Norsulfazole structural formula. Pharmaceutical chemistry - Kulbakh V.O. General methods of quantitation

II. Pharmacological

Based on the ability of sulfonamides to be eliminated from the body over time:

It is necessary to increase the first doses of sulfonamides by 2–3 times (loading dose). It is necessary for the next doses to be maintenance.

III. Depending on the application:

1. On lung microorganisms.

2. On the intestines (phthalazole).

3. Urinary tract (urosulfan).

4. Microflora of the eyes (sodium sulfacyl).

general description: Sulfonamide preparations are white or white with a yellowish tint, odorless crystalline substances. The exceptions are sulfapyridazine, which is yellow in color, and salazopyridazine, which is an orange powder.

Common authenticity reactions:

1. For the free amino group:

A. Diazotization – nitrogen coupling:

b. Lignin test:

2. With Br 2, I 2:

3. On the sulfo group. Wet mineralization:

4. Pyrolysis. They give melts with individual coloring:

5. The presence of acidic properties in sulfanilamide allows, if necessary, to obtain a sodium derivative and then react with copper sulfate (see the colors of the reaction products in the table below):

6. It is also possible to carry out hydrolysis and determine substituents (The presence of phthalic acid in phthalazole makes it possible to carry out a reaction with resorcinol).

7. For the azo group (discoloration occurs):

8. Sodium derivatives react with Na (flame coloring and with zinc acetate).

NaCl + Zn[(UO 2) 3 (CH 3 COO) 8 ] + CH 3 COOH + 9H 2 O à NaZn[(UO 2) 3 (CH 3 COO) 9 ] 9H 2 O¯ + HCl

9. Solutions of sulfonamide drugs in the presence of caustic alkalis, with the addition of a 1% solution of sodium nitroprusside and subsequent acidification with mineral acid, form red or red-brown colored solutions (streptocide, soluble streptocide, sulgin, sulfacyl sodium, urosulfan) or precipitates (ethazol, norsulfazole, sulfadimezin).

Name	Solubility	Effects of reactions
H2O	HCl	NaOH	Private
NaOH, CuSO 4	Swims.
Streptocide.	MR	LR	R	Green-turquoise
Streptocide soluble.	R	LR	LR	Green	Purple-blue color, smell of ammonia and aniline
Sulgin.	OMR	t°	-	Blue solution	Purple-red color, ammonia smell
Etazol.	Poland	MR	LR	Grass-green sediment turning black	Dark brown color, smell of hydrogen sulfide
Norsulfazole.	OMR	R	R	Dirty purple precipitate fading to dark purple	Dark brown color, smell of hydrogen sulfide
Sulfadimezin.	Poland	LR	LR	Yellow-green precipitate turning into red-brown	Dark brown color
Phthalazol.	Poland		LR	Dirty gray-turquoise	Dark brown color
Salazodimethoxin.	MR		LR		Dark brown color
Urosulfan.	MR	LR	LR	Bright turquoise, needle-like crystals appear on the wall of the test tube when standing	Purple-red color, ammonia release
Sulfacyl-Na.	LR			The sediment is blue with a greenish tint (bluish-turquoise)	Dark brown color
Salazopyridazine.	MR		LR	Green-brown	Dark brown color
Sulfapyridazine-Na.				Taupe

General methods of quantification:

1. Nitritometry.

2. Bromatometry: The method is based on the halogenation reaction of sulfonamides. Titrate with a solution of potassium bromate in an acidic medium in the presence of bromide. The end of the titration is determined either by the discoloration (with bromine) of the methyl orange indicator, or iodometrically:

KBrO 3 + 5KBr + 6HCl à 3Br 2 + 6KCl + 3H 2 O

Br 2 + 2KI à I 2 + 2KBr

3. Reverse iodatometry f=1/4. KIO 3.

4. Reverse iodochlorometry: Like bromatometry, this method is based on the halogenation reaction. Iodization is carried out using a titrated hydrochloric acid solution of iodine chloride. The excess of the latter is determined iodometrically:

ICl + KI à I 2 + KCl

I 2 + 2Na 2 S 2 O 3 à 2NaI + Na 2 S 4 O 6

5. Acid-base titration.

A. acidimetry for sodium salts: Titrant HCl, indicator – methyl orange in an alcohol-acetone medium. f=1.

b. alkalimetry if K dis of a sodium derivative is equal to 10 -7 -10 -8.

