Studies on the slow release characteristic parameters based on the interaction between drugs and HPMC

LI Shao-zhi; HUANG Zi-yu; REN Xiao-wen; MENG Fan-cui; TANG Li-da; XU Wei-ren

Abstract：Objective:By studying the blocking effects of hydroxypropyl methyl cellulose (HPMC) gel on the penetration of 5 drugs with different properties,to investigate the applicability of the parameters of sustained release of HPMC,and to clarify the sustained release mechanism of hydrophilic gel from the interaction view.Methods:Five drugs with different properties (torasemide,lomerizine hydrochloride,ibuprofen,ambroxol hydrochloride,metformin hydrochloride) were selected as model drugs.Three-compartment penetrating detection devices were used in experiments.The detection times were 1,3,7,10,24 h.Permeability rate and blocking rate were observed.The interaction energies of drug-HPMC were calculated by blend module of Material Studio's software.Results:The blocking rates form three concentrations (5,10 and 20 mg·mL-1) of HPMC were applied as the parameters to describ the chracteristics of sustained relase.The results showed that the existence of HPMC had different influences on the 5 drugs.HPMC had weak ablity to block the panetration of ambroxol and metformin,and had strong absorption to torasemide and ibuprofen,torasemide.HPMC can block the penatration of lomerizine with saturation effect.The interaction energies form theoretical calculation correlated the experimental blocking rate at 24 hours well.Conclusion:The sustained release paramters baseed on the bloking rate form concentration and low concentration of HPMC are useful to elucidate the interactiom modes between-HPMC and drugs,and to help the selectin of excipients for sustained release formulaton.The parameter can also be used to ensure the quality consistency of excipient itself.