Coenzyme Q10 100 mg and Lipoic Acid 100 mg Chewable Troches

US Pharm. 2011;36(2):60-61.

Method of Preparation: Calibrate the mold and adjust the gelatin troche base for the total amount of preparation needed. Calculate the quantity of each ingredient for the amount to be prepared. Accurately weigh or measure each ingredient. Mix together the coenzyme Q₁₀, lipoic acid, aspartame, acacia, and citric acid powders until uniform. Using a water bath, slowly melt the gelatin troche base until fluid. Incorporate the blended powders and mix until uniform. Remove from heat, add the flavor, and mix until uniform. Pour into the required number of molds. Cool, package, and label.

Use: This combination has been used as supplemental treatment in patients taking cholesterol-lowering agents.

Packaging: Package in light-resistant, well-closed containers.

Labeling: Use only as directed. Keep out of the reach of children. Discard after ____ [time period].

Stability: A beyond-use date of 14 days when stored in a refrigerator may be used for this preparation.¹

Quality Control: Quality-control assessment can include weight, specific gravity, active drug assay, color, texture of surface, appearance, feel, physical observation, and physical stability.²

Discussion: Coenzyme Q₁₀ (Ubiquinone 50, CoQ₁₀, ubidecarenone, ubiquinone 10, C₅₉H₉₀O₄, MW 836.3) is a naturally occurring coenzyme involved in electron transport in the mitochondria. It is claimed to have antioxidant and membrane-stabilization properties and to be a free-radical scavenger. Coenzyme Q₁₀ has been used orally as an adjunct in cardiovascular disorders. It occurs as a yellow to orange crystalline powder that melts at about 48°C. It is practically insoluble in water and very slightly soluble in dehydrated alcohol. Coenzyme Q₁₀ should be protected from light.^3,4

Lipoic acid (thioctic acid, alpha lipoic acid, C₈H₁₄O₂S₂, MW 206.3), DL form, occurs as yellow needles that are practically insoluble in water and soluble in fat solvents. It has a melting point of 60°C to 61°C and can form a water-soluble sodium salt. It is used for its antioxidant effects in the treatment of diabetic neuropathy, and it has been used to treat liver dysfunction, hepatitis, and Amanita phalloides mushroom poisoning.^3,4

Aspartame (NutraSweet, Equal) is an off-white, almost odorless, crystalline powder with an intensely sweet taste and a molecular weight (MW) of 294.31. It melts at 246°C to 247°C and has a density of about 0.3 g/mL to 0.4 g/mL (bulk). Aspartame is sparingly soluble in water and only slightly soluble in 95% ethanol. In aqueous solutions, its solubility increases with a decrease in pH and an increase in temperature. Aspartame is stable when dry, but it can hydrolyze in the presence of moisture. In solution, its stability is improved by the addition of cyclodextrins to the formulation. Aspartame degrades during prolonged heating, but this can be minimized by using higher temperatures for short time periods, followed by rapid cooling.⁵

Acacia (gum acacia, gum arabic) is the dried gummy exudate obtained from the stems and branches of some species of acacia (fam. Leguminosae) occurring primarily in the Sudan and Senegal regions of Africa. It is a complex aggregate of sugars and hemicelluloses with an MW in the range of 240,000 to 580,000. The aggregate consists mainly of arabic acid as a nucleus, connected to calcium, magnesium, and potassium in conjunction with arabinose, galactose, and rhamnose.⁶

Citric acid (citric acid monohydrate, C₆H₈O₇.H₂O) occurs as colorless or translucent crystals or as a white, crystalline, efflorescent powder that is odorless and has a strong, tart, acidic taste. It is present at about the 5% to 8% level in lemon juice. In 0.3% to 2% concentration, it is used to improve flavor in liquid formulations and as a sequestering agent. It may also be used in the preparation of effervescent granules and in solid and semisolid (chewable) dosage forms. The hydrated form will effloresce and the anhydrous form will be hygroscopic, depending upon the humidity in the air. One gram is soluble in less than 1 mL of water and 1.5 mL of ethanol.⁷

Gelatin troche base, also called pediatric chewable gummy gel base, may be prepared from gelatin, glycerin, and purified water.⁸

REFERENCES

1. USP Pharmacists' Pharmacopeia. 2nd ed. Rockville, MD: U.S. Pharmacopeial  Convention, Inc; 2008:775-779.
2. Allen LV Jr. Standard operating procedure for performing physical quality assessment of suppositories, troches, lollipops and sticks. IJPC. 1999;3:56-57.
3. Sweetman SC, ed. Martindale: The Complete Drug Reference. Pharmaceutical Press; 2009:2400,2407. 36th ed. London, England:
4. O'Neil MJ, ed. The Merck Index. 14th ed. Whitehouse Station, NJ: Merck & Co, Inc; 2006:1603, 1692.
5. Cram A. Aspartame. In: Rowe RC, Sheskey PJ, Quinn ME, eds. Handbook of Pharmaceutical Excipients. 6th ed. London, England: Pharmaceutical Press; 2009:48-50.
6. Kibbe AH. Acacia. In: Rowe RC, Sheskey PJ, Quinn ME, eds. Handbook of Pharmaceutical Excipients. 6th ed. London, England: Pharmaceutical Press; 2009:1-3.
7. Amidon GE. Citric acid monohydrate. In: Rowe RC, Sheskey PJ, Quinn ME, eds. Handbook of Pharmaceutical Excipients. 6th ed. London, England: Pharmaceutical Press; 2009:181-183.
8. Allen LV Jr. Pediatric chewable gummy gel base. IJPC. 1997;1:106.

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