Dry powder inhalers: mechanistic evaluation of lactose formulations containing salbutamol sulphate.

2.50
Hdl Handle:
http://hdl.handle.net/2436/575939
Title:
Dry powder inhalers: mechanistic evaluation of lactose formulations containing salbutamol sulphate.
Authors:
Kaialy, Waseem; Ticehurst, Martyn; Nokhodchi, Ali
Abstract:
The purpose of this study was to evaluate the relationships between physicochemical properties and aerosolisation performance of different grades of lactose. In order to get a wide range of physicochemical properties, various grades of lactose namely Flowlac 100 (FLO), Lactopress anhydrous 250 (LAC), Cellactose 80 (CEL), Tablettose 80 (TAB), and Granulac 200 (GRA) were used. The different lactose grades were carefully sieved to separate 63-90 μm particle size fractions and then characterised in terms of size, shape, density, flowability, and solid state. Formulations were prepared by blending each lactose with salbutamol sulphate (SS) at ratio of 67.5:1 (w/w), and then evaluated in terms of SS content uniformity, lactose-SS adhesion properties, and in vitro aerosolisation performance delivered from the Aerolizer. Sieved lactose grades showed similar particle size distributions (PSDs) and good flow properties but different particle shape, particle surface texture, and particle solid state. Content uniformity assessments indicated that lactose particles with rougher surface produced improved SS homogeneity within DPI formulation powders. Lactose-SS adhesion assessments indicated that lactose particles with more elongated shape and the rougher surface showed smaller adhesion force between lactose and salbutamol sulphate. Lactose powders with higher bulk density and higher tap density produced smaller emission (EM) and higher drug loss (DL) of SS. In vitro aerosolisation for various lactose grades followed the following rank order in terms of deposition performance: GRA>TAB>LAC ≈ CEL>FLO. Linear relationships were established showing that in order to maximize SS delivery to lower airway regions, lactose particles with more elongated shape, more irregular shape, and rougher surface are preferred. Therefore, considerable improvement in DPI performance can be achieved by careful selection of grade of lactose included within DPI formulations.
Citation:
Dry powder inhalers: mechanistic evaluation of lactose formulations containing salbutamol sulphate. 2012, 423 (2):184-94 Int J Pharm
Publisher:
Elsevier
Journal:
International journal of pharmaceutics
Issue Date:
28-Feb-2012
URI:
http://hdl.handle.net/2436/575939
DOI:
10.1016/j.ijpharm.2011.12.018
PubMed ID:
22197772
Type:
Article
Language:
en
ISSN:
1873-3476
Appears in Collections:
Pharmacy and Natural Products Research Group

Full metadata record

DC FieldValue Language
dc.contributor.authorKaialy, Waseemen
dc.contributor.authorTicehurst, Martynen
dc.contributor.authorNokhodchi, Alien
dc.date.accessioned2015-08-25T14:01:26Zen
dc.date.available2015-08-25T14:01:26Zen
dc.date.issued2012-02-28en
dc.identifier.citationDry powder inhalers: mechanistic evaluation of lactose formulations containing salbutamol sulphate. 2012, 423 (2):184-94 Int J Pharmen
dc.identifier.issn1873-3476en
dc.identifier.pmid22197772en
dc.identifier.doi10.1016/j.ijpharm.2011.12.018en
dc.identifier.urihttp://hdl.handle.net/2436/575939en
dc.description.abstractThe purpose of this study was to evaluate the relationships between physicochemical properties and aerosolisation performance of different grades of lactose. In order to get a wide range of physicochemical properties, various grades of lactose namely Flowlac 100 (FLO), Lactopress anhydrous 250 (LAC), Cellactose 80 (CEL), Tablettose 80 (TAB), and Granulac 200 (GRA) were used. The different lactose grades were carefully sieved to separate 63-90 μm particle size fractions and then characterised in terms of size, shape, density, flowability, and solid state. Formulations were prepared by blending each lactose with salbutamol sulphate (SS) at ratio of 67.5:1 (w/w), and then evaluated in terms of SS content uniformity, lactose-SS adhesion properties, and in vitro aerosolisation performance delivered from the Aerolizer. Sieved lactose grades showed similar particle size distributions (PSDs) and good flow properties but different particle shape, particle surface texture, and particle solid state. Content uniformity assessments indicated that lactose particles with rougher surface produced improved SS homogeneity within DPI formulation powders. Lactose-SS adhesion assessments indicated that lactose particles with more elongated shape and the rougher surface showed smaller adhesion force between lactose and salbutamol sulphate. Lactose powders with higher bulk density and higher tap density produced smaller emission (EM) and higher drug loss (DL) of SS. In vitro aerosolisation for various lactose grades followed the following rank order in terms of deposition performance: GRA>TAB>LAC ≈ CEL>FLO. Linear relationships were established showing that in order to maximize SS delivery to lower airway regions, lactose particles with more elongated shape, more irregular shape, and rougher surface are preferred. Therefore, considerable improvement in DPI performance can be achieved by careful selection of grade of lactose included within DPI formulations.en
dc.language.isoenen
dc.publisherElsevieren
dc.rightsArchived with thanks to International journal of pharmaceuticsen
dc.subjectInhalationen
dc.subjectCommercial lactoseen
dc.subjectSalbutamol sulphateen
dc.subjectPulmonary deliveryen
dc.subjectAerolizeren
dc.subjectShapeen
dc.subjectSurface roughnessen
dc.subjectContent uniformityen
dc.subjectAdhesionen
dc.subject.meshAdhesivenessen
dc.subject.meshAdministration, Inhalationen
dc.subject.meshAerosolsen
dc.subject.meshAlbuterolen
dc.subject.meshChemistry, Pharmaceuticalen
dc.subject.meshDrug Carriersen
dc.subject.meshDrug Compoundingen
dc.subject.meshDry Powder Inhalersen
dc.subject.meshLactoseen
dc.subject.meshLinear Modelsen
dc.subject.meshMicroscopy, Electron, Scanningen
dc.subject.meshParticle Sizeen
dc.subject.meshPowdersen
dc.subject.meshRheologyen
dc.subject.meshSurface Propertiesen
dc.subject.meshTechnology, Pharmaceuticalen
dc.titleDry powder inhalers: mechanistic evaluation of lactose formulations containing salbutamol sulphate.en
dc.typeArticleen
dc.identifier.journalInternational journal of pharmaceuticsen

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