The Difference in Pharmacokinetics and Pharmacodynamics between Extended-Release Fluvastatin and Immediate-Release Fluvastatin in Healthy Chinese Subjects.

The aim of this study was to evaluate the difference in pharmacokinetics and pharmacodynamics between extended-release (ER) fluvastatin tablet and its immediate-release (IR) capsule in Chinese healthy subjects. This was an open-label, single/multiple-dose, two-period, two-treatment, crossover, rando...

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Publicado en:Journal of Biomedicine & Biotechnology Vol. 2012; pp. 1 - 5
Autores principales: Xu, H. R., Chen, W. L., Chu, N. N., Li, X. N., Zhu, J. R.
Formato: research tables/charts randomized controlled trial Journal Article
Publicado: Wiley-Blackwell 2012
Acceso en línea:Ver este registro en EBSCOhost
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      pub: Wiley-Blackwell
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        atl: The Difference in Pharmacokinetics and Pharmacodynamics between Extended-Release Fluvastatin and Immediate-Release Fluvastatin in Healthy Chinese Subjects.
      aug:
        au:
          Xu, H. R.
          Chen, W. L.
          Chu, N. N.
          Li, X. N.
          Zhu, J. R.
        affil: Department of Clinical Pharmacology, Zhongshan Hospital, Fudan University, Shanghai 200032, China
      sug:
        subj:
          Antilipemic Agents Therapeutic Use
          Fluvastatin Pharmacokinetics
          Fluvastatin Pharmacodynamics
          Fluvastatin Administration and Dosage
          Delayed-Action Preparations
          Biological Availability
          Male
          Young Adult
          Human
          Time Factors
          Adult
          Randomized Controlled Trials
          China
          Crossover Design
          Fluvastatin Blood
          Data Analysis Software
          Descriptive Statistics
          Analysis of Variance
          Confidence Intervals
          Adult: 19-44 years
          Male
      ab: The aim of this study was to evaluate the difference in pharmacokinetics and pharmacodynamics between extended-release (ER) fluvastatin tablet and its immediate-release (IR) capsule in Chinese healthy subjects. This was an open-label, single/multiple-dose, two-period, two-treatment, crossover, randomized trial with a minimum washout period of 7 days. Twenty healthy male adult subjects were given fluvastatin ER tablet 80mg QD by oral administration or fluvastatin IR capsule 40 mg BID for seven days. Blood samples were collected up to 24 hours after dosing on day 1 and day 7. Serum concentrations of fluvastatin were determined by LC-MS/MS. For fluvastatin ER tablet 80 mg QD, Cmax was 61.0 ± 39.0 and 63.9 ± 29.7 ng/mL, and AUC0-24 h was 242 ± 156 and 253 ± 91.1 ng·h/mL on day 1 and 7, respectively. For fluvastatin IR capsule 40 mg BID, Cmax was 283 ± 271 and 382 ± 255 ng/mL, and AUC0-24 h was 720 ± 776 and 917 ± 994 ng·h/mL on day 1 and day 7, respectively. The relative bioavailability of fluvastatin ER tablet 80 mg QD to fluvastatin IR capsule 40mg BID is (45.3 ± 23.9)% and (43.3 ± 24.1)% on day 1 and day 7, respectively. Tmax for fluvastatin ER tablet was 2.50 and 2.60 h and for capsule was 0.78 and 0.88 h on day 1 and day 7, respectively. In the first period, compared to baseline, cholesterol decreased 15.3% in fluvastatin ER tablet 80 mg QD and 16.9% in fluvastatin IR capsule 40mg BID. Triglyceride decreased 3.7% in fluvastatin ER tablet 80 mg QD and 19.1% in fluvastatin IR capsule 40mg BID. The difference has no statistical significance at P > 0.05 in reduction percent of cholesterol and triglyceride between the two groups. No adverse events were recorded. The results indicated that Cmax of fluvastatin ER tablet is reduced and Tmax is prolonged compared with IR capsule. There is no accumulation for ER formulation after multiple doses.
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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