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Alkaloids indol

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Title: Alkaloids indol


1
Lecture ?25
  • Alkaloids indols derivatives, purine alkaloids
    and their salts some synthetic analogues
    according to the biological action as substances
    of the medical drugs and components of the dosage
    forms.
  • Ass. Medvid I. I.

2
Indole - condensed system of pyrrole and
benzene cycles which have two share
atomsIndole is a structural basis of
physostigmine, strychnine, reserpine alkaloids.
3
Group reaction on indole derivatives Van-Urks
reaction
4
  • In the base of reaction is the process of
    electrophyllic substitution. Reagent
    p-dimethylaminobenzaldehyde. Reaction conducts at
    the presence of conc. H2SO4 and FeCl3 as oxidant.
  • Derivatives of indole which have free 2 and 3
    positions give this reaction. Reserpine gives
    this reaction by the opening of ring C in the
    presence of acids, as a result position 2 becomes
    free.
  • Product of reaction can exist in 2 forms. Color
    of the reaction product depends on the chemical
    structure of primer compounds conditions of the
    reaction. Van-Urks reaction can be hold with
    another aldehyde. So, for reserpine solution of
    vanillin in chloride acid is used.

5
Physostigmine salicylate (Physostigmini
salicylas)Eserini salicylas
  • Salicylate of ester of methylcarbaminic acid and
    eseroline or 5-methylcarbaminoiloxy-1,3,1-trimeth
    yl-2,3,2,3-tetrahydropyrrole indole

6
Physostigmine the main alkaloid of calabaric
beans (Faba calabarica) poisonous seeds of West
African plant Physostigma venenosus , Fabaceae
7
  • Physical properties
  • Physostigmine salicylate - brilliant
    colorless or almost colourless prismatic
    crystals. Soluble in water, easily soluble in
    alcohol, practically insoluble in ether. Aqueous
    solutions are unstable. It melts at about 182 C,
    with decomposition Optic active compound. When
    heated with water easy hydrolyze and therefore
    its solutions for parenteral usage produce in
    aseptic introductions. On the air and light
    product paints in the red color pharmacological
    inactive rubrezerine formed.
  • Pharmacological action cased by the
    methylurethane group.
  • Proserine - white crystalline powder with
    bitter taste. Very easily soluble in water,
    easily soluble in alcohol and chloroform, ether.
    Hygroscopic. Becomes pink on the light.

8
  • Identification of Physostigmine salicylate
  • Melting point, the specific rotation.
  • Substance gives reaction to salicylates (2
    reactions in SPU).
  • Total Pharmacopeial reaction on alkaloids (with
    Dragendorff's reagent)
  • After evaporation of the preparation with
    ammonium forms blue residue (physostigmine base),
    which is dissolved in ethanol with formation of a
    blue solution which after the acidification by
    ??3???? becomes red.
  • Drug solution in H2SO4 conc. gradually becomes
    yellow.
  • Erdman and Frede reagents with medication give
    reddish-yellow color, with HNO3 conc. yellow
    color.

9
  • 7. When heated with alkalis (and gradually when
    heated with water) physostigmine salycilate
    hydrolyzed and appears character odor
    methylamine
  • 8. At the heating with 0,1 ninhydrine solution
    in conc. H2SO4 on the water bath at 60 0? during
    10 min. And than after cooling solution have
    green fluorescence. Proserine gives blue
    fluorescence at this conditions.
  • 9. At the gradually adding to the solution boric
    acid, 0,1 ? solution of nitrate acid and sodium
    nitrite, after 1 min. add sodium hydroxide
    solution, violet color appears.

