ABSTRACT
OBJECTIVE: To evaluate the pharmacokinetics characteristics and safety of antipsytrotic ziprasidone mesylate with single dose intramuscularly injected in healthy volunteers. METHODS: A total of 12 healthy Chinese volunteers(male 6 cases and female 6 cases) were received intramuscularly single dose of ziprasidone mesylate, the dosage was 10 mg.Blood samples were collected at different time after intramuscularly injection.The concentrations of ziprasidone in serum were determined by LC-MS/MS, and the pharmacokinetic parameters were calculated. RESULTS: The concentration-time curves of ziprasidone fitted to two-compartment model.The pharmacokinetic parameters were stated as follows, ρmax was (97.85± 29.24) ng·mL-1;tmax was (0.56±0.30)h;MRT was (5.35±0.96) h; t1/2 was (4.29±0.88)h; AUC0→t was (405.6±98.68) ng·h·mL-1, AUC0→∞was (413.3± 100.69)ng·h·mL-1; CL was (25.50±6.10)L·h-1; Vd was (157.48±47.60)L; Kel was (0.168±0.035)h. There were no significant differences of the parameters between the male and female subjects. The common adverse events were somnolence, nausea and weakness with the severity of mild to moderate. CONCLUSION: The pharmacokinetic parameters in 12 healthy volunteers after intramuscular injection of 10 mg ziprasidone mesylate are in line with that reported in the literature. This medicine has effect of sedation, so that it could be used to control the excited agitation.
ABSTRACT
Objective To investigate the clinical efficacy and safety of ziprasidone mesylate injection on the acute agitation symptom in mental retardation. Methods The total of 80 patients of mental retardation with acute agitation symptoms were randomly divided into two groups:the treatment group (40 patients) were intra-muscarly given with ziprasidone mesylate injection at the initial dose of 10 mg, 20 mg 4 h later, and 30 mg once on the second day and third day. And the control group (40 patients) were treated with haloperidol injection. The volume dose of haloperidol was 20 mg everyday. Other antipsychotic drugs, antimanic drugs and benzodiazepines were not allowed to be used during the observation, neither does the prophylactic use of drugs against parkinson's disease. Before and 1, 2, 4, 6, 8, 12, 24, 48, 72 h after treatment, the positive and negative scale ( PANSS) reduction rate, the end of the clinical global impression scale ( CGI) were assessed. By the end of the treatment, the adverse reactions symptom, cale ( TESS) was assessed for the safety. Results By the end of treatment PANSS reduction rate was 46. 31% in the test group and 48. 81% in the control group, the clinical improvement rate was 80. 00% in the treatment group and 82. 50% in the control group. No statistically significant difference on efficacy was found between two groups. The side reaction rate in the treatment group was 27. 5%, that in the control group was 40. 0%, there was significant difference ( P<0. 05) between two groups, but the extrapyramidal reaction in the control group was significantly more than that in the treatment group(P<0. 05). Conclusion Ziprasidone mesylate injection is effective on treating the symptoms of mental retardation, in corresponding to the effect of haloperidol injection,and with less extrapyramidal reactions.
ABSTRACT
OBJECTIVE:To study the pharmacokinetics of a single dose of intramuscularly injected ziprasidone mesylate in healthy volunteers.METHODS:A total of10healthy volunteers were received intramuscularly single dose of ziprasidone me-sylate20mg,venous blood samples were taken at different time after intramuscular injection,the concentrations of ziprasidone in serum were determined by HPLC,and the pharmacokinetic parameters were calculated with3p97program.RESULTS:The concentration-time curves of ziprasidone fitted to two-compartment model.The pharmacokinetic parameters were stated as follows,C max was(866.32?482.88)ng/ml;t max was(0.57?0.23)h,t 1/2ke was(2.17?1.04)h,CL was(17.0?9.00)ml/h,AUC 0～12 was(1467.94?644.80)(ng?h)/ml and ACU 0～∝ was(1603.48?722.47)(ng?h)/ml.CONCLUSIONS:The pharmacoki-netics parameters in10healthy volunteers after intramuscular injection of20mg ziprasidone mesylate are in line with that re-ported in the literature.