Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica

Acta Academiae Medicinae Sinica ›› 2019, Vol. 41 ›› Issue (1): 57-62.doi: 10.3881/j.issn.1000-503X.10536

• Original Articles • Previous Articles     Next Articles

Pharmacokinetics of Nimodipine after Intraocular Administration in Rats

LI Fang1,MAO Dan1,DAI Manman1,ZHANG Huimin1,MA Qun1,BAI Luyu1,HE Ning1,2,3()   

  1. 1 Department of Pharmaceutics,School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012,China
    2 Institute of Pharmaceutics,Anhui Academy of Chinese Medicine,Hefei 230012,China
    3 Anhui Province Key Laboratory of Chinese Medicinal Formula,Hefei 230012,China
  • Received:2018-05-11 Online:2019-02-28 Published:2019-03-06
  • Contact: Ning HE
  • Supported by:
    Supported by Anhui Province:“Special Support Plan” for the Second Batch of Innovative Leading Talents


Objective To explore the pharmacokinetics of nimodipine in plasma of rats after intraocular administration.Methods Totally 135 SD rats were randomly divided into three groups according to drug administration routes:intraocular(io group),intravenous (iv group),and intragastric (ig group). The doses were 5.0 mg/kg for IO and IV groups and 10.0 mg/kg for IG group. The serum nimodipine level was analyzed by high performance liquid chromatography. The main pharmacokinetic parameters were calculated and compared.Results The pharmacokinetic parameters in io group were as follows:Cmax:0.52 mg/ml;tmax:5.0 min;and AUC0-t:21.10 mg/(ml·min). The main pharmacokinetic parameters in iv group were as follows:Cmax:3.62 mg/ml;and AUC0-t:52.58 mg/(ml·min). The main pharmacokinetic parameters in ig group were as follows:Cmax:0.20 mg/ml;tmax:5.0 min;and AUC0-t:5.98 mg/(ml·min).Conclusions Nimodipine is rapidly absorbed after io administration,and the ophthalmic formulation has a higher bioavailability than the oral solution. Therefore,the io route may help to improve the treatment effectiveness of cardiovascular diseases.

Key words: nimodipine, ophthalmic administration, pharmacokinetics

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