Intrinsic Dissolution Rate Profiling of Poorly Water-Soluble Compounds
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Investigating the Influence of Polymers on Supersaturated
Page 1 of 45 Molecular Pharmaceutics 1 2 3 4 5 6 7 Investigating the Influence of Polymers on 8 9 10 11 12 Supersaturated Flufenamic Acid Cocrystal Solutions 13 14 15 16 1 1 2 2 1 17 Minshan Guo , Ke Wang , Noel Hamill , Keith Lorimer and Mingzhong Li * 18 19 20 1School of pharmacy, De Montfort University, Leicester, UK 21 22 23 2Almac Science, Seagoe Industrial Estate, Craigavon, UK 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 1 Molecular Pharmaceutics Page 2 of 45 1 2 3 4 5 6 7 Table of contents graphic 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 ACS Paragon Plus Environment 2 Page 3 of 45 Molecular Pharmaceutics 1 2 3 Abstract 4 5 6 7 The development of enabling formulations is a key stage when demonstrating the effectiveness 8 9 10 of pharmaceutical cocrystals to maximize the oral bioavailability for poorly water soluble drugs. 11 12 Inhibition of drug crystallization from a supersaturated cocrystal solution through a fundamental 13 14 understanding of the nucleation and crystal growth is important. In this study, the influence of 15 16 17 the three polymers of polyethylene glycol (PEG), polyvinylpyrrolidone (PVP) and a copolymer 18 19 of N-vinly-2-pyrrodidone (60%) and vinyl acetate (40%) (PVP-VA) on the flufenamic acid 20 21 22 (FFA) crystallization from three different supersaturated solutions of the pure FFA and two 23 24 cocrystals of FFA-NIC CO and FFA-TP CO has been investigated by measuring nucleation 25 26 induction times and desupersaturation rates in the presence and absence of seed crystals. -
Optum Essential Health Benefits Enhanced Formulary PDL January
PENICILLINS ketorolac tromethamineQL GENERIC mefenamic acid amoxicillin/clavulanate potassium nabumetone amoxicillin/clavulanate potassium ER naproxen January 2016 ampicillin naproxen sodium ampicillin sodium naproxen sodium CR ESSENTIAL HEALTH BENEFITS ampicillin-sulbactam naproxen sodium ER ENHANCED PREFERRED DRUG LIST nafcillin sodium naproxen DR The Optum Preferred Drug List is a guide identifying oxacillin sodium oxaprozin preferred brand-name medicines within select penicillin G potassium piroxicam therapeutic categories. The Preferred Drug List may piperacillin sodium/ tazobactam sulindac not include all drugs covered by your prescription sodium tolmetin sodium drug benefit. Generic medicines are available within many of the therapeutic categories listed, in addition piperacillin sodium/tazobactam Fenoprofen Calcium sodium to categories not listed, and should be considered Meclofenamate Sodium piperacillin/tazobactam as the first line of prescribing. Tolmetin Sodium Amoxicillin/Clavulanate Potassium LOW COST GENERIC PREFERRED For benefit coverage or restrictions please check indomethacin your benefit plan document(s). This listing is revised Augmentin meloxicam periodically as new drugs and new prescribing LOW COST GENERIC naproxen kit information becomes available. It is recommended amoxicillin that you bring this list of medications when you or a dicloxacillin sodium CARDIOVASCULAR covered family member sees a physician or other penicillin v potassium ACE-INHIBITORS healthcare provider. GENERIC QUINOLONES captopril ANTI-INFECTIVES -
What Are the Acute Treatments for Migraine and How Are They Used?
