DOCSLIB.ORG

United States Patent (19) 11) Patent Number: 4,758,433 Johnson Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
United States Patent (19) 11) Patent Number: 4,758,433 Johnson Et Al United States Patent (19) 11) Patent Number: 4,758,433 Johnson et al. (45. Date of Patent: Jul.19, 1988 54, OIL EXTRACT OF TANACETUM (56) References Cited PARTHENIUM FOR TREATING MIGRAINE PUBLICATIONS El-Ferally et al., Chem. 89: 87138k. 75) Inventors: Edward S. Johnson, Maidenhead; Joshi, Chem. Abst. 86: 72888u. Peter J. Hylands; Deborah M. Edriguez et al., 86: 72889y. Hylands nee Jessup, both of Picman et al., Chem. Abs. 100:99724g. Hausen et al., Chem. Abs. 100: 1884.5 x. Wickham, all of England Djermanovic et al., Chem. Abst. 97: 212667a. Mladenovic et al., Chen. Abst. 97: 212668b. (73) Assignee: R. P. Scherer Corp., Troy, Mich. Bohlmann et al., Chem. Abst. 97: 1594.79n. Stevens, Chem. Abst. 97: 159480t. 21 Appl. No.: 749,008 Hladon et al., Chem. Abst. 91: 68299p. Ogura et al., Chem. Abst. 90: 23285u. Lee et al., Cancer Research 31, 1649-1654, Nov. 1971. 22 Filed: Jun. 26, 1985 Soucek et al., Collective Czech. Chem. Comm., 1961, vol. 26, pp. 803-809. Blakeman, Chem. Abst. 91: 2076.14c. Related U.S. Application Data Romo et al., Tetrahedron, 1965, vol. 21, pp. 1744-1745. 63 Continuation-in-part of Ser. No. 494,964, May 16, Hall et al., Journal of Pharmaceutical Sciences, vol. 68, 1983, abandoned. No. 5, May 1979. Primary Examiner-Jane T. Fan (30) Foreign Application Priority Data Attorney, Agent, or Firm-Omri M. Behr May 19, 1982 (GB) United Kingdom ................. 82.14572 (57 ABSTRACT Sep. 22, 1982 GB United Kingdom ................. 8227062 A preparation for pharmaceutical use, especially in the treatment of migraine, arthritis and bronchial com 51) Int. Cl............................................... A61K 35/78 plaints contains a sesquiterpene lactone and is recovered 52 U.S. Cl. ................................. 424/195.1; 514/468; from the plant Tanacetum parthenium by extraction 549/299 using a pharmaceutically acceptable oil. 58) Field of Search ........................ 549/299; 514/468; 424/195.1 4 Claims, No Drawings 4,758,433 1. 2 culatory collapse caused by the release of histamine or OIL EXTRACT OF TANACETUM PARTHENIUM other endogenous substances. FOR TREATING MIGRAINE Drugs with spasmolytic actions such as aminophyl line are used to treat bronchospasm. Drugs with antihis This is a continuation-in-part of Ser. No. 494,964 filed 5 tamine activity are also used in asthma and for wheezing 5/16/83 now abandoned. and other symptoms associated with allergic phenom ena such as hay fever. FIELD OF THE INVENTION It has been known for many years that sesquiterpene This invention relates to sesquiterpene lactones and lactones are present in plants, for example, in the family sesquiterpene lactone-containing plant extracts and 10 Compositae (see Yoshio, Mabry and Timmermann, preparations for pharmaceutical use, and particularly to "Sesquiterpene Lactones, Chemistry, NMR and Plant compositions which are useful in the treatment of mi Distribution', University of Tokyo Press 1973). graine and various arthritic and bronchial conditions. Of these plant Tanacetum parthenium (formerly BACKGROUND OF THE INVENTION called Chrysanthemum parthenium and commonly 15 known as feverfew, featherfoil, flirtwort and Bachelor's The incidence of migraine is said to be in the region of Buttons) has been put forward in herbal medicine as a 12% of the population. Its precise causes have not been possibly effective treatment for migraine when con determined but certain elements in its causation are well sumed. No serious medical study of this treatment for documented. migraine has apparently been published, nor has there Neurohumoral and local hormone (autacoid) factors 20 been any consideration of what ingredient or ingredi such as noradrenaline, 5-hydroxytryptamine (seroto ents of the plant might be involved in