The pharmacokinetics and bioequivalence of acipimox sustained-release tablets after a single and multiple oral administration in healthy dogs / 药学学报
Acta Pharmaceutica Sinica
; (12): 457-461, 2005.
Article
在 Zh
| WPRIM
| ID: wpr-353435
Responsible library:
WPRO
ABSTRACT
<p><b>AIM</b>To study the pharmacokinetics and bioequivalence of acipimox sustained-release tablets (SRT) after a single and multiple oral dose in healthy dogs.</p><p><b>METHODS</b>The plasma concentrations of of SRT and reference capsules with a single and multiple oral doses.</p><p><b>RESULTS</b>The drug concentration-time profiles fitted to a noncompartment model. After a single dose administration of sustained-release tablets and capsules, the pharmacokinetic parameters were as follows: AUC were (158 +/- 30) and (147 +/- 37) microg x h x mL(-1); Tmax were (4.3 +/- 0.8) and (2.6 +/- 1.3) h; Cmax were (29 +/- 6) and (42 +/- 10) microg x mL(-1); T(1/2) were (2.3 +/- 0.7) and (1.60 +/- 0.10) h; MRT were (6.0 +/- 0.8) and (3.9 +/- 0.7) h, respectively. The relative bioavailability of the sustained-release tablet was (108 +/- 16) %. After a multiple oral administration of sustained-release tablets and capsules, the pharmacokinetic parameters were as follows: AUC were (209 +/- 23) and (195 +/- 26) microg x h x mL(-1); Tmax were (6.3 +/- 0.8) and (3.4 +/- 1.5) h; Cmax were (27 +/- 4) and (36 +/- 5) microg x mL(-1); Cmmin were (2.2 +/- 1.0) and (0.20 +/- 0.20) microg x mL(-1); Cav were (8.7 +/- 1.0) and (8.1 +/- 1.1) micro x mL(-1); FI were (293 +/- 73) % and (448 +/- 91) % , respectively. The relative bioavailability of the sustained-release tablet was (114 +/- 19) %.</p><p><b>CONCLUSION</b>The results of two one-side test from single dose administration shown that two preparations were bioequivalent. The Cmax of sustained-release tablet was lower than that of capsules, while the Tmax and MRT of sustained-release tablet were higher than that of capsule, which indicating a good retarding effect. The results from multiple dose administration also shown that two preparations were bioequivalent and the DF of sustained-release tablet was significant lower than that of capsule.</p>
全文:
1
索引:
WPRIM
主要主题:
Pyrazines
/
Tablets
/
Capsules
/
Pharmacokinetics
/
Biological Availability
/
Therapeutic Equivalency
/
Random Allocation
/
Administration, Oral
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Area Under Curve
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Delayed-Action Preparations
研究类型:
Prognostic_studies
限制:
Animals
语言:
Zh
期刊:
Acta Pharmaceutica Sinica
年:
2005
类型:
Article