• 대한기관식도과학회지
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• 제9권1호
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• pp.67-74
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• 2003

Larygopharyngeal reflux(LPR) is one form of the Gastroesophageal Reflux Diseases(GERD). It is known to cause various kinds of otolaryngologic symptoms such as hoarseness, globus sensation in throat, chronic throat clearing, and chronic cough, Disease entities diagnosed by otolaryngologists as posterior laryngitis, globus pharyngeus and reflux laryngitis should be suspected as LPR-related diseases. The nizatidine(AXID), as a Histamine H2-receptor antagonist, reduces gastric acid secretion and improves gastric motility function. Objectives : The effect of nizatidine using 150mg b.i.d was evaluated for symptom relief and improvement of laryngoscopic findings in patients with LPR. Materials and Methods : In 30 multicenter, observational trial performed nationalwidely in Korea. 308 patients with LPR symptom were observed to evaluate their symptoms and larygnoscopic findings after 4weeks, 8weeks, 12weeks of treatment with nizatidine. Results : The symptoms of LPR including globus sensation, chronic throat clearing and hoarseness, are reduced significantly after 4 weeks, 8weeks, and 12weeks of treatment(p<0.05). The laryngoscopic findings including diffuse erythema, edema and granulation are improved after nizatidine treatment(p<0.05). and the efficacy of nizatidine on LPR-related sympoms after 4 weeks is 88.6%, and those of after 8 weeks and 12weeks were 92.6%, and 99.1% in ITT(Intent To Treatment) group(p<0.05). And PPA(Per Protocol Analysis)group showed 93.7%, 97.3%, and 99.1% of efficacy after 4, 8, and 12 weeks of nizatidine treatment(p<0.05). Conclusion : These results indicate that in patient with LPR, nizatidine 150mg b.i.d treatment very effectively reduces LPR symptoms and improves laryngoscopic findings as well as reduces gastric acid secretion and improves gastric motility function.

• Journal of Pharmaceutical Investigation
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• 제34권6호
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• pp.483-489
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• 2004

Fexofenadine HCl is non-sedating histamine H1 receptor antagonist that can be used for the treatment of seasonal allergic rhinitis. The objective of this study was to investigate whether the carriers of deformable liposomes can enhance the transepithelial permeability of fexofenadine HCl across the in vitro ALI human nasal monolayer model. Characterization of this model was achieved by bioelectric measurements and morphological studies. The passage 2 and 3 of cell monolayers exhibited the TEER value of $2852\;{\pm}\;482\;ohm\;{\times}\;cm^2$ on 11 days of seeding and maintained high TEER value for 5 days. The deformable liposome of fexofenadine HCl was prepared with phosphatidylcholine (PC) and cholic acid using extruder method. The mean particle size was about 200 nm and the maximum entrapment efficiency of 33.0% was obtained in the formulation of 1% PC and $100\;{\mu}g/ml$ fexofenadine HCl. The toxicity of the deformable liposome to human nasal monolayers was evaluated by MTT assay and TEER value change. MTT assay showed that it has no toxic effect on the nasal epithelial cells in 2-hour incubation when the PC concentration was below 1%. However, deformable liposome could not enhance the transepithelial permeability $(P_{app})$ and cellular uptake of fexofenadine HCl. In conclusion, the in vitro model could be used in nasal drug transport studies and evaluation of transepithelial permeability of formulations.

• 대한통합의학회지
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• 제8권4호
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• pp.79-92
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• 2020

