• Biomolecules & Therapeutics
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• v.5 no.3
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• pp.246-252
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• 1997

This study was performed to evaluate antiulcer effects of traditional folk medicines such as heat-treated acumen, halloysitum rubrum and os sepiae against stomach ulcer induced by acetic acid in Sprague-Dawley rats. Various pharmacological parameters were utilized to compare the antiulcer effects of aforementioned drugs based on the size of ulcer lesion, pepsin activity, free and total acidity, gastric secretory volume, and 5-HT (hydxoytrytamine) content. All folk medicines and ranitidine as control drus were shown to decrease ulcer lesion size after 5-day treatments, with the order of halloysitum rubrum, os sepiae, heat-treated acumen and ranitidine. All treated drugs except os sepiae inhibited the gastric volume as compared with that in the control group. Ranitidine most significantly inhibited the gastric volume. All the experimented drugs in this study lowered the gastric acidity. Halloysitum rubrum decreased it most remarkably, followed by ranitidine, os sepiae and heat-treated alumen after 5-day treatments. All used drugs alleviated the pepsin activity as compared with the control group, os sepiae being the highest then halloysitum rubrum, heat-treated alumen and ranitidine in turn. Heat-treated alumen and halloysitum rubrum showed mucin production to the great extent, and ranitidine had slight increasing effect thereon. At the end of observation period, all drugs except ranitidine increased 5-HT contents as compared to the normal group. From the above results, we could confirm the folk medicines such as heat-treated alumen, halloysitum rubrum and os sepiae have not only remarkable antiulcer effects but also preventing effects for the stomach ulcer recurrence, which suggest the experimented folk medicines could be developed as new antiulcer agents.

• 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.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.262-265
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• 1993

Acute toxicities of DWH-01 (Ranitidine : Bismuth : Sucralfate= 1.5: 2 : 6) were investigated in Sprague-Dawley rats. Seven days after oral administration of DWH-01 with different doses (10 g/kg, 5 g/kg, 2.5 g/kg, 1.25 g/kg, 0.625 g/kg), we examined numbers of deaths, general signs, weight measurement and histopathological examination for both sexes of rats. Summaried results are: 1) No deaths were occurred, 2) There were no pathological and clinical differences compared with control group, 3) No significant changes of body weights were observed, and 4) In histopathological examinations of organs and tissues, there was some hemorrhage in a lung tissue of low dose group for male and female respectively, but it was thought to be caused by environmental factor. The results suggest that toxicity of DWH-01 is low and its $LD_{50}$ is over 10 g/kg in Sprague-Dawley rats.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.273-273
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• 1996

Recently a novel in vivo approach in dogs, using a regional segmental intestinal perfusion technique, has been developed. The perfusion tube consists of a highly sophisticated multichannel tube with two inflatable occluding balloons, which are placed in 10cm apart. The tube was introduced orally from the stomach through the upper jejunum under the guidance of solid-state pH meter. In the present study, four healthy dogs were infused in the proximal jejunum on two periods. The two perfusion experiments used the same flow rate, 2 $m\ell$/min, and the same perfusion solution to determine the intrasubject variability. The mean (${\pm}$ S. E.) fractions of ranitidine absorbed calculated from the perfusion data were 21.32${\pm}$2.01% (n=3) (1st period), 27.88 ${\pm}$ 17.54% (n=4) (2nd period), respectively. The effective permeabilities (Peffs${\times}$10$\^$4/) of ranitidine were 1.51${\pm}$0.47cm/sec (n=3) (1st period), 1.50 ${\pm}$ 0.31 cm/sec (n=4) (2nd period), respectively. The pH and osmolarity of perfusion solution were 7.50 ${\pm}$ 0.03 and 300 ${\pm}$ 0.06 mOsm/L, There was no significant intrasubject variation. Mixing equilibrium (steady-state) was reached at about 50 min. l-Phenylalanine was absorbed almost completely. Intrinsic intestinal wall permeability of ranitidine showed low permeable characteristics, suggesting permeability-limited absorption. The absorption of 1-phenylalanine, an actively transported nutrient, was not inhibited by ranitidine. The low intestinal membrane permeability is one of the important factors responsible for the variable oral absorption of ranitidine. Supported by FDA Grant FD01462-04 and KOSEF Grant.

• YAKHAK HOEJI
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• v.37 no.4
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• pp.408-419
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• 1993

Subacute toxicities of DWH-Ol(Ranitidine : Bismuth : Sucralfate=1.5:2:6) were inverstigated in Sprague-Dawley rats. After oral administration of DWH-01 with different dosages of 5 g/kg, l g/kg, and 0.2 g/kg, we examined the number of deaths, general signs, food intake, water intake, body weight and histopatholgical changes for both sexes of rats. During the adminstration period, urinalysis and opthalmological examination were also performed in the treated animals. 1) Animals were all survived for 4 weeks. 2) There were no significant differences in pathological and opthalmological findings between the control and treated animals. 3) There were no significant changes in body weight, food intake and water intake compared with control group. 4) In hematological examination and blood chemical analysis, there was no significant change compared with control group. 5) In histopathological examinations of organs and tissues, there was some hemorrhage in a lung tissue of low dose group, but it was thought to be caused by environmental factor. These data suggest that DWH-01 is not subacutely toxic in Sprague-Dawley rats.