V. if Kdis = 10 -9, then use titration in non-aqueous media:

Titrant is a solution of sodium methoxide in the presence of dimethylformamide (DMF). BTS indicator: color transition from yellow to blue. See phthalazole.

6. Argentometry (Mohr’s method only) – see phthalazole.

7. Physico-chemical methods of analysis

A. Photometry.

b. UV spectroscopy.

V. Refractometry.

g. Polarography.

Streptocidum (Streptocide)

p-Aminobenzenesulfamide.

Description

Solubility: Slightly soluble in water, easily in boiling water, in diluted HCl, solutions of caustic alkalis and acetone, difficult in alcohol.

Authenticity:

1. The drug gives characteristic reactions to primary aromatic amines.

2. The drug is heated, a violet-blue melt is formed and the smell of ammonia and aniline is felt (unlike other sulfonamide drugs).

1. When heated with alkali, an ammonia smell is observed:

2. When streptocide is exposed to oxidizing agents, for example hydrogen peroxide, and then iron III chloride, a red-violet color appears (the chemistry has not been fully studied, but apparently the amino group is somehow converted into an OH group, through which it goes reaction with ferric chloride).

Purity:

1. Melting point.

2. Acidity.

3. General acceptable impurities: chlorides, sulfates, organic impurities, sulfate ash and heavy metals.

quantitation:

1. Nitritometry. f=1

Storage: List B, in a well-closed container.

Application: streptocide is used to treat tonsillitis, erysipelas, cystitis, pyelitis, enterocolitis, for the prevention and treatment of wound infections and other infectious diseases.

Release form: powder; tablets of 0.3 and 0.5 g in a package of 10 pieces; 10% ointment; 5% liniment.

Streptocidum solubile (Streptocide soluble)

para-Sulfamido-benzolaminomethane-sodium sulfate.

Description: White crystalline powder.

Solubility: Soluble in water. Practically insoluble in organic solvents.

Authenticity:

1. Reactions to the primary aromatic amino group after hydrolysis.

2. Formation of aurine dye after hydrolysis with c.H 2 SO 4 (difference from streptocide):

3. The drug gives a characteristic reaction to Na +, unlike streptocide (colors the burner flame yellow).

1. Reaction with hydrogen peroxide and iron III chloride gives a cherry-red color.

Purity:

1. Transparency and color.

2. pH=4.0 - 5.0.

3. Weight loss during drying.

4. General acceptable impurities: chlorides, heavy metals.

5. A specific impurity - sodium sulfite, is determined by titration with a 0.01 M solution of I 2.

quantitation: Nitritometry after hydrolysis.

Storage: List B. In well-sealed jars.

Application: indications for use are the same as for streptocide. Good solubility in water allows the drug to be used for parenteral use. Solutions can be administered subcutaneously, intramuscularly and intravenously.

Release form: powder.

Sulginum. Sulfaguanidine*. Sulgin

p-Aminobenzenesulfoguanidine.

Description: White fine crystalline powder

Solubility: Very little soluble in water and in alkali solutions, little in alcohol, with diluted hydrochloric and nitric acids it forms salts that are soluble in water.

Authenticity:

2. The drug is heated, a violet-red melt is formed and the smell of ammonia is felt (destruction of the guanidine residue):

Where R is the sulfanilic acid residue. This reaction combines sulgin with urosulfan, but distinguishes it from all other sulfonamide drugs.

3. To distinguish sulgin from urosulfan, shake sulgin with alkali and add 2 - 3 drops of phenolphthalein to the solution - the solution will turn red. Urosulfan does not give this reaction.

