ANTIOXIDATION AND HYDROLYSIS MICROCAPSULES OF PENICILLIN V POTASSIUM: FORMULATION OPTIMISATION, CHARACTERISATION AND PHARMACOKINETICS

摘要

In order to conceal the unpleasant smell penicillin V potassium, and meet the needs of children, we deal with preparation of penicillin V potassium by microencapsulated process. For the future it is prepared into a stable solid formulation. We use ethyl cellulose as shells, penicillin V potassium as cores, sucrose as pore inducer, acetone as the dispersed phase, liquid paraffin as continuous phase. The liquid drying method is used for preparation of penicillin V potassium microcapsules and the characterisation is made by Scanning electron microscopy (SEM), Differential scanning calorimeter (DSC) and X-ray diffraction (XRD). Based on the results obtained from the orthogonal experimental design, the optimum preparation process are summarised as follows: ethyl cellulose : penicillin V potassium =1:1 (molar ratio), sucrose : ethyl cellulose = 0.2:1.0, temperature 30°C, stirring speed - 200 r/rnin, amount of surfactant Span-80 in 400 ml liquid paraffin - 1.0 g, stirring time - 4 h, encapsulation efficiency - 88.0%. The pharmacokinetic parameters indicate that penicillin V potassium microcapsules are bioequivalent to commercial penicillin V potassium granules in dogs. SEM shows that particle size is uniform, roundness is good, and the penicillin V potassium microcapsules show positive results over the commercial product in terms of the pharmacokinetics in dogs.