Pharmacokinetics evaluation of soft agglomerates for prompt delivery of enteric pantoprazole-loaded microparticles

Raffin, RP; Colomé, LM; Hoffmeister, CRD; Colombo, P; Rossi, A; Sonvico, F; Natalini, CC; Pohlmann, AR; Costa, TD; Guterres, SS

Pharmacokinetics evaluation of soft agglomerates for prompt delivery of enteric pantoprazole-loaded microparticles

Raffin, RP Colomé, LM Hoffmeister, CRD Colombo, P Rossi, A Sonvico, F

Natalini, CC Pohlmann, AR Costa, TD Guterres, SS

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Publication Type:: Journal Article
Citation:: European Journal of Pharmaceutics and Biopharmaceutics, 2010, 74 (2), pp. 275 - 280
Issue Date:: 2010-02-01

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Field	Value	Language
dc.contributor.author	Raffin, RP	en_US
dc.contributor.author	Colomé, LM	en_US
dc.contributor.author	Hoffmeister, CRD	en_US
dc.contributor.author	Colombo, P	en_US
dc.contributor.author	Rossi, A	en_US
dc.contributor.author	Sonvico, F https://orcid.org/0000-0001-7372-1456	en_US
dc.contributor.author	Natalini, CC	en_US
dc.contributor.author	Pohlmann, AR	en_US
dc.contributor.author	Costa, TD	en_US
dc.contributor.author	Guterres, SS	en_US
dc.date.available	2009-11-30	en_US
dc.date.issued	2010-02-01	en_US
dc.identifier.citation	European Journal of Pharmaceutics and Biopharmaceutics, 2010, 74 (2), pp. 275 - 280	en_US
dc.identifier.issn	0939-6411	en_US
dc.identifier.uri	http://hdl.handle.net/10453/29612
dc.description.abstract	Soft agglomerates containing pantoprazole-loaded microparticles were developed with the aim of prompt delivery of gastro-resistant particles. The objective was to evaluate the relative bioavailability in dogs after the oral administration of soft agglomerates. Gastro-resistant pantoprazole-loaded microparticles prepared by spray drying were mixed with mannitol/lecithin spray-dried powder and agglomerated by vibration. One single oral dose (40 mg) was administered to dogs. Each dog received either a reference tablet or hard gelatin capsules containing the agglomerates. The plasma profiles were evaluated by non-compartmental and compartmental approaches, and the pharmacokinetic parameters were determined. The agglomerates presented 100% of drug particle loading and a production yield of 80.5%. The amount of drug absorbed after oral dosing was similar after reference or agglomerate administration, leading to a relative bioavailability of 108%. The absorption lag-time was significantly reduced after agglomerate administration (from 135.5 ± 50.6 to 15.0 ± 2.5 min). The agglomerated gastro-resistant pantoprazole-loaded microparticles reduced time to peak plasma. The agglomerates were equivalent to the reference tablets in terms of extent but not in terms of rate of absorption, showing that this formulation is an alternative to single-unit oral dosing with enteric coating and with the advantage of reducing time to effect. © 2009.	en_US
dc.relation.ispartof	European Journal of Pharmaceutics and Biopharmaceutics	en_US
dc.relation.isbasedon	10.1016/j.ejpb.2009.11.015	en_US
dc.subject.classification	Pharmacology & Pharmacy	en_US
dc.subject.mesh	Animals	en_US
dc.subject.mesh	Dogs	en_US
dc.subject.mesh	Anti-Ulcer Agents	en_US
dc.subject.mesh	Drug Carriers	en_US
dc.subject.mesh	Administration, Oral	en_US
dc.subject.mesh	Drug Compounding	en_US
dc.subject.mesh	Microspheres	en_US
dc.subject.mesh	Biological Availability	en_US
dc.subject.mesh	Intestinal Absorption	en_US
dc.subject.mesh	Particle Size	en_US
dc.subject.mesh	2-Pyridinylmethylsulfinylbenzimidazoles	en_US
dc.subject.mesh	Pantoprazole	en_US
dc.title	Pharmacokinetics evaluation of soft agglomerates for prompt delivery of enteric pantoprazole-loaded microparticles	en_US
dc.type	Journal Article
utslib.citation.volume	2	en_US
utslib.citation.volume	74	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	closed_access
pubs.issue	2	en_US
pubs.publication-status	Published	en_US
pubs.volume	74	en_US

Abstract:

Soft agglomerates containing pantoprazole-loaded microparticles were developed with the aim of prompt delivery of gastro-resistant particles. The objective was to evaluate the relative bioavailability in dogs after the oral administration of soft agglomerates. Gastro-resistant pantoprazole-loaded microparticles prepared by spray drying were mixed with mannitol/lecithin spray-dried powder and agglomerated by vibration. One single oral dose (40 mg) was administered to dogs. Each dog received either a reference tablet or hard gelatin capsules containing the agglomerates. The plasma profiles were evaluated by non-compartmental and compartmental approaches, and the pharmacokinetic parameters were determined. The agglomerates presented 100% of drug particle loading and a production yield of 80.5%. The amount of drug absorbed after oral dosing was similar after reference or agglomerate administration, leading to a relative bioavailability of 108%. The absorption lag-time was significantly reduced after agglomerate administration (from 135.5 ± 50.6 to 15.0 ± 2.5 min). The agglomerated gastro-resistant pantoprazole-loaded microparticles reduced time to peak plasma. The agglomerates were equivalent to the reference tablets in terms of extent but not in terms of rate of absorption, showing that this formulation is an alternative to single-unit oral dosing with enteric coating and with the advantage of reducing time to effect. © 2009.

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http://hdl.handle.net/10453/29612