Purity:

1. Melting point.

2. Acidity.

3. Loss of weight during drying.

4. General acceptable impurities: chlorides, sulfates, organic impurities, sulfate ash and heavy metals.

quantitation: Nitritometry.

Storage

Application: prescribed orally for adults and children for acute, subacute and chronic bacterial dysentery, for colitis and enterocolitis with diarrhea. It is also used in cases of carriage of dysentery bacilli and typhoid bacilli, in preparation for operations on the large and small intestine.

Release form: powder; tablets of 0.5 g in a package of 10 pieces.

Aethazolum, Sulfaethidole* (Etazol)

2-(p-Aminobenzenesulfamido)-5-ethyl-1,3,4-thiadiazole.

Description

Solubility: Practically insoluble in water; soluble in alcohol, easily in alkali solutions, slightly soluble in dilute acids.

Authenticity:

1. Gives reactions to primary aromatic amines.

2. A specific reaction is a test with salts of heavy metals: with a solution of copper sulfate, a grass-green precipitate is formed, turning black.

Purity:

1. Melting point.

2. Color of the solution.

3. Acidity.

4. General acceptable impurities: chlorides, sulfated ash and heavy metals, sulfates.

quantitation: Nitritometry.

Storage: List B. In a well-closed container.

Application: used for pneumonia, dysentery, pyelitis, cystitis, erysipelas, sore throat, peritonitis, wound infections.

Release form

Norsulfazolum, Sulfathiazole* (Norsulfazole)

2-(p-Aminobenzenesulfaido)-thiazole.

Description: White or white with a slightly yellowish tint, crystalline powder, odorless.

Solubility: Very little soluble in water, little in alcohol, soluble in diluted mineral acids and solutions of caustic and carbonic alkalis.

Authenticity:

2. When CuSO4 solution is added to the alkaline filtrate, a dirty purple precipitate is formed (unlike other sulfonamide drugs)

3. The drug is heated in a dry test tube, a dark brown melt is formed and a strong smell of hydrogen sulfide is felt (unlike other sulfonamide drugs, except phthalazole).

Purity:

1. Melting point.

2. Acidity.

3. General acceptable impurities: sulfates, chlorides, sulfate ash and heavy. Meh.

quantitation: Nitritometry.

Storage: List B. In a well-closed container.

Application: taken orally for pneumonia, meningitis, staphylococcal and streptococcal sepsis and other infectious diseases.

Release form: powder; tablets of 0.25 and 0.5 g in a package of 10 pieces.

Sulfadimezinum. Sulfadimidine* (Sulfadimezin)

2-(p-Aminobenzenesulfamido)-4,6-dimethyl pyrimidine.

Description: White or slightly yellowish crystalline powder.

Solubility: Practically insoluble in water, easily soluble in acids and alkalis.

Authenticity:

1. The drug gives a characteristic reaction to aromatic primary amines.

2. When a CuSO4 solution is added to the alkaline filtrate, a yellowish-auto-green precipitate is formed that quickly turns brown (unlike other sulfonamide drugs)

3. The drug gives a violet color with a solution of oxidized sodium nitroprusside (difference from other sulfonamide drugs).

Purity:

1.Melting point

2. Acidity.

3. Transparency and color of the solution.

4. General acceptable impurities: sulfates, sulfate ash and heavy metals, chlorides.

quantitation: Nitritometry.

Storage: List B. In a well-closed container, protected from light.

Application: for pneumococcal, streptococcal, meningococcal infections, sepsis, gonorrhea, as well as for infections caused by E. coli and other microorganisms.

Release form: powder; tablets of 0.25 and 0.5 g in a package of 10 pieces.

Phthalazolum, Phthalylsulfathiazole* (Phthalazole)

2-(p-Phthaliloaminobenzenesulfamido)-thiazole.

Description: White or white with a slightly yellowish tint powder.

Solubility: Practically insoluble in water, very slightly soluble in alcohol. Soluble in aqueous sodium carbonate solution.