10
Assay Physostigmine salicylate
  • Alkalimetriya, direct titration . The drug is
    dissolved in a mixture of ethanol and chloroform
    and titrated by 0,1 ? N??? to the pink color
    (indicator phenolphthalein). ? ?.m.
  • Acidimetry in non-aqueous medium. The drug is
    dissolved in a mixture of chloroform and conc.
    CH3COOH, titrated by 0,1 ? ?Cl?4. For
    determination of the end-point use potentiometry.
    Equivalent point is fixed by potentiometric
    method. ? ?.m./2.
  • Complexonometry, reverse titration. As a stable
    titrant acetic-acidic solution of bismuth nitrate
    is used in the presence of potassium iodide.
    Scheme of reaction
  • Product of the interaction is filtrated
    and an excess of reagent is titrated by 0,1 ?
    sodium EDTA solution. ? ?.m.

11
  • STORAGE and USAGE of Physostigmine salicylate
  • In an airtight containers of dark
    glass, protected from light. Poison compound.
  • Cholinesterase inhibitor, myotic
    mean (atropine antagonist). Used for the
    treatment of glaucoma as 0,25-1 eye drops.
    Introduce subcutaneous 0,1 -1,0 solution the
    neuromuscular diseases (Alzheimer's disease). H.
    d. 0,0005 g, H. d. d. 0,001 g.

12
Synthetic substitute of physostigmine Proserine
(Proserinum) Neostigmine methylsulfate
  • N-(m-dimethylcarbamoiloxiphenyl)-N,N,N-trimethylam
    monium methylsulfate

13
  • Identification of proserine
  • Reaction to methylsulfate-ion. If after heating
    the drug with HNO3 conc. add solution of BaCl2,
    white precipitate falls (BaSO4).
  • With a solution of iodine preparation forms brown
    sediment of periodide.
  • At the heating of drug with alkali dissolution
    of urethane group takes place (m-dimethylaminophen
    ol formed, which is detected by the condensation
    with diazotative sulfanylic acid cherry-red
    color (azo-dyes))

14
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15
  • Assay
  • The modified K'yeldal method. The drug is boiled
    in a K'yeldal flask with NaOH. Dimethylamine,
    which evaporates, distilled with water vapor in
    the receiver with a solution of boric acid.
    Metaborate and tetraborate of dimethylamine
    formed, which are titrated by 0,1 ? solution of
    HCl (mixed indicator). ? ?.m.

16
  • STORAGE and USAGE of proserine
  • In an airtight containers of dark glass,
    protected from light. Poison compound.
  • Substitute of physostigmine.
    Anticholinesterase, antimyasthenic mean. Curare
    antagonist drugs. Used for treatment of
    myasthenia, paralysis, neuritis, atony of
    intestine and urinary bladder, glaucoma, for
    stimulating labor activity as 0,25-1 as eye
    drops.
  • Issue tablets 0,015 g, amp. 0,05-1,0.
  • H. d., internally 0,015 g, H. d. d.,
    internally 0,05 g H. d. subcutaneous 0,002
    g, H. d. d. s/c 0,006 g.

17
Strychnine nitrate (Strychnini nitras)
  • Cycles ??, BD, ED derivatives of indole.
  • Cycle ? aromatic and strychnine can be
    nitrated and halogenated.
  • N19 tertiary atom, has a base character and
    gives salts with acids.
  • N9 is in the lactam group, which may be
    disclosed by the interaction with alcohol
    solution of KOH with formation of carboxyl and
    secondary amino-groups.

18
Strychnine can be found with brucine in the seeds
of tropical plant Strychnos Nux Vomica (emetic
nut)
19
Reserpine (Reserpinum)

11,17-dimethoxy-16-carbmethoxy-18(3,4,5,-trimet
hoxibenzoyloxy)-alloyohimban
20
  • Reserpine molecule contains indole (??),
    dihydroquinolysidine (?D),
  • partially hydrogenated 3-carbolynic (???),
    hydrogenated isoquinoline (ED) cycles.