2. Acute Treatment CQ II-2-1 What are the acute treatments for migraine and how are they used? Recommendation The mainstay of acute treatment for migraine is pharmacotherapy. The drugs used include (1) acetaminophen, (2) non-steroidal anti-inflammatory drugs (NSAIDs), (3) ergotamines, (4) triptans and (5) antiemetics. Stratified treatment according to the severity of migraine is recommended: use NSAIDs such as aspirin and naproxen for mild to moderate headache, and use triptans for moderate to severe headache, or even mild to moderate headache when NSAIDs were ineffective in the past. It is necessary to give guidance and cautions to patients having acute attacks, and explain the methods of using medications (timing, dose, frequency of use) and medication use during pregnancy and breast-feeding. Grade A Background and Objective The objective of acute treatment is to resolve the migraine attack completely and rapidly and restore the patient’s normal functions. An ideal treatment should have the following characteristics: (1) resolves pain and associated symptoms rapidly; (2) is consistently effective; (3) no recurrence; (4) no need for additional use of medication; (5) no adverse effects; (6) can be administered by the patients themselves; and (7) low cost. Literature was searched to identify acute treatments that satisfy the above conditions. Comments and Evidence The acute treatment drugs for migraine generally include (1) acetaminophens, (2) non-steroidal anti-inflammatory drugs (NSAIDs), (3) ergotamines, (4) triptans, and (5) antiemetics. For severe migraines including status migrainosus and migraine attacks refractory to treatment, (6) anesthetics, and (7) corticosteroids (dexamethasone) are used (Tables 1 and 2).1)-9) There are two approaches to the selection and sequencing of these medications: “step care” and “stratified care”. -
Effect of Felodipine Against Pilocarpine Induced Seizures in Rats
Int. J. Pharm. Sci. Rev. Res., 52(1), September - October 2018; Article No. 10, Pages: 54-60 ISSN 0976 – 044X Research Article Effect of Felodipine against Pilocarpine induced Seizures in Rats Osama Q. Fadheel 1, Faruk H. AL-Jawad 1, Waleed K. Abdulsahib 2, Haider F. Ghazi 3 1Pharmacology Department, College of Medicine, Al-Nahrain University, Baghdad, Iraq. 2Pharmacy department, Al- Farahidi University College, Baghdad, Iraq. 3Microbiology Department, College of Medicine, Al-Nahrain University, Iraq. *Corresponding author’s E-mail: [email protected] Received: 25-07-2018; Revised: 22-08-2018; Accepted: 05-09-2018. ABSTRACT Epilepsy is a standout amongst the most well-known genuine cerebrum issue, can happen at all ages. The examination was performed to investigate the conceivable antiepileptic impact of Felodipine against pilocarpine prompted seizure in male rats. The investigation did on forty male Wister rats similarly assigned to four gathering: (1) typical gathering (not got any medication). Gathering (2) negative control gathering (got just pilocarpine amid acceptance of seizure. Gathering (3) positive control gathering (Valproic corrosive gathering got 20 mg/kg orally twice every day). Gathering (4) Felodipine gathering (1 mg/kg got orally once every day). Rats of each gathering (aside from typical gathering) were infused intraperitoneal with pilocarpine hydrochloride (400 mg/kg) following 21 long stretches of tried medications organization orally. The mean beginning and term of seizure were resolved to assess the viability of tried medications and to contrast these impact and that of typical gathering and Valproic corrosive gathering. Additionally, neuroprotective impact (Neu N), NMDA receptor, Sodium diverts were estimated in all gatherings. -
Association of Hypertensive Status and Its Drug Treatment with Lipid and Haemostatic Factors in Middle-Aged Men: the PRIME Study
Journal of Human Hypertension (2000) 14, 511–518 2000 Macmillan Publishers Ltd All rights reserved 0950-9240/00 $15.00 www.nature.com/jhh ORIGINAL ARTICLE Association of hypertensive status and its drug treatment with lipid and haemostatic factors in middle-aged men: the PRIME Study P Marques-Vidal1, M Montaye2, B Haas3, A Bingham4, A Evans5, I Juhan-Vague6, J Ferrie`res1, G Luc2, P Amouyel2, D Arveiler3, D McMaster5, JB Ruidavets1, J-M Bard2, PY Scarabin4 and P Ducimetie`re4 1INSERM U518, Faculte´ de Me´decine Purpan, Toulouse, France; 2MONICA-Lille, Institut Pasteur de Lille, Lille, France; 3MONICA-Strasbourg, Laboratoire d’Epide´miologie et de Sante´ Publique, Strasbourg, France; 4INSERM U258, Hoˆ pital Broussais, Paris, France; 5Belfast-MONICA, Department of Epidemiology, The Queen’s University of Belfast, UK; 6Laboratory of Haematology, La Timone Hospital, Marseille, France Aims: To assess the association of hypertensive status this effect remained after multivariate adjustment. Cal- and antihypertensive drug treatment with lipid and hae- cium channel blockers decreased total cholesterol and mostatic levels in middle-aged men. apoproteins A-I and B; those differences remained sig- Methods and results: Hypertensive status, antihyperten- nificant after multivariate adjustment. ACE inhibitors sive drug treatment, total and high-density lipoprotein decreased total cholesterol, triglycerides, apoprotein B (HDL) cholesterol, triglyceride, apoproteins A-I and B, and LpE:B; and this effect remained after multivariate lipoparticles LpA-I, -