Authenticity:

1. On the primary amino group after acid hydrolysis.

2. Add resorcinol and sulfuric acid and fuse in the flame of an alcohol lamp for 1-2 minutes. Then cool, dissolve in alkali, dilute with water. Green fluorescence (GF 10) is observed. This is a reaction to phthalic acid resulting from hydrolysis:

Purity:

Free phthalic acid– determined by adding phenolphthalein. The acidic properties of phthalic acid prevent the solution from turning pink.

Norsulfazole– determined nitritometrically (by the primary amino group). The content of norsulfazole should not exceed permissible limits.

quantitation:

1. (GF) Non-aqueous titration in DMF. Indicator: thymol blue. Titrant - NaOH in a mixture of methyl alcohol and benzene (sodium methoxide is obtained). Titrate until a blue color appears.

2. (Not GF) Argentometry (using Mohr's method) - see phthalazole.

2AgNO 3 + K 2 CrO 4 à AgCrO 4 ¯ + 2KNO 3

2HNO 3 + Na 2 B 4 O 7 + 5H 2 O à 4H 3 BO 3 + 2NaNO 3

Application: for dysentery (acute and chronic in the acute stage), colitis, gastroenteritis, as well as for surgical interventions on the intestines to prevent purulent complications.

Storage: List B. In a well-closed container.

Salazodimethoxinum (Salazodimethoxin)

5-(p-phenylazo)-salicylic acid

Description: Brownish-orange, odorless, fine-crystalline powder.

Solubility: Practically insoluble in water, very slightly soluble in alcohol, easily soluble in sodium hydroxide solution.

Application: having anti-inflammatory and antibacterial effects in the intestines.

Storage: List B. In a place protected from light.

Urosulfanum, Sulfacarbamid* (Urosulfan)

p-Aminobenzenesulfonylurea.

Description: White crystalline powder, odorless.

Solubility: Slightly soluble in water, slightly soluble in alcohol, easily soluble in diluted acids and solutions of caustic alkalis.

Authenticity:

1. General reactions to primary amines.

2. Heat with 1 ml of 5% sodium nitrite solution to a boil - ruby ​​red color (specific reaction).

quantitation: nitritometry.

Application: Used for cystitis, pyelitis, cystopyelitis, pyelonephritis, infected hydronephrosis and other urinary tract infections. Most effective for pyelitis and cystitis without urinary disorders.

Storage: List B. In a well-closed container.

Sulfacylum-natrium, Sulfacetamidum natricum* (Sulfacylum-sodium)

p-Aminobenzenesulfacetamide sodium.

Description: White crystalline powder, odorless.

Solubility: Easily soluble in water, practically insoluble in alcohol.

Authenticity:

1. General reactions to primary aromatic amines.

2. Reaction of formation of copper salt. The sediment is bluish-green.

quantitation: nitritometry.

Application: The drug is effective against streptococcal, gonococcal, pneumococcal and coli-bacillary infections.

Storage: List B (except ointment). The powder is stored in a container protected from light; solutions and ointments - in a cool place, protected from light.

Salazopyridazinum, Salazodin* (Salazopyridazine)

5-(p-phenylazo)-salicylic acid.

Description: Fine crystalline orange powder.

Solubility: Salazopyridazine is practically insoluble in water, slightly soluble in alcohol, soluble in sodium hydroxide solution.

Authenticity:

Specific reaction (discoloration of salazopyridazine solution).

1. Phthalic acid in phthalazole is determined by the formation reaction of fluorescein (sulfuric acid in the presence of resorcinol).

green fluorescence

2. Salazopyridazine turns orange due to the chromophore of the azo group when exposed to zinc dust in an alkaline environment.

Purity.

1. Transparency and color of an aqueous or alkaline solution depending on pH.

2. Limit of acidity and alkalinity.

5. Determination of the content of organic substances with sulfuric acid (charring).

Determination of specific impurities.

1. The limit of phthalic acid content in phthalazole is determined. It is highly soluble in water; phthalazole is practically insoluble in water; aqueous extraction is analyzed. FA is determined by the neutralization method (titrant – NaOH, indicator – phenolphthalein, f eq. = 1/2).