this alleged effi nin), histamine and prostaglandins are implicated in cacy. migraine probably acting at the cerebro-vascular level. Many years ago, it was reported that the sesquiter There is much evidence to suggest that a disturbance pene lactones parthenolide and santamarine may be of blood vessel diameter is involved in the migraine 25 extracted from feverfew using light petroleum and process. Thus reports have demonstrated a constriction chloroform respectively (see Sorm et al, Coll. Czech. of cerebral cortical vessels followed by a dilatation Chem. Comm., (1961), 26, 803 and Romo et al, Tetrahe during a migraine attack. The vasoconstriction is be dron, (1965), 21, 1741 respectively). In those publica lieved to be due to the release of amines such as nor tions, there was no indication of any possible medical adrenaline from neurones and 5-hydroxytryptamine 30 use for the sesquiterpene lactones. from platelets. Histamine is also released from mast cells Some cytotoxic activity of parthenolide and several and plays an important role in the migraine variant other sesquiterpene lactones has also been reported known as cluster headache (migrainous neuralgia). some time ago (Lee et al, Cancer Research, (1971), 31, Drugs with antinoradrenaline, anti 5-hydroxytrypta 1649). There is, however, no suggestion in this article mine and antihistamine activities are all used to alleviate 35 that any sesquiterpene lactone or extract containing it the symptoms of migraine. Evidence that prostaglan may be useful in the treatment of migraine, arthritis or dins (PG), such as PGE2, PGF2, PGI2 (prostacyclin) bronchial complaints. or thromboxane A2 are involved comes from the fact More recently it has been shown that certain sesquit that non-steroidal anti-inflammatory drugs such as aspi erpene lactones are potent inhibitors of carrageenan rin, which act by inhibiting the synthesis of prostaglan induced edema and chronic adjuvant-induced arthritis dins, are highly effective for both the prophylactic and in rodents (see Hall, Starnes, Lee and Waddell, J. acute treatment of migraine. Pharm. Sci., (1979), 68,537). This article does not, how As to the causes of arthritic conditions, the suppres ever, suggest that any sesquiterpene lactone has phar sion of prostaglandin synthesis by non-steroidal anti-in maceutical activity against any complaint, let along flammatory drugs such as aspirin or indomethacin 45 against migraine. strongly implicates prostaglandins as inflammatory me diators at least in rheumatoid arthritis. Prostaglandin SUMMARY OF THE INVENTION like material is present in inflammatory perfusates of By repeated selective extraction of feverfew material, experimental animals. The E-prostaglandins in low con and extensive in vitro testing of the extracts for biologi centrations are striking potentiators of the pain-produc 50 cal activity, in particular spasmolytic activity in smooth ing properties of other agonists such as histamine, 5 muscle tests, we have found surprisingly that, of the hydroxytryptamine and plasmakinins (e.g. bradykinin) very many constituents of the plant, extracts containing as well as other features of the inflammatory response certain of the compounds within the range of sesquiter such as increased vascular permeability, erythema, pene lactones present have properties strongly indica white cell accumulation and platelet aggregation. 