Purpose : The purpose of this study was to evaluate the prescription pattern of NSAIDs and GPAs in the arthritis patients over 65 years old to prevent the GI adverse events. Nonsteroidal anti-inflammatory drugs (NSAIDs) are the most commonly used agents to treat arthritis, can cause gastrointestinal (GI) adverse effects. Recent guidelines recommend that moderate risk patients who have one or two risk factors, should be prescribed either combination of non-selective NSAID (nsNSAIDs) and gastroprotective agent (GPAs) or selective NSAID alone. Methods : Study population was National Patient Sample of 2011. Number of drugs used were 138 for NSAIDs and 21 for GPAs. Chi-square test was used to compare prescribing patterns. Results : The appropriate prescription rate follows the guideline was 11.2%: co-prescription with nsNSAID and proton pump inhibitor (PPI) or misoprostol was 1.6% and selective NSAID alone was 9.6%. Inappropriate prescription rates were as follows: co-prescription with nsNSAID and Histamine-2 receptor antagonist (H2RA) or antiacid was 53.8% and nsNSAID alone was 35.0%. The appropriate prescription rate among the types of medical institute was 54.4% in tertiary hospital, 31.2% in secondary hospital, and 6.0% in primary hospital. The appropriate prescription rate among the regions was 19.4%, highest in Seoul and 4.2%, lowest in Jeju. The appropriate prescription rate among the medical departments was as follow: 12.2% in orthopaedic surgery, 11.0% in internal medicine, and 7.7% in other departments. Conclusion : This finding suggests the needs to revise the national medical insurance imbursement policy, provide continuing medical education about the guideline of medical doctors.

• Journal of Pharmaceutical Investigation
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• 제36권6호
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• pp.405-411
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• 2006

Epinastine is an antiallergic drug effective for bronchial asthma, allergic rhinitis, urticaria and dermatitis. Epinastine is topically active, direct H1-receptor antagonist and an inhibitor of the release of histamine from the mast cell. The purpose of the present study was to evaluate the bioequivalence of two epinastine hydrochloride tablets, Alesion Tablet (Boehringer Ingelheim Korea Ltd.) and S-napine tablet 10 mg(Sam Chun Dang Pharm. Co., Ltd), according to the guidelines of the Korea Food and Drug Administration(KFDA). The release of epinastine from the two epinastine formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media(pH 1.2, 4.0, 6.8 buffer solution and water). Twenty six healthy male subjects, $23.35{\pm}1.57$ years in age and $66.29{\pm}10.61kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After two tablets containing 20 mg as epinastine hydrochloride was orally administered, blood was taken at predetermined time intervals and the concentrations of epinastine in serum were determined using HPLC with UV detector. The dissolution profiles of two formulations were similar at all dissolution media. In addition, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t.\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Alesion tablet, were 1.50, 1.46 and -13.48% for $AUC_t,\;C_{max}\;and\;T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25(e.g., log 0.95$\sim$log 1.12 and log 0.93$\sim$log 1.10 for $AUC_t\;and\;C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating S-napine tablet 10 mg was bioequivalent to Alesion tablet.

• Journal of Pharmaceutical Investigation
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• 제34권6호
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• pp.521-527
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• 2004

Cimetidine is a histamine $H_2-receptor$ antagonist, used for the treatment of endoscopically or radiographically comfirmed duodenal ulcer, pathologic GI hypersecretory conditions, and active, benign and gastric ulcer. Simple method for determining cimetidine in human plasma has been developed and validated. The analytical procedure for cimetidine showed a linear relationship in the concentration ranges from $0.05\;to\;5\;{\mu}g/ml$. Coefficient of variance (CV, %) for intraday and interday validation and relative error (RE, %) were less than ${\pm}15%$. Based on this analytical method, the bioequivalence of two cimetidine 400 mg tablets, reference (Tagamet 400 mg) and test drug (Sinil CIMETIDINE 400 mg) was evaluated according to the guidelines set by the Korea Food and Drug Administration (KFDA). Release of cimetidine from the tablets in vitro was tested using KP VIII Apparatus II with various dissolution media (pH 1.2, 4.0, 6.8 buffer solutions and water). Twenty-four healthy volunteers, $21.38{\pm}1.86$ years in age and $68.71{\pm}8.68\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was performed. After oral administration of a tablet containing 400 mg of cimetidine, blood samples were taken at predetermined time intervals and concentrations of cimetidine in plasma were determined using HPLC equipped with UV detector. The dissolution profiles of the two tablet formulations were very similar at all dissolution media. In addition, pharmacokinetic parameters such as $AUC_t$ and $C_{max}$ were calculated and ANOVA was employed for the statistical analysis of parameters. The results were revealed that the differences in $AUC_t$ and $C_{max}$ between the two tablets were 4.17 % and 0.97% respectively. At 90% confidence intervals, the differences in these parameters were also within ${\pm}20%$. All of the above mentioned parameters have met the criteria of KFDA guidelines for bioequivalence, indicating that the test drug tablet (Sinil CIMETIDINE tablet) is bioequivalent to Tagamet 400 mg tablet.

