• Journal of Pharmaceutical Investigation
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• v.31 no.1
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• pp.19-25
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• 2001

The purpose of this study was to use a ternary polymeric matrix system for high drug loading of a highly soluble drug for controlled release delivery. The controlled drug delivery of diltiazem HCl (solubility > 50% in water at $25^{\circ}C$) with high loading dose (the final loading dose of drug was 34%) from a ternary polymeric matrix (gelatin, pectin, HPMC) was successfully accomplished. This simple monolithic system with 240 mg drug loading provided near zero-order release over a 24 hour-period by which time the system was completely dissolved. The release kinetics of diltiazem HCl tablet with high loading dose from the designed ternary polymeric system was dependent on the ratios of HPMC : pectin binary mixture. The release rate increased as pectin : HPMC ratio were increased. Swelling behavior of the ternary system and the ionic interaction of formulation components with cationic diltiazem molecule appear to control drug diffusion and the release kinetics. Comparable release profiles between commercial product and the designed system were obtained. The binding study between gelatin with diltiazem HCl showed the presence of two binding sites for drug interaction with subsequent controlled diffusion upon swelling. This designed delivery system is easy to manufacture and drug release behavior is highly reproducible and offers advantages over the existing commercial product.

• Natural Product Sciences
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• v.9 no.3
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• pp.186-191
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• 2003

The hepatoprotective effect of methanol extract of leaves of Caesalpinia bonducella was studied by means of paracetamol induced liver damage in rats. The degree of protection was measured by using biochemical parameters such as serum transaminase (SGPT and SGOT), alkaline phosphatase (ALP), bilirubin, and total protein. Further, the effects of the extract on lipid peroxidation (LPO), glutathione (GSH), superoxide dismutase (SOD), and catalase (CAT) were estimated. The methanol extract of C. bonducella (MECB) (50,100 and 200 mg/kg) produced significant (P<0.01) hepatoprotective effect by decreasing the activity of serum enzymes, bilirubin, and lipid peroxidation, while it significantly increased increased the levels of GSH, SOD, CAT, and protein in a dose dependent manner. The effects of MECB were comparable to that of standard drug Silymarin. However, at a lower dose (25 mg/kg) it could not restore the deleterious effect produced by paracetamol. The results indicate that Caesalpinia bonducella had antioxidant and hepatoprotective effects.

• The Korea Journal of Herbology
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• v.33 no.1
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• pp.71-76
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• 2018

Objectives : This study was performed to investigate the single oral toxicity of HBX-6 in Sprague-Dawley (SD) rats. Methods : Twenty SD rats were randomly assigned to four groups of 5 rats each and were administrated singly to female and male SD rats, as an oral dose of 2000 mg/kg. HBX-6 is a newly combined Korean herbal medicine formula 30 % Ethanol extract derived from The Dongui Bogam. Now we are developing the prescription for the aim of improving benign prostatic hyperplasia (BPH) without undesirable side effects. HBX-6 is composed of nine medicinal herbs: Aconiti Lateralis Radix Preparata, Corni Fructus, Cistanchis Herba, Psoraleae Semen, Dendrobii Herba, Morindae Radix, Cuscutae Semen, Trigonellae Semen, Foeniculi Fructus. Animals were monitored for the mortality and changes in the body weight, clinical signs, gross observation and necropsy findings for the 14 days according to "Standard for Toxicity Study of Pharmaceuticals" of Korea Food and Drug Administration (KFDA) guideline and "Acute Oral Toxicity - Fixed Dose Procedure" of OECD Test Guideline. Results : We could not find any mortality. Compared with the control group, significant weight change was not observed in the experimental group. After administration, the more common symptoms were not observed. There were no gross abnormalities in all cases. Conclusions : Taken together, these results suggest that the approximate lethal dose of HBX-6 in both female and male SD rats were considered as over 2000 mg/kg.

• YAKHAK HOEJI
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• v.30 no.6
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• pp.301-305
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• 1986

Dose-dependent pharmacokinetics of acetaminophen was studied in the rat. Acetaminophen was injected intravenously at doses of 10, 30, 50, 100 and 200mg/kg to the adult male rats. The well-known dose-dependent pharmacokinetic behavior was found even at 30mg/kg dose. It implies that metabolism of acetaminophen in the liver, probably sulfation, is saturated at very low concentration of acetaminophen. Dosage regimen establishment based on this characteristics would be necessary even at usual does level (300-600mg/day/body).