55 tive of efficacy in the treatment of migraine. This is Patients with bronchial asthma and chronic bronchi particularly surprising because the existence of some tis suffer attacks of wheezing and difficulty in breathing. such compounds in the plant has been known for many These are due to bronchial narrowing from spasm of the years and yet there has been no disclosure or suggestion bronchial smooth muscle or from sticky secretions, or anywhere in the literature that they possess any useful more commonly from a combination of the two. The activity against migraine. Furthermore, at least some of precise causes of the bronchoconstriction in asthma the reports on the use of feverfew in the treatment of have not been fully elucidated, but it is believed endoge migraine suggest taking an aqueous extract of the plant nous neurohumoral and autocoid spasmogens such as as "tea'. This points away from sesquiterpene lactones acetylcholine, 5-hydroxytryptamine (serotonin), hista being active ingredients since they are unlikely to be mine, some prostaglandins and leukotrienes may be 65 extracted from the plant by this method. involved. Allergic reactions to substances in inhaled The indications are that such compounds are alos dust or those absorbed from food may be manifested by likely to be efficacious in the treatment not only of bronchoconstriction or urticaria ("nettle-rash') or cir migraine but also of bronchial asthmas and arthritic 4,758,433 3 4 conditions such as rheumatoid arthritis, osteoarthritis thritis: prostaglandins, histamine, 5-hydroxytryptamine and related arthritides. This could not have been pre and bradykinin; in the case of asthma: histamine, 5 dicted from the completely unrelated cytotoxic activity hydroxytryptamine, bradykinin, acetylcholine, prosta reported by Lee et al (see above). glandins and the leukotrienes. We have surprisingly found a plant extract which has 5 All of these endogenous substances have in common biological activity strongly indicative of excellent phar the ability to cause smooth muscle to contract (i.e. go maceutical use, especially in the treatment of migraine, into spasm). Any drug which will act as an antagonist to asthma or arthritic conditios. The extract is a sesquiter a wide variety of chemically dissimilar spasmogens is pene lactone-containing extract from the plant Tanace termed a non-selective antagonist or a spasmolytic tum parthenium (hereinafter
Load more

Recommended publications
  • The Single Cyclic Nucleotide-Specific Phosphodiesterase of the Intestinal Parasite Giardia Lamblia Represents a Potential Drug Target
    RESEARCH ARTICLE The single cyclic nucleotide-specific phosphodiesterase of the intestinal parasite Giardia lamblia represents a potential drug target Stefan Kunz1,2*, Vreni Balmer1, Geert Jan Sterk2, Michael P. Pollastri3, Rob Leurs2, Norbert MuÈ ller1, Andrew Hemphill1, Cornelia Spycher1¤ a1111111111 1 Institute of Parasitology, Vetsuisse Faculty, University of Bern, Bern, Switzerland, 2 Division of Medicinal Chemistry, Faculty of Sciences, Amsterdam Institute of Molecules, Medicines and Systems (AIMMS), Vrije a1111111111 Universiteit Amsterdam, Amsterdam, The Netherlands, 3 Department of Chemistry and Chemical Biology, a1111111111 Northeastern University, Boston, Massachusetts, United States of America a1111111111 a1111111111 ¤ Current address: Euresearch, Head Office Bern, Bern, Switzerland * [email protected] Abstract OPEN ACCESS Citation: Kunz S, Balmer V, Sterk GJ, Pollastri MP, Leurs R, MuÈller N, et al. (2017) The single cyclic Background nucleotide-specific phosphodiesterase of the Giardiasis is an intestinal infection correlated with poverty and poor drinking water quality, intestinal parasite Giardia lamblia represents a potential drug target. PLoS Negl Trop Dis 11(9): and treatment options are limited. According to the Center for Disease Control and Preven- e0005891. https://doi.org/10.1371/journal. tion, Giardia infections afflict nearly 33% of people in developing countries, and 2% of the pntd.0005891 adult population in the developed world. This study describes the single cyclic nucleotide- Editor: Aaron R. Jex, University of Melbourne, specific phosphodiesterase (PDE) of G. lamblia and assesses PDE inhibitors as a new gen- AUSTRALIA eration of anti-giardial drugs. Received: December 5, 2016 Accepted: August 21, 2017 Methods Published: September 15, 2017 An extensive search of the Giardia genome database identified a single gene coding for a class I PDE, GlPDE.
