Clonazepam oral droplets for the treatment of acute epileptic seizures

Drug Development and Industrial Pharmacy
Osamu SakataYoshiharu Machida

Abstract

Oral droplet formulations of clonazepam (CZ) were developed to examine their potentials as an alternative to i.v. administration for the treatment of acute epileptic seizures. Propylene glycol containing 2.5% (wt/wt) CZ with or without 5.0% (wt/wt) oleic acid (OA) was prepared as a solution by heating at 90 degrees C and subsequently lowering the temperature to 30 degrees C. The droplet (20 microL) was administered to the oral cavity between the lower gum and bottom lip before CZ precipitation started. With a droplet of propylene glycol loaded with 2.5% (wt/wt) CZ and 5.0% (wt/wt) OA, the plasma concentration reached 20 ng/mL (minimal effective concentration) within 10 min and was maintained between 20 and 60 ng/mL, less than a toxic level, for a period of 60 min. For a droplet of propylene glycol loaded only with CZ at 2.5% (wt/wt), it took more than 15 min for the plasma concentration to reach 20 ng/mL. It is suggested that a droplet of CZ/OA/propylene glycol (2.5:5.0:92.5, wt/wt) might be useful as an alternative to i.v. injection of CZ for the treatment of acute epileptic seizures.

References

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Oct 7, 2005·Drug Development and Industrial Pharmacy·Hiraku OnishiYoshiharu Machida
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Citations

Jan 21, 2011·Drug Development and Industrial Pharmacy·Osamu SakataHiraku Onishi
Jul 12, 2012·Drug Development and Industrial Pharmacy·Osamu Sakata, Hiraku Onishi
Jun 2, 2015·Biological & Pharmaceutical Bulletin·Hiraku OnishiKei Yumoto
Jan 5, 2010·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Osamu SakataYoshiharu Machida
Apr 22, 2011·Current Neurology and Neuroscience Reports·Valeriya S PoukasChristopher Todd Anderson

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