Menstrually Related and Nonmenstrual Migraines in A
MENSTRUALLY RELATED AND NONMENSTRUAL MIGRAINES IN A FREQUENT MIGRAINE POPULATION: FEATURES, CORRELATES, AND ACUTE TREATMENT DIFFERENCES A dissertation presented to the faculty of the College of Arts and Sciences of Ohio University In partial fulfillment of the requirements for the degree Doctor of Philosophy Brenda F. Pinkerman March 2006 This dissertation entitled MENSTRUALLY RELATED AND NONMENSTRUAL MIGRAINES IN A FREQUENT MIGRAINE POPULATION: FEATURES, CORRELATES, AND ACUTE TREATMENT DIFFERENCES by BRENDA F. PINKERMAN has been approved for the Department of Psychology and the College of Arts and Sciences by Kenneth A. Holroyd Distinguished Professor of Psychology Benjamin M. Ogles Interim Dean, College of Arts and Sciences PINKERMAN, BRENDA F. Ph.D. March 2006. Clinical Psychology Menstrually Related and Nonmenstrual Migraines in a Frequent Migraine Population: Features, Correlates, and Acute Treatment Differences (307 pp.) Director of Dissertation: Kenneth A. Holroyd This research describes and compares menstrually related migraines as defined by recent proposed guidelines of the International Headache Society (IHS, 2004) to nonmenstrual migraines in a population of female migraineurs with frequent, disabling migraines. Migraines are compared by frequency per day of the menstrual cycle, headache features, use of abortive and rescue medications, and acute migraine treatment outcomes. In addition, this study explores predictors of acute treatment response and headache recurrence within 24 hours following acute migraine treatment for menstrually related migraines. Participants are 107 menstruating female migaineurs who met IHS (2004) proposed criteria for menstrually related migraines and completed headache diaries using hand-held computers. Diary data are analyzed using repeated measures logistic regression. The frequency of migraines is significantly increased during the perimenstrual period, and menstrually related migraines are of longer duration and greater frequency with longer lasting disability than nonmenstrual migraines. -
Use of Analgesics in Exotic Felids Edward C. Ramsay, DVM Professor, Department of Small Animal Clinical Sciences, University Of
Use of Analgesics in Exotic Felids Formatted: Centered Edward C. Ramsay, DVM Professor, Department of Small Animal Clinical Sciences, University of Tennessee, and Consulting Veterinarian, Knoxville Zoological Gardens, Knoxville, Tennessee. Corresponding address: Ed Ramsay Dept. of Sm Animal Clin Sci C247, Veterinary Teaching Hospital University of Tennessee Knoxville, TN 37996-4544 Phone: 865-755-8219 FAX: 865-974-5554 Email: [email protected] 2 Treatment of pain in domestic and non-domestic cats has been a challenge for the clinician. Many cat species are stoic and show few or very subtle external signs of pain. Additionally, the adverse effects of nonsteroidal antiinflammatory drugs (NSAIDs) in domestic cats are well documented and have discouraged many practitioners from trying novel NSAID’s in exotic felids. As in other animals, each cat’s response to pain and analgesics will vary, necessitating an individualized treatment plan. As a rule, always treat painful felids to effect, and not by rote reliance on published dosages. It is frequently necessary to try different agents and combinations to find which produces the optimal analgesic effect in exotic felids. In order to minimize adverse effects, it is desirable to work toward treatment with the lowest effective dose when treating chronic pain. Non-steroidal Antiinflammatory Drugs NSAIDs are antiinflammatory drugs which act both centrally and peripherally. The primary effects are believed to be caused by their ability to inhibit cyclooxygenase (COX) enzymes in the arachidonic acid metabolism cascade. The COX-1 isoform is regarded as constitutive (continuously expressed) and is responsible for many homeostatic processes, such as maintenance of gastric mucosal integrity, platelet function, and renal autoregulation. -
