The Preparation Of Buspirone Hydrochloride Extended-release Tablets

The physicochemical,pharmacokinetic and pharmacological properties of Buspirone Hydrochloride decide how itshould be administrated in a therapeutic situation It should be administered in short dosing intervals to maintain the plasma concentration levels that provide the pharmacologic action because Buspirone Hydrochloride is of a short biologicalhalf-life(t1/2=2.63+ 0.48h). In this study,Buspirone Hydrochloride was slowly released from matrix by using different pharmaceutical excipients like HPMC,CBP and PCL in the extended- release tablets. Administration of these formulation increases Buspirone Hydrochloride bioavailability,Meanwhile it improved patient tolerability convenience and compliancity.The UV method was established for the BPR-HPMC extended-release tablets to determine the BPR content. This method was valid with respect to simpliciry,accuracy,sensitivity and precision.lt could be used in this studies.Buspirone Hydrochloride extended-release tablets were prepared by using HPMC in uniform- design. The best prescription was evaluated by determination Buspirone Hydrochloride in vitro release profile. This matrix system(BPR-HPMC extended release Tablets,BPR-HPMC) shows some characterization of extended-release,for example,Buspirone Hydrochloride release in vitro 24 for hours. but somedisadvantages in this matrix system still existAnother two kinds of extended-release formulations were prepared by adding CBP and PCL excipient into the BPR-HPMC matrix respectively to reduce quickly drug release in the early stage of drug release.The results show that BPR-HPMC/PCL extended-release tablets is better than BPR-HPMC/CBP in the extended release properties.BPR-HPMC/PCL tablet were administrated to rabbit with daily dosing. The drug concentration of plasma was determinated byHPLC.The result showed that:t,=2.14 h,C=9.06 ng/ml,AUC=211.70 ngh/ml compared with the immediated release tablets:t=0.5-1.0h,C=51.6+0.54 ng/ml,AUO135.86 ng h/ml. This formulation could keep the drug concentration in therapeutic window:1.27+0.52ng/ml-148.36+1.00ng/ml .BPR-HPMC/PCL formulation could extend drug release to 24 hours,It was an expective extended-release preparation,which could be continued to study in the clinic application.