US Pharm. 2024;49(9):59-60.


Method of Preparation: Calculate the precise amount of each ingredient needed for the desired total quantity. Calibrate the mold, accounting for approximately 10% overage to accommodate any excess material required. Accurately weigh or measure each ingredient. Next, secure the appropriate troche mold to a clean, nonporous surface, taping one side down firmly. Lightly coat the top side of the mold with food-grade nonstick spray. Triturate the progesterone into a fine powder and combine it with the silica gel and stevia powder, mixing thoroughly until uniform. Melt the troche base of choice to around 60°C to 65°C and incorporate the powdered mixture; then add the flavorings and blend thoroughly. Once the mixture has cooled slightly, draw it into a syringe and fill each cavity of the mold. When the troches have cooled, carefully remove the tape and press each one out of the mold. Sample the troche weights for consistency. Package and label.1

Use: Progesterone troches can help alleviate symptoms of endometriosis and uterine fibroids. They have also been used to treat amenorrhea and prevent early pregnancy loss.

Packaging: Package in an airtight container. Store at controlled room temperature. Protect from light.

Labeling: Keep out of reach of children. Discard after ____ [time period].

Stability: The USP default beyond-use date for solid formulations is 180 days when stored at controlled room temperature.2

Quality Control: Weight/volume, pH, specific gravity, active drug assay, color, rheologic properties/pourability, physical observation, and physical stability (discoloration, foreign materials, gas formation, mold growth) are all examples of quality-control assessments).3

Discussion: Progesterone is essential for regulating the menstrual cycle and maintaining pregnancy. In this formulation, the hormone is delivered via a square-shaped troche that dissolves slowly in the mouth for absorption through the oral mucosa. This method ensures the sustained release and consistent therapeutic levels of progesterone. Progesterone troches have been used to alleviate endometriosis pain and inflammation, treat uterine fibroids, regulate menstrual cycles in polycystic ovary syndrome, restore regular cycles in amenorrhea, and relieve dysmenorrhea.4

Progesterone (Prometrium, C21H30O2, MW 314.47) is a white, odorless, crystalline powder. It is insoluble in water; soluble in alcohol, acetone, and dioxane; and sparingly soluble in vegetable oils. Progesterone has a melting point of 126°C to 131°C, and it is stable in air. Common side effects of progesterone therapy include changes in menstrual flow, spotting, breakthrough bleeding, weight gain, nausea, vomiting, breast tenderness, and mild headache. Melasma, chloasma, changes in libido, and breast discharge are among its less common effects.4-6

Stevia is a natural sweetener that is extracted from the Stevia rebaudiana Bertoni plant. It occurs as a white, crystalline, hygroscopic powder and is 200 to 300 times sweeter than sugar. Stevia is safe and nontoxic, and it is suitable for both hot and cold preparations.7

Silica gel is derived from silicon dioxide and is obtained by insolubilizing dissolved silica in sodium silicate solution. It occurs as a fine, white, odorless, amorphous, hygroscopic powder. Silica gel absorbs moisture and acts as a suspending agent and viscosity enhancer; it also is a stabilizer and controls viscosity. It is insoluble in water and organic solvents and dissolves in hot alkali hydroxide solutions.8

By dissolving in the mouth, troches allow a medication—including hormones—to enter the bloodstream directly and bypass the liver, enabling a rapid onset of action. One example of a troche base is polyethylene glycol (PEG) sweetened with stevia. PEG (Carbowax) is an addition polymer of ethylene oxide and water that is available in various grades; it is soluble in water and is compatible with many flavorings. PEG bases, including PEG 1000 with aspartame and flavoring agents, are chemically stable and do not support microbial growth.9

REFERENCES

1. Medisca. Suggested formula: progesterone 100 mg oral troches. www.medisca.net/pdf/additional-sample-formulas/F%20005%20854v2%20Progesterone%20100%20mg%20Oral%20Troche.pdf. Accessed August 1, 2024.
2. U.S. Pharmacopeia/National Formulary [current revision]. Rockville, MD: U.S. Pharmacopeial Convention, Inc; September 2022.
3. Allen LV Jr. Standard operating procedure for performing physical quality assessment of suppositories, troches, lollipops and sticks. IJPC. 1999;3:56-57.
4. Progesterone [monograph]. United States Pharmacopeia 37/National Formulary 32. Rockville, MD: US Pharmacopeial Convention, Inc; 2014:4428.
5. Prometrium (progesterone) product information. North Chicago, IL: Abbott Laboratories; 2011.
6. Endometrin (progesterone) product information. Parsippany, NJ: Ferring Pharmaceuticals Inc; January 2018.
7. Reynolds JE, ed. Martindale: The Extra Pharmacopoeia. 30th ed. London, England: Pharmaceutical Press; 1993:1049.
8. Hapgood KP. Colloidal silicon dioxide. In: Rowe RC, Sheskey PJ, Quinn ME, eds. Handbook of Pharmaceutical Excipients. 6th ed. London, England: Pharmaceutical Press; 2009:185-188.
9. Wallick D. Polyethylene glycol. In: Rowe RC, Sheskey PJ, Quinn ME, eds. Handbook of Pharmaceutical Excipients. 6th ed. London, England: Pharmaceutical Press; 2009:517-522.

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