• Archives of Pharmacal Research
• /
• v.26 no.8
• /
• pp.644-648
• /
• 2003

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

• Journal of Pharmaceutical Investigation
• /
• v.33 no.1
• /
• pp.45-49
• /
• 2003

The solubility and stability of ondansetron hydrochloride (OS) in various vehicles were determined. The effect of cyclodextrins (CD) on the solubility of OS in water was determined by equilibrium solubility method. The solubility of OS at $32^{\circ}C$ increased in the rank order of isopropyl myristate (IPM) < propylene glycol laurate (PGL) ${\ll}$ propylene glycol monolaurate < propylene glycol monocaprylate (PGMC) < poly(ethylene glycol) 400 < diethylene glycol mono ethyl ether (DGME) < ethanol < poly(ethylene glycol) 300 < water (36.1 mg/ml) ${\ll}$ propylene glycol (PG) (283 mg/ml). The addition of PG or DGME to non-aqueous vehicles such as IPM, PGL and PGMC markedly increased the solubility of OS. The addition of CDs in water increased the solubility. Apparent stability constant for the CD complexation with OS was calculated to be $25.5\;M^{-1}$ for $2-hydroxypropyl-{\beta}-CD\;(2HP{\beta}CD)$. Twenty mM ${\beta}-CD$, 69.4 mM sulfobutyl ether ${\beta}-CD$ and 115.4 mM $2HP{\beta}CD$ increased the aqueous solubilty of OS 1.27, 2.18 and 1.85 times, respectively. OS was stable in buffered aqueous solution (pH 5.0). However, OS was relatively unstable in non-aqueous vehicles in the order of PG

• Proceedings of the PSK Conference
• /
• 2002.10a
• /
• pp.414.1-414.1
• /
• 2002

To improve the compliance of oral administration of drugs in cancer patients, who are unable to swallow tablets, FDT containing ondansetron HCI($Onseran^{TM}$) was developed with a low-cost manufacturing process. $Onseran^{TM}$ was prepared from ondansetron. mannitol, crospovidone. and others with a direct compression method. The disintegration time and dissolution rate of $Onseran^{TM}$ were assessed according to the USP method. The results were compared with those of the reference drug ($Zofran^{TM}$). (omitted)

• Proceedings of the PSK Conference
• /
• 2000.04a
• /
• pp.206.2-206.2
• /
• 2000

• Korean Journal of Clinical Pharmacy
• /
• v.10 no.2
• /
• pp.74-79
• /
• 2000

Y-Site 투여시 $5\%$포도당액과 생리식염수에서 탁솔과 은단세트론의 안정성에 관해 실온과 형광등 아래서 연구하였다. 온단세트론 0.03 mg/ml, 0.1 mg/ml, 0.3 mg/ml와 탁솔 0.3 mg/ml, 1.2mg/ml를 각각 1:1로 혼합한 후 0, 1, 2, 4, 12시간에서 즉시 약물농도를 HPLC로 분석하였다. 방해물질에 의한 분석오차를 줄이기 위해 분석법을 여러상태에서 확인하였으며, 각 농도에서 3차례씩 실험하였고 각 샘플은 2차례 연속 HPLC 분석하였다. 분석전에 각 시료의 투명도, 색의변화, 침전상태 및 pH를 검사하였다. 온단세트론 0.03, 0.1 및 0.3 mg/ml와 탁솔 0.3 및 1.2mg/ml를 각각 혼합하였을 때 12시간 동안 안정성이 있었다. 혼탁이나 색의 변화 및 침전은 나타나지 않았으며 12시간 동안 pH의 변화는 특별한 경향이 없었다.

• The Korean Journal of Physiology and Pharmacology
• /
• v.15 no.5
• /
• pp.267-272
• /
• 2011

A number of studies have demonstrated that 5-hydroxytryptamine (5-HT) can induce muscle contraction or relaxation response and enhance secretion in the gastrointestinal tract via a multiplicity of 5-HT receptor subtypes. In the present study, we investigated the pharmacological characterization of the 5-HT-induced contractile response in longitudinal smooth muscle isolated from the feline ileum. Addition of 5-HT into muscle chambers enhanced the basal tone and spontaneous activity in a concentration-dependent manner. The neurotoxin tetrodotoxin did not alter the 5-HT-induced contraction of the longitudinal muscles. Neither atropine nor guanethidine affected the contraction. The 5-HT agonists, 5-methylserotonin hydrochloride and mosapride, also evoked concentration-dependent contractions. The 5-HT-induced contraction was enhanced by the $5HT_2$ receptor antagonist ketanserin and the $5-HT_3$ receptor antagonist ondansetron but was inhibited by the 5-$HT_1$ receptor antagonist methysergide and 5-$HT_4$ receptor antagonist GR113808. These results indicate that 5-$HT_1$ and 5-$HT_4$ receptors may mediate the contraction of the 5-HT-induced response and 5-$HT_2$ and 5-$HT_3$ receptors may mediate 5-HT-induced relaxation in feline ileal longitudinal smooth muscles.