    [Show full text]
  • Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017
    Q UO N T FA R U T A F E BERMUDA PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 BR 111 / 2017 The Minister responsible for health, in exercise of the power conferred by section 48A(1) of the Pharmacy and Poisons Act 1979, makes the following Order: Citation 1 This Order may be cited as the Pharmacy and Poisons (Third and Fourth Schedule Amendment) Order 2017. Repeals and replaces the Third and Fourth Schedule of the Pharmacy and Poisons Act 1979 2 The Third and Fourth Schedules to the Pharmacy and Poisons Act 1979 are repealed and replaced with— “THIRD SCHEDULE (Sections 25(6); 27(1))) DRUGS OBTAINABLE ONLY ON PRESCRIPTION EXCEPT WHERE SPECIFIED IN THE FOURTH SCHEDULE (PART I AND PART II) Note: The following annotations used in this Schedule have the following meanings: md (maximum dose) i.e. the maximum quantity of the substance contained in the amount of a medicinal product which is recommended to be taken or administered at any one time. 1 PHARMACY AND POISONS (THIRD AND FOURTH SCHEDULE AMENDMENT) ORDER 2017 mdd (maximum daily dose) i.e. the maximum quantity of the substance that is contained in the amount of a medicinal product which is recommended to be taken or administered in any period of 24 hours. mg milligram ms (maximum strength) i.e. either or, if so specified, both of the following: (a) the maximum quantity of the substance by weight or volume that is contained in the dosage unit of a medicinal product; or (b) the maximum percentage of the substance contained in a medicinal product calculated in terms of w/w, w/v, v/w, or v/v, as appropriate.
    [Show full text]
  • Penile Injection Therapy | Memorial Sloan Kettering Cancer Center
    PATIENT & CAREGIVER EDUCATION Penile Injection Therapy This information will help you learn to inject medication into your penis. This is called penile injection therapy. Penile injections can help you achieve an erection if you have erectile dysfunction (ED). Read this resource carefully before starting injection therapy. If you do not follow the instructions in this resource, your doctor or APP may stop prescribing your penile injection medications and supplies. About Penile Injection Therapy The tissue that causes you to get an erection (erectile tissue) is a muscle. Going long periods of time without an erection is unhealthy for erectile tissue and may damage it. We believe having erections keeps erectile tissue healthy. A penile injection helps you have an erection. It works best if it’s given about 5 to 15 minutes before you want an erection. Penile Injection Therapy 1/19 Giving Yourself the Injection Your advanced practice provider (APP) will review the instructions below with you. Generally, the training for the injections takes 2 office visits. Please be aware that each visit may take up to 1 hour, so you should plan your schedule on the day of your appointment. Use this resource to help you the first few times you inject on your own. Do not take the following medications within 18 hours of injecting (before or after): Sildenafil (Viagra®) - 20 mg to 100 mg Vardenafil (Levitra®) - 10 mg to 20 mg Avanafil (Stendra®) - 50 mg to 200 mg If you take tadalafil (Cialis®) 10 mg or 20 mg, do not inject within 72 hours (3 days) of taking the medication.
