Synthesis and evaluation of octenyl succinate anhydride derivative of fenugreek gum as extended release polymer
Synthesis and evaluation of octenyl succinate anhydride derivative of fenugreek gum as extended release polymer
Ajay Kumar Sav(Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, India); Ritesh Amol Fule(Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, India); Meer Tarique Ali(Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, India); Purnima Amin(Institute of Chemical Technology, India)
43권 5호, 417~429쪽
초록
In current study, fenugreek gum (FG) plant derived product was investigated as a release retarding polymer. The octenyl succincate anhydride derivative of fenugreek gum (OSFG) was synthesized to introduce hydrophobic property and investigated for its drug release retarding property with reference to FG. The reaction was carried out in anhydrous conditions at different temperature (40–98 C) using NaHCO3 as a mild base catalyst and the influences of three factors such as reagent/substrate concentration,reaction temperature and time on the degree of substitution of OSFG were studied. Highly water-soluble metoprolol succinate (MPS) and poorly water-soluble carbamazepine (CBZ) were selected as model drug as for release studies. It was observed that increase in reaction temperature and reagent concentration resulted in high degree of substitution with significant decrease in viscosity. Reaction carried out at 98 C for 2 h showed high degree of substitution (0.133) with moderate retention of viscosity compared to plain FG. FTIR, DSC, XRD, solid state CPMAS 13C-NMR, and SEM studies provide structural information of synthesized OSFG. MPS ER tablet prepared with drug:OSFG:FG at the weight of 1:4:2 and CBZ ER tablet with drug:OSFG at the weight ratio of 1:3, respectively. Both formulations showed similar drug release profile compared to marketed formulations. Optimized tablet formulations were found to be stable under stability condition according to ICH guidelines. It was concluded that the developed formulations with OSFG have a release retarding property and can be used alone or in combination with other polymers for a controlled release.
Abstract
In current study, fenugreek gum (FG) plant derived product was investigated as a release retarding polymer. The octenyl succincate anhydride derivative of fenugreek gum (OSFG) was synthesized to introduce hydrophobic property and investigated for its drug release retarding property with reference to FG. The reaction was carried out in anhydrous conditions at different temperature (40–98 C) using NaHCO3 as a mild base catalyst and the influences of three factors such as reagent/substrate concentration,reaction temperature and time on the degree of substitution of OSFG were studied. Highly water-soluble metoprolol succinate (MPS) and poorly water-soluble carbamazepine (CBZ) were selected as model drug as for release studies. It was observed that increase in reaction temperature and reagent concentration resulted in high degree of substitution with significant decrease in viscosity. Reaction carried out at 98 C for 2 h showed high degree of substitution (0.133) with moderate retention of viscosity compared to plain FG. FTIR, DSC, XRD, solid state CPMAS 13C-NMR, and SEM studies provide structural information of synthesized OSFG. MPS ER tablet prepared with drug:OSFG:FG at the weight of 1:4:2 and CBZ ER tablet with drug:OSFG at the weight ratio of 1:3, respectively. Both formulations showed similar drug release profile compared to marketed formulations. Optimized tablet formulations were found to be stable under stability condition according to ICH guidelines. It was concluded that the developed formulations with OSFG have a release retarding property and can be used alone or in combination with other polymers for a controlled release.
- 발행기관:
- 한국약제학회
- 분류:
- 약학