• Journal of Pharmaceutical Investigation
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• 제34권6호
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• pp.471-475
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• 2004

Tamsulosin has been frequently used for the treatment of benign prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin matrix tablets and assess their formulation variables. We designed enteric coated sustained-release tamsulosin matrices to fulfill above statement. Aqueous microchannels in the enteric film need to be formed in order to obtain tamsulosin release even in an acidic environment such as gastric region. In the sustained-release tamsulosin matrix, low viscosity hydroxypropylmethylcellulose was used as a rate controller. Povidone K30 was also added to the matrices to facilitate water uptake so that a decrease in the release rate of tamsulosin as time elapses was prevented, possibly leading to pseudo zero-order release of the drug. The matrices were enteric-coated with hydroxypropylmethylcellulose phthalate (HPMCP), along with povidone K30 as an aqueous microchannel former. With the aqueous microchannels formed within the enteric film, tamsulosin could be released in an acidic condition. The release of tamsulosin decreased with increasing thickness of HPMCP membrane while the release rates of tamsulosin from those having different HPMCP thickness in pH 7.2 aqueous media were not considerably different, indicating that the enteric film was promptly dissolved at pH 7.2. These results clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the KFDA.

• International Neurourology Journal
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• 제22권4호
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• pp.252-259
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• 2018

Purpose: Naftopidil ((${\pm}$)-1-[4-(2-methoxyphenyl) piperazinyl]-3-(1-naphthyloxy) propan-2-ol) is prescribed in several Asian countries for lower urinary tract symptoms suggestive of benign prostatic hyperplasia. Previous animal experiments showed that intrathecal injection of naftopidil abolished rhythmic bladder contraction in vivo. Naftopidil facilitated spontaneous inhibitory postsynaptic currents in substantia gelatinosa (SG) neurons in spinal cord slices. These results suggest that naftopidil may suppress the micturition reflex at the spinal cord level. However, the effect of naftopidil on evoked excitatory postsynaptic currents (EPSCs) in SG neurons remains to be elucidated. Methods: Male Sprague-Dawley rats at 6 to 8 weeks old were used. Whole-cell patch-clamp recordings were made using SG neurons in spinal cord slices isolated from adult rats. Evoked EPSCs were analyzed in $A{\delta}$ or C fibers. Naftopidil or prazosin, an ${\alpha}1$-adrenoceptor blocker, was perfused at $100{\mu}M$ or $10{\mu}M$, respectively. Results: Bath-applied $100{\mu}M$ naftopidil significantly decreased the peak amplitudes of $A{\delta}$ and C fiber-evoked EPSCs to $72.0%{\pm}7.1%$ (n=15) and $70.0%{\pm}5.5%$ (n=20), respectively, in a reversible and reproducible manner. Bath application of $100{\mu}M$ prazosin did not inhibit $A{\delta}$ or C fiber-evoked EPSCs. Conclusions: The present study suggests that a high concentration of naftopidil reduces the amplitude of evoked EPSCs via a mechanism that apparently does not involve ${\alpha}1$-adrenoceptors. Inhibition of evoked EPSCs may also contribute to suppression of the micturition reflex, together with nociceptive stimulation.

• 대한본초학회지
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• 제33권1호
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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.

• Asian Pacific Journal of Cancer Prevention
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• 제17권4호
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• pp.2255-2258
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• 2016