    [Show full text]
  • Meeting Materials)
    California State Board of Pharmacy BUSINESS, CONSUMER SERVICES AND HOUSING AGENCY 1625 N. Market Blvd, N219, Sacramento, CA 95834 DEPARTMENT OF CONSUMER AFFAIRS Phone: (916) 574-7900 GOVERNOR EDMUND G. BROWN JR. Fax: (916) 574-8618 www.pharmacy.ca.gov ENFORCEMENT AND COMPOUNDING COMMITTEE REPORT April 18, 2017 Amy Gutierrez, PharmD, Licensee Member, Chair Allen Schaad, Licensee Member, Vice Chair Greg Lippe, Public Member Stan Weisser, Licensee Member Valerie Muñoz, Public Member Ricardo Sanchez, Public Member I. Call to Order, Establishment of Quorum, and General Announcements II. Public Comments on Items Not on the Agenda/Agenda Items for Future Meetings Note: The board may not discuss or take action on any matter raised during this public comment section that is not included on this agenda, except to decide whether to place the matter on the agenda of a future meeting. [Government Code sections 11125, 11125.7(a)] III. Enforcement Matters a. University of California, San Diego’s Pilot Program to Permit Patients to Access Medications from an Automated Drug Delivery System Not Immediately Adjacent to the Pharmacy Background At the April 2015 Board Meeting, the board approved an 18-month pilot study under the auspices of the University of California, San Diego (UCSD) School of Pharmacy involving use of an automated drug delivery system (ADDS) for prescription medication from which staff of Sharp Hospital in San Diego and their families, who opted in, could pick up their outpatient medications. Consultation would be provided via telephone before medication could be dispensed to a patient for first time fills. Since that time the committee has received quarterly updates on the study, including usage of the system.
    [Show full text]
  • (Medical and Mechanical) Treatment of Erectile Dysfunction
    130 SOP Conservative (Medical and Mechanical) Treatment of Erectile Dysfunctionjsm_12023 130..171 Hartmut Porst, MD,* Arthur Burnett, MD, MBA, FACS,† Gerald Brock, MD, FRCSC,‡ Hussein Ghanem, MD,§ Francois Giuliano, MD,¶ Sidney Glina, MD,** Wayne Hellstrom, MD, FACS,†† Antonio Martin-Morales, MD,‡‡ Andrea Salonia, MD,§§ Ira Sharlip, MD,¶¶ and the ISSM Standards Committee for Sexual Medicine *Private Urological/Andrological Practice, Hamburg, Germany; †The James Buchanan Brady Urological Institute, The Johns Hopkins Hospital, Baltimore, MD, USA; ‡Division of Urology, University of Western, ON, Canada; §Sexology & STDs, Cairo University, Cairo, Egypt; ¶Neuro-Urology-Andrology Unit, Department of Physical Medicine and Rehabilitation, Raymond Poincaré Hospital, Garches, France; **Instituto H.Ellis, São Paulo, Brazil; ††Department of Urology, Section of Andrology and Male Infertility, Tulane University School of Medicine, New Orleans, LA, USA; ‡‡Unidad Andrología, Servicio Urología Hospital, Regional Universitario Carlos Haya, Málaga, Spain; §§Department of Urology & Urological Reseach Institute (URI), Universiti Vita Saluta San Raffaele, Milan, Italy; ¶¶University of California at San Francisco, San Francisco, CA, USA DOI: 10.1111/jsm.12023 ABSTRACT Introduction. Erectile dysfunction (ED) is the most frequently treated male sexual dysfunction worldwide. ED is a chronic condition that exerts a negative impact on male self-esteem and nearly all life domains including interper- sonal, family, and business relationships. Aim. The aim of this study
    [Show full text]
  • Author Index Page Numbers in Italics Refer to Bibliography