Alloyohiban
21
Reserpine contains in the roots of the plant
Rauwolfia serpentina Benth
22
  • Physical properties
  • Strychnine nitrate - a colorless brilliant
    crystals with very bitter taste. Difficultly
    soluble in water and alcohol, easily soluble in
    boiling water, practically insoluble in ether.
  • Reserpine - colorless, white or slightly
    yellow, small crystals or crystalline powder with
    melting point 261-265?. Insoluble in water,
    soluble in chloroform, acetone, pyridine and
    ether, darkening slowly on the exposure to
  • light. Optic active compound. At the heating with
    acids or alkalis hydrolysis takes place
    (reserpinic acid, methanol, trimethoxybenzoic
    acid form).

23
  • Identification of strychnine nitrate
  • Pharmacopeial reaction on alkaloids.
  • Solution of the drug in H2SO4 conc. crystal of
    K2Cr2O7 formed the blue-violet strips which
    pass into the red and lilac-green.
  • Vitali-Morens reaction. At the interaction with
    HNO3 conc. drug becomes yellow (as opposed to
    brucine, which becomes blood-red) by nitration of
    benzene cycle ? after the evaporation of
    reaction product the residue gives with alcohol
    solution of ??? formed red-violet color.
  • Van-Urks reaction (on indole cycles). With 1
    vanillin in glycerol in the presence of H2SO4
    dil. Pink-violet color appears.

24
  • 5. Reaction on nitrate ions NO3-
  • ?) SPU. The interaction with nitrobenzene in the
    presence of sulfate acid
  • Quantity of substance, listed in a separate
    article, add to the mixture of 0,1 ml of
    nitrobenzol R and 0,2 ml of sulfate acid R and
    after 5 min. cooled in ice water. Continuing to
    cool slowly and while stirring add 5 ml of water
    R, 5 ml of sodium hydroxide concentrated solution
    R NaOH, 5 ml of acetone R, shake and put for
    standing the apper layer becomes dark purple.
  • b) SPU, N. Not discolors potassium permanganate
  • The solution of the substance,
    acidified by acid sulfate diluted R H2SO4, not
    discolors solution of 1 g/l potassium
    permanganate R (difference of nitrite ).
  • ?) Not pharmacopeial reaction. Interaction with
    iron (??) sulfate FeSO4 in the medium of conc.
    H2SO4 brown ring is formed (FeSO4?NO) (on the
    clock glass )
  • 2 Strychnine?NO3 6FeSO4 4H2SO4 2NO
    3Fe2(SO4)3 (Strychnine)2?2SO4 4H2O
  • NO Fe2 SO42 ? Fe(NO)SO4

25
  • d) Unpharmacopeial reaction. Interaction with
    diphenylamine in acidic medium. (conc. H2SO4),
    formed an bright blue organic dye
  • diphenylbenzidine
  • Sulfimmonium salt of diphenylbenzidine (blue dye)

26
  • Identification of reserpine
  • Specific optical rotation (6 assymetric carbon
    atoms).
  • UV-spectroscopy (chromophor groups indole and
    trimethoxybenzoatic acid 2 maximum of
    absorption on UV-spectrum).
  • Reactions of indole cycle. With chloric water
    purple, with KMnO4 dark lilac, with vanillin
    in the presence of HCl - pink, with ?2?2
    yellow-lilac color.
  • Water solutions of reserpine in UV-light blue
    fluorescence.
  • Alcohol solution of the preparation H2SO4
    NaNO2 green fluorescence.

27
  • With Frede reagent red color, which goes to the
    blue.
  • On ester groups
  • ?) alkali hydrolysis
  • ?) hydroxame sample.
  • Van-Urks reaction. With p- dimethylaminobenzaldeh
    yde H2SO4 ??3???? green coloring that goes
    into the red. With vanillin in chloride acid
    pink color.

28
Assay
  • Strychnine nitrate Alkalimetry, direct
    titration. Titration of the drug in
    alcohol-chloroform solution of 0,1 ? NaOH
    (phenolphthalein indicator).
  • ? ?.m.
  • Specific additive - brucine.
  • Reserpine Acidimetry in non-aqueous medium.
    Hatch is titrated in the medium of anhydrous
    ??3???? by 0,1 ? solution HClO4 (indicator
    crystal violet) to the appearance of green color.
    ? ?.m.