2. The limit for the content of norsulfazole in phthalazole is determined by the content of free Ar – NH 2, and conditions are created under which norsulfazole goes into solution. Norsulfazole is determined by nitritometry.

Quantitation.

1. Nitritometry (primary aromatic amino group)

2. Alclimetric neutralization method. The medium is protophilic solvent DMF. The protophilic solvent accepts a proton from sulfonamide drugs and thereby enhances the acidic properties of the drug.

Titrate with 0.1 M NaOH in a mixture (methanol + benzene) to enhance the nucleophilic properties, the indicator is thymol blue. Titrate to a blue color at the equivalence point:

f eq. =1, for phthalazole f eq. =1/2.

3. Acidimetric displacement method. For sodium sulfacyl, sodium sulfapyridazine. The method is based on the displacement of a weak organic acid from its salt under the action of a hydrochloric acid titrant. Indicator: a mixture of methyl orange and methylene blue. Color transition from green to purple.

4. Halogenation method: bromatometric, iodometric, iodochlorometric. Based on the property of drugs to react with S E . Bromatometry, a back titration method, is most often used. Titrant KBrO 3 in the presence of KBr in an acidic medium, indicator – methyl orange. At the equivalence point, a drop of free Br 2 destroys the indicator and discoloration occurs.

5. FEC – photoelectrocolorimetric method. Use colored reaction products with aldehydes, with heavy metal salts, and the reaction of azo dye formation (construct a calibration graph).

6. SFC – in the visible region of the spectrum.

7. Polarography

Storage. List B.

Application. As antibacterial agents.

Release form. Powders, tablets (orally), some water-soluble drugs - in the form of injections, sodium sulfacyl - eye drops, sodium sulfopyride 25-30% - eye drops.

Complex drug

Biseptol consists of two active ingredients: sulfamethoxazole and a diaminopyrimidine derivative - trimethoprim. Used for infections of the respiratory, urinary tract, and gastrointestinal tract. Has a prolonged effect.

3-(n-aminobenzenesulfamido)-2,4-diamino-5-(3`,4`,5`-

5-methyloxazole. trimethoxybenzyl)-pyrimidine.

Literature

1. Belikov V.G. Textbook on pharmaceutical chemistry. - M.: Medicine, 1979. - 552 p.

2. Belikov V.G. Pharmaceutical chemistry. - M.: Higher school. 1985. - 768 p.

3. Glinka N.L. General chemistry: Textbook for universities. - 27th ed., stereotypical. / Ed. V.A. Rabinovich. - L.: Chemistry. 1988.-1079 pp.

4. State Pharmacopoeia of the USSR. - 10th ed. - M.: Medicine. 1968. - 1079 p.

5. State Pharmacopoeia of the USSR: Vol. 1. General methods of analysis / Ministry of Health of the USSR. - 11th ed., add. - M.: Medicine. 1987.-336p.

6. State Pharmacopoeia of the USSR: Issue 2. General methods of analysis. / Ministry of Health of the USSR. - 11th ed. add. - M.: Medicine. 1989. - 400 p.

7. Mashkovsky M.D. Medicines: In 2 volumes. T. 1. 14th ed., erased. - M.: New wave. 2001.-540s.

8. Mashkovsky M.D. Medicines: In 2 volumes. vol. 2.- 14th ed., erased. - M . New wave.2001.-608s.

9. Melentyeva G.A. Pharmaceutical chemistry. - 2nd ed. reworked and additional - T 1. - M.: Medicine. 1976. - 478 p.

10. Melentyeva G.A. Pharmaceutical chemistry. - 2nd edition reworked and additional - T.2.- M.: Medicine. 1976. - 478c.

11. International Pharmacopoeia. - Ed. 3rd-M., Geneva: Medicine. WHO. 1981-1990. T.1. General methods of analysis. - 242 pp.; T.2. Specification for quality control of pharmaceuticals. - 364s. T.3. Specification for quality control of pharmaceuticals. - 435c.