    Author Index Page Numbers in italics refer to bibliography Aaron,T.H., Criep,L.H. 180. Adams,M.R., see Litchfield,J. Albert,A., Serjeant,E.P. 176, 207 T., Jr. 386, 409, 432, 441, 207 Aaron, T. H., see Criep, L. H. 465,496 Albert,J.R., see Lish,P.M. 398,427 Adamson,D.W., Barrett,P.A., 449, 465, 466, 495 Aarsen,P.N., Zeegers,A. 15, Billinghurst, J. W., Green, A. Albert, U., see Giertz, H. 444, 30 F .. Jones,T.S.G. 190,192, 489 Abbozzo, G., Genazzani, E., 207 Alberty,J. 387,425, 442, Donatelli, L. 562,570 Adamson, D. W., Barrett, P. A., 452--455,480 Abdel-Galil, A. A. M., Marshall, Billinghurst,J. W., Jones, T. Alberty, J., Huurrekorpi, L. P. B. 114, 122 S.G. 190,207 399, 425, 455, 480 Aborg, e.-H .. Novotny,J., Adamson, D. W., Billinghurst, Alberty,J., Schiede,M. 399, Uvniis,B. 86.90 J.W. 189,194,207 425,455,480 Aborg,e. H., Uvniis,B. 87, 90 Adashek, D., Grossman, M. I. Alberty, J., Takkunen, R. 467, Aborg, C.-H., see Uvniis,B. 58. 46,47,55 480 74. 75, 82, 84-87. 92 Adlerova, E., see Protiva, M. Albinus,M., Sewing.K.F. 2, Abram, L. E., see Cohen, M. B. 201, 212 3, 6, 8, 11, 21, 30, 264, 287, 421,427 Ado,A.D., Abrossimow,W.N. 463,480 Abrams,G., see Lear,E. 566, 453.480 Albrecht, I., see Cort, J. H. 579, 571 Ado, A. D., Ishimova, L. M., 597 Abramson, D.
    [Show full text]
  • The Current Treatment of Erectile Dysfunction Maria Isabela Sarbu Carol Davila University, Department of Dermatology and Venereology, Isabela [email protected]
    Journal of Mind and Medical Sciences Volume 3 | Issue 2 Article 4 2016 The current treatment of erectile dysfunction Maria Isabela Sarbu Carol Davila University, Department of Dermatology and Venereology, [email protected] Mircea Tampa Carol Davila University, Department of Dermatology and Venereology Mădălina I. Mitran Victor Babes Hospital for Infectious and Tropical Diseases, Department of Dermatology and Venereology Cristina I. Mitran Victor Babes Hospital for Infectious and Tropical Diseases, Department of Dermatology and Venereology Vasile Benea Victor Babes Hospital for Infectious and Tropical Diseases, Department of Dermatology and Venereology See next page for additional authors Follow this and additional works at: http://scholar.valpo.edu/jmms Part of the Endocrine System Diseases Commons, Marriage and Family Therapy and Counseling Commons, Psychiatry and Psychology Commons, Reproductive and Urinary Physiology Commons, and the Urology Commons Recommended Citation Sarbu, Maria Isabela; Tampa, Mircea; Mitran, Mădălina I.; Mitran, Cristina I.; Benea, Vasile; and Georgescu, Simona R. (2016) "The current treatment of erectile dysfunction," Journal of Mind and Medical Sciences: Vol. 3 : Iss. 2 , Article 4. Available at: http://scholar.valpo.edu/jmms/vol3/iss2/4 This Review Article is brought to you for free and open access by ValpoScholar. It has been accepted for inclusion in Journal of Mind and Medical Sciences by an authorized administrator of ValpoScholar. For more information, please contact a ValpoScholar staff member at [email protected]. The current treatment of erectile dysfunction Authors Maria Isabela Sarbu, Mircea Tampa, Mădălina I. Mitran, Cristina I. Mitran, Vasile Benea, and Simona R. Georgescu This review article is available in Journal of Mind and Medical Sciences: http://scholar.valpo.edu/jmms/vol3/iss2/4 J Mind Med Sci.
    [Show full text]
  • Pharmaco-Induced Erections for Penile Color-Duplex Ultrasound: Oral PDE5 Inhibitors Or Intracavernosal Injection?
