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Pharmaceutical Devices for Oral Cavity-based Local and Systemic Drug Delivery
Yun, Gyi-Ae,Choi, Sung-Up,Park, Ki-Hwan,Rhee, Yun-Seok,Lee, Beom-Jin,Lee, Jae-Hwi The Korean Society of Pharmaceutical Sciences and 2010 Journal of Pharmaceutical Investigation Vol.40 No.special
Pharmaceutical technology has primarily focused on the development of the best dosage forms depending on the route of administration. The design of dosage forms is greatly influenced by the route of administration. Due to a variety of advantages such as avoidance of first-pass effect, abundant blood supply and easy access to the absorption site, the oral cavity has frequently been selected as a site for drug delivery. Since the oral cavity is relatively unique from the anatomical and physiological viewpoint, one should always consider these conditions when designing the drug delivery systems for the oral cavity. In this regard, the current review paper was prepared to summarize the essential features of the drug delivery systems utilized in the oral cavity, along with the introduction of various dosage forms developed to date.
( Ik Soo Kim ),( Hyeong Min Kim ),( Jie Un Ro ),( Kang Hee Jo ),( San Deep Karki ),( Prakash Khadka ),( Gyi Ae Yun ),( Jae Hwi Lee ) 한국응용약물학회 2015 Biomolecules & Therapeutics(구 응용약물학회지) Vol.23 No.3
β-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of β-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of β-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of β-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of β-lapachone was 15.5%. The considerable degradation of β-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of β-lapachone may be resulted from the first-pass metabolic degradation of β-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.