• Analytical Science and Technology
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• v.22 no.5
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• pp.432-438
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• 2009

In order to develop the analytical method for the pharmaceutical tablets containing ranitidine HCl by square wave voltammetry (SWV), $5.00{\times}10^{-5}M$ ranitidine HCl solutions prepared with phosphate buffers of various pH values were investigated by SWV. The well defined main peak due to the electrochemical reduction of $-NO_2$ in the structure of ranitidine moved towards the cathodic direction by -70 mV/pH as the pH values were increased indicating the involvement of hydrogen in its reduction. The calibration curve, the plot of peak currents (Ip) vs. concentrations of ranitidine HCl in the range between $1.00{\times}10^{-7}M$ and $1.00{\times}10^{-5}M$ showed linearity with slopes of $232,530{\mu}A/M$ (pH 6.14), $289,015{\mu}A/M$ (pH 7.07) and $232,843{\mu}A/M$ (pH 8.01). When one pharmaceutical tablet was simply dissolved in the phosphate buffer with a pH value of 6.14 and determined by standard addition method using SWV, the within-day precision study (n=4) resulted in the contents of ranitidine HCl as $171{\pm}2.1mg$ ($102{\pm}1.3%$ of the specified contents, RSD of 1.2%) in a tablet of Curan$^{(R)}$. The inter-day precision for 5 days was 1.1% of RSD. For Zantac$^{(R)}$ the within-day precision study (n=4) showed the contents of ranitidine HCl as $167{\pm}0.8mg$ ($99{\pm}0.5%$ of the specified contents, RSD of 0.5%) in a tablet and the inter-day precision for 5 days was 0.3% of RSD.

• Journal of Physiology & Pathology in Korean Medicine
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• v.28 no.5
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• pp.537-547
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• 2014

The object of this study was to observe the effect of Banhasasim-tang (BHSST) on the HCl/EtOH-induced gastric ulcer in mice. Three different dosages of BHSST extract (400, 200 and 100 mg/kg) were once orally administered 1 hr before HCl/EtOH mixture treatment. One hour after HCl/EtOH mixture single oral treatment, the changes on the gross hemorrhagic lesion scores, fundic histopathology, gastric nitrate/nitrite contents, lipid peroxidation and antioxidant defense system (catalase and superoxide dismutase (SOD) activities) were observed, and compared with that of ranitidine 100 mg/kg. As results of all three different dosages of BHSST extract treatment in the HCl/EtOH-induced gastric ulcer mice, significant and dose-dependent decreased gastric damages. BHSST extracts also increased gastric nitrate/nitrite contents and strengthened the antioxidant defense systems, and increased the activities of catalase and SOD, respectively. BHSST extracts 200 mg/kg showed similar anti-ulcerative effect as compared with ranitidine 100 mg/kg, in this experiment. BHSST has favorable protective effects against to the HCl/EtOH-induced gastric damages, through the strengthening of the body antioxidant defense systems. These gastroprotective effects of BHSST against HCl/EtOH-induced gastric ulcer considered as results of complicated synergic effects of their 8 kinds of herbal components, but exact synergic or individual herbal effects are difficult to discuss in this study. Therefore, more detail synergic effects between 8 kinds of individual herbal component of BHSST should be tested with screening of active anti-inflammatory chemical ingredients, in future.

• Journal of Physiology & Pathology in Korean Medicine
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• v.26 no.1
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• pp.67-73
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• 2012

The exposure of gastric mucosa to ethanol produces acute ulcers mediated by inflammatory processes, hemorrhagic erosions and increase of reactive oxygen species. The purpose of this study was to assess the effects of Coptidis Rhizoma(CR) aqueous extracts on hydrochloride (HCl)/ethanol induced gastric ulcer in mice as compared with rebamipide (30 mg/kg) and ranitidine (100 mg/kg). Stomach ulcers were induced by oral ingestion of HCl/ethanol. CR extracts (125, 250 and 500 mg/kg) were orally administered, once a day for 7 continuous days, and 1 hr after last 7th treatment of CR extracts stomach ulcers were induced. Effects of CR extracts on HCl/ethanol-induced gastric ulcer were evaluated based on gross and microscopic observations with anti-oxidant activities. All three different dosages of CR extract significantly decreased HCl/ethanol-induced gastric ulcer compared with the HCl/ethanol control mice. CR extracts also strengthened the antioxidative defense systems - decreased the level of lipid peroxidation but increased the level of catalase, superoxide dismutase and nitrate/nitrite compared with the HCl/ethanol control. The effects of CR extract 500 mg/kg were similar to that of 30 mg/kg rebamipide, and CR extract 250 mg/kg showed similar anti-ulcer effects as compared with ranitidine 100 mg/kg. These results suggest that the gastroprotective effects of CR extracts on mice ulcer models can be attributed to its ameliorating effect on oxidative damages.