29
Storage, usage
  • Reserpine
  • In airtight containers, in a dark place. Powder
    - poisonous substance.
  • Neuroleptic , treatment of hypertension.
    Included in tablets Adelphane (0.1 mg of
    reserpine,10 mg of dihydralasine), Adelphan
    esidrex (Triresid) (Adelfane 10 mg of
    dichlorothiazide), Adelphane esidrex -?
    (Triresid ?)(0,6 g of ??l), Crystepin,
    Neocrystepin. Raunatinethe amount of Rauwolfia
    alkaloids.
  • Strychnine nitrate
  • In airtight containers. Poison compound.
  • CNS stimulant, tonic mean.
  • Issue - amp. 0,1-1,0.
  • H. d. s/c 0,002 g H. d. d. s/c 0,005 g.

30
Alkaloids, purine derivatives Purine condensed
system of pyrimidine and imidazol
If in the core of purine hydrogen atoms in the
pyrimidine nucleus replaced by hydroxyl groups,
we will get xantine
31
Caffeine is contained in coffee beans (Coffea
arabica), tea leaves (Thea sinensis), cola (Cola
acuminata)
32
  • Pharmacology
  • Caffeine stimulates the central nervous system
    first at the higher levels, resulting in
    increased alertness and wakefulness, faster and
    clearer flow of thought, increased focus, and
    better general body coordination, and later at
    the spinal cord level at higher doses. Once
    inside the body, it has a complex chemistry, and
    acts through several mechanisms as described
    below.
  • Metabolism and half-life

33
  • Theophylline first was isolated from tea leaves
    (Thea sinensis)
  • Theobromine is extracted from cocoa beans
    (Theobroma cacao)

34
Three natural alkaloids, derivatives xantine
caffeine, theophylline, theobromine
  • Extracted from semi-synthetic uric acid, guanine
    and urea.

35
Very convenient is the method of extraction of
caffeine and theobromine from xantine, which can
be extracted from uric acid (waste poultry farms)
and guanine (fish flakes, waste of paper)

36
Synthesis of caffeine and theophyllin by method
Hmelevskiy - Abramova( firs was synthesed by
Traube in1900 year).
37
Caffeine Medications
  • Caffeine (??ff??nu?) , Caffeine monohydrate
    (??ff??nu? monohydricum) (SPhU)
  • 1,3,7-Trimethyl-3,7-dihydro- 1H-purine-2,6-dione
  • 1,3,7-trimethylxantine
  • Caffeine-sodium benzoate (Coffeinum-natrii
    benzoas)

38
Physical properties
  • Caffeine - White or almost white, crystalline
    powder or silky crystals, sublimes readily.
    Moderately soluble
  • in water, freely soluble in boiling water,
    slightly soluble in ethanol and ether. Soluble in
    the concentrated solutions of alkali benzoate or
    salicylates. Very weak base, forms unstable salts
    with acids by nitrogen in position 9.
  • Caffeine-sodiume benzoate white powder,
    odorless, bitter taste.
  • Easily soluble in water, slightly soluble in
    ethanol. Contains 38-40 caffeine.
  • Extracted by the mixing and evaporation to the
    dry state of aqueous solutions containing
    equimolar quantity of caffeine and sodium
    benzoate.