Background: Awareness about prostate cancer has increased in the community, and prostate cancer screening examinations, including prostate specific antigen (PSA) assays, are now widely available. Prior to the PSA era, up to 27% of prostate cancers were detected incidentally at the time of transurethral resection of prostate (TURP). After PSA testing became widely available, the incidence of incidentally detected carcinoma prostate in TURP specimens without prior diagnosis reduced to 5-13%. However, the incidence of incidentally detected carcinoma prostate has been reported to vary across the globe since various factors can influence the identification of this malignancy in TURP specimens. In this paper, we focus on rates of incidentally detected prostate cancer in TURP specimens in our hospital and correlate it with various parameters. Materials and Methods: This retrospective study of histopathological findings of biopsy specimens was conducted for patients undergoing TURP during a period of 5 years from April 2010. The inclusion criteria were patients diagnosed with benign prostatic hyperplasia (BPH) (digital rectal examination (DRE) not showing any abnormally hard areas and normal age adjusted PSA values). Patients with elevated PSA, abnormal DRE, documented urinary tract infection and proved adenocarcinoma prostate (CaP) were excluded from the study. The total weight of prostatectomy specimen, occurrence of carcinoma prostate in the chips, percentage of total tissue resected showing malignancy and Gleason's scores were recorded. Results: A total of 597 patients belonging to the inclusion criteria were studied. The incidence of occult CaP in the study group was 5.2 % (31/597). Out of these, 8 belonged to T1a and 23 belonged to T1b stages. The age group 70 - 79 years had the maximum incidence of occult CaP. It was observed that the clinical grading of prostate did not have a bearing on the incidence of occult CaP whereas the weight of resected specimen correlated with the incidence of CaP. The incidence of occult CaP was greater with low volume prostates (<20 g). (P=0.15). Conclusions: The rate of incidentally detected adenocarcinoma prostate in patients undergoing TURP for clinically diagnosed BPH was found to be only 5.2 % in our study which is low when compared with similar studies done elsewhere. The age of the patient and weight of the resected specimen correlated with incidence of occult prostate cancer. The clinical grading of prostate by DRE however, demonstrated no correlation.

• Asian Pacific Journal of Cancer Prevention
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• 제17권7호
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• pp.3437-3445
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• 2016

Background: There is an increasing concern in the role of microRNA (miRNA) in the pathogenesis of bone metastasis (BM) secondary to prostate cancer (CaP). In this exploratory study, we hypothesized that the expression of vinculin (VCL) and chemokine X3C ligand 1 (CX3CL1) might be down-regulated in clinical samples, most likely due to the post-transcriptional modification by microRNAs. Targeted genes would be up-regulated upon transfection of the bone metastatic prostate cancer cell line, PC3, with specific microRNA inhibitors. Materials and Methods: MicroRNA software predicted that miR-21 targets VCL while miR-29a targets CX3CL1. Twenty benign prostatic hyperplasia (BPH) and 16 high grade CaP formalin-fixed paraffin embedded (FFPE) specimens were analysed. From the bone scan results, high grade CaP samples were further classified into CaP with no BM and CaP with BM. Transient transfection with respective microRNA inhibitors was done in both RWPE-1 (normal) and PC3 cell lines. QPCR was performed in all FFPE samples and transfected cell lines to measure VCL and CX3CL1 levels. Results: QPCR confirmed that VCL messenger RNA (mRNA) was significantly down-regulated while CX3CL1 was up-regulated in all FFPE specimens. Transient transfection with microRNA inhibitors in PC3 cells followed by qPCR of the targeted genes showed that VCL mRNA was significantly upregulated while CX3CL1 mRNA was significantly down-regulated compared to the RWPE-1 case. Conclusions: The down-regulation of VCL in FFPE specimens is most likely regulated by miR-21 based on the in vitro evidence but the exact mechanism of how miR-21 can regulate VCL is unclear. Up-regulated in CaP, CX3CL1 was found not regulated by miR-29a. More microRNA screening is required to understand the regulation of this chemokine in CaP with bone metastasis. Understanding miRNA-mRNA interactions may provide additional knowledge for individualized study of cancers.

