Name: Lactose, Spray-Dried
CAS No: O-b-D-galactopyranosyl (1!4), D-glucopyranose monohydrate [5989-81-1]; [10039-26-6]; [64044-51-5].
None adopted
FlowLac 90; FlowLac 100; Lactopress Spray-Dried; Lactopress Spray-Dried 250; NF Lactose–315; NF Lactose–316 Fast Flo; SuperTab 11SD; SuperTab 14SD.
O-b-D-galactopyranosyl (1!4), D-glucopyranose monohydrate [5989-81-1]; [10039-26-6]; [64044-51-5].
C12H22O11 342.30 (for amorphous) C12H22O11H2O 360.31 (for monohydrate)
See Lactose, Anhydrous and Lactose, Monohydrate.
Spray-dried lactose is widely used as a binder, filler-binder, and flow aid in direct compression tableting. See also Lactose, Monohydrate; Lactose, Anhydrous.
Lactose occurs as white to off-white crystalline particles or powder. It is odorless and slightly sweet-tasting. Spray-dried directcompression grades of lactose are generally composed of 80–90% specially prepared pure a-lactose monohydrate along with 10–20% of amorphous lactose.
Angle of repose 298 for FlowLac 90; 288 for FlowLac 100. Bonding index 0.0044 for NF Lactose–315 (at compression pressure 54.90 MPa)(1) Brittle fracture index 0.1671 for NF Lactose–315 (at compression pressure 54.90 MPa)(1) Density bulk see Table I. Loss on drying 0.3% for NF Lactose–315; 0.6% for NF Lactose– 316. Particle size distribution see Table II. Reduced modulus of elasticity 5648 for NF Lactose–315 (at compression pressure 54.90MPa)(1) Tensile strength 2.368MPa for NF Lactose–315 (at compression pressure 54.90 MPa)(1) Water content Methods for characterizing the mechanical properties of compacts of pharmaceutical ingredients are specified in the Handbook of Pharmaceutical Excipients, 3rd edn.(1)
Spray-dried lactose should be stored in a well-closed container in a cool, dry place.
Lactose is a reducing sugar. The amorphous lactose, which is the most reactive form of lactose present in spray-dried lactose, will interact more readily than conventional crystalline grades.(2) Typical reactions include the Maillard reaction with either primary(3) or secondary(4) amines
A suspension of a-lactose monohydrate crystals in a lactose solution is atomized and dried in a spray drier.(5,6) Approximately 10–20% of the total amount of lactose is in solution and the remaining 80–90% is present in the crystalline form. The spray-drying process predominantly produces spherical particles. The compactibility of the material and its flow characteristics are a function of the primary particle size of the lactose monohydrate and the amount of amorphous lactose.
Lactose is widely used in pharmaceutical formulations as a diluent in oral capsule and tablet formulations. It may also be used in intravenous injections. Adverse reactions to lactose are largely due to lactose intolerance, which occurs in individuals with a deficiency of the enzyme lactase. See Lactose, Monohydrate.
Observe normal precautions appropriate to the circumstances and quantity of material being handled. Excessive generation of dust, or inhalation of dust, should be avoided.
See Lactose, Monohydrate.
Lactose, anhydrous; lactose, inhalation; lactose, monohydrate.
Spray-dried lactose was one of the first direct-compression excipients. Spray-dried lactose typically comprises lactose monohydrate and amorphous lactose (see Section 8); see Lactose, Monohydrate for the relevant pharmacopeial information. It has been shown that during the spray-drying process the effects of nozzle orifice diameter and atomization air flow control the droplet size during atomization; however, it has also been demonstrated that increasing feed concentration results in increased shell thickness of hollow particles that are formed.(8) The physical properties of spray-dried lactose produced from alcoholic media are directly affected by the ethanol-to-water ratio in the feed solution. Lactose spray-dried from pure ethanol was shown to be 100% crystalline, whereas lactose spray-dried from pure water was 100% amorphous. Furthermore, the surface area of the spray-dried lactose increased as a function of amorphous content.(9) Spray-dried lactoses exhibit good flow properties.(10) Polyethylene glycol (PEG) 4000, when spray-dried with lactose, has been shown to accelerate the rate and extent of crystallization of lactose.(11) It has also been shown that spray-dried lactose composite particles containing an ion complex of chitosan are suitable for the dry-coating of tablets.(12) Spray-dried lactose and crystallized spray-dried lactose have been evaluated for dry powder inhalation application.(13,14) Amorphous spray-dried lactose has also been studied in composites with PVP.(15) See also Lactose, Anhydrous, Lactose, Inhalation and Lactose, Monohydrate.