• Title/Summary/Keyword: Eperisone

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Long-Lasting Muscle Relaxant Effect of Patch Containing Centrally Acting Muscle Relaxant (중추성 근이완패취제의 지속성 근이완효과)

  • 양상인;이승진;박하영;이상호;장춘곤;이완석;신영희;김정주;이석용
    • YAKHAK HOEJI
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    • v.47 no.2
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    • pp.120-124
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    • 2003
  • Due to its profound intestinal first-pass metabolism, oral eperisone hydrochloride produces a very low bioavailability and a very short muscle relaxant activity. To improve the efficacy and compliance of eperisone, we designed a new dosage form, the transdermal patch and evaluated the muscle relaxant effects of this patch in rats. The muscle relaxant activity was assessed by measurement of forelimb grip strength and hanging test in rats. The transdermal patch of eperisone hydrochloride showed significant muscle relaxant activity at 0.5, 1.5 and 3 cm$^2$/200 g rat (1.39, 4.17 and 8.33 mg of eperisone hydrochloride/kg, respectively) in a dose-dependent manner and the effects were lasted over 24 hours. The oral eperisone hydrochloride showed significant activity at 12.5, 25 and 50 mg/kg in a dose-dependent manner but the activity was within 1 or 2 hours after administration. These results suggest that the eperisone hydrochloride is absorbed efficiently from transdermal patch and the patch can exert potent and long-lasting muscle relaxant activity. This transdermal patch will increase the efficacy and compliance in the clinical use of eperisone hydrochloride.

Drug Delivery into the Blood-Brain Barrier by Endogenous Substances-A Role of Amine and Monocarboxylic Acid Carrier Systems for the Drug Transport- (내인성물질의 수송계를 이용한 혈액-뇌관문에의 약물송달V-약물의 혈액-뇌관문 투과성에 대한 염기성 아민 및 모노카르본산 수송계의 역할-)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.20 no.4
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    • pp.223-228
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    • 1990
  • The contribution of endogenous transport systems to the blood-brain barrier (BBB) transport of basic and acidic drugs was studied by using a carotid injection technique in rats and an isolated bovine cerebrovascular disease state were compared between the normotensive rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP) which have been well established as an animal model with pathogenic similarities to humans. Basic drugs such as eperisone, thiamine and scopolamine inhibited, in a concentration dependent manner the in vivo uptake of $[{^3}H]choline$ through BBB, whereas amino acids and acidic drugs such as salicylic acid and valproic acid did not inhibit the uptake. The uptake of $[^3H]choline$ by B-CAP increased with time and showed a remarkable temperature dependency. The uptake of $[^3H]choline$ by B-CAP showed the very similar inhibitory effects as observed in the in vivo brain uptake, and was competitively inhibited by a basic drug, eperisone. The in vivo BBB uptakes of $[^3H]acetic$ acid and $[^{14}C]salicylic$ acid were dependent on pH of the injectate and the concentration of drugs. Several acidic drugs such such as salicylic acid, benzoic acid and valproic acid inhibited the in vivo uptake of $[^3H]acetic$ acid, whereas amino acid, choline and a basic drug such as eperisone did not inhibit the uptake. The uptake of acetic acid by B-CAP was competitively inhibited by salicylic acid. The permeability surface area product (PS) through BBB for $[^3H]choline$ in SHRSP was significantly lower than that in WKY. The concentration of choline in the brain dialysate in SHRSP was about half of that in WKY, while no significant difference was observed in the plasma concentration of choline between SHRSP and WKY. No significant difference was observed in the transport of monocarboxylic acids, glucose and neutral amino acid through BBB between SHRSP and WKY. From these results, it was concluded that BBB transport system of choline contributes to the transport of basic drugs through BBB, that acidic drugs can be transported via a moncarboxylic acid BBB transport system and that the specific dysfuntion of the BBB choline transport in SHRSP was ascribed to the reduction of the maximum velocity of choline concentration in the brain interstitial fluids.

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Role of Endogenous Transport Systems for the Transport of Basic and Acidic Drugs at Blood-Brain Barrier (염기성 및 산성 약물의 혈액-뇌관문 투과에 관여하는 내인적 수송계)

  • Kang, Young-Sook
    • Journal of Pharmaceutical Investigation
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    • v.23 no.1
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    • pp.1-9
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    • 1993
  • The endothelial cell of brain capillary called the blood-brain barrier (BBB) has carrier-mediated transport systems for nutrients and drugs. The mechanism of the BBB transport of basic and acidic drugs has been reviewed and examined for endogenous transport systems in BBB in WKY and SHRSP. Acidic drugs such as salicylic acid and basic drugs such as eperisone are taken up in a carrier mediated manner through the BBB via the monocarboxylic acid and amine transport systems. The specific dysfunction for the choline transport at the BBB in SHRSP would affect the function of the brain endothelial cell and brain parenchymal cell. The utilization of the endogenous transport systems of monocarboxylic acid and amine could be promising strategy for the effective drug delivery to the brain.

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