39
General Pharmacopeial reaction - a reaction on
xantines (Murexide reaction or reaction on purine
alkaloids)
40
Identification of caffeine
  1. By the physico-chemical constants melting point,
    IR-spectroscopy.
  2. With potassium iodide in iodine in the presence
    of HCl dil.- brown precipitate formed(periodide
    ?8?10N4?2J2HJ), which dissolves in NaOH dil.
    solution at the neutralization.
  3. Murexide sample.
  4. Unpharmacopoeial reaction - with 1 solution of
    tannin white precipitate dissolved in excess of
    reagent.
  5. With HgCl2 white crystalline sediment, which is
    a complex compound with the following content
    C5H10N4O2 HgCl2.
  6. With acetylacetone and dimethylaminobenzaldehyde.
    Solution of the substance in a mixture of
    acetylacetone and dil. NaOH heated in a water
    bath, cooled, than add solution of
    dimethylaminobenzaldehyde and heat again, cool
    and add water - appears an intense blue color

41
Caffeine monohydrate gives all reactions on
caffeine after a preliminary drying at 100-105
C.
42
Identification of caffeine-sodium benzoate
  • 1. Caffeine identify by
  • a) melting temperature (234-237 C) after
    extraction by chloroform from alkaline solution
  • b) Murexide sample
  • c) reaction with 1 solution of tannin
  • d) reaction with iodine solution
  • 2. Sodium benzoate identify by
  • e) the reaction with solution of iron (III)
    chloride - pink-yellow sediment
  • f) the sodium cation paints the flame in yellow
    color.

43
Assay
  • Caffeine
  • Acidimetry in non-aqueous medium in a mixture of
    acetic acid anhydrous, acetic anhydride and
    toluene, a direct titration. Potentiometric
    indication, the control experiment (??.m).
  • Iodometry, reverse titration, indicator - starch
    (??.m/4).
  • Cerimetry, reverce titration, with iodometric
    ending. An excess of cerium is neutralized by
    potassium iodide solution. Sodium thiosulfate
    used as titrant. (??.m/4).
  • Caffeine-sodium benzoate
  • Caffeine content is determined by iodometric
    method (??.m/4). ). In the dry matter it should
    be 38,0 - 40,0 .
  • Sodium is determined in the presence of mixed
    indicator (methyl orange solution and methylene
    blue at a ratio of 11) and ether (for the
    extraction of benzoic acid, available in the
    titration) (??.m). Sodium benzoate in the dry
    matter must be not less than 58,0 and not more
    than 62,0 .

44
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45
Cerimetric determination of caffeine
  • 2 Ce(SO4)2 2 KI ? I2 K2SO4 Ce2(SO4)3
  • I2 2 Na2S2O3 ? 2 NaI Na2S4O6

46
Storage, Usage
  • Caffeine-sodium benzoate
  • In a dry, dark place.
  • Central nervous system stimulant, cardiotonic
    mean. Thanks to the solubility in water used in
    the form of injection solutions. Issue - powder,
    tablets 0,1 and 0,2 g, 0,075 g (for children)
    10 ? 20 solutions in amp. by 1,0-2,0 ml.
    Included in the tablets Anaprylline, Pentalgin.
  • Caffeine
  • In a dry, dark place.
  • Central nervous system stimulant, cardiotonic
    mean, at the angiospasms enuresis in children
    stimulant of mental and physical disability,
    poisoning with drugs. Produced as powder.
  • Caffeine monohydrate is part of the tablets
    Theophedrine, Cytramone, Cytropak, Askofene,
    Cofficyll, Cophetamine, Benalgin, Coldrex,
    Solpadein, Panadol-??????. Apply in doses by
    0,05-0,1 g as CNS stimulant.

47
  • Theobromine Theobrominum (SPhU)
  • 3,7-Dimethyl-3,7- dihydro-1?-purine-2,6-dione, or
    3,7- dimethylxantine
  • Theophylline monohydrate Theophyllinum
    monohydricum (SPhU)
  • 1,3-Dimethyl-3,7- dihydro-1?-purine-2,6-dione
    monohydrate, or monohydrate of 1,3-
    dimethylxantine

48
Properties
  • Theobromine
  • White crystalline powder, with bitter taste.
    very slightly soluble in water, ethanol ,ether
    and chloroform slightly soluble in hot water
    easily in dil. Solutions of alkalis and acids.
  • Theophylline
  • White crystalline powder. Sightly soluble in
    water, ethanol and chloroform easily soluble in
    hot water soluble in dil. Solutions of acids and
    alkalis.

