Omeprazole 2 mg/mL Suspension

US Pharm. 2020;45(10):46-47.

Method of Preparation: Hold neck of bottle containing the omeprazole powder; tap bottom edges on a hard surface to loosen powder. Remove cap from bottle. Tap top of induction seal liner to loosen any powder adhering to liner. Carefully and slowly peel back inner foil seal liner from bottle. Using enclosed tool, scrape any omeprazole powder from seal into bottle. Using smaller end of tool, with firm strength loosen any powder from inside lower edges of bottle. Ensure that no omeprazole powder remains trapped in inside lower edges of bottle. Using tool, distribute omeprazole powder evenly over bottom surface of bottle. Shake FIRST-PPI Suspension bottle for a few seconds. Open FIRST-PPI Suspension bottle; empty about one-half of contents into omeprazole powder bottle. Replace cap; vigorously shake omeprazole powder bottle for approximately 60 seconds. Empty remaining FIRST-PPI Suspension into omeprazole powder bottle. Allow suspension to drain for 10 seconds. Replace cap; shake omeprazole powder bottle vigorously for about 30 seconds. As appropriate, dispense enclosed adapter cap and oral syringe with accompanying instructions for use.

Use: Omeprazole is a proton pump inhibitor (PPI) used to treat gastric hyperacidity.

Packaging: Package in the containers in which it is provided and compounded.

Labeling: Keep out of reach of children. Protect from light. Protect from freezing. Shake well before each use. Refrigerate. Discard after ____ [time period].

Stability: A beyond-use date of not more than 30 days when stored at refrigerated temperature may be used.^1,2

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

Discussion: Omeprazole (Prilosec, C₁₇H₁₉N₃O₃S, MW 345.42) occurs as a white to off-white powder that melts with decomposition at about 155°C; it is a weak base. It is very slightly soluble in water (1 g in 8,000 mL) and sparingly soluble in alcohol (1 g in 25 mL). Its degradation rate increases with decreasing acidic pH values, but it has acceptable stability under alkaline conditions.⁴

Also available is a FIRST-Omeprazole Compounding Kit comprising omeprazole powder USP and FIRST-PPI Suspension containing artificial strawberry flavor, benzyl alcohol, FD&C Red #40, Magnasweet 100 (ammonium glycyrrhizate), poloxamer 188, propylene glycol, purified water, simethicone emulsion, sodium bicarbonate, sodium citrate (dihydrate), sucralose, and xanthan gum. The final compounded product provides a homogenous suspension containing 2 mg per mL of omeprazole in FIRST-PPI Suspension comparable to the active ingredient in Simplified Omeprazole Suspension.²

Benzyl alcohol (C₇H₈O, MW 108.14) is an antimicrobial preservative, disinfectant, and solvent. As an antimicrobial, it is commonly used in concentrations up to 2% in pharmaceutical formulations. It is a clear, colorless, oily liquid with a faint, aromatic odor and a sharp, burning taste. It is soluble 1 g in 25 mL of water and is miscible with ethanol.⁵

FD&C Red #40 (C₁₈H₁₄N₂Na₂O₈S₂ 496.42 g·mol^–1, Allura Red AC, FD&C Red 40, E129, Food Red 17) is a red azo dye occurring as a red powder with a melting point of 300°C. It is usually supplied as a sodium salt, but the calcium and potassium salts may be used. The salts are soluble in water. In solution, maximum absorbance lies at about 504 nm.⁶

Magnasweet (ammonium glycyrrhizate, C₄₂H₆₅NO₁₆-anhydrous MW 840.08; C₄₂H₆₅NO₁₆.5H₂O-pentahydrate, MW 930.04) is a white to yellowish-white or brown, hygroscopic, intensely sweet-tasting powder. It is used as a sweetening, flavoring, taste-masking, and emulsifying agent. It is slightly soluble in water and very slightly soluble in anhydrous ethanol.⁷

