Functional Category
Confectionery base; coating agent; granulation aid; suspending agent; sweetening agent; tablet binder; tablet and capsule diluent; tablet filler; therapeutic agent; viscosity-increasing agent.
Applications in Pharmaceutical Formulation
Sucrose is widely used in oral pharmaceutical formulations. Sucrose syrup, containing 50–67% w/w sucrose, is used in tableting as a binding agent for wet granulation. In the powdered form, sucrose serves as a dry binder (2–20% w/w) or as a bulking agent and sweetener in chewable tablets and lozenges.(1–3) Tablets that contain large amounts of sucrose may harden to give poor disintegration. S Sucrose 703 Sucrose syrups are used as tablet-coating agents at concentrations between 50% and 67% w/w. With higher concentrations, partial inversion of sucrose occurs, which makes sugar coating difficult. Sucrose syrups are also widely used as vehicles in oral liquiddosage forms to enhance palatability or to increase viscosity.(4,5) Sucrose has been used as a diluent in freeze-dried protein products.(6,7) Sucrose is also widely used in foods and confectionery, and therapeutically in sugar pastes that are used to promote wound healing.(8,9)
Description
Sucrose is a sugar obtained from sugar cane (Saccharum officinarum Linne´ (Fam. Gramineae)), sugar beet (Beta vulgaris Linne´ (Fam. Chenopodiaceae)), and other sources. It contains no added substances. Sucrose occurs as colorless crystals, as crystalline masses or blocks, or as a white crystalline powder; it is odorless and has a sweet taste.
Stability and Storage Conditions
Sucrose has good stability at room temperature and at moderate relative humidity. It absorbs up to 1% moisture, which is released upon heating at 908C. Sucrose caramelizes when heated to temperatures above 1608C. Dilute sucrose solutions are liable to fermentation by microorganisms but resist decomposition at higher concentrations, e.g. above 60% w/w concentration. Aqueous solutions may be sterilized by autoclaving or filtration. When sucrose is used as a base for medicated confectionery, the cooking process, at temperatures rising from 110 to 1458C, causes some inversion to form dextrose and fructose (invert sugar). The fructose imparts stickiness to confectionery but prevents cloudiness due to graining. Inversion is accelerated particularly at temperatures above 1308C and by the presence of acids. The bulk material should be stored in a well-closed container in a cool, dry place
Incompatibilities
Powdered sucrose may be contaminated with traces of heavy metals, which can lead to incompatibility with active ingredients, e.g. ascorbic acid. Sucrose may also be contaminated with sulfite from the refining process. With high sulfite content, color changes can occur in sugar-coated tablets; for certain colors used in sugarcoating the maximum limit for sulfite content, calculated as sulfur, is 1 ppm. In the presence of dilute or concentrated acids, sucrose is hydrolyzed or inverted to dextrose and fructose (invert sugar). Sucrose may attack aluminum closures.(11)
Safety
Sucrose is hydrolyzed in the small intestine by the enzyme sucrase to yield dextrose and fructose, which are then absorbed. When administered intravenously, sucrose is excreted unchanged in the urine. Although sucrose is very widely used in foods and pharmaceutical formulations, sucrose consumption is a cause of concern and should be monitored in patients with diabetes mellitus or other metabolic sugar intolerance.(12) Sucrose is also considered to be more cariogenic than other carbohydrates since it is more easily converted to dental plaque. For this reason, its use in oral pharmaceutical formulations is declining. Although sucrose has been associated with obesity, renal damage, and a number of other diseases, conclusive evidence linking sucrose intake with some diseases could not be established.(13,14) It was, however, recommended that sucrose intake in the diet should be reduced.(14) LD50 (mouse, IP): 14 g/kg(15) LD50 (rat, oral): 29.7 g/kg