Dorset Medicines Advisory Group
DORSET CARDIOLOGY WORKING GROUP GUIDELINE FOR CALCIUM CHANNEL BLOCKERS IN HYPERTENSION SUMMARY The pan-Dorset cardiology working group continues to recommend the use of amlodipine (a third generation dihydropyridine calcium-channel blocker) as first choice calcium channel blocker on the pan-Dorset formulary for hypertension. Lercanidipine is second choice, lacidipine third choice and felodipine is fourth choice. This is due to preferable side effect profiles in terms of ankle oedema and relative costs of the preparations. Note: where angina is the primary indication or is a co-morbidity prescribers must check against the specific product characteristics (SPC) for an individual drug to confirm this is a licensed indication. N.B. Lacidipine and lercandipine are only licensed for use in hypertension. Chapter 02.06.02 CCBs section of the Formulary has undergone an evidence-based review. A comprehensive literature search was carried out on NHS Evidence, Medline, EMBASE, Cochrane Database, and UK Duets. This was for recent reviews or meta-analyses on calcium channel blockers from 2009 onwards (comparative efficacy and side effects) and randomised controlled trials (RCTs). REVIEW BACKGROUND Very little good quality evidence exists. No reviews, meta-analyses or RCTs were found covering all calcium channel blockers currently on the formulary. Another limitation was difficulty obtaining full text original papers for some of the references therefore having to use those from more obscure journals instead. Some discrepancies exist between classification of generations of dihydropyridine CCBs, depending upon the year of publication of the reference/authors’ interpretation. Dihydropyridine (DHP) CCBs tend to be more potent vasodilators than non-dihydropyridine (non-DHP) CCBs (diltiazem, verapamil), but the latter have greater inotropic effects. -
Evaluation of Therapeutic Drug Monitoring (TDM) on Older Antiepileptic Medications
Available online a t www.scholarsresearchlibrary.com Scholars Research Library Der Pharmacia Lettre, 2015, 7 (2):243-250 (http://scholarsresearchlibrary.com/archive.html) ISSN 0975-5071 USA CODEN: DPLEB4 Evaluation of therapeutic drug monitoring (TDM) on older antiepileptic medications Dayana Nicholas* 1, Azmi Bin Sarriff 2, Tharmalingam Palanivelu 3, Kenneth Nelson 4 and Samson P. George 5 1Department of Clinical Pharmacy & Pharmacy Practice, Faculty of Pharmacy, AIMST University, Bedong, Kedah, Malaysia 2School of Pharmaceutical Sciences, Department of Clinical Pharmacy & Faculty of Pharmacy, University Sains Malaysia, Penang, Malaysia 3Consultant Physician and Head of Department, Department of Medicine, Hospital Sultan Abdhul Halim, Malaysia 4Department of Pharmacy Practice, Faculty of Pharmacy, Grace College of Pharmacy, Kerala, India 5Drug Information Centre, Karnataka State Pharmacy Council, Bangalore, Karnataka, India _____________________________________________________________________________________________ ABSTRACT The Prospective study was conducted to evaluate the measure of Therapeutic Drug Monitoring (TDM) services on conventional antiepileptic drugs (AEDs) in 160 epileptic patients’ data of children and adults with both genders was on AEDs. The study results have shown 66 patients (50.38%), under subtherapeutic range on single AEDs with phenytoin and Na.valproate. In 160 patients, 13 of 98 (13.54%) adult patients received co-medication and 3 of 62 (6.25%) children with co-medications. Overall average (Vd) for carbamazepine in adult and children patients was found to be 78.25L which was higher than Vd for phenytoin (35.12L) and Na.Valproate (11.73L). The overall mean of clearance (Cl) for phenytoin (35.59L/hr) was found to be the highest, followed by Carbamazepine (3.81L/hr) and Na.Valproate (0.40L/hr). -
Flufenamic Acid, Mefenamic Acid and Niflumic Acid Inhibit Single Nonselective Cation Channels in the Rat Exocrine Pancreas
View metadata, citation and similar papers at core.ac.uk brought to you by CORE provided by Elsevier - Publisher Connector Volume 268, number 1, 79-82 FEBS 08679 July 1990 Flufenamic acid, mefenamic acid and niflumic acid inhibit single nonselective cation channels in the rat exocrine pancreas H. Gagelein*, D. Dahlem, H.C. Englert** and H.J. Lang** Max-Planck-Institutfir Biophysik, Kennedyallee 70, D-600 Frankfurt/Main 70, FRG Received 17 May 1990 The non-steroidal anti-inflammatory drugs, flufenamic acid, mefenamic acid and niflumic acid, block Ca2+-activated non-selective cation channels in inside-out patches from the basolateral membrane of rat exocrine pancreatic cells. Half-maximal inhibition was about 10 PM for