Drug-Excipient Interaction and Its Importance in Dosage Form
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Comparative Evaluation of Dehydroepiandrosterone Sulfate
Supplemental material to this article can be found at: http://dmd.aspetjournals.org/content/suppl/2016/12/01/dmd.116.072355.DC1 1521-009X/45/2/224–227$25.00 http://dx.doi.org/10.1124/dmd.116.072355 DRUG METABOLISM AND DISPOSITION Drug Metab Dispos 45:224–227, February 2017 Copyright ª 2017 by The American Society for Pharmacology and Experimental Therapeutics Short Communication Comparative Evaluation of Dehydroepiandrosterone Sulfate Potential to Predict Hepatic Organic Anion Transporting Polypeptide Transporter-Based Drug-Drug Interactions s Received July 4, 2016; accepted November 30, 2016 ABSTRACT Pharmacokinetic drug-drug interactions (DDIs) on hepatic organic 59 ml/rat. Comparison of the in vitro IC50 of rifampicin for DHEAS anion transporting polypeptides (OATPs) are important clinical issues. uptake by isolated rat hepatocytes and in vivo plasma rifampicin Previously, we reported that plasma dehydroepiandrosterone sulfate concentration suggested that the effect of rifampicin on the plasma Downloaded from (DHEAS) could serve as an endogenous probe to predict OATP-based DHEAS concentration was explained mostly by the inhibition of DDIs in monkeys using rifampicin as an OATP inhibitor. Since the hepatic OATPs, demonstrating that DHEAS could be a biomarker of contribution of hepatic OATPs to the changes in plasma DHEAS by hepatic OATP activity. Next, previously reported rifampicin-induced rifampicin remains unclear, however, we performed an in vivo phar- changes in plasma concentrations evaluated as an AUC ratio (AUCR) macokinetic study to explore this issue. Since plasma DHEAS of possible probe compounds were compared on the basis of concentrations were low in our rat model, the disposition of externally rifampicin dose/body surface area. -
Role of Citicoline in the Management of Traumatic Brain Injury
pharmaceuticals Review Role of Citicoline in the Management of Traumatic Brain Injury Julio J. Secades Medical Department, Ferrer, 08029 Barcelona, Spain; [email protected] Abstract: Head injury is among the most devastating types of injury, specifically called Traumatic Brain Injury (TBI). There is a need to diminish the morbidity related with TBI and to improve the outcome of patients suffering TBI. Among the improvements in the treatment of TBI, neuroprotection is one of the upcoming improvements. Citicoline has been used in the management of brain ischemia related disorders, such as TBI. Citicoline has biochemical, pharmacological, and pharmacokinetic characteristics that make it a potentially useful neuroprotective drug for the management of TBI. A short review of these characteristics is included in this paper. Moreover, a narrative review of almost all the published or communicated studies performed with this drug in the management of patients with head injury is included. Based on the results obtained in these clinical studies, it is possible to conclude that citicoline is able to accelerate the recovery of consciousness and to improve the outcome of this kind of patient, with an excellent safety profile. Thus, citicoline could have a potential role in the management of TBI. Keywords: CDP-choline; citicoline; pharmacological neuroprotection; brain ischemia; traumatic brain injury; head injury Citation: Secades, J.J. Role of 1. Introduction Citicoline in the Management of Traumatic brain injury (TBI) is among the most devastating types of injury and can Traumatic Brain Injury. result in a different profile of neurological and cognitive deficits, and even death in the most Pharmaceuticals 2021, 14, 410. -
Sodium Prasterone Sulfate Hydrate Sodium Pyrosulfite
