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Sucrose Excipient | Uses, Suppliers, and Specifications
Sucrose is common sugar or more precisely, β-D-Fructofuranosyl-α-D-glucopyranose, a naturally-occurring disaccharide formed from Glucose and Fructose. When graded as a pharmaceutical excipient, Sucrose can be obtained from sugar cane or sugar beet and contains no other substances. It is supplied as colourless crystals, crystalline masses, or as a white crystalline powder. It is odourless and sweet to taste.
Pharmacopoeial Compliance: USP-NF; Ph.Eur; B.P; J.P; I.P
Synonyms and Trade Names: Sucrose; Beet Sugar; Cane Sugar; β-D-Fructofuranosyl-α-D-glucpyranoside; Refined Sugar; Saccharose
Uses and Applications: Sweetening Agent; Tablet Binder; Tablet and Capsule Diluent; Viscosity-increasing Agent; Confectionery Base; Coating Agent; Granulation Aid; Suspending Agent; and Therapeutic Agent
Description
Sucrose, which is commonly known as sugar, but more precisely α-D-glucopyranosyl β-D-fructofuranoside, is a naturally-occurring disaccharide formed from equimolar quantities of glucose and fructose. Its chemical name is β- d -fructofuranosyl-α- d -glucopyranoside and an empirical chemical formula of C12H22O11.
Sucrose is the most abundant disaccharide and the major product of photosynthesis. Being a nonreducing sugar it has very low chemical reactivity and is the reason for its use as a transport and storage molecule in plants. It is mainly synthesised in leaves, although the ability to synthesize sucrose is fairly widespread among plant cells.
At present, the main crops cultivated for their sugar are sugar cane (Saccharum officinarum Linne (Fam. Gramineae) and sugar beet (Beta vulgaris Linne (Fam. Chenopodiaceae), with sugar cane accounting for over 75% of the world’s production. The major cane sugar producers are Brazil, India, China, Thailand, Mexico and Australia accounting for over 60% of the total cane sugar produced and close to 50% of the world’s total production.
Pharmaceutical-grade Sucrose is either obtained from sugar cane or sugar beet. It contains no added substances. It is supplied as colourless crystals, as crystalline masses or blocks, or as a white crystalline powder; it is odourless and has a characteristic sweet taste.
Chemical Structure & Identifiers
| Chemical Name | β-D-Fructofuranosyl-alpha-D-glucopyranoside |
| CAS Registry Number | [57-50-1] |
| Empirical Formula | (C12H22O11) |
| Molecular Weight | 342.30 Daltons |
| EC/ECS Number | 200-334-9 |
| UNII Code (FDA) | C151H8M554 |
| Chemical Name | β-D-Fructofuranosyl-alpha-D-glucopyranoside |
| CAS Registry Number | [57-50-1] |
| Empirical Formula | (C12H22O11) |
| Molecular Weight | 342.30 Daltons |
| EC/ECS Number | 200-334-9 |
| UNII Code (FDA) | C151H8M554 |
Regulatory Status
Sucrose is an approved pharmaceutical excipient. It is listed in the USP-NF, Ph.Eur, BP, J.P, IP and Ch.P. Sucrose is part of the normal human and animal diet and approved for use in food products (A specification for Sucrose is contained in the Food Chemicals Codex, FCC). Excipient grade Sucrose is GRAS listed and included in the US FDA Inactive Ingredients Database (covering injections, oral tablets and capsules, oral solutions, syrups, and topical products).
Physicochemical Properties
| Form | Solid, powder |
| Appearance | Colourless crystals, crystalline mass or white crystalline powder |
| Bulk density | 0.55 – 0.65 g/ml (powdered sucrose)
0.92 – 0.94 g/ml (crystalline sucrose) |
| Tapped density | 0.80-0.84 g/ml (powdered sucrose)
1.03 g/ml (crystalline sucrose) |
| True density | 1.6 g/ml |
| pKa | 12.62 |
| Flowability | Crystalline sucrose is free flowing. Powdered grades are cohesive and flow poorly |
| Melting point | 160-186 OC (with decomposition) |
| Moisture content | Sucrose is hygroscopic. Below 75% RH, the material absorbs little moisture. Above 75% RH, Sucrose absorbs enough moisture to dissolve |
| Osmolarity | A 9.25 % w/v aqueous solution is iso-osmotic with plasma |
| Particle morphology | Granular Sucrose is irregularly-shaped powder. Crystalline material consists of crystalline, roughly cubic granules |
| Particle size distribution | D50 = 540-560 µm (Crystalline Sucrose)
D50 = 60-70 µm (Powdered Sucrose) |
| Refractive index (10% w/v aqueous solution) | 1.34783 |
| Solubility | Soluble in water and Ethanol |
| Specific gravity | 1.0381 (10% w/w solution) |
Pharmacopeoeal Specifications
| Test | USP-NF | Ph.Eur | J.P |
| Name | Sucrose | Sucrose | Sucrose |
| Authorised used | Excipient | Excipient | Excipient |
| Definition | specified | specified | specified |
| Identification | n/a | specified | specified |
| Characters | n/a | specified | n/a |
| Appearance of solution | n/a | specified | specified |
| Acidity or alkalinity | n/a | specified | specified |
| Specific optical rotation | ≥ +65.90 | +66.30 to 67.00 | +66.30 to 67.00 |
| Color value | n/a | ≤ 45 | n/a |
| Conductivity | n/a | 35µ Scm-1 | specified |
| Loss on drying | n/a | ≤ 0.1% | ≤ 0.1% |
| Bacterial endotoxins
≤ 0.25 IU/mg |
n/a | n/a | specified* |
| Dextrins | n/a | specified | specified |
| Reducing sugars | n/a | specified | n/a |
| Invert sugar | specified | n/a | specified |
| Chloride | ≤ 0.0035% | n/a | n/a |
| Sulfate | ≤ 0.006% | n/a | n/a |
| Sulfites | n/a | ≤ 10 ppm | ≤ 15 ppm |
| Calcium | specified | n/a | n/a |
| Heavy metals | ≤ 5 ppm | n/a | n/a |
| Lead | n/a | ≤ 0.5 ppm | ≤ 0.5 ppm |
| Residue on ignition | ≤ 0.05% | n/a | n/a |
| Assay | n/a | n/a | n/a |
| Labelling | specified | n/a | n/a |
Key: n/a Specification is not listed
*All claims with respect to conformity are subject to our Terms and Conditions. No express or implied warranty is made for specific properties or fitness for any particular application or purpose.
