Sucralose + Acesulfame Potassium

Approved Indications:

• Non-nutritive sweetener: Used in pharmaceuticals, oral liquid medications, chewable tablets, nutraceuticals, and food/dietary products as a sugar substitute for:
• Calorie-controlled diets
• Diabetic dietary management
• Weight loss and obesity control
• Patients requiring sugar-free formulations

Clinically Accepted Uses:

• Adjunct in taste-masking formulations: Improves palatability in bitter-tasting medications (e.g., antacids, antibiotics, syrups).
• Used in enteral and parenteral nutrition products as a flavor-enhancing agent where sugar restriction is necessary.

Route of Administration:

• Oral (typically included in formulations as an excipient or additive)

Recommended Use in Products:

• Sucralose: Typically used at 0.2%–0.6% w/v concentration
• Acesulfame Potassium: Used at 0.1%–0.3% w/v concentration

Population Use:

• Adults & Elderly: No dose limitation when used as a sweetening excipient
• Children: Safe for pediatric products at standard concentrations
• Pregnant/Lactating Women: Considered safe at regulated levels
• Renal/Hepatic Impairment: No adjustment needed; not systemically active

Duration of Use:

• Can be used indefinitely as part of long-term dietary or medicinal regimens

Sucralose is a chlorinated derivative of sucrose that binds to sweet taste receptors on the tongue (T1R2/T1R3) but is not metabolized by the body, thus providing sweetness without calories or glycemic effects.
Acesulfame Potassium also activates sweet taste receptors but is completely excreted unchanged. Combined, these agents create a synergistic sweetness effect (approximately 200–600 times sweeter than sucrose) without contributing to caloric intake or affecting insulin or glucose levels.

Sucralose:

• Absorption: Poorly absorbed (<15%)
• Distribution: Not significantly distributed in tissues
• Metabolism: Minimal hepatic metabolism
• Excretion: ~85% excreted unchanged in feces; small absorbed portion excreted via urine
• Half-life: ~13 hours

Acesulfame Potassium:

• Absorption: Rapid and nearly complete absorption
• Distribution: Does not accumulate in tissues
• Metabolism: Not metabolized
• Excretion: Entirely eliminated unchanged via the kidneys
• Half-life: ~2–3 hours

• Pregnancy: Considered safe (Category B equivalent in many global reviews); no evidence of teratogenicity or fetal toxicity at normal dietary levels
• Lactation: Trace amounts may be excreted into breast milk, but considered safe; no known effects on infants
• Note: Excessive intake is discouraged due to limited long-term reproductive studies; moderate use advised

• Primary Class: Non-nutritive Sweetener / Artificial Sweetening Agent
• Subclassification: High-intensity sweetener combination

• Known hypersensitivity or allergy to sucralose or acesulfame potassium
• Rare hereditary problems such as sucrose-isomaltase deficiency (with sucralose-based excipients)
• Severe renal impairment may require caution (for acesulfame K due to renal excretion)

• Use in Renal Disease: Monitor total potassium intake when used in large amounts (Acesulfame K contains potassium)
• Allergic Reactions: Though rare, hypersensitivity (e.g., rash, swelling) may occur in sensitive individuals
• Neurological Sensitivity: Some reports of migraines linked to excessive artificial sweetener intake
• Phenylketonuria (PKU): Though not directly related, some combination sweeteners contain phenylalanine; verify formulations

Common (usually mild):

• Gastrointestinal: Bloating, gas, nausea
• Oral: Bitter aftertaste or metallic sensation (at high concentrations)
• Neurological: Headache, dizziness (in sensitive individuals)

Rare but Serious:

• Hypersensitivity reactions (rash, itching, anaphylaxis – extremely rare)
• Behavioral changes or seizures (reported anecdotally in very high exposure cases)

• Drug-Drug: No clinically significant interactions documented
• Drug-Food: No adverse food interactions
• Drug-Alcohol: No known interaction
• Metabolism-Related: Neither sucralose nor acesulfame K significantly interacts with CYP450 enzymes

• WHO (2023): Issued a conditional recommendation limiting non-sugar sweetener (NSS) use for weight control in healthy populations, though no safety concerns were raised
• FDA & EFSA: No recent bans or major safety warnings; current Acceptable Daily Intake (ADI) upheld
• Sucralose ADI: 5 mg/kg/day
• Acesulfame K ADI: 15 mg/kg/day
• Codex Alimentarius: Reaffirmed both compounds as safe additives in food and pharmaceuticals

• Temperature: Store below 30°C (room temperature)
• Light: Protect from direct sunlight
• Humidity: Store in dry conditions
• Handling: Keep tightly closed to avoid degradation of sweetening potency
• Formulated Products: No special reconstitution or refrigeration required unless combined with unstable ingredients