The clinical pharmacokinetics of osmotic pump controlled release tablets of terazosin hydrochloride in healthy volunteers was studied.A sensitive and rapid HPLC method was used to determine the terazosin plasma concen...The clinical pharmacokinetics of osmotic pump controlled release tablets of terazosin hydrochloride in healthy volunteers was studied.A sensitive and rapid HPLC method was used to determine the terazosin plasma concentrations,and single and multiple doses of terazosin hydrochloride regular tablets（reference tablets）and osmotic pump controlled release tablets were orally administrated in randomized crossover design.The results showed that the C_（max）of the reference tablets after single oral dose（（120.56±23.15）ng/mL）in 20 healthy volunteers was significantly higher than that of controlled release tablets （（95.27±16.35）ng/mL）.The T_（max）of the controlled release tablets（（2.65±0.82）h）was significantly longer than that of reference tablets（（1.27±0.61）h）（P0.05）.The relative bioavailability of the controlled release tablets was found to be（105.85±6.12）%. The multiple oral dose pharmacokinetic parameters of the regular tablets and controlled release tablets were as follows：AUC_（SS） were（1275.17±175.35）and（1382.65±205.31）ng·h/mL respectively,C_（max）were（128.15±22.37）and（98.57±18.16）ng/mL respectively,T_（max）were（1.35±0.71）and（2.76±0.85）h respectively,C_（av）were（53.13±9.12）and（57.61±9.25）ng/mL respectively, and DF were（2.25±0.26）%and（1.62±0.25）%respectively.The relative bioavailability of the controlled release tablets to the reference tablets was（108.43±6.26）%.The controlled release tablet of terazosin hydrochloride was bioequivalent to the reference tablet.The controlled release tablet exhibited a sustained-release property with a significantly longer T_（max）and lower C_（max）.展开更多
In an open multicenter prospective study, the effects of short-term (4weeks, n= 101) and long-term (6 months, n = 38) terazosin treatment on blood pressure, serum lipids and safety in the patients with mild to moderat...In an open multicenter prospective study, the effects of short-term (4weeks, n= 101) and long-term (6 months, n = 38) terazosin treatment on blood pressure, serum lipids and safety in the patients with mild to moderate essential hypertension were observed. Mean systolic and diastolic blood pressure in sitting position were significantly reduced by 16. 4 % and 14. 0 % respectively (P<0.01 ) after 4 weeks of terazosin therapy, with the total efficacy rate being 87.1 %.During a 6 month therapy, antihypertensive effect of terazosin could be main-tained- Total cholesterol (TC) and low density lipoprotein (LDL ) cholesterol in serum were significantly decreased P < 0. 05-0.01) in patients with hyperc-holesterolemia (TC≥6 mmol/ml)after 4 week terazosin treatment; the levels of TC, LDL and triglyceride were significantly improved in hypertensive patients af-ter 3-6 month terazosin treatment. The improvement of lipid metabolism was re-lated to the dosage of terazosin but not to antihypertensive effects of terazosin.The results suggested that terazosin is effective in decreasing blood pressure and improving lipid metabolism. It may serve as a good antihypertensive agent for hy-pertensive patients with hypercholesterolemia.展开更多
Objective: To evaluate the efficacy and safety of terazosin and plasma kinetic resection of the prostate (PKRP) in the treatment of benign prostatic hyperplasia (BPH) patients with coexisting hypertension. Methods: A ...Objective: To evaluate the efficacy and safety of terazosin and plasma kinetic resection of the prostate (PKRP) in the treatment of benign prostatic hyperplasia (BPH) patients with coexisting hypertension. Methods: A total of 205 men who suffered from BPH with concomitant hypertension were enrolled in this study. They all received PKRP surgery and terazosin medication from one week before to 3 months after the operation. The procedures of efficacy and safety were evaluated by analysis of the changes in blood pressures, IPSS, Qmax and the drug related adverse events 4 weeks and 3 months after the operation. Results: The systolic blood pressure decreased from 161 ± 12.33 mmHg at baseline to 148 ± 7.27 mmHg four weeks (P?P?P?P?P?P?展开更多