Applications in Pharmaceutical Formulations or Technology
Sucrose is a widely utilised excipient in oral pharmaceutical formulations, principally solids and liquids. It functions as a bulking agent (filler-diluent) and binder in tablets (both swallow, chewable and lozenges), as a sweetener and as a carrier syrup (viscosity-enhancer, palatability enhancer, thickening agent and suspending agent) in oral liquid formulations.
Sucrose syrups (in concentrations of 50-67% w/w) can be used as wet granulation binders for tablets. Powdered Sucrose functions as a dry binder (typical concentration levels of 2-20 % w/w) and as a bulking agent and sweetener in chewable tablets and lozenges. Similarly, Sucrose syrups are suitable for tablet coating (sugar coatings) or as additives to tablet film coatings.
Sucrose is also used as an excipient to provide solution-state stabilization, as well as cryo- and lyo-protection of biological products (e.g therapeutic proteins). Sucrose is generally considered suitable and works with most products unless limited by specific formulation constraints, such as low-pH formulations.
Safety and Precautions
Sucrose, together with other saccharides, are common dietary sugars. It is listed by the US FDA as a GRAS food additive and a direct food contact material. Upon oral ingestion, Sucrose is hydrolyzed in the small intestine into its constituent sugars, Dextrose and Fructose, which are then absorbed. When administered intravenously, sucrose is excreted unchanged in the urine. While Sucrose is part of the normal diet and has been used in pharmaceutical formulations for centuries, its consumption is not without risks, especially for individuals with diabetes or other metabolic sugar intolerance. It is also a major concern for dental health as it can be easily transformed into dental plaque. Consequently, the usage of Sucrose in oral pharmaceutical products has been decreasing.
Despite a link with increased incidences of obesity, renal damage, and other conditions, there is still no conclusive evidence to link Sucrose consumption with some diseases. Therefore, an ADI (acceptable daily intake) has not been established. Health authorities, however, advise that Sucrose intake should be reduced.
Toxicology: LD5o (mouse, IP); 14 g/kg, LD50 (rat, oral}: 29.7 g/kg
Stability and Storage Conditions
Sucrose exhibits good stability when correctly stored (at room temperature and at moderate relative humidity. The assigned shelf life is 24-36 months. However, the material can absorb moisture from the environment (this can be released when heated at 90 °C). Sucrose may caramelise when heated to temperatures above 160 °C. Thus, the bulk material should be stored in a well-closed container in a cool, dry place.
Dilute Sucrose solutions are susceptible to microbial attack (fermentation) whereas high concentrations (≥60% w/w) are resistant. Sucrose can be autoclaved without significant degradation. However, during processing (e.g during the fabrication of medicated confectionery), the heating process (110 to 145 °C) can cause a level of inversion forming Dextrose and Fructose (invert sugar).
When processing bulk Sucrose powders, observe SHEQ protocols appropriate to the particular work circumstances and quantity of material. The use of PPE (eye protection and gloves) is recommended. The workplace exposure limit for Sucrose is reported as 10 mg/m3 long-term (8-hour TWA) and 20 mg/m3 short-term.
Sustainability and Environmental Impact
A sustainability assessment for Sucrose excipient has not been conducted. However, it is a naturally-derived substance that is biodegradable with minimum impact on ecology or marine life.
Manufacturers & Suppliers
- Icing Sugar
- Compresuc® MS Compressible Sugar
- Compresuc® PS Compressible Sugar
- Granulated SugarCalibrated Sugar No. 1-600
- Sucrose Solution
British Sugar Plc
- Powder Sugar
- DC Sugar
- Liquid Sugar
- Screened Sugar
- UltraFine Sugar
Agrana/Sudzucker AG
- COMPRI® O
- COMPRI® M3
- COMPRI® M300
- White Sugar
- Icing Sugar
- Liquid Sugar
DFE Pharma
- BioHale® Sucrose (Low Endotoxin grade)
Additional Resources (Downloads)
References and Literature Used
Stelios T. Tzannis, Steven J. Prestrelski, Moisture effects on Protein—Excipient Interactions in Spray-dried Powders. Nature of Destabilizing effects of Sucrose, Journal of Pharmaceutical Sciences, 88, 3, 1999, 360-370, https://doi.org/10.1021/js9800127.
(https://www.sciencedirect.com/science/article/pii/S0022354915507818
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