    International Journal of Impotence Research (2012) 24, 191 -- 195 & 2012 Macmillan Publishers Limited All rights reserved 0955-9930/12 www.nature.com/ijir ORIGINAL ARTICLE Pharmaco-induced erections for penile color-duplex ultrasound: oral PDE5 inhibitors or intracavernosal injection? Y Yang1,2, J-l Hu1,2,4,YMa1,2, H-x Wang1,2, Z Chen3, J-g Xia3, Y-x Wang1,2, Y-r Huang1,2 and B Chen1,2 To prospectively compare the clinical responses and penile color-duplex ultrasound (PCDU) results of oral PDE5 inhibitors (PDE5-Is) with papaverine intracavernosal injection (ICI) and to evaluate whether PDE5-Is could be used as alternatives to vasoactive agent injections, 25 ED patients underwent PCDU three times with an interval of at least 1 week, using different pharmacological induction: ICI mode (30--60 mg papaverine), sildenafil mode (100 mg sildenafil) and tadalafil mode (20 mg tadalafil). The preference of the patients was collected when all tests were completed. No significant differences were found in peak systolic velocity and acceleration time among all three modes. However for the ICI mode, end diastolic velocity of the right cavernosal artery was significantly higher than those of the sildenafil and tadalafil modes 5 min after erection induction, and at 15 min it became lower than those of two PDE5-I modes. Consequently, resistance index of the right cavernosal artery in ICI mode was reversed at 5 and 15 min. In all, 60.0 and 56.0% patients managed to reach full erection in PDE5-Is modes, which was significantly lower than in ICI mode (80.0%).
    [Show full text]
  • Papaverine Hydrochloride Injection, Solution American Regent, Inc
    PAPAVERINE HYDROCHLORIDE- papaverine hydrochloride injection, solution American Regent, Inc. Disclaimer: This drug has not been found by FDA to be safe and effective, and this labeling has not been approved by FDA. For further information about unapproved drugs, click here. ---------- PAPAVERINE HYDROCHLORIDE INJECTION, USP Rx Only This product is to be used by or under the direction of a physician. Each vial contains a sufficient amount to permit withdrawal and administration of the volume specified on the label. DESCRIPTION Papaverine Hydrochloride, USP, is the hydrochloride of an alkaloid obtained from opium or prepared synthetically. It belongs to the benzylisoquinoline group of alkaloids. It does not contain a phenanthrene group as do morphine and codeine. Papaverine Hydrochloride, USP, is 6,7-dimethoxy-1- veratrylisoquinoline hydrochloride and contains, on the dried basis, not less than 98.5% of C20H21NO4•HCI. The molecular weight is 375.85. The structural formula is as shown. Papaverine Hydrochloride occurs as white crystals or white crystalline powder. One gram dissolves in about 30 mL of water and in 120 mL of alcohol. It is soluble in chloroform and practically insoluble in ether. Papaverine Hydrochloride Injection, USP, is a clear, colorless to pale-yellow solution. Papaverine Hydrochloride, for parenteral administration, is a smooth-muscle relaxant that is available in vials containing 30 mg/mL. Each vial also contains edetate disodium 0.005%. The 10 mL vials also contain chlorobutanol 0.5% as a preservative. pH may be adjusted with sodium citrate and/or citric acid. CLINICAL PHARMACOLOGY The most characteristic effect of papaverine is relaxation of the tonus of all smooth muscle, especially when it has been spasmodically contracted.