12. Methods of drug analysis / N.L. Maksyutina, F.E. Kagan, F.A. Mitchenko. - K.: 3dorovya, 1984. - 224 p.

13. Guide to laboratory classes in pharmaceutical chemistry / E.N. Aksenova., O.P. Andrianova., A.P. Arzamastsev, L.I. Kovalenko, etc. - M.: Medicine. 1987.-304 p.

14. Analysis of dosage forms manufactured in pharmacies / M.I. Kuleshova, L.N. Guseva, O.K. Sivitskaya - Manual. - 2nd ed. reworked and additional M: Medicine. 1989.-288p.

15. Directory of pharmacist-analyst / Ed. D.S. Volokh, N.P. Maksyutina. - K.: Health. 1989. - 200 p.

16. Guide to laboratory classes in pharmaceutical chemistry: Textbook. manual./ E.N. Aksenova, O.P. Andrianova, A.P. Arzamastsev and others; Edited by A.P. Arzamastsev. - 2nd ed., revised. and additional - M.: Medicine, 1995.-320 p.

17. Plemenkov V.V. Introduction to the chemistry of natural compounds. – Kazan:, 2001 – 376 p.

18. Terney A. Modern organic chemistry, vol. 1, 2 - M.: Mir, 1981.

1. When assessing the quality of norsulfazole and streptocide in samples of several batches, the appearance did not meet the requirements of the ND in the “Description” section - the powders were wet and yellow in color. Give justification for the reasons for changes in their quality under this section in accordance with storage conditions and properties. Provide a set of tests to characterize the quality of norsulfazole and streptocide.

· Give their chemical formulas, Latin and rational names, characterize the structure, justifying the physical and chemical properties of each of them (appearance, solubility in water, spectral characteristics) and the possibility of using them to assess the quality of the substance.

· Suggest group and differentiating reactions for their detection in drugs.

· Give methods for the quantitative determination of streptocide and norsulfazole.

Streptocide and norsulfazole are derivatives of n-aminobenzenesulfamide (sulfanilic acid amide). They differ in the character of the R in the sulfamide group. They are acidic forms of sulfonamide and exhibit amphoteric properties:

Basic properties due to the aromatic NH 2 group (solubility in acids)

Acidic properties due to the H imide group (solubility in alkalis)

They are white or white with a slightly yellowish tint, odorless crystalline powders, streptocide - slightly, norsulfazole - very slightly soluble in water, soluble in alcohol, soluble in solutions of mineral acids, solutions of caustic and carbonated alkalis.

Tpl.str.=164-167° Tpl.norst.=198-203° (with unfolded)

Spectral characteristics:

1) Streptocide, 0.0008% solution in 0.01 M NaOH or lmax = 251 nm; 0.015% solution in 1M HCI lmax = 264, 271 nm, lmin = 241, 268 nm and shoulder from 257 to 261 nm.

2) Norsulfazole

Authenticity:

Based on qualitative reactions to functional groups.

1) Reaction caused by an aromatic amino group (general)

1.1 GF X reaction of azo dye formation

Azo dye (cherry red)

1.2 Condensation reaction

1.3 Oxidation reaction

2) Reaction of pyrolysis (thermal decomposition) of GF X

Streptocide forms a purple melt and ammonia is released

Norsulfazole forms a dark brown melt and there is a strong smell of hydrogen sulfide

Pb(CH 3 COO) 2 + H 2 S PbS ↓ + 2CH 3 COOH

3) Reaction caused by the sulfamide group (acidic properties, formation of complex salts).

According to GF X for norsulfazole - a difference reaction: a dirty purple precipitate is formed with CuSO 4.