Cyclodextrin-modified CZE was applied to the chiral separation of two basic drugs,i.e.,esmolol and terazosin.Selector screening and concentration optimization experiments were performed.Resolution 3.1 for esmolol,1.2 ...Cyclodextrin-modified CZE was applied to the chiral separation of two basic drugs,i.e.,esmolol and terazosin.Selector screening and concentration optimization experiments were performed.Resolution 3.1 for esmolol,1.2 for terazosin were achieved when using 60 mmol/L gamma-CD and 60 mmoL/L DM-P-CD,respectively,in 50 mmol/L pH 2.5 sodium phosphate buffer.展开更多
文摘The clinical pharmacokinetics of osmotic pump controlled release tablets of terazosin hydrochloride in healthy volunteers was studied.A sensitive and rapid HPLC method was used to determine the terazosin plasma concentrations,and single and multiple doses of terazosin hydrochloride regular tablets（reference tablets）and osmotic pump controlled release tablets were orally administrated in randomized crossover design.The results showed that the C_（max）of the reference tablets after single oral dose（（120.56±23.15）ng/mL）in 20 healthy volunteers was significantly higher than that of controlled release tablets （（95.27±16.35）ng/mL）.The T_（max）of the controlled release tablets（（2.65±0.82）h）was significantly longer than that of reference tablets（（1.27±0.61）h）（P0.05）.The relative bioavailability of the controlled release tablets was found to be（105.85±6.12）%. The multiple oral dose pharmacokinetic parameters of the regular tablets and controlled release tablets were as follows：AUC_（SS） were（1275.17±175.35）and（1382.65±205.31）ng·h/mL respectively,C_（max）were（128.15±22.37）and（98.57±18.16）ng/mL respectively,T_（max）were（1.35±0.71）and（2.76±0.85）h respectively,C_（av）were（53.13±9.12）and（57.61±9.25）ng/mL respectively, and DF were（2.25±0.26）%and（1.62±0.25）%respectively.The relative bioavailability of the controlled release tablets to the reference tablets was（108.43±6.26）%.The controlled release tablet of terazosin hydrochloride was bioequivalent to the reference tablet.The controlled release tablet exhibited a sustained-release property with a significantly longer T_（max）and lower C_（max）.
文摘In an open multicenter prospective study, the effects of short-term (4weeks, n= 101) and long-term (6 months, n = 38) terazosin treatment on blood pressure, serum lipids and safety in the patients with mild to moderate essential hypertension were observed. Mean systolic and diastolic blood pressure in sitting position were significantly reduced by 16. 4 % and 14. 0 % respectively (P<0.01 ) after 4 weeks of terazosin therapy, with the total efficacy rate being 87.1 %.During a 6 month therapy, antihypertensive effect of terazosin could be main-tained- Total cholesterol (TC) and low density lipoprotein (LDL ) cholesterol in serum were significantly decreased P < 0. 05-0.01) in patients with hyperc-holesterolemia (TC≥6 mmol/ml)after 4 week terazosin treatment; the levels of TC, LDL and triglyceride were significantly improved in hypertensive patients af-ter 3-6 month terazosin treatment. The improvement of lipid metabolism was re-lated to the dosage of terazosin but not to antihypertensive effects of terazosin.The results suggested that terazosin is effective in decreasing blood pressure and improving lipid metabolism. It may serve as a good antihypertensive agent for hy-pertensive patients with hypercholesterolemia.
文摘Objective: To evaluate the efficacy and safety of terazosin and plasma kinetic resection of the prostate (PKRP) in the treatment of benign prostatic hyperplasia (BPH) patients with coexisting hypertension. Methods: A total of 205 men who suffered from BPH with concomitant hypertension were enrolled in this study. They all received PKRP surgery and terazosin medication from one week before to 3 months after the operation. The procedures of efficacy and safety were evaluated by analysis of the changes in blood pressures, IPSS, Qmax and the drug related adverse events 4 weeks and 3 months after the operation. Results: The systolic blood pressure decreased from 161 ± 12.33 mmHg at baseline to 148 ± 7.27 mmHg four weeks (P?P?P?P?P?P?
基金jointly provided by the Doctoral Program Foundation of the State Commission of EducationNational Science Foundation of China are gratefully acknowledged.
文摘Cyclodextrin-modified CZE was applied to the chiral separation of two basic drugs,i.e.,esmolol and terazosin.Selector screening and concentration optimization experiments were performed.Resolution 3.1 for esmolol,1.2 for terazosin were achieved when using 60 mmol/L gamma-CD and 60 mmoL/L DM-P-CD,respectively,in 50 mmol/L pH 2.5 sodium phosphate buffer.
