Sulfasalazine

METHOD OF PREPARATION

Note: It is best to use the sulfasalazine powder when preparing this oral liquid. As an alternative, sulfasalazine immediate-release tablets can be used.

1. Calculate the required quantity of each ingredient for the total amount to be prepared.

2. Accurately weigh and/or measure each ingredient.

3. Mix the sulfasalazine with the glycerin to form a smooth paste.

4. Geometrically, incorporate the Ora-Plus and mix thoroughly.

5. Add sufficient Ora-Sweet or Ora-Sweet SF to volume and mix well.

6. Package and label.

PACKAGING

Package in tight, light-resistant containers.1

LABELING

Shake well before taking. Keep out of reach of children. Use only as directed.

STABILITY

A beyond-use date of 30 days would be appropriate for this preparation.1

USE

Sulfasalazine oral liquid is used in the treatment of inflammatory bowel disease and rheumatoid arthritis.2

QUALITY CONTROL

Quality-control assessment can include weight/volume, pH, specific gravity, active-drug assay, color, rheological properties/pourability, physical observation and physical stability (discoloration, foreign materials, gas formation, mold growth).3

DISCUSSION

Sulfasalazine 250 mg/5 mL was formerly manufactured by Pharmacia-Upjohn under the brand name of Azulfidine. The formulation presented here can be easily modified if a more or less concentrated preparation is required. Since this formulation is not the same as the commercial preparation, a conservative beyond-use date of 30 days is recommended.

Sulfasalazine (C^sub 18^H^sub 14^N^sub 4^O^sub 5^S, MW 398.39) occurs as a bright yellow or brownish-yellow, odorless, fine powder that melts at about 255°C with decomposition. It is very slightly soluble in alcohol (1 g in 2900 mL) and practically insoluble in water. It is soluble in aqueous solutions of alkali hydroxides. It should be protected from light.1

Glycerin (C^sub 3^H^sub 8^O^sub 3^, MW 92.10, glycerol, 1,2,3-propane triol) occurs as a clear, colorless, odorless, viscous, hygroscopic liquid with a sweet taste about two thirds as sweet as that of sucrose. It has a specific gravity of about 1.25 and a melting point of 17.8°C; if cooled to crystallization, it will need to be heated to about 20°C to melt. It is miscible with water, methanol and 95% ethanol; practically insoluble in oils and chloroform and slightly soluble in acetone. It is hygroscopic and should be stored in airtight containers in a cool place. It is not prone to oxidation but will decompose on heating. When mixed with water, ethanol and propylene glycol, the mixtures are chemically stable.4

Ora-Plus is an oral suspending vehicle that accepts dilution of up to 50% or more with water, flavoring agents or syrups and still retains its suspending properties. It has a pH of approximately 4.2 and an osmolality of about 230 mOsm/Kg. It is a thixotropic vehicle with a viscosity of approximately 1000 cps at 25°C. It contains purified water, microcrystalline cellulose, sodium carboxymethylcellulose, xanthan gum, carrageenan, sodium phosphate and citric acid as buffering agents, simethicone as an antifoaming agent, and potassium sorbate and methylparaben as preservatives.5

Ora-Sweet syrup vehicle is a flavoring vehicle for oral extemporaneous preparations. It is flavored with a citrus-berry flavor blend and contains glycerin and sorbitol to prevent "cap-lock," a problem associated with many syrups. It is buffered to a pH of approximately 4.2 and has an osmolality of about 3240 mOsm/Kg. It contains purified water, sucrose, glycerin, sorbitol (5%), flavoring, sodium phosphate and citric acid as buffering agents, and potassium sorbate and methylparaben as preservatives.5

Ora-Sweet SF is a flavoring vehicle for oral extemporaneous preparations. It is a sugar-free, alcohol-free syrup flavored with a citrus-berry flavor blend. It is buffered to a pH of approximately 4.2 and may be used alone or in combination with other vehicles. It will tolerate a dilution to 50% with dissolved actives in water or suspending agents and still retain an acceptable taste. It has an osmolality of 2150 mOsm/Kg. It contains water, sodium saccharin, xanthan gum, glycerin, sorbitol, citric acid and sodium citrate as buffers; methylparaben, propylparaben and potassium sorbate as preservatives; and flavoring agents.5

REFERENCES

1. US Pharmacopeial Convention, Inc. United States Pharmacopeia 26-National Formulary 21. Rockville, MD:US Pharmacopeial Convention, Inc.; 2003:2197-2201, 2583.

2. Sweetman Sean C. MARTINDALE: The Extra Pharmacopeia. 33rd ed. London:Pharmaceutical Press; 2002:1251-1253.

3. Allen LV Jr. Standard operating procedure for performing physical quality assessment of oral and topical liquids. IJPC 1999;3:146-147.

4. Price JC. Glycerin. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington, DC:American Pharmaceutical Association; 2000:220-222.

5. Ora-Plus/Ora-Sweet/Ora-Sweet SF [product information]. Minneapolis, MN:Paddock Laboratories, Inc.

Copyright International Journal of Pharmaceutical Compounding Nov/Dec 2003
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