    [Show full text]
  • Order in Council 1243/1995
    PROVINCE OF BRITISH COLUMBIA ORDER OF THE LIEUTENANT GOVERNOR IN COUNCIL Order in Council No. 12 4 3 , Approved and Ordered OCT 121995 Lieutenant Governor Executive Council Chambers, Victoria On the recommendation of the undersigned, the Lieutenant Governor, by and with the advice and consent of the Executive Council, orders that Order in Council 1039 made August 17, 1995, is rescinded. 2. The Drug Schedules made by regulation of the Council of the College of Pharmacists of British Columbia, as set out in the attached resolution dated September 6, 1995, are hereby approved. (----, c" g/J1"----c- 4- Minister of Heal fandand Minister Responsible for Seniors Presidin Member of the Executive Council (This pan is for adnwustratlye purposes only and is not part of the Order) Authority under which Order Is made: Act and section:- Pharmacists, Pharmacy Operations and Drug Scheduling Act, section 59(2)(1), 62 Other (specify): - Uppodukoic1enact N6145; Resolution of the Council of the College of Pharmacists of British Columbia ("the Council"), made by teleconference at Vancouver, British Columbia, the 6th day of September 1995. RESOLVED THAT: In accordance with the authority established in Section 62 of the Pharmacists, Pharmacy Operations and Drug Scheduling Act of British Columbia, S.B.C. Chapter 62, the Council makes the Drug Schedules by regulation as set out in the attached schedule, subject to the approval of the Lieutenant Governor in Council. Certified a true copy Linda J. Lytle, Phr.) Registrar DRUG SCHEDULES to the Pharmacists, Pharmacy Operations and Drug Scheduling Act of British Columbia The Drug Schedules have been printed in an alphabetical format to simplify the process of locating each individual drug entry and determining its status in British Columbia.
    [Show full text]
  • EUROPEAN PHARMACOPOEIA 10.0 Index 1. General Notices
    EUROPEAN PHARMACOPOEIA 10.0 Index 1. General notices......................................................................... 3 2.2.66. Detection and measurement of radioactivity........... 119 2.1. Apparatus ............................................................................. 15 2.2.7. Optical rotation................................................................ 26 2.1.1. Droppers ........................................................................... 15 2.2.8. Viscosity ............................................................................ 27 2.1.2. Comparative table of porosity of sintered-glass filters.. 15 2.2.9. Capillary viscometer method ......................................... 27 2.1.3. Ultraviolet ray lamps for analytical purposes............... 15 2.3. Identification...................................................................... 129 2.1.4. Sieves ................................................................................. 16 2.3.1. Identification reactions of ions and functional 2.1.5. Tubes for comparative tests ............................................ 17 groups ...................................................................................... 129 2.1.6. Gas detector tubes............................................................ 17 2.3.2. Identification of fatty oils by thin-layer 2.2. Physical and physico-chemical methods.......................... 21 chromatography...................................................................... 132 2.2.1. Clarity and degree of opalescence of
    [Show full text]
  • Drug Delivery to the Back of the Eye Following Topical Administration: an Update on Research and Patenting Activity
    Send Orders for Reprints to [email protected] Recent Patents on Drug Delivery & Formulation 2014, 8, 27-36 27 Drug Delivery to the Back of the Eye Following Topical Administration: An Update on Research and Patenting Activity Sai H.S. Boddu*, Himanshu Gupta and Soohi Patel Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, Ohio, USA – 43614 Received: December 31, 2013; Revised: January 26, 2014; Accepted: January 29, 2014 Abstract: Drug delivery to the back of the eye following topical administration remains an unmet need for the scientific community. Treatment of posterior segment diseases requires localized and long-term drug delivery to the retina, choroid, and Bruch’s membrane. Until the last decade, there was limited evidence from large clinical trials that demonstrated the usefulness of pharmacotherapy compared to laser therapy or other vitreoretinal surgical techniques for the treatment of retinal diseases. This paradigm has shifted in recent years, with strong evidence demonstrating superior efficacy of oph- thalmic drugs compared to previous gold standards. However, ophthalmologists are left with no options other than admin- istering the therapeutics via implants and intravitreal injections, which are highly invasive and associated with patient non-compliance. A non-invasive topical therapy would enhance patient compliance and minimize the side-effects associ- ated with intraocular implants and intravitreal injections. In an attempt to enhance patient compliance, the focus of re- search has shifted to the development of novel small molecule-based eye drop formulations. This review article discusses the relevant patents and summarizes the resurgence in the treatment of posterior segment eye diseases through topical drug administration.
    [Show full text]