Theobromine and theophylline - amphoteric
compounds with a predominance of acidic
properties (by moving the hydrogen atom at the
nitrogen atom in position 1 or 7).
49
Identification of theobromine
  1. IR-spectrophotometry.
  2. Dissolve the substance in ammonium solution at
    the heating. After cooling add silver nitrate
    solution solution must still be colorless.
    After the boiling during few minutes white
    precipitate formed.
  3. Reaction on xantines (murexide sample). At the
    oxidation of theobromine 3-methylalloxane and
    methylurea formed. Ammonium salt of
    dimethylpuepuric acid formed as a result of
    murexide reaction

50
  • Unpharmacopoeial reactions
  • Reaction of the sodium salt of theobromine,
    obtained by the interaction of alkali with an
    excess of preparation, with cobalt (II)chloride
    solution intense violet color appears, which
    quickly disappears, grey-blue precipitate

51
  1. The reaction of theobromine sodium salt with
    silver nitrate - formed a dense gelatin mass
    (silver salt), which is thinning by heating to
    80 ? and solidifies again at the cooling.
  2. With HgCl2 white crystalline precipitate.

52
Identification of theophylline
  1. Determination of the melting temperature alter
    the drying.
  2. IR spectrophotometry.
  3. Theophylline in the alkali medium decomposes to
    teophyllidine, which can be identified by the
    reaction of azojoining with diazonium salts, red
    color azo-dye formed.

53
  1. Determination of the water by semimicromethod (?.
    Fisher) (8-9,5 ).
  2. Reaction on xantines (murexide sample). At the
    oxidation of theophylline 1,3-dimethylalloxane
    and urea. Ammonium salt of tetramethylpuepuric
    acid forme as a result of murexide reaction

54
  1. The reaction of theobromine sodium salt obtained
    by the interaction of alkali with an excess of
    drug, with a solution of cobalt (II) chloride -
    formed white with pink tinge precipitate of
    cobalt salt.
  2. With HgCl2 white crystalline precipitate.
  3. With alkali solution of sodium nitroprusside
    green color formed dissappears at the adding an
    excess of acid.

55
  • The reaction of theobromine sodium salt with
    silver nirate - formed a dense gelatin mass.
  • Theophylline with 2,6-dichloroqiunonechloroimide
    in borate
  • buffer solution
  • (?? 8,5) gives intense blue
  • merocyanic dye

56
AssayTheophylline and TheobromineAlkalimetry by
the substituent (indirect alkalimetry).Indicator
phenolphthalein (theobromine) or Bromothymol
blue (theophylline). ? ?.m.
57
Storage, usage
  • Theophylline
  • In airtight containers, place protected
    from light.
  • Non-selective phosphodiesterase inhibitor
    (xanthine) treatment of reversible airways
    obstruction. Broncholitic, cardiotonic and
    diuretic mean with moderate influence on the
    stagnation phenomena in the cardiac and renal
    origin organs. Issue powder and tablets by 0,1
    and 0,3 g amp. 2-5,0 candles by 0,2 g. Teopek,
    Theotard, Neophylline, Euphylline. Included in
    tablets Theoephedrine.
  • Theobromine
  • In airtight containers, place protected from
    light.
  • Stimulates the activity of the heart, somewhat
    expands the coronary vessels and bronchi, shows
    diuretic effect. Issue - powder and tablets by
    0,25 g.
  • Included in tablets Theminal (with amidopyrine
    and Phenobarbital), Theodibaverine (with
    papaverine and dibazole), Theoephedrine.

