Analgesic Rectal Suppositories Containing a Nonsteroidal Anti-Inflammatory Drug in Combination with a Tricyclic Antidepressant and Transmucosal Conductor

Abstract

A composition and preparation method for new analgesic rectal suppositories containing a nonsteroidal anti-inflammatory drug (ketorolac), tricyclic antidepressant (amitriptyline), and transmucosal conductor (silicon glycerolates) as the active ingredients in a poly(ethylene glycol) (PEG-4000) base were proposed. The acute toxicity was determined and showed they were safe to use. The high analgesic activity of the suppositories was confirmed using electrical stimulation. Their high transmucosal activity in vitro was revealed by measuring the degree of diffusion of one of the active ingredients (amitriptyline) through a natural biological membrane. The results indicated that the developed suppositories could be recommended for further investigations of future medical use to relieve pain of various etiologies.