Faculty Articles

PubMed Identifier

30324360

In Vivo Evaluation of Taste-Masked Fast-Disintegrating Sublingual Tablets of Epinephrine Microcrystals

Publication Title

AAPS PharmSciTech [electronic resource]

Publication Date

11-1-2018

Keywords

Administration, Sublingual, Anaphylaxis, Animals, Bronchodilator Agents, Drug Evaluation, Preclinical, Epinephrine, Excipients, Female, Injections, Intramuscular, Microspheres, Rabbits, Random Allocation, Tablets, Taste

Abstract

In community settings, IM injection of 0.3 mg epinephrine (Epi) using an auto-injector is the drug of choice for treatment of anaphylaxis. Previously, a taste-masking (TM) formulation of fast-disintegrating sublingual tablets (FDSTs) was developed in our lab. Also, Epi was micronized (Epi-MC) successfully and reduced the previously achieved bioequivalent sublingual Epi dose to 0.3 mg IM injection by half using non-taste-masked fast-disintegrating sublingual tablets (TM-FDSTs). Our objective for this study was to evaluate the sublingual absorption of Epi-MC using TM-FDST. These sublingual Epi tablets have potential for out-of-hospital treatment of anaphylaxis and are suitable for human studies. TM-FDSTs containing Epi-MC were manufactured by direct compression. The rate and extent of Epi absorption from our developed 20 mg Epi-MC-TM-FDSTs (n = 5) were evaluated in rabbits and compared to the previous result from 20 mg Epi-MC in non-TM-FDSTs and EpiPen® auto-injector. Blood samples were collected over 1 h, and Epi concentrations were measured using HPLC with electrochemical detection. Mean ± SEM AUC

DOI

10.1208/s12249-018-1171-4

Volume

19

Issue

8

First Page

3886

Last Page

3894

Disciplines

Medicine and Health Sciences | Pharmacy and Pharmaceutical Sciences

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