Characterisation of rectal amoxicillin (RAMOX) for the treatment of pneumonia in children

Abstract

Access to medicines, including their availability and affordability, is a major public health challenge worldwide. This research aimed to characterise rectal formulations containing amoxicillin for the treatment of pneumonia in children under five, as an accessible alternative to existing formulations. Lipophilic Suppocire (S-NA15) and hydrophilic polyethylene glycol (PEG; 80% PEG 1500 and 20% PEG 4000, w/w) suppositories containing 250 mg amoxicillin were prepared. Hardness, apparent viscosity, uniformity of mass, uniformity of content, disintegration and dissolution time were determined. Irritation potential was screened using a slug mucosal assay and antibacterial efficacy against Staphylococcus aureus determined by isothermal microcalorimetry. Both lipophilic and hydrophilic formulations met the European Pharmacopoeia standards for suppositories when tested in vitro. They disintegrated within 30 min with rapid amoxicillin release profiles (98.6 ± 0.9%, 94.9 ± 1.2% over 30 min, respectively). Over-encapsulation of S-NA15 suppositories with hydroxypropyl methylcellulose shells slowed drug release and improved stability over 2 months. S-NA15 suppositories were classified as non-irritant and PEG suppositories only mildly irritant. Antibacterial efficacy of formulations was equivalent to amoxicillin alone. Both PEG and over-encapsulated S-NA15 rectal formulations developed in the present work have shown promise based on pre-clinical screening, and further development is justified to develop a product with commercial potential.

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

“…The formulations showed a disintegration time between 13 and 19 minutes (Table 1). These values are in agreement with the literature and compatible with the compendial data [14,29].…”

“…Hardness or breaking force was determined by using a tablet hardness tester (PharmaTest, Germany) at room temperature. As previously reported, the minimum mechanical force was measured to break the suppositories (ten suppositories were tested for a formulation group) [29]. Briefly, each suppository was placed the same way such that the apex was pointed up and the longest side remained parallel with the jaws of the instrument.…”

Rektalna primjena lijekova u pedijatrijskoj populaciji

“…Amoxicillin, Azithromycin, etc. and the outcomes indicate that the rectal delivery of the same would be effective (14,15). Another study's results suggest that development of new formulations of suppositories resulted in improved bioavailability and absorption of B-lactams (e.g., Benzathine benzylpenicillin) and aminoglycosides (e.g., Amikacin) (16).…”

Rectal Bioavailability of Amoxicillin from Hollow-Type Suppositories: Effect of Chemical Form of Amoxicillin

“…Though minimally invasive, amoxicillin instability was reported due to the moisture and temperature in microneedle arrays [ 3 ]. Amoxicillin-containing rectal drug delivery systems have been identified as an alternative paediatric dosage form that is relatively inexpensive to manufacture compared with other non-oral dosage forms, and may be able to overcome these stability challenges by protecting the drug from moisture and high temperatures [ 4 , 5 , 6 ].…”