JP XVI Official Monographs / Sodium Pyrosulfite 1411 50 mL. Perform the test using this solution as the test solu- Sodium Prasterone Sulfate Hydrate tion. Prepare the control solution as follows: to 0.40 mL of 0.005 mol/L sulfuric acid VS add 20 mL of acetone, 1 mL of プラステロン硫酸エステルナトリウム水和物 dilute hydrochloric acid and water to make 50 mL (not more than 0.032z). (4) Heavy metals <1.07>—Proceed with 2.0 g of Sodium Prasterone Sulfate Hydrate according to Method 2, and per- form the test. Prepare the control solution with 2.0 mL of Standard Lead Solution (not more than 10 ppm). (5) Related substances—Dissolve 0.10 g of Sodium Prasterone Sulfate Hydrate in 10 mL of methanol, and use C19H27NaO5S.2H2O: 426.50 this solution as the sample solution. Pipet 1 mL of the sam- Monosodium 17-oxoandrost-5-en-3b-yl sulfate dihydrate ple solution, add methanol to make exactly 200 mL, and use [1099-87-2, anhydride] this solution as the standard solution. Perform the test with these solutions as directed under Thin-layer Chromatogra- Sodium Prasterone Sulfate Hydrate contains not phy <2.03>. Spot 5 mL each of the sample solution and stand- less than 98.0z of sodium prasterone sulfate ard solution on a plate of silica gel with fluorescent indicator (C19H27NaO5S: 390.47), calculated on the dried basis. for thin-layer chromatography. Develop the plate with a mixture of chloroform, methanol and water (75:22:3) to a Description Sodium Prasterone Sulfate Hydrate occurs as distance of about 10 cm, and air-dry the plate. -
Reproductive DHEA-S
Reproductive DHEA-S Analyte Information - 1 - DHEA-S Introduction DHEA-S, DHEA sulfate or dehydroepiandrosterone sulfate, it is a metabolite of dehydroepiandrosterone (DHEA) resulting from the addition of a sulfate group. It is the sulfate form of aromatic C19 steroid with 10,13-dimethyl, 3-hydroxy group and 17-ketone. Its chemical name is 3β-hydroxy-5-androsten-17-one sulfate, its summary formula is C19H28O5S and its molecular weight (Mr) is 368.5 Da. The structural formula of DHEA-S is shown in (Fig.1). Fig.1: Structural formula of DHEA-S Other names used for DHEA-S include: Dehydroisoandrosterone sulfate, (3beta)-3- (sulfooxy), androst-5-en-17-one, 3beta-hydroxy-androst-5-en-17-one hydrogen sulfate, Prasterone sulfate and so on. As DHEA-S is very closely connected with DHEA, both hormones are mentioned together in the following text. Biosynthesis DHEA-S is the major C19 steroid and is a precursor in testosterone and estrogen biosynthesis. DHEA-S originates almost exclusively in the zona reticularis of the adrenal cortex (Fig.2). Some may be produced by the testes, none is produced by the ovaries. The adrenal gland is the sole source of this steroid in women, whereas in men the testes secrete 5% of DHEA-S and 10 – 20% of DHEA. The production of DHEA-S and DHEA is regulated by adrenocorticotropin (ACTH). Corticotropin-releasing hormone (CRH) and, to a lesser extent, arginine vasopressin (AVP) stimulate the release of adrenocorticotropin (ACTH) from the anterior pituitary gland (Fig.3). In turn, ACTH stimulates the adrenal cortex to secrete DHEA and DHEA-S, in addition to cortisol. -
DNA Modifications in Models of Alcohol Use Disorders
Alcohol 60 (2017) 19e30 Contents lists available at ScienceDirect Alcohol journal homepage: http://www.alcoholjournal.org/ DNA modifications in models of alcohol use disorders * Christopher T. Tulisiak a, R. Adron Harris a, b, Igor Ponomarev a, b, a Waggoner Center for Alcohol and Addiction Research, The University of Texas at Austin, 2500 Speedway, A4800, Austin, TX 78712, USA b The College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, A1900, Austin, TX 78712, USA article info abstract Article history: Chronic alcohol use and abuse result in widespread changes to gene expression, some of which Received 2 September 2016 contribute to the development of