Preparation and characterization of timolol maleate phospholipid complex

ObjectiveTo prepare the timolol maleate phospholipid complex for improving the liposolubility of timolol maleate.

MethodsThe timolol maleate phospholipid complex was prepared using solvent evaporation method.According to the recombination rate, the ratio of timolol maleate and soybean phosphatide, formation temperature and time were optimized and screened using single-factor experiment.The phospholipid complex prepared by optimal prescription was verified using differential scanning calorimetry, Fourier infrared spectroscopy and ultraviolet spectroscopy, and its property characterization was investigated.The dissolubilities of timolol maleate and its phospholipid complex in distilled water or chloroform were determined and compared.

ResultsThe 10 mL tetrahydrofuran acted as the solvent, the molar ratio of timolol maleate to phospholipid was 1:2.5, the water bath temperature was 40 ℃, and the formation time was 3 h, the recombination rate of timolol maleate phospholipid complex was the highest, which arrived at (96.54±2.46)%.The solubility test results showed that the solubility of timolol maleate phospholipid complex in distilled water was significantly lower than that of timolol maleate, and the solubility of timolol maleate phospholipid complex in chloroform was significantly higher than that of timolol maleate(P < 0.01).

ConclusionsTimolol maleate is prepared into phospholipid complex, which improves its lipid solubility, and is beneficial to increase the drugs residence time in skin and mucosa, and prolongs the efficacy.