flufenamic acid and mefenamic acid, whereas niflumic acid was less potent (IC,, about 50 PM). Indomethacin, aspirin, diltiazem and ibuprofen (100 /IM) had not effect. It is concluded that the inhibitory effect of flufenamate, mefenamate and niflumate is dependent on the specific structure, consisting of two phenyl rings linked by an amino bridge. Mefenamic acid; Flufenamic acid; Niflumic acid; Indomethacin; Non-selective cation channel; Rat exocrine pancreas 1. INTRODUCTION indomethacin, ibuprofen, diltiazem and acetylsalicylic acid (aspirin) were obtained from Sigma (Munich, FRG). The substances were dissolved in dimethylsulfoxide (DMSO, Merck, Darmstadt, FRG, Recently it was reported that the drug, 3 ’ ,5-dichloro- 0.1% of total volume) before addition to the measuring solution. diphenylamine-2-carboxylic acid (DCDPC), blocks DMSO alone had no effect on the single channel recordings. non-selective cation channels in the basolateral mem- 2.2. Methods brane of rat exocrine pancreatic cells [ 11. -
Synthesis and Pharmacological Evaluation of Fenamate Analogues: 1,3,4-Oxadiazol-2-Ones and 1,3,4- Oxadiazole-2-Thiones
Scientia Pharmaceutica (Sci. Pharm.) 71,331-356 (2003) O Osterreichische Apotheker-Verlagsgesellschaft m. b.H., Wien, Printed in Austria Synthesis and Pharmacological Evaluation of Fenamate Analogues: 1,3,4-Oxadiazol-2-ones and 1,3,4- Oxadiazole-2-thiones Aida A. ~l-~zzoun~'*,Yousreya A ~aklad',Herbert ~artsch~,~afaaA. 2aghary4, Waleed M. lbrahims, Mosaad S. ~oharned~. Pharmaceutical Sciences Dept. (Pharmaceutical Chemistry goup' and Pharmacology group2), National Research Center, Tahrir St. Dokki, Giza, Egypt. 3~nstitutflir Pharmazeutische Chemie, Pharrnazie Zentrum der Universitilt Wien. 4~harmaceuticalChemistry Dept. ,' Organic Chemistry Dept. , Helwan University , Faculty of Pharmacy, Ein Helwan Cairo, Egypt. Abstract A series of fenamate pyridyl or quinolinyl analogues of 1,3,4-oxadiazol-2-ones 5a-d and 6a-r, and 1,3,4-oxadiazole-2-thiones 5e-g and 6s-v, respectively, have been synthesized and evaluated for their analgesic (hot-plate) , antiinflammatory (carrageenin induced rat's paw edema) and ulcerogenic effects as well as plasma prostaglandin E2 (PGE2) level. The highest analgesic activity was achieved with compound 5a (0.5 ,0.6 ,0.7 mrnolkg b.wt.) in respect with mefenamic acid (0.4 mmollkg b.wt.). Compounds 6h, 61 and 5g showed 93, 88 and 84% inhibition, respectively on the carrageenan-induced rat's paw edema at dose level of O.lrnrnol/kg b.wt, compared with 58% inhibition of mefenamic acid (0.2mmoll kg b.wt.). Moreover, the highest inhibitory activity on plasma PGE2 level was displayed also with 6h, 61 and 5g (71, 70,68.5% respectively, 0.lmmolkg b.wt.) compared with indomethacin (60%, 0.01 mmolkg b.wt.) as a reference drug. -
Package Insert Template for Felodipine Extended Release Tablet
PACKAGE INSERT TEMPLATE FOR FELODIPINE EXTENDED RELEASE TABLET Brand or Product Name [Product name] ER Tablet 2.5mg [Product name] ER Tablet 5mg [Product name] ER Tablet 10mg Name and Strength of Active Substance(s) Felodipine 2.5mg Felodipine 5mg Felodipine 10mg Product Description [Visual description of the appearance of the product (eg colour, markings etc) eg White, circular flat beveled edge extended release tablets marked ‘10’ on one side] Pharmacodynamics Felodipine is a vascular selective calcium antagonist which lowers arterial blood pressure by decreasing systemic vascular resistance. Due to the high degree of selectivity for smooth muscle in the arterioles, felodipine in therapeutic doses has no direct effect on cardiac contractility or conduction. Because there is no effect on venous smooth muscle or adrenergic vasomotor control, felodipine is not associated with orthostatic hypotension. Felodipine possesses a mild natriuretic/diuretic effect and fluid retention does not occur. Felodipine is effective in all grades of hypertension. It can be used as monotherapy or in combination with other antihypertensive drugs, e.g. ß-adrenoceptor blockers, diuretics or ACE-inhibitors, in order to achieve an increased antihypertensive effect. Felodipine reduces both systolic and diastolic blood pressure and can be used in isolated systolic hypertension. Felodipine maintains its antihypertensive effect during concomitant therapy with non-steroidal anti-inflammatory drugs (NSAID). Felodipine has anti-anginal and anti-ischaemic effects due to improved myocardial oxygen supply/demand balance. Coronary vascular resistance is decreased and coronary blood flow and myocardial oxygen supply are increased by felodipine due to dilatation of both epicardial arteries and arterioles. Felodipine effectively counteracts coronary vasospasm.