alcohol-use disorders (AUD). Gene expression is controlled, in part, by a Received in revised form group of regulatory systems often referred to as epigenetic factors, which includes, among other 3 November 2016 mechanisms, chemical marks made on the histone proteins around which genomic DNA is wound to Accepted 5 November 2016 form chromatin, and on nucleotides of the DNA itself. In particular, alcohol has been shown to perturb the epigenetic machinery, leading to changes in gene expression and cellular functions characteristic of Keywords: AUD and, ultimately, to altered behavior. DNA modifications in particular are seeing increasing research Alcohol fi Epigenetics in the context of alcohol use and abuse. To date, studies of DNA modi cations in AUD have primarily fi fi fi DNA methylation looked at global methylation pro les in human brain and blood, gene-speci c methylation pro les in DNMT animal models, methylation changes associated with prenatal ethanol exposure, and the potential DNA hydroxymethylation therapeutic abilities of DNA methyltransferase inhibitors. -
A Single-Label Phenylpyrrolocytidine Provides a Molecular Beacon-Like Response Reporting HIV-1 RT Rnase H Activity Alexander S
1048–1056 Nucleic Acids Research, 2010, Vol. 38, No. 3 Published online 20 November 2009 doi:10.1093/nar/gkp1022 A single-label phenylpyrrolocytidine provides a molecular beacon-like response reporting HIV-1 RT RNase H activity Alexander S. Wahba1, Abbasali Esmaeili2, Masad J. Damha1 and Robert H. E. Hudson3,* 1Department of Chemistry, McGill University, Montreal, QC, H3A 2K6 Canada, 2Department of Chemistry, University of Birjand, Birjand, Iran and 3Department of Chemistry, University of Western Ontario, London, ON, N6A 5B7 Canada Downloaded from https://academic.oup.com/nar/article/38/3/1048/3112336 by guest on 27 September 2021 Received August 15, 2009; Revised and Accepted October 19, 2009 ABSTRACT identified as a potential target for antiretroviral therapy as it is required for virus infectivity (3); yet there are no 6-Phenylpyrrolocytidine (PhpC), a structurally con- antiRNase H agents in clinical use. Few inhibitors of HIV- servative and highly fluorescent cytidine analog, 1 RNase H were identified until the transition of testing was incorporated into oligoribonucleotides. The methods from gel-based techniques to fluorescent assays PhpC-containing RNA formed native-like duplex amenable to high-throughput screening (HTS) (4–8). The structures with complementary DNA or RNA. The most widely used assay was developed by Parniak and co- PhpC-modification was found to act as a sensitive workers (6) and utilizes a two label, molecular beacon reporter group being non-disruptive to structure and strategy (9) in which the RNA strand is labeled with a 0 the enzymatic activity of RNase H. A RNA/DNA 3 -terminal fluorophore (fluorescein, F) and a DNA 0 hybrid possessing a single PhpC insert was an strand with a quencher (dabcyl, Q) at the 5 -terminus excellent substrate for HIV-1 RT Ribonuclease H (Scheme 1). -
Polymeric Derivative of Cytidine Metabolic Antagonist Polymer-Derivat Von Cytidin Metabolit Antagonist Derive Polymere D’Un Antagoniste Metabolique De La Cytidine
(19) & (11) EP 1 881 020 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: C08G 65/08 (2006.01) A61K 38/00 (2006.01) 11.08.2010 Bulletin 2010/32 C08G 65/333 (2006.01) C08G 69/48 (2006.01) (21) Application number: 06745754.9 (86) International application number: PCT/JP2006/308826 (22) Date of filing: 27.04.2006 (87) International publication number: WO 2006/120914 (16.11.2006 Gazette 2006/46) (54) POLYMERIC DERIVATIVE OF CYTIDINE METABOLIC ANTAGONIST POLYMER-DERIVAT VON CYTIDIN METABOLIT ANTAGONIST DERIVE POLYMERE D’UN ANTAGONISTE METABOLIQUE DE LA CYTIDINE (84) Designated Contracting States: • MASHIBA, Hiroko, AT BE