Fast-disintegrating sublingual tablets: Effect of epinephrine load on tablet characteristics

Faculty of Pharmacy, University of Manitoba, Winnipeg, Manitoba, Canada.
AAPS PharmSciTech (Impact Factor: 1.64). 02/2006; 7(2):E41. DOI: 10.1208/pt070241
Source: PubMed


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, and D, containing 0%, 6%, 12%, and 24% of epinephrine bitartrate, respectively, and 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, and 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 and content uniformity. A linear increase in compression force resulted in an exponential increase in hardness for all formulations, a linear increase in disintegration and wetting times of A, and an exponential increase in disintegration and wetting times of B, C, and D. At a mean +/- SD hardness of > or = 2.3 +/- 0.2 kg, all tablet formulations passed the USP friability test. At a mean +/- SD hardness of < or = 3.1 +/- 0.2 kg, all tablet formulations resulted in disintegration and wetting times of <10 seconds and <30 seconds, respectively. Tablets with drug loads from 0% to 24% epinephrine can be formulated with hardness, disintegration times, and wetting times suitable for sublingual administration.

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Available from: Mutasem M Rawas-Qalaji, Mar 29, 2014
    • "The advantage of the sublingual drug delivery is that the drug can be directly absorbed into systemic circulation avoiding the first pass effect in the liver and gut. Moreover, sublingual mucosa is very thin compared to the intestinal or buccal mucosa and highly vascular allowing excellent drug absorption with a rapid onset of action [1] [2] [3]. A rapid onset of therapeutic effect is required in many acute conditions such as angina pectoris (sublingual nitroglycerine), cancer pain (sublingual fentanyl) and acute migraine attacks (oral zolmitriptan). "
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