• Journal of the Korean Society of Laryngology, Phoniatrics and Logopedics
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• v.9 no.2
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• pp.115-127
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• 1998

Laryngopharyngeal reflux(LPR) is one firm of the gastroesophageal reflux diseases(GERD). It is known to cause various kinds of otolaryngologic symptoms such as hoarseness, foreign body sensation in throat, chronic throat clearing, chronic cough, etc. Disease entities diagnosed by otolaryngologists as posterior laryngitis, globus pharyngeus should be suspected as LPR-related diseases. In this multi-center trial, we tried to evaluate the effect of cisapride(10mg tid) on LPR-related symptoms as the part I study(CIS-KOR-051) in 19 centers, and as the part II study(CIS-KOR-052) comparative evaluation of effect between cisapride(10mg tid) and ranitidine(150mg bid) on LPR-related symptoms in 4 centers. In part I study, efficacy of cisapride on LPR-related symptoms after 4 weeks was 53.5% and that of after 8weeks was 77.9% in per protocol(PPA) analysis group. In part II study, efficacy of the cisapride was much better than that of ranitidine not only from 8 weeks trial(p<0.001) but also from 4 weeks trial(p<0.021) in PPA group. In the multiple logistic regression analysis among the parameters which affect the efficacy of the treatment, cisapride prescribed group showed 10 times greater than that of ranitidine prescribed group(p<0.0001, Odds ratio : 10) in PPA group. LPR was proved by 24Hr double probe pHmetry in 13 patients out of 19 patients tested(68.4%). Thus these results indicated that inducing the improvement of motility functions could affect the amelioration of the LPR-related symptoms much better than reducing acid secretion from the stomach. And maybe it suggests that LPR-related symptoms mainly developed by the reduced motility functions of the esophagus and/or delayed gastric emptying.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.720-726
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• 2004

Two Spectrophotometric procedures are presented for the determination of two commonly used H2-receptor antagonists, nizatidine (I) and ranitidine hydrochloride (II). The methods are based mainly on charge transfer complexation reaction of these drugs with either ${\rho}-chloranilic$ acid (${\rho}-CA$) or 2, 3 dichloro-5, 6-dicyanoquinone (DDQ). The produced colored products are quantified spectrophotometrically at 515 and 467 nm in chloranilic acid and 000 methods, respectively. The molar ratios for the reaction products and the optimum assay conditions were studied. The methods determine the cited drugs in concentration ranges of 20-200 and $20-160\;\mu\textrm{g}/mL$ for nizatidine and ranges of 20-240 and $20-140\;\mu\textrm{g}/mL$ for ranitidine with chloranilic acid and DDQ methods, respectively. A more detailed investigation of the complexes formed was made with respect to their composition, association constant, molar absorptivity and free energy change. The proposed procedures were successfully utilized in the determination of the drugs in pharmaceutical preparations. The standard addition method was applied by adding nizatidine and ranitidine to the previously analyzed tablets or capsules. The recovery of each drug was calculated by comparing the concentration obtained from the spiked mixtures with those of the pure drug. The results of analysis of commercial tablets and the recovery study (standard addition method) of the cited drugs suggested that there is no interference from any excipients, which are present in tablets or capsules. Statistical comparison of the results was performed with regard to accuracy and precision using student's t-test and F-ratio at 95％ confidence level. There is no significant difference between the reported and proposed methods with regard to accuracy and precision.

• Journal of Veterinary Science
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• v.23 no.2
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• pp.19.1-19.9
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• 2022

Background: Gastric ulcer is one of the prevalent diseases in racehorses. However, it has not been recognized as important in Korea, and drugs used to treat gastric ulcers are included in the doping test list, so they are not allowed to be administered to racehorses in training. Objectives: This study was performed 1) to investigate the prevalence and the severity of gastric ulcers in Thoroughbred racehorses in Korea, 2) to confirm the therapeutic effect of ranitidine and omeprazole, and 3) to compare the efficacy between ranitidine and omeprazole. Methods: Forty-nine horses were randomly recruited, and gastroscopy was performed within two days after racing. Twelve horses with a sum grade of five or higher were randomly assigned to two treatment groups. Seven horses were administered ranitidine, and five horses were administered omeprazole. Follow-up gastroscopy was scheduled within one to five days after finishing the treatment. Results: The prevalence of gastric ulcer in Korean Thoroughbred racehorses after racing was 100%, and the grade was more severe in the non-glandular region than in the pyloric region. There was no correlation between the severity of gastric ulcer in the two regions. Omeprazole had a greater therapeutic effect than ranitidine. Conclusions: This study shows the importance of recognizing gastric ulcers as an important factor, and omeprazole as a possible treatment option in Korea, as it has been removed from the list of prohibited substances for racehorses. Thus, the use of omeprazole is currently recommended until one day before the race.

• Archives of Pharmacal Research
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• v.15 no.3
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• pp.246-250
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• 1992

Acetaminophen (AAP) and ranitidine (RT) were coadministered orally to nine rats, and the possible contribution of the gastric emptying to the plasma concentration profiles of them was examined. The drugs showed multiple plasma peaks similar to the respective ones after separated administration of each durg. IT Implies that there is no significant interaction between AAP and RT in terms of the gastric emptying or drug absorption. There were no significant linear correlations of the peak patterns (peak height and peak time) between AAP andd RT. It is contrary to the expectation from the biphasic gastric emptying (BGE) theory previously suggested for AAP and RT. The BGE theory. Therefore, seemed to have some draw-backs in explaining satisfactorily the multiple plasma peaks of AAP and RT. Two more doubts raised previously against the BGE theory were also discussed.

• 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.