BG CH CY CZ DE DK EE ES FI FR GB GR NIPPON KAYAKU KABUSHIKI KAISHA HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI Tokyo 1150042 (JP) SK TR • YAMAMOTO, Keiichirou, Designated Extension States: c/o NIPPON KAYAKU K.K. AL BA HR MK YU Tokyo 1150042 (JP) • TAKASHIO, Kazutoshi, (30) Priority: 11.05.2005 JP 2005138249 NIPPON KAYAKU K.K. Tokyo 1150042 (JP) (43) Date of publication of application: 23.01.2008 Bulletin 2008/04 (74) Representative: Wablat, Wolfgang Patentanwalt (73) Proprietor: NIPPON KAYAKU KABUSHIKI KAISHA Dr. Dr. W. Wablat Tokyo 102-8172 (JP) Potsdamer Chaussee 48 14129 Berlin (DE) (72) Inventors: • MASUDA, Akira, (56) References cited: c/o NIPPON KAYAKU KABUSHIKI KAISHA EP-A- 0 097 307 EP-A- 0 685 504 Tokyo 1150042 (JP) WO-A-01/21135 WO-A-02/065988 • ONDA, Takeshi, JP-A- 6 206 832 JP-A- 02 300 133 c/o NIPPON KAYAKU KABUSHIKI KAISHA JP-A- 06 206 832 JP-A- 08 048 766 Tokyo 1150042 (JP) JP-A- 2003 524 028 JP-A- 2004 532 289 Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. -
Non-Enzymatic Synthesis of the Coenzymes, Uridine Diphosphate
N O N - E N Z Y M A T I C S Y N T H E S I S OF THE C O E N Z Y M E S , U R I D I N E D I P H O S P H A T E G L U C O S E A N D C Y T I D I N E D I P H O S P H A T E C H O L I N E , A N D O T H E R P H O S P H O R Y L A T E D M E T A B O L I C I N T E R M E D I A T E S A. M A R , J. D W O R K I N , and J. ORO* Department of Biochemical and Biophysical Sciences, University of Houston, Houston, TX 77004, U.S.A. (Received 3 November, 1986) Abstract. The synthesis of uridine diphosphate glucose (UDPG), cytidine diphosphate choline (CDP- choline), glucose-l-phosphate (G1P) and glucose-6-phosphate (G6P) has been accomplished under simulated prebiotic conditions using urea and cyanamide, two condensing agents considered to have been present on the primitive Earth. The synthesis of UDPG was carried out by reacting G1P and UTP at 70 °C for 24 hours in the presence of the condensing agents in an aqueous medium. CDP-choline was obtained under the same conditions by reacting choline phosphate and CTP. G1P and G6P were synthesized from glucose and inorganic phosphate at 70°C for 16 hours. -
Minocycline As a Candidate Treatment
Behavioural Brain Research 235 (2012) 302–317 Contents lists available at SciVerse ScienceDirect Behavioural Brain Research j ournal homepage: www.elsevier.com/locate/bbr Review Novel therapeutic targets in depression: Minocycline as a candidate treatment a,b c,d c,d f,g Joanna K. Soczynska , Rodrigo B. Mansur , Elisa Brietzke , Walter Swardfager , a,b,e b b Sidney H. Kennedy , Hanna O. Woldeyohannes , Alissa M. Powell , b a,b,e,f,∗ Marena S. Manierka , Roger S. McIntyre a Institute of Medical Science, University of Toronto, Toronto, Canada b Mood Disorders Psychopharmacology Unit, University Health Network, Toronto, Canada c Program of Recognition and Intervention in Individuals in at Risk Mental States (PRISMA), Department of Psychiatry, Universidade Federal de São Paulo, São Paulo, Brazil d Interdisciplinary Laboratory of Clinical Neurosciences (LINC), Department of Psychiatry, Universidade Federal de São Paulo, São Paulo, Brazil e Department of Psychiatry, University of Toronto, Toronto, Canada f Departments of Pharmacology and Toxicology, University of Toronto, Toronto, Canada g Neuropsychopharmacology Research Group, Sunnybrook Health Sciences Centre, Toronto, Canada h i g h l i g h t s Regional cell loss and brain atrophy in mood disorders may be a consequence of impaired neuroplasticity. Neuroplasticity is regulated by neurotrophic, inflammatory, oxidative, glutamatergic pathways. Abnormalities in these systems are implicated in the pathophysiology of mood disorders. Minocycline exerts effects on neuroplasticity and targets these interacting systems. Evidence indicates that minocycline may be a viable treatment option for mood disorders. a r t i c l e i n f o a b s t r a c t Article history: Mood disorders are marked by high rates of non-recovery, recurrence, and chronicity, which are insuf- Received 1 December 2011 ficiently addressed by current therapies. -
