sources and biological activities specifically focusing on the anti-inflammatory effect of kaempferol. -
Recent Progress Regarding Kaempferol for the Treatment of Various Diseases (Review)
EXPERIMENTAL AND THERAPEUTIC MEDICINE 18: 2759-2776, 2019 Recent progress regarding kaempferol for the treatment of various diseases (Review) JIE REN1,2*, YIFEI LU1,2*, YANHONG QIAN1,2, BOZHOU CHEN1,2, TAO WU1,2 and GUANG JI2 1Center of Chinese Medical Therapy and Systems Biology, Institute of Interdisciplinary Integrative Medicine Research, Shanghai University of Traditional Chinese Medicine, Shanghai 201203; 2Institute of Digestive Disease, Longhua Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai 200032, P.R. China Received March 3, 2019; Accepted July 16, 2019 DOI: 10.3892/etm.2019.7886 Abstract. Kaempferol, also known as kaempferol-3 or 4. Application of KP in liver and metabolic diseases kaempferide, is a flavonoid compound that naturally occurs 5. KP protects the vascular endothelium in tea, as well as numerous common vegetables and fruits, 6. KP protects heart function including beans, broccoli, cabbage, gooseberries, grapes, 7. KP protects the cranial nerve kale, strawberries, tomatoes, citrus fruits, brussel sprouts, 8. KP for fibroproliferative disorders apples and grapefruit. The present review mainly summarizes 9. Conclusion the application of kaempferol in treating diseases and the underlying mechanisms that are currently being studied. Due to its anti‑inflammatory properties, it may be used to treat 1. Introduction numerous acute and chronic inflammation‑induced diseases, including intervertebral disc degeneration and colitis, as Kaempferol (KP; chemical name, 3,5,7‑trihydroxy‑2‑ well as post‑menopausal bone loss and acute lung injury. In (4‑hydroxyphenyl)‑4H‑1‑benzopyran‑4‑one; also known as addition, it has beneficial effects against cancer, liver injury, kaempferol‑3, kaempferide or kaempferol flavonol) is a type of obesity and diabetes, inhibits vascular endothelial inflamma- flavonoid. -
SARS-Cov-2: Repurposed Drugs and Novel Therapeutic Approaches—Insights Into Chemical Structure—Biological Activity and Toxicological Screening
Journal of Clinical Medicine Review SARS-CoV-2: Repurposed Drugs and Novel Therapeutic Approaches—Insights into Chemical Structure—Biological Activity and Toxicological Screening 1, 2,3, 1, 1, Cristina Adriana Dehelean y, Voichita Lazureanu y, Dorina Coricovac * , Marius Mioc *, Roxana Oancea 4, Iasmina Marcovici 1, Iulia Pinzaru 1 , Codruta Soica 1, Aristidis M. Tsatsakis 5 and Octavian Cretu 2 1 Faculty of Pharmacy, “Victor Babes” University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania; [email protected] (C.A.D.); [email protected] (I.M.); [email protected] (I.P.); [email protected] (C.S.) 2 Faculty of Medicine, “Victor Babes” University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania; [email protected] (V.L.); [email protected] (O.C.) 3 “Dr. Victor Babes” Clinical Hospital for Infectious Diseases and Pneumophthisiology, 300310 Timisoara, Romania 4 Faculty of Dental Medicine, “Victor Babes” University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., 300041 Timisoara, Romania; [email protected] 5 Department of Forensic Sciences and Toxicology, Faculty of Medicine, University of Crete, Heraklion, 71003 Crete, Greece; [email protected] * Correspondence: [email protected] (D.C.); [email protected] (M.M.); Tel.: +4-07-4309-2959 (D.C.); +4-07-5623-6715 (M.M.) Equal contribution as first authors. y Received: 21 May 2020; Accepted: 26 June 2020; Published: 2 July 2020 Abstract: SARS-CoV-2 (severe acute respiratory syndrome coronavirus 2) pandemic represents the primary public health concern nowadays, and great efforts are made worldwide for efficient management of this crisis. Considerable scientific progress was recorded regarding SARS-CoV-2 infection in terms of genomic structure, diagnostic tools, viral transmission, mechanism of viral infection, symptomatology, clinical impact, and complications, but these data evolve constantly.