Adrenaline (epinephrine) microcrystal sublingual tablet formulation: enhanced absorption in a preclinical model

Objectives For anaphylaxis treatment in community settings, adrenaline (epinephrine) administration using an auto‐injector in the thigh is universally recommended. Despite this, many people at risk of anaphylaxis in community settings do not carry their prescribed auto‐injectors consistently and hes...

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Bibliographic Details
Published in:Journal of pharmacy and pharmacology 2015-01, Vol.67 (1), p.20-25
Main Authors: Rawas-Qalaji, Mutasem, Rachid, Ousama, Mendez, Belacryst A., Losada, Annette, Simons, F. Estelle R., Simons, Keith J.
Format: Article
Language:English
Subjects:
absorption
Administration, Sublingual
adrenaline
anaphylaxis
Anaphylaxis - drug therapy
Animals
Area Under Curve
Chemistry, Pharmaceutical
Epinephrine - administration & dosage
Epinephrine - pharmacokinetics
Epinephrine - therapeutic use
Female
Injections, Intramuscular
Metabolic Clearance Rate
microcrystals
Particle Size
Prospective Studies
Rabbits
sublingual tablets
Tablets - chemistry
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Summary:Objectives For anaphylaxis treatment in community settings, adrenaline (epinephrine) administration using an auto‐injector in the thigh is universally recommended. Despite this, many people at risk of anaphylaxis in community settings do not carry their prescribed auto‐injectors consistently and hesitate to use them when anaphylaxis occurs.The objective of this research was to study the effect of a substantial reduction in adrenaline (Epi) particle size to a few micrometres (Epi microcrystals (Epi‐MC)) on enhancing adrenaline dissolution and increasing the rate and extent of sublingual absorption from a previously developed rapidly disintegrating sublingual tablet (RDST) formulation in a validated preclinical model. Methods The in‐vivo absorption of Epi‐MC 20 mg RDSTs and Epi 40 mg RDSTs was evaluated in rabbits. Epi 0.3 mg intramuscular (IM) injection in the thigh and placebo RDSTs were used as positive and negative controls, respectively. Key findings Epimean(standard deviation) area under the plasma concentration vs time curves up to 60 min and Cmax from Epi‐MC 20 mg and Epi 40 mg RDSTs did not differ significantly (P > 0.05) from Epi 0.3 mg IM injection. After adrenaline, regardless of route of administration, pharmacokinetic parameters were significantly higher (P 
ISSN:0022-3573
2042-7158
DOI:10.1111/jphp.12312