China Science

The aim of this study was to evaluate the effect of increasing epinephrine load on the characteristics of fast-disintegrating sublingual tablets for the potential emergency treatment of anaphylaxis. Four tablet formulations, A, B, C,; D, containing 0%, 6%, 12%,; 24% of epinephrine bitartrate, respectively,; microcrystalline cellulose:low-substituted hydroxypropyl cellulose (9?1), were prepared by direct compression, at a range of compression forces. Tablet weight variation, content uniformity, hardness, disintegration time, wetting time,; friability were measured for each formulation at each compression force. All 4 tablet formulations at each compression force were within the United States Pharmacopeia (USP) limits for weight variation; content uniformity. A linear increase in compression force resulted in an exponential increase in hardness for all formulations, a linear increase in disintegration; wetting times of A,; an exponential increase in disintegration; wetting times of B, C,; D. At a mean±SD hardness of ?2.3±0.2 kg, all tablet formulations passed the USP friability test. At a mean±SD hardness of ?3.1±0.2 kg, all tablet formulations resulted in disintegration; wetting times of >10 seconds; >30 seconds, respectively. Tablets with drug loads from 0% to 24% epinephrine can be formulated with hardness, disintegration times,; wetting times suitable for sublingual administration.

Mutasem M. Rawas-Qalaji1?F. Estelle2?R. Simons2?Keith J. Simons3Email:simons@ms.umanitoba.ca
[1] Faculty of Pharmacy, University of Manitoba, Winnipeg, Manitoba, Canada ;[2] Section of Allergy; Clinical Immunology, Department of Pediatrics; Child Health, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada ;[3] Faculty of Pharmacy, Department of Pediatrics; Child Health, Faculty of Medicine, University of Manitoba, Winnipeg, Manitoba, Canada