• 약학회지
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• 제52권3호
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• pp.188-194
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• 2008

Fexofenadine, ($\pm$)-4-1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}-butyl-a,a-dimethyl benzeneacetic acid, is a selective histamine $H_1$ receptor antagonist, and is clinically effective in the treatment of seasonal allergic rhinitis and chronic idiopathic urticaria as a first-line therapeutic agent. The purpose of the present study was to evaluate the bioequivalence of two fexofenadine hydrochloride tablets, $Allegra^{(R)}$ (Handok Pharmaceuticals Co., Ltd.) and Alecort (Samchundang Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of fexofenadine from the two fexofenadine hydrochloride formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media. Twenty six healthy male subjects, 25.62$\pm$3.35 years in age and 70.05$\pm$11.71 kg in body weight, were divided into two groups and a randomized 2$\times$2 cross-over study was employed. After a single tablet containing 120 mg as fexofenadine hydrochloride was orally administered, blood samples were taken at predetermined time intervals and the concentrations of fexofenadine in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The harmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, $Allegra^{(R)}$, were -1.37, 5.22 and 16.50% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.83$\sim$log 1.08 and log 0.81$\sim$log 1.03 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Alecort tablet was bioequivalent to $Allegra^{(R)}$ tablet.

• 한국임상약학회지
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• 제22권1호
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• pp.30-40
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• 2012

In Korea, elderly population aged 65 and older are about 5.0% and 10.7% in 1990 and 2009, respectively. Since elderly people may experience physiologic changes with aging and their pharmacodynamic and pharmcokinetic parameters also have been undergone changes, several adverse drug reactions can occur more frequently than young people. Especially, neuropsychiatric adverse drug reactions such as delirium and drowsiness endanger elderly patients more. The purpose of this study is to evaluate the outpatient prescriptions using drug causing delirium and drowsiness in elderly patients aged 65 and older. We retrospectively reviewed prescriptions for elderly patients collected from four community pharmacies from January 2nd to February 1st, 2010. One pharmacy was located closed to a general hospital, and others were located closed to a internal medicine or an ENT clinic. The each number of the collected prescriptions was followings; Group A (n=496) from internal medicine department of a general hospital; Group B (n=44) from ENT department of general hospital; Group C (n=144) from internal medicine clinic; Group D (n=110) from ENT clinic. In result, in Group A, the average number of prescribed drugs causing delirium or drowsiness per Rx was 2.38 In Group B, the average number of prescribed drugs causing delirium or drowsiness per Rx was 2.09 In Group C, the average number of prescribed drugs causing delirium or drowsiness per Rx was 2.51. In Group D, the average number of prescribed drugs causing delirium or drowsiness per Rx was 2.72. Especially, in Group D, the percentage of prescription that drugs causing delirium or drowsiness per Rx prescribed more than 3 is 52.73% In all the 4 groups, over the 60% of drugs causing delirium and/or drowsiness per prescription of elderly patients were prescribed. It means elderly patients take 2 drugs causing delirium and/or drowsiness among 3 drugs, which is very serious. Frequently prescribed drugs causing delirium and/or drowsiness were followings; GI agents, antitussives & expectorants, histamine H1 antagonist, analgesics, antibiotics. Among these drugs, GI agents was high raking in all the 4 groups, and pharmacists should caution elderly patients when counseling. In the internal medicine groups (Group A,C), drugs concerning chronic diseases were prescribed frequently. In conclusion, pharmacist's role is important. Pharmacists are well informed of the drugs causing delirium or drowsiness and it is important to explain about ADRs slowly and easily to the elderly patients that receive drugs causing delirium or drowsiness. And institutional device is needed. For example, when doctors prescribe drugs for the elderly patients, message is needed that supply some informations about drugs causing delirium or drowsiness.