Zerocal

• Approved Indications:
  Sucralose is used as a non-nutritive artificial sweetener in food, beverages, pharmaceuticals, and nutraceuticals. It is intended as a sugar substitute for individuals who require calorie reduction, including those with diabetes mellitus and obesity.
• Off-label (Clinically Accepted) Uses:
• Taste-masking agent in oral medications to improve palatability
• Ingredient in sugar-free dental products to reduce caries risk
• Used in enteral nutrition products to improve taste without raising blood glucose

• Administration Route: Oral (as part of foods, drinks, or medicinal formulations)
• Dosing:
  Sucralose is approximately 600 times sweeter than sucrose, so effective doses are very low. In formulations, it is typically used at concentrations ranging from 0.01% to 1% w/v.
• Population:
• Adults, elderly, and children: Safe within the Acceptable Daily Intake (ADI) of 5 mg/kg body weight per day
• No dosage adjustments necessary for renal or hepatic impairment
• Usage: Incorporated as an excipient in products; no direct dosing by patients
• Duration: Can be used indefinitely as part of sugar-free regimens

Sucralose binds to the sweet taste receptors (T1R2/T1R3) on the tongue, stimulating sweetness perception without being metabolized for energy. Its structure—chlorinated sucrose derivative—prevents enzymatic breakdown and absorption, enabling it to pass through the gastrointestinal tract without increasing blood glucose or insulin levels, thus providing a sweet taste without caloric intake.

• Absorption: Approximately 11–27% absorbed from the GI tract
• Distribution: Minimal systemic distribution, no tissue accumulation
• Metabolism: Negligible hepatic metabolism; largely excreted unchanged
• Excretion: Majority excreted unchanged in feces (~85%); absorbed portion excreted unchanged via urine
• Half-life: Approximately 13 hours for absorbed fraction

• Pregnancy: Classified as FDA Category B—no evidence of harm in animal studies; limited human data but considered safe within recommended intake levels.
• Lactation: Small amounts may pass into breast milk but are unlikely to affect the infant; use is considered safe.
• Recommendation: Use within ADI; avoid excessive consumption.

• Non-nutritive Sweetener
• Artificial high-intensity sweetener

• Known hypersensitivity to sucralose or excipients
• Rare congenital conditions affecting sugar metabolism may warrant caution

• Caution in patients with gastrointestinal disorders prone to sensitivity (possible bloating or gas)
• Use moderate intake due to potential, though unproven, effects on gut microbiota with high chronic consumption
• Monitor for rare hypersensitivity reactions

• Common: Bloating, gas, mild diarrhea (usually dose-related)
• Rare: Allergic reactions such as rash or itching
• Serious side effects are very rare and typically associated with excessive intake

• No clinically significant drug interactions identified
• Does not affect CYP450 enzymes or drug metabolism
• Does not interact adversely with food or alcohol

• Regulatory agencies (FDA, EFSA, WHO) reaffirmed safety with ADI of 5 mg/kg/day
• Emerging research into effects on gut microbiome ongoing, but no change in recommendations
• Recognized as safe sweetener in diabetic and calorie-controlled diets

• Store at 20–25°C (68–77°F), allowed range 15–30°C (59–86°F)
• Protect from moisture and direct sunlight
• Store in tightly closed containers
• No refrigeration or special handling required