US Pharm. 2019;44(12):48-CV3.
Method of Preparation: Calculate the required quantity of each ingredient for the total amount to be prepared. Accurately weigh and/or measure each ingredient. Thoroughly pulverize the required number of alosetron hydrochloride (Lotronex) tablets to a fine powder. Incorporate a small quantity of Ora-Plus to form a smooth paste. Geometrically, add the remainder of the Ora-Plus with thorough mixing. Incorporate the Ora-Sweet or Ora-Sweet SF to final volume and mix well. Alternatively, Ora-Blend or Ora-Blend SF could be used to replace the Ora-Plus and Ora-Sweet or Ora-Sweet SF vehicles noted above. Package and label.
Use: Alosetron (Lotronex) is indicated only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have chronic IBS symptoms (generally lasting 6 months or longer); have had anatomical or biochemical abnormalities of the gastrointestinal tract ruled out; and have not responded sufficiently to conventional therapy. Clinical studies have not been conducted to adequately confirm alosetron’s benefits in men.1 This formulation is appropriate for patients who have trouble swallowing or cannot take oral tablets.
Packaging: Package in tight, light-resistant containers.
Labeling: Keep out of reach of children. Use only as directed. Shake well. Refrigerate. Discard after ____ [time period].
Stability: A beyond-use date of 14 days when stored in a refrigerator may be used for this preparation.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).3,4
Description: Alosetron hydrochloride (Lotronex, C17H18N4O.HCl, MW 330.81) is a potent and selective antagonist of the serotonin 5-HT3 receptor type. Alosetron hydrochloride occurs as a white or beige solid that has a solubility of 61 mg/mL in water. Lotronex is supplied as tablets of 0.5 mg (white) and 1 mg (blue); the 0.5-mg tablet contains 0.562 mg alosetron HCl equivalent to 0.5 mg alosetron, and the 1-mg tablet contains 1.124 mg alosetron HCl equivalent to 1 mg alosetron. In addition, each tablet also contains the inactive ingredients lactose (anhydrous), magnesium stearate, microcrystalline cellulose, and pregelatinized starch. The white film coating for the 0.5-mg tablet contains hypromellose, titanium dioxide, and triacetin. The blue film coating for the 1-mg tablet contains hypromellose, titanium dioxide, triacetin, and indigo carmine.1
Ora-Plus is an oral suspending vehicle that accepts dilution of up to 50% or more with water, flavoring agents, or syrups while still retaining its suspending properties. It has a pH of approximately 4.2 and an osmolality of about 230 mOsm/kg. Ora-Plus is a thixotropic vehicle with a viscosity of approximately 1,000 cps at 25°C. Ora-Plus 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. Ora-Sweet is buffered to a pH of approximately 4.2 and has an osmolality of about 3,240 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.6
Ora-Sweet SF sugar-free syrup vehicle is a flavoring vehicle for oral extemporaneous preparations. It is a sugar-free, alcohol-free syrup flavored with a citrus-berry flavor blend. Ora-Sweet SF is buffered to a pH of approximately 4.2, and it may be used alone or in combination with other vehicles. Ora-Sweet SF 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 2,150 mOsm/kg. Ora-Sweet SF 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.7
REFERENCES
1. RxList. Lotronex. www.rxlist.com/lotronex-drug.htm#side_effects. Accessed November 5, 2019.
2. U.S. Pharmacopeia/National Formulary [current revision]. Rockville, MD: U.S. Pharmacopeial Convention, Inc; November 2019.
3. Allen LV Jr. Summary of quality-control testing for sterile and nonsterile compounded preparations, part 1: physical and chemical testing. IJPC. 2019;23(3):211-216.
4. Allen LV Jr. Summary of quality-control testing for sterile and nonsterile compounded preparations, part 2: microbiological testing. IJPC. 2019;23(4):299-303.
5. Ora-Plus product information. Allegan, MI: Perrigo; 2018.
6. Ora-Sweet product information. Allegan, MI: Perrigo; 2018.
7. Ora-Sweet SF product information. Allegan, MI: Perrigo; 2018.
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