• Journal of Pharmaceutical Investigation
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• v.7 no.1_4
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• pp.22-27
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• 1977

Absorption of sulfisoxazole after oral administration was significantly increased by small dose(60mg/kg) of alloxan but not increased significantly by large dose (160mg/kg) of alloxan from that of normal rabbits. Pretreatment with alloxan did not give any effect on clearance of sulfisoxazole. As the results, It could come to conclusion that in creased absorption of the sulfisoxazole administered small dose of the alloxan was influenced by transport of intestinal membrane or intestinal enzyme activation or increase of intestinal absorption function.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.309.2-310
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• 2003

The pharmacokinetics and pharmacodynamics of torasemide were evaluated after an intravenous administration of the same total dose of torasemide at a dose of 1 mg/kg to rabbits with different infusion times, 1 min (treatment I), 30 min (treatment II), and 2 h (treatment III). The loss of water and electrolytes in urine induced by torasemide was immediately replaced with infusion of equal volume of lactated Ringer…s solution. (omitted)

• Journal of Pharmaceutical Investigation
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• v.39 no.5
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• pp.373-379
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• 2009

This study was conducted to develop a pharmacokinetic-pharmacodynamic (PK/PD) model of a direct thrombin inhibitor, argatroban to predict the concentration-effect profiles in rats. Argatroban was i.v. injected to rats at 0. 2, 0.8 and 3.2 mg/kg doses (n = 4-5 per dose), and plasma drug levels were determined by a validated LC/MS/MS assay. The pharmacokinetics of argatroban was linear over the i.v. dose range studied. The thrombin time (TT) and the activated partial thromboplastin time (aPTT) were measured in rat plasma and they were found to linearly increase with increasing the dose. A 2-compartment pharmacokinetic model linked with an indirect response pharmacodynamic model was successfully utilized to evaluate the drug concentration-response relationship.

• Journal of Pharmaceutical Investigation
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• v.16 no.1
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• pp.31-35
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• 1986

Effect of ethanol on the absorption rate, blood level and bioavailability of sulfamethazine (SM) in rats was determined. Absorption rate of SM was determined both by the in vitro and in situ experiment. In vitro, absorption rate of SM in rat small intestine was increased by 0.3, 1.0 and 3.0% ethanol. In situ, absorption rate of SM was increased by 0.3 and 1.0% ethanol but not by 3.0% ethanol. After oral administration, blood level of SM was elevated and relative bioavailability was significantly increased to 114.8% at the dose of 0.6g/kg ethanol but not significantly at the dose of 3.0g/kg ethanol. The time for attainment of peak blood level was changed from 2.5 to 1.5hr. Ethanol enhanced absorption rate constant of SM significantly and reduced elimination rate constant of SM administered orally at the dose of 0.6g/kg ethanol.

• Natural Product Sciences
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• v.5 no.2
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• pp.70-74
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• 1999

In the course of a search for tumor necrosis factor $(TNF)-{\alpha}$ inhibitory compounds from medicinal plants, we identified neolignans, honokiol and magnolol, from the alcoholic extract of Magnolia offcinalis as active inhibitory principles. These compounds dose-dependently inhibited $TNF-{\alpha}$ production without displaying cytotoxicity and their inhibitory activities measured by $IC_{50}$ values were 53.7 and $61.4\;{\mu}M$, respectively.

• Natural Product Sciences
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• v.12 no.1
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• pp.44-49
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• 2006

The aqueous extract of Hydrilla verticillata (AEHV) was tested for possible pharmacological effects on experimental animals. AEHV significantly potentiated the sleeping time of mice induced by standard hypnotics viz. pentobarbitone sodium, diazepam, and meprobamate in a dose dependent manner. AEHV showed significant analgesic properties as evidenced by the significant reduction in the number of writhes and stretches induced in mice by 1.2% acetic acid solution. It also potentiated analgesia induced by morphine and pethidine in mice. Pretreatment with AEHV caused significant protection against strychnine and leptazol-induced convulsions. The behavioral studies on mice indicate CNS depressant activity of the aqueous extract of H. verticillata.