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Effect of Diallyl Trisulfide on the Pharmacokinetics of Nifedipine in Rats

Authors

  • Yue Wang,

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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  • Mei-Juan Zou,

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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  • Nan Zhao,

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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  • Jun-Gang Ren,

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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  • Hong Zhou,

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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  • Gang Cheng

    1. Authors are with Dept. of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical Univ., Mailbox 32#, 103 Wenhua Rd., Shenyang 110016, China. Author Ren is also with School of Pharmacy, Harbin Univ. of Commerce, Harbin 150076, China. Direct inquiries to author Cheng (E-mail: chenggang63@hotmail.com).
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Abstract

Abstract:  This study aimed to evaluate the effect of diallyl trisulfide (DATS), a major component derived from garlic, on the pharmacokinetics of nifedipine. Pharmacokinetic parameters of nifedipine were determined in rats following an oral gavage (3 mg/kg) or intravenous administration (0.75 mg/kg) of nifedipine with co-administration of DATS (20 mg/kg) and long-term pretreatment of DATS (20 mg/kg/d for 15 consecutive days). Compared to the control groups, higher Cmax and AUC0–24 h were observed for oral gavage of nifedipine after short-term and long-term pretreatment of DATS, whereas those for intravenous nifedipine were little changed. The oral bioavailabilities of nifedipine were remarkably enhanced via the concomitant use of DATS. In conclusion, DATS increased the oral exposure of nifedipine in rats likely by the modification of intestinal metabolism of nifedipine, indicating that combined use of DATS or DATS-containing supplement with nifedipine may require caution because high plasma concentrations may lead to an undesired toxicity of this agent.

Practical Application:  Patients suffering from cardiovascular disease should take caution in combined use of DATS or DATS-rich garlic supplement with nifedipine because long-term treatment of DATS could lead high plasma concentrations of nifedipine.

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