Chemical and compositional characterisation of lactose as a carrier in dry powder inhalers

TY - CHAP

T1 - Chemical and compositional characterisation of lactose as a carrier in dry powder inhalers

AU - Jawad, Rim

AU - Martin, Gary P.

AU - Royall, Paul G.

N1 - Publisher Copyright: © 2015 John Wiley & Sons, Ltd. Copyright: Copyright 2021 Elsevier B.V., All rights reserved.

PY - 2015/1/1

Y1 - 2015/1/1

N2 - [T]The principal component of many solid pharmaceutical formulations and indeed of dry powder inhalers, rather than being an active pharmaceutical ingredient (API), is most likely to be lactose. It is an excipient that fulfils a number of functions including those of diluent, flow-aid and API carrier. Despite it being such a major component, it is a natural product that has been poorly characterised previously in terms of its crystalline/amorphous content and especially in terms of the different anomer composition (i.e., the α and β content) of the specific sample. The complexities of characterising the physicochemical properties of lactose, given that epimerisation can occur in solution during production processes, such as freeze- and spray drying require careful consideration. The different methods and techniques available to undertake such an investigation, including in particular the use of nuclear magnetic resonance, infrared techniques, differential scanning calorimetry and polarimetry, also demand critical evaluation. Finally, the potential implications of utilising lactose containing different α:β anomer ratios, alongside other differences in physicochemical properties (such as size, size distribution, shape, rugosity, etc.), should be taken into account when formulating future aerosolisable powdered medicines.

AB - [T]The principal component of many solid pharmaceutical formulations and indeed of dry powder inhalers, rather than being an active pharmaceutical ingredient (API), is most likely to be lactose. It is an excipient that fulfils a number of functions including those of diluent, flow-aid and API carrier. Despite it being such a major component, it is a natural product that has been poorly characterised previously in terms of its crystalline/amorphous content and especially in terms of the different anomer composition (i.e., the α and β content) of the specific sample. The complexities of characterising the physicochemical properties of lactose, given that epimerisation can occur in solution during production processes, such as freeze- and spray drying require careful consideration. The different methods and techniques available to undertake such an investigation, including in particular the use of nuclear magnetic resonance, infrared techniques, differential scanning calorimetry and polarimetry, also demand critical evaluation. Finally, the potential implications of utilising lactose containing different α:β anomer ratios, alongside other differences in physicochemical properties (such as size, size distribution, shape, rugosity, etc.), should be taken into account when formulating future aerosolisable powdered medicines.

KW - Differential scanning calorimetry

KW - Dry powder inhalers

KW - Epimerisation

KW - Infrared spectroscopy

KW - Inverse gas chromatography

KW - Lactose

KW - Nuclear magnetic resonance

KW - Polarimetry

KW - Powder x-ray diffraction

KW - Pulmonary drug delivery

UR - http://www.scopus.com/inward/record.url?scp=85057100877&partnerID=8YFLogxK

U2 - 10.1002/9781118799536.ch7

DO - 10.1002/9781118799536.ch7

M3 - Chapter

AN - SCOPUS:85057100877

SN - 9781118799529; 9781118799505; 9781118799482; 9781118799543

SP - 143

EP - 169

BT - Pulmonary Drug Delivery

PB - WILEY-BLACKWELL

ER -