Dirty fillet sediment

4) Reaction of the benzene ring (halogenation)

Quantitation:

1) GF X nitritometry, based on the property of primary ar. amino groups form diazonium salts

feq =1 FPT

Ind tropeolin 00 (norsulfazole)

tropeolin 00 + m/blue (streptocide)

In t.eq. 2KBr + 2NaNO 2 + 4HCI Br 2 + 2NO + 2KCI + 2NaCI + 2H 2 O

	Discoloration Ind

Conditions – cooling (18°-20°, 0°-10°) so that diazonium salts do not decompose;

catalyst – KBr

2) UV spectrophotometry is possible, the concentration of a certain substance is based on a comparison of the absorption of the test substance with the absorption of RSO.

Cx = Cst×Dx / Dst

Solvent 0.1M NaOH or HCI; region l = 210-360nm

Storage: in a well-closed container.

Samples of several series did not meet the requirements of the RD in the “Description” section; the powders were wet and yellow in color, because storage conditions were not met - they became damp in humid air and, having reducing properties due to the aromatic amino group, oxidized to quinoneimide and turned yellow.

Procainamidi Hydrochloridum *

B-Diethylaminoethylamide P-aminobenzoic acid hydrochloride

C 13 H 21 N 3 O HC1 ​​M. c. 271.79

Description. White or white with a slightly creamy tint crystalline powder, odorless.

Solubility. Very soluble in water, easily soluble in alcohol, slightly soluble in chloroform, practically insoluble in ether.

Storage. List B. In well-closed dark glass jars.

The highest single oral dose is 1.0 g.

The highest daily dose orally is 4.0 g.

The highest single dose into a vein is 1.0 g.

The highest daily dose into a vein is 3.0 g.

See also the article “Solutio Novocainamidi 10% pro injectionibus”.

Antiarrhythmic drug.

458. Norsulfazolum

Norsulfazole

Sulfathiazolum*

2- (P-Aminobenzenesulfamido)-thiazole

C 9 H 9 N 3 O 2 S 2 M.c. 255.32

Description. White or white with a slightly yellowish tint, odorless crystalline powder.

Solubility. Very slightly soluble in water, slightly soluble in alcohol, sparingly soluble in acetone, practically insoluble in ether, soluble in dilute mineral acids and solutions of caustic and carbonic alkalis.

Storage. List B. In a well-closed container.

Antibacterial agent.

460. Norsulfazolum- sodium

Norsulfazole sodium

Norsulfazolum solubile

Norsulfazole soluble

Sulfathiazolum Natricum *

2- (P-Aminobenzenesulfamido)-thiazole-sodium

C 9 H 8 N 3 NaO 2 S 2 bH2O M. c. 385.39

Description. Lamellar, shiny, colorless or odorless crystals with a slightly yellowish tint.

Solubility. Easily soluble in water.

Storage. List B. In a container protected from moisture and light.

The highest single oral dose is 2.0 g.

The highest daily oral dose is 7.0 g.

Antibacterial agent.

488. Oxacillinum- sodium

Oxacillin sodium salt

Sodium salt of 3-phenyl-5-methyl-4-isoxazolyl-penicillin monohydrate

C l 9 H 18 N 3 NaO 5 S H 2 O M. c. 441.4

The content of the amount of penicillins in the preparation is not less than 90% and the content of C l 9 H 18 N 3 NaO 5 S H 2 0 is not less than 90%. Note. When determining activity by biological method, the total activity of the drug (sum of penicillins) must be at least 820 µg/mg(U/l(g) (p. 943). Theoretical activity of oxacillin sodium salt monohydrate 909 mcg/mg. One microgram of chemically pure anhydrous oxacillin acid corresponds to a specific activity equal to one Action Unit (AU). The accuracy of the determination should be such that the confidence limits at P=95% deviate from the mean value by no more than ±5% (p. 963). The average value of the activity found must be at least 820 µg/mg(U/mg).

Description. White fine crystalline powder, bitter taste. Resistant in a slightly acidic environment and to the action of penicillinase.

Solubility. Easily soluble in water, slightly soluble in 95% alcohol, slightly soluble in chloroform, practically insoluble in acetone. ether and benzene.

Storage. List B. In a dry place, at room temperature. For doses see page 1028. Antibiotic.

486. Osarsollim