Poloxamer 188, a block copolymer of ethylene oxide and propylene oxide, occurs as white-colored, waxy, free-flowing granules that are practically odorless and tasteless. Poloxamers are used as emulsifying, solubilizing, and wetting agents. They are stable, and aqueous solutions are stable in the presence of acids, alkalis, and metal ions. Poloxamer 188 is freely soluble in water and alcohol.⁸

Propylene glycol (C₃H₈O₂) is a clear, colorless, viscous, hygroscopic, practically odorless liquid with a sweet taste somewhat resembling glycerin. It is miscible with acetone, chloroform, 95% ethanol, glycerin, and water.⁹

Simethicone {CH₃[Si(CH₃)₂.O]nSi(CH₃)_å, dimethyl silicone fluid, poly(dimethylsiloxane)} is a fluid silicone occurring as a clear, colorless, odorless liquid. It is insoluble in water, alcohol, acetone, and methyl alcohol.¹⁰

Sodium citrate dihydrate (trisodium citrate, C₆H₅Na₃O₇, MW 258.07, anhydrous; dihydrate, MW 294.10) occurs as colorless crystals or a white, crystalline powder. The hydrous form is freely soluble in water (1 g in 1.5 mL) and very soluble in boiling water (1 g in 0.6 mL); it is insoluble in alcohol.¹¹

Sucralose (Unisweet, C₁₂H₁₉C_l3O₈, MW 397.64) is a white to off-white, free-flowing, crystalline powder. It is freely soluble in ethanol (95%) and water (0.283 g/mL). Its sweetening power is about 300 to 1,000 times that of sucrose. It has no aftertaste.¹²

Xanthan gum (corn sugar gum) is a high-molecular-weight polysaccharide gum. It is a cream-colored or white, odorless, free-flowing, fine powder. It is soluble in cold or warm water but practically insoluble in ethanol and ether. It is used as a stabilizing agent and as a viscosity-increasing agent in suspensions. It is nontoxic, is compatible with most other excipients, and has good stability (in the presence of enzymes, salts, acids, and bases) and viscosity properties over a wide range (pH 3-12).¹³

REFERENCES

1. U.S. Pharmacopeia/National Formulary [current revision]. Rockville, MD: U.S. Pharmacopeial Convention, Inc; April 2019.
2. FIRST-Omeprazole package insert. Wilmington, MA: Cutis Pharma; October 2016.
3. Allen LV Jr. Standard operating procedure for performing physical quality assessment of oral and topical liquids. IJPC. 1999;3:146-147.
4. Allen LV Jr., ed. Remington: The Science and Practice of Pharmacy. 22nd ed. London, England: Pharmaceutical Press; 2013:1634-1635.
5. Quinn ME. Benzyl alcohol. In: Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:108-110.
6. Rappoport Z, ed. The Chemistry of Phenols. Chichester, England: John Wiley & Sons; 2004.
7. Quinn ME. Ammonium glycyrrhizate. In Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:73-74.
8. Pirjanian A, Alvarez-Nunez F. Poloxamer. In: Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:688-693.
9. Driver S. Propylene glycol. In: Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:795-798.
10. Sweetman SC, ed. Martindale: The Complete Drug Reference. 36th ed. London, England: Pharmaceutical Press; 2009:1770-1771.
11. Amidon GE. Sodium citrate dihydrate. In: Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:858-860.
12. Hutchins A, Mullarney MP. Sucralose. In Sheskey PJ, Cook WG, Cable CG, eds. Handbook of Pharmaceutical Excipients. 8th ed. London, England: Pharmaceutical Press; 2017:937-937.
13. Shah HC, Singh KK. Xanthan gum. In: Rowe RC, Sheskey PJ, Cook WG, Fenton ME, eds. Handbook of Pharmaceutical Excipients. 7th ed. London, England: Pharmaceutical Press; 2012:897-900.

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