Sac Sweet

Approved Indications:

• Non-nutritive sweetener: Used as a sugar substitute in various pharmaceutical, food, and beverage products due to its high-intensity sweetness and absence of calories.
• Diabetes mellitus (Type 1 and 2): Recommended as a sugar alternative to help manage blood glucose levels.
• Obesity and weight control: Aids in reducing overall caloric intake when substituted for sugar.
• Dental caries prevention: Commonly used in sugar-free oral care products like toothpaste and mouthwash, as it does not promote dental decay.
• Pharmaceutical excipient: Widely included in chewable tablets, lozenges, and syrups to improve palatability without affecting blood sugar.

Off-label and Ancillary Uses:

• Cosmetics: Used as a flavoring agent in lipsticks and lip balms.
• Veterinary formulations: Employed as a palatability enhancer in animal medications.
• Flavoring additive: Included in products requiring sugar replacement for taste or formulation reasons.

Route of Administration:

• Oral (as a sweetener or excipient in medicinal formulations)
• Topical (e.g., mouth rinses)
• Parenteral (used rarely in injectable solutions as an inactive component)

Acceptable Daily Intake (ADI):

• 0–5 mg/kg body weight/day (as per WHO/FAO JECFA guidelines)

Typical Use in Medications:

• Tablet or granule form: Each tablet typically contains 12–30 mg of saccharin sodium.
• Syrups and chewable medications: Used in concentrations to achieve palatability without exceeding ADI.

Adults:

• No therapeutic dosing; intake should remain within ADI limits.
• Commonly used in diabetic diets and sugar-free medicinal formulations.

Pediatrics:

• Safe when used within ADI limits in pediatric medications such as oral drops or syrups.

Elderly:

• No specific dose adjustment necessary.

Renal or Hepatic Impairment:

• In severe renal impairment, accumulation may occur due to decreased excretion; intake should be minimized.

Administration Advice:

• Can be taken with or without food.
• Do not exceed the recommended daily intake.
• Instruct patients to report any signs of hypersensitivity.

Saccharin Sodium is a high-intensity artificial sweetener that binds to sweet taste receptors (T1R2 and T1R3) on the tongue, activating the gustatory G-protein-coupled receptor pathway, thereby producing a sensation of sweetness. Unlike sugar, it is not metabolized or absorbed for energy use, making it non-caloric. Its sweetness potency is approximately 200–700 times that of sucrose, allowing very small quantities to achieve desired sweetness, particularly in diabetic and calorie-restricted diets.

• Absorption: Rapidly absorbed from the gastrointestinal tract after oral ingestion.
• Distribution: Distributes in extracellular fluids; does not significantly bind to plasma proteins.
• Metabolism: Not metabolized by the human body; remains unchanged.
• Excretion: Excreted primarily unchanged via urine; renal clearance is the main route.
• Bioavailability: Approximately 100%.
• Half-life: 1 to 2 hours in individuals with normal renal function.
• In Renal Impairment: Clearance is reduced; drug may accumulate with frequent use.

• Pregnancy:
• FDA Category (prior system): Category C (based on older classification; now replaced by narrative summaries).
• Animal studies have not shown teratogenic effects at standard intake. However, saccharin crosses the placenta and can accumulate in fetal tissues; thus, use should be limited and within ADI.
• Lactation:
• Saccharin is excreted in breast milk in small quantities.
• Although not proven harmful in humans, caution is advised when used during breastfeeding, especially in neonates or premature infants due to immature renal clearance.
• Recommendation: Use only if clearly needed and within ADI limits during pregnancy or lactation.

• Class: Non-nutritive Artificial Sweetener
• Subclass: Benzoic Sulfimide Derivative
• Pharmaceutical Role: Inactive excipient / taste enhancer / sugar substitute

• Hypersensitivity to saccharin or any of its components
• History of allergic reactions to benzoic acid derivatives or sulfonamides (possible cross-reactivity)
• Severe renal impairment (relative contraindication due to potential accumulation)
• Not advised for use in infants with immature renal function (e.g., premature neonates)

• Use in renal dysfunction: Excretion is significantly reduced; accumulation can occur in renal failure.
• Pregnancy caution: Use only within acceptable intake limits due to placental transfer and fetal tissue accumulation.
• Allergic reactions: Though rare, hypersensitivity reactions such as urticaria, bronchospasm, or anaphylaxis may occur, particularly in sulfa-allergic individuals.
• Historical carcinogenicity: Previously linked to bladder cancer in rats, but extensive human data have shown no cancer risk in humans. Saccharin has been delisted from carcinogen classifications by major health agencies.

Common (Mild):

• Gastrointestinal: Nausea, flatulence, abdominal discomfort
• Oral: Metallic or bitter aftertaste (dose-dependent)
• Neurological: Headache (rare)

Hypersensitivity Reactions (Rare):

• Skin rash, pruritus
• Urticaria
• Bronchospasm
• Anaphylaxis (very rare)

Special Populations:

• In children, excessive intake may lead to irritability or sleep disturbances (rare and unproven).

• Drug-Drug Interactions: No significant pharmacokinetic or pharmacodynamic drug interactions reported.
• Drug-Food Interactions: Compatible with all foods; commonly used in beverages and sugar-free products.
• Drug-Alcohol Interactions: No known interactions.
• CYP450 System: Not involved in cytochrome metabolism; no CYP450-related interactions.

• FDA Update: Saccharin was removed from the U.S. National Toxicology Program’s list of potential carcinogens in 2000, confirming its safety for human use.
• WHO/FAO (JECFA): Reconfirmed the ADI at 0–5 mg/kg/day.
• EMA & Codex Alimentarius: Regulates saccharin as an approved food additive (E954) with concentration limits for specific food categories.
• Product Labeling: Required to declare saccharin content in the U.S. if used in significant amounts.

• Storage Temperature: Store at 20°C to 25°C (68°F to 77°F)
• Humidity: Store in a dry environment, away from moisture
• Light Protection: Not required for solid dosage forms
• Handling Precautions:
• Keep tightly sealed
• Protect from heat and moisture
• No refrigeration required
• Liquid or Prepared Solutions (if applicable):
• Follow specific storage instructions on product labeling
• Shake well before use (if formulated as suspension)