Abstract
While nano-suspension amoxicillin is one of the approaches for improving dissolution rate of amoxicillinan antibiotic used widely. Stabilizing these nanodosage forms is always a challenge. The present study utilizes nanoprecipitation solvent evaporation technique for preparation of amoxicillin nanoparticles andproposed stability study approach of the same. The methodology was based on investigating stability of amoxicillin nano suspension in vitro, the optimized drug(polymer ratio re-formulated into nano-suspensions) and we compared our results with marketed suspensions. Samples were initially characterized and then subjected to stability testing at ambient temperature and relative humidity up to 6 months assayed using a validated HPLC method. During initial characterization, increase in saturation solubility and dissolution rate observed in all samples. During stability testing, there was gradual decrease in saturation solubility and dissolution rate of the samples, over the period of 3 months. This study considers long-term isothermal measurements, consistent with short-term non-isothermal (accelerating) measurements, providing predictive model to calculate the isothermal degradation periods. As per our results, we agree with the possibility to calculate the value of kinetic constants based on a fixed degradation limit, regardless of the shape of the curve. The accuracy of the prediction would be assessed by comparison of estimated shelf life versus data coming from traditional stability studies.
Highlights
Nano-suspensions are frequently used as an approach for solubility enhancement
Base-catalysed self-amino lysis, and dimerization occurs by nucleophilic attack of βLactamcarbonyl moiety of one molecule by the free side chain amino group of a neighbouring molecule
Concentrations of amoxicillin and the pH of the solution determine the corresponding input of the hydrolysis and amino lysis to the overall degradation reaction [1]
Summary
Nano-suspensions are frequently used as an approach for solubility enhancement. One of the overlooked aspects in the development of these dosage forms are the stability concerns and the degradation of the carried drugs. Amoxicillin is subject, in common with all penicillins, to hydrolytic degradation of the β-Lactamring under alkaline conditions. Decomposition of penecilloic acid to penilioc acid follows first order kinetic reaction [1]. Concentrations of amoxicillin and the pH of the solution determine the corresponding input of the hydrolysis and amino lysis to the overall degradation reaction [1]. The degradation of amoxicillin trihydrate over pH 3-10.5 at 35°C. follows first order kinetic. Nano-suspensions are advantageous in achieving quick onset of action for drugs that are completely but slowly absorbed, i.e. those having high tmax values. This is illustrated by the study carried out for naproxen, a nonsteroidal anti-inflammatory drug [3]. Among many administration routes of drug delivery, due to its advantages such as ease of ingestion, versatility to accommodate various types of drug candidates, low production cost, high safety, good patient compliance, and pain avoidance [4,5]
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