RESUMO
The direct Pd-catalyzed ß-C-H arylation of aldehydes and ketones was developed by using 2-amino-N,N'-diisopropylsuccinamide as a novel transient directing group (TDG). The TDG showed good versatility in functionalizing unactivated ß-C-H bonds of aldehydes and ketones. It was effective not only for aliphatic aldehydes and ketones but also for aromatic aldehydes and ketones. Besides, it was applicable to o-methylbenzaldehydes.
RESUMO
OBJECTIVE: To prepare poly(lactide-co-glycolide) (PLGA) microspheres containing Oxymatrine (OMT-PLGA-MS) and study their release characteristics in vitro. METHODS: OMT-PLGA-MS was prepared with PLGA as carriers using double emulsion solvent evaporation method (W/O/W). The preparation technology of microspheres was optimized by orthogonal design, and the microspheres were characterized in terms of morphology, the rate of drug loading, encapsulation efficiency, and in vitro drug release. RESULTS: The formed microspheres were spherical with smooth surfaces and the average size was (98.3 +/- 3.4) microm. The encapsulation efficiency and rate of drug loading were (70.14 +/- 3.47)% and (21.59 +/- 1.07)%, respectively. In vitro release study revealed that 84.63% of OMT was released from OMT-PLGA-MS in 240 hours, and the Higuchi model fitted OMT release pattern best. CONCLUSION: OMT-PLGA-MS is prepared successfully and shows good sustained release characteristics.