58
Pentoxifylline (Pentoxifyllinium)Agapurine,
Pentyline, Trental A synthetic analogue of
theobromine
  • 3,7-dimethyl-1-(5-oxohexyl)-3,7-dihydro-7?-purine
    -2,6-dion or 1-(5-oxohexyl)-theobromine

59
Identification of pentoxifylline
  • Temperature of melting
  • IR-spectroscopy
  • TLC
  • Reaction on xantines
  • Formation of azo-dye (look theophylline)
  • Assay
  • pentoxifylline
  • Acidimetry in non-aqueous media in a mixture of
    anhydrous acetic acid and acetic anhydride,
    direct titration. Potentiometric indication.
    (??.m).

60
Usage of pentoxifylline
  • Has a vasodilator effect, improves tissue oxygen
    supply, decreases thrombosis aggregation and
    reduces blood viscosity. Apply at the peripheral
    circulatory disorders, atherosclerotic disorders,
    ischemic condition after heart attack, in
    ophthalmology, at the hearing disorders. Issue
    tablets of 0,1 g, ampoules of 2-5,0. Adopt
    inside by 0,2 g 3 times daily after meals. In
    the acute disorders of peripheral or cerebral
    circulation injected 0,1 g intravenous in 250-500
    ml of NaCl or 5 glucose solution.

61
Synthetic analogues of theophylline
  • Theophylline-ethylenediamine (Theophyllinum et
    ethylenediaminum) (SPhU),
  • Euphylline (Euphyllinum), Aminophilline

Theophylline
with 1,2-ethylenediamine White, sometimes with
yellowish crystalline powder with slight ammonia
odor. On the air absorbs carbon dioxide, thus
decreasing its solubility. Soluble in water,
aqueous solutions have an alkaline reaction.
62
Identification of euphylline
  • 1. Theophylline is identified after the
    separation by HCl of ethylenediamine according
    to SPhU
  • ?) By the melting temperature of theophylline
    (269 - 274?) after HCl acidification to ?? 4-5
  • b) IR-spectroscopy
  • c) Reaction of azojoining (look theophylline)
  • d) murexide sample.

63
  • 2. Ethylenediamine can be confirmed by the
    following reactions
  • ?) determination of the melting temperature of
    the product of reaction with benzoyl in alkali
    medium (dibenzoylethylenediamine) (SPhU)
  • b) with a solution of copper (II) sulfate a
    bright purple color forms
  • c) with 2,4-dinitrochlorobenzene yellow
    precipitate falls.

64
AssayEuphylline
  • Ethylenediamine can be determined by acidimetry,
    indicator methyl orange. ? ?.m./2.
  • Ethylenediamine in euphylline should be 13,515
    in the dry matter.
  • 2. Theophylline can be determined by
    alkalimetry by substituent 1 after drying in a
    drying cabinet at 25-130 ? to the disappearance
    of amine odor.
  • The content of waterless theophylline in
    euphylline should be 84- 87,4 .

65
Storage, usage of euphylline
  • Given the ability to absorb carbon dioxide,
    stored in a well corked filled to the end
    container, protected from the effects of light
    and moisture.
  • Antispasmodic, bronchodilatin, diuretic mean. At
    the bronchial asthma and bronchospasm,
    hypertension, cardiac asthma, to improve blood
    circulation to the brain, decreasing the
    intraperitoneal pressure and brain edema in
    ischemic stroke.
  • Used oral by 0,15g after food, i/v (2,4
    solutions by 5,0) and i/m (24 solution by 1
    ml).

66
Diprophylline (Diprophyllinum)
  • 7-(2',3'-Dioxipropyl)-theophylline
  • Less toxic than theophylline. Used for treatment
    of coronary spasm, cardiac and bronchial asthma,
    hypertension. Issue tablets by 0,2 g amp.
    10-5,0 candles by 0,5 g.

67
Xantinole nicotinate (Xantinoli nicotinas)
Complamine, Theonicol
  • Used to improve peripheral and cerebral
    circulation
  • Issue tablets by 0,15 g amp. 15-2,0 ?
    10,0.
  • 7-2-oxi-3-(N'-methyl-ß-oxiethylamino)-propyl-t
    heophylline nicotinate

68
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