• 대한중풍순환신경학회지
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• 제15권1호
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• pp.57-65
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• 2014

■ Objectives The purpose of this case report is to show an effect of korean medicine for patient with bilateral abducens nerve palsy. ■ Methods This patient was 58 year-old man who was diagnosed with bilateral abducens nerve palsy. The patient had Diabetes Mellitus, hypertension, benign prostatic hyperplasia and dyslipidemia as underlying diseases. The patient had symptoms of limited eye movement to lateral, diplopia, dizziness and mild headache. He was treated by korean medicine, containing electroacupuncture, pharmacoacupuncture, moxibustion and herb medicines during 13 days of hospitalization and following outpatient department. His eye movement was evaluated by the method of Scott and kraft and discomfort from his symptoms was scored by the Numerous Rating Scale. And other general conditions were measured. ■ Results After that period, patient's abduction deficit was improved and subjective discomfort from his symptoms was getting better. His other conditions were also better, compared with his admission. ■ Conclusion This study suggests that Korean medicine could have a therapeutic effect for bilateral abducens nerve palsy. So, It could help to relieve patient's symptoms and make general conditions better.

• 대한수의학회지
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• 제63권3호
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• pp.27.1-27.9
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• 2023

Lespedeza cuneata (LC) is a perennial plant used in herbal medicine to treat numerous diseases, including prostatic hyperplasia, diabetes, early atherosclerosis, and hematuria. Reference collections of bioactive compounds of LC are crucial for the determination of their pharmacological properties. However, little is known regarding its anti-oxidative and anti-inflammatory effects in alveolar macrophage (MH-S) cells. This study examined whether LC can inhibit reactive oxygen species and Coal fly ash (CFA) induced inflammation in MH-S cells. The anti-oxidative effects of LC were evaluated using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays, anti-inflammatory effects were examined using nitric oxide (NO) assay, and cytotoxicity was analyzed using methyl thiazolyl tetrazolium assay. The expression of inflammatory cytokine genes was assessed through a reverse-transcription polymerase chain reaction. Our results revealed that LC exhibited high radical scavenging activity and a dose-dependent (7.8-1,000 ㎍/mL) inhibition of oxidation as compared to ascorbic acid and Trolox. It also inhibited CFA-induced NO production in MH-S cells. Moreover, it suppressed the CFA exposure-mediated expression of pro-inflammatory mediators and cytokines, including inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), interleukin (IL)-1β, IL-6, and tumor necrosis factor-α. These results suggest that LC is a potent antioxidant and anti-inflammatory agent that can be useful as a nutraceutical product.

• 농촌의학ㆍ지역보건
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• 제25권2호
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• pp.265-273
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• 2000

농촌 지역 사회의 40대 이상의 남성 300명을 대상으로, 번역의 타당성과 신뢰도가 검증된 국문 I-PSS를 이용하여, 하부요로 증상의 유병률, I-PSS와 혈압의 관계를 조사하여 다음과 같은 결론을 얻었다. 1. I-PSS를 이용한 증상접수 8이상인 하부 요로증상의 유병률은 40, 50, 60 및 70대에서 각각 20.5, 32.2, 40.6 및 72.0%로 관찰되었으며 증상점수 20 이상의 중증군은 각각 0.82, 5.6, 11.0%로 미국, 일본에 비하여 높게 나타났다. 2. 평균 I-PSS와 연령과의 관계는 연령이 증가함에 따라 증가하였으며(r=0.29, p=0.0001), 무학인 군이 전문대 이상인 군에 비하여 I-PSS가 유의하게 높게 관찰되었다(p<0.05). 3. 평균 I-PSS와 배뇨만족도 사이에는 유의한 상관관계(r=0.63, p=0.0001)를 보였으나 I-PSS(평균 8.2)에 비해 상대적으로 불편감이 없는 배뇨만족도(평균 1.9)를 나타내었다. 4. 고혈압군의 평균 I-PSS는 7.85이었으며 정상혈압군의 평균 I-PSS는 8.39이었으나 I-PSS와 혈압과의 관계는 고혈압군과 정상 혈압군 간에 유의한 차이를 보이지 않았다(p>0.05).