• Journal of Pharmaceutical Investigation
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• v.36 no.3
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• pp.193-199
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• 2006

A bioequivalence study of $Sudo^{TM}$ Ranitidine HCI tablet (Sudo Pharma. Ind. Co., Ltd.) to $Curan^{TM}$ tablet (Il Dong Pharma. Ind. Co., Ltd.) was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korean volunteers received each medicine at the ranitidine hydrochloride dose of 150 mg in a 2x2 crossover study. There was a one week wash-out period between the doses. Plasma concentrations of ranitidine were monitored by a high-turbulent liquid chromatography (HTLC) for over a period of 12 hours after drug administration. $AUC_t$ (the area under the plasma concentration-time curve from time zero to 12 hr) was calculated by the linear trapezoidal rule method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t$ and $C_{max}$. No significant sequence effect was found far all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the $C_{max}$ ratio for $Sudo^{TM}$ Ranitidine $HCl/Curan^{TM}$ were 0.92-1.00 and 0.90-1.03, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the bioequivalence of $Sudo^{TM}$ Ranitidine HCI and $Curan^{TM}$ with respect to the rate and extent of absorption.

• Journal of Pharmaceutical Investigation
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• v.38 no.2
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• pp.99-104
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• 2008

PLGA micro/nano particles encapsulating ranitidine as a hydrophilic model drug were prepared by the double-emulsion solvent evaporation method. Surface morphology investigation by scanning electron microscope (SEM) showed that the emulsification by sonication could produce nanoparticles, whereas microparticles were prepared using high speed homogenizer. Moreover, while nanohalf-shell structure instead of spherical nanoparticle could be produced by adding poloxamer into oil phase (MC) with PLGA 504H, the addition of poloxamer didn't change particle shape in case of PLGA 502H. On the other hand, microparticle with poloxamer had more surface pores than those without poloxamer. The size and polydispersity (PDI) of particles were determined by particle size analyzer. Effective diameters of particles were in the range of $400{\sim}800\;nm$ and $1200{\sim}3300\;nm$ in case of nanoparticles and microparticles, respectively. Encapsulation efficiencies were in the range of $1.2{\sim}2.9%$. The addition of poloxamer produced the particles with higher encapsulation efficiency. In vitro release study in phosphate buffer (pH 7.4) at $37^{\circ}C$ showed common large initial burst release. However, the relative slower release profile could be observed in case of microparticles. Poloxamer addition increased the release rate, which was thought to be related to the increased surface area of particles.

• CELLMED
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• v.6 no.2
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• pp.11.1-11.7
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• 2016

The aimed of the presence study was to determine the antiulcer potential of virgin coconut oil (VCO), either extracted by wet process (VCO_A) or fermentation process (VCO_B), and to compare their effectiveness against the copra oil (CO) using the HCl/ethanol-induced gastric ulcer model. Earlier, the oils underwent chemical analysis to determine the free fatty acids composition, physicochemical properties and anti-oxidant capability. In the antiulcer study, rats (n=6) were pre-treated orally for 7 consecutive days with distilled water (vehicle), 100 mg/kg ranitidine (positive group) or the respective oils (10, 50, and 100% concentration). One hour after the last test solutions administration on Day 7^th, the animals were subjected to the gastric ulcer assay. Macroscopic and microscopic analyses were performed on the collected rat's stomachs. From the results obtained, the chemical analysis revealed i) the presence of high content of lauric acid followed by myristic acid and palmitic acid in all oils and; ii) the significant (^*p< 0.05) different in anisidine- and peroxide-value, percentage of free fatty acid, total phenolic content and total antioxidant activity among the oils. The animal study demonstrated that all oil possess significant (^*p< 0.05) antiulcer activity with VCO_B being the most effective oil followed by VCO_A and CO. The macroscopic observations were supported by the microscopic findings. Interestingly, all oils were more effective than 100 mg/kg ranitidine (reference drug). In conclusion, coconut oils exert remarkable antiulcer activity depending on their methods of extraction, possibly via the modulation of its antioxidant and anti-inflammatory activity.

• The Journal of Internal Korean Medicine
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• v.34 no.2
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• pp.204-214
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• 2013

Objectives : This study was designed to investigate the cellular and molecular mechanisms of anti-inflammatory activity of the water extract of Polygala tenuifolia Willd. (Pt-WE). Methods : Using lipopolysaccharide (LPS)-stimulated murine RAW264.7 cells, we examined inflammatory mediators such as nitric oxide (NO), inducible NO synthase (iNOS), cyclooxygenase (COX)-2 and prostaglandin $E_2$ ($PGE_2$). Also, the inhibitory effect of Pt-WE on the activity of activator protein 1 (AP-1) and upstream signaling molecules was evaluated. To assess the protective effect of Pt-WE on hydrochloride/ethanol (HCl/EtOH)-induced gastric ulcer in mice, we compared Pt-WE (200 mg/kg) with ranitidine (50 mg/kg) treated mice's gastric mucosa, based on gross observations. Results : Pt-WE inhibited LPS-induced production of NO, $PGE_2$ in a dose-dependent manner, without causing cytotoxicity. Pt-WE suppressed AP-1 activation by reducing generations of both c-Jun and c-Fos. In addition, Pt-WE inhibited the p-MKK 4/7 (mitogen-activated protein kinase kinase 4/7) and p-JNK (c-Jun N-terminal kinase) 1 in LPS-stimulated RAW264.7 cells. HCl/EtOH-induced gastric ulcer lesions were inhibited by pre-treatment of Pt-WE based on gross observations. In addition, Pt-WE decreased the phosphorylation level of JNK. Conclusions : These results demonstrate that Pt-WE has anti-inflammatory and gastroprotective effects. Thus, Pt-WE may be used widely in treatment of not only neurodegenerative diseases but also inflammatory diseases.