Customs Tariff - Schedule
CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2019 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels. -
Ep 0882734 A2
Patentamt Europaisches |||| ||| 1 1|| ||| ||| || || || ||| || ||| || || || (19) J European Patent Office Office europeen des brevets (11) EP 0 882 734 A2 (12) EUROPEAN PATENT APPLICATION (43) Date of publication:ation: (51) |nt. ci.6: C07H 19/167, A61 K 31/70 09.12.1998 Bulletin 1998/50 (21) Application number: 98109318.0 (22) Date of filing: 22.05.1998 (84) Designated Contracting States: • Ishikawa, Tohru AT BE CH CY DE DK ES Fl FR GB GR IE IT LI LU Kanagawa-ken (JP) MC NL PT SE • Ishitsuka, Hideo Designated Extension States: Yokohama-shi, Kanagawa-ken (JP) AL LT LV MK RO SI • Kohchi, Yasunori Fujisawa-shi, Kanagawa-ken (JP) (30) Priority: 02.06.1997 EP 97108791 • Oikawa, Nobuhiro Yokohama-shi, Kanagawa-ken (JP) (71) Applicant: . Shimma, Nobuo F. HOFFMANN-LA ROCHE AG Chigasaki-shi, Kanagawa-ken (JP) 4070 Basel (CH) . Sudaj Hjtomi Fujisawa-shi, Kanagawa-ken 252 (JP) (72) Inventors: • Hattori, Kazuo Kanagawa-ken (JP) (54) 5'-Deoxy-cytidine derivatives (57) Novel 5'-deoxy-cytidine derivatives repre- group which may be substituted for use in medical ther- sented by the general formula (I) apy, especially tumor therapy. (I) wherein R1 is a hydrogen atom or a group easily hydro- lyzable under physiological conditions; R2 is a hydrogen atom, or -CO-OR4 group [wherein R4 is a saturated or branched CM unsaturated, straight or hydrocarbon group < consisting of one to fifteen carbon atoms, or a group of the formula -(CH2)n-Y (in which Y is cyclohexyl or phe- CO nyl; n is an integer from 0 to 4)]; R3 is a hydrogen atom, r»- bromo, iodo, cyano, a -
The Epigenetic Link Between Polyphenols, Aging and Age-Related Diseases
G C A T T A C G G C A T genes Review The Epigenetic Link between Polyphenols, Aging and Age-Related Diseases Itika Arora 1, Manvi Sharma 1, Liou Y. Sun 1,2 and Trygve O. Tollefsbol 1,2,3,4,5,* 1 Department of Biology, University of Alabama at Birmingham, Birmingham, AL 35294, USA; [email protected] (I.A.); [email protected] (M.S.); [email protected] (L.Y.S.) 2 Comprehensive Center for Healthy Aging, University of Alabama Birmingham, 1530 3rd Avenue South, Birmingham, AL 35294, USA 3 Comprehensive Cancer Center, University of Alabama Birmingham, 1802 6th Avenue South, Birmingham, AL 35294, USA 4 Nutrition Obesity Research Center, University of Alabama Birmingham, 1675 University Boulevard, Birmingham, AL 35294, USA 5 Comprehensive Diabetes Center, University of Alabama Birmingham, Birmingham, AL 35294, USA * Correspondence: [email protected]; Tel.: +1-205-934-4573; Fax: +1-205-975-6097 Received: 26 May 2020; Accepted: 16 September 2020; Published: 18 September 2020 Abstract: Aging is a complex process mainly categorized by a decline in tissue, cells and organ function and an increased risk of mortality. Recent studies have provided evidence that suggests a strong association between epigenetic mechanisms throughout an organism’s lifespan and age-related disease progression. Epigenetics is considered an evolving field and regulates the genetic code at several levels. Among these are DNA changes, which include modifications to DNA methylation state, histone changes, which include modifications of methylation, acetylation, ubiquitination and phosphorylation of histones, and non-coding RNA changes. As a result, these epigenetic modifications are vital targets for potential therapeutic interventions against age-related deterioration and disease progression.