우심방을 침범한 거대 비호지킨씨 림프종 1예

강상범,진승원,이은경,박용현,최용호,김용주,박준철,김재형,홍순조,최규보,권종범,원용순,박건,이은희 대한순환기학회 2000 Korean Circulation Journal Vol.30 No.4

흰쥐에서의 신규 항암제 BR-28702-2의 체내동태

용철순,이신웅,전철수,채희상,신원섭,백우현 영남대학교 약품개발연구소 1995 영남대학교 약품개발연구소 연구업적집 Vol.5 No.-

The purpose of this study was to determine pharmacokinetic parameters of BR-28702-2, a new antineoplastic agent which is the conjugate of nucleotide and phospholipid, and to compare them with those of ara-C. Male rats were cannulated in the left femoral vein and received a single i.v. bolus dose of either BR-28702-2 or ara-C. BR-28702-2 was also administered i.p. and plasma samples were analyzed by reversed-phase HPLC. The t_(L/2(β)) of ara-C(1.22 hr.) was significantly smaller than that of BR-28702-2(4.420 hr.). The absolute bioavailability of BR-28702-2 after i.p. injection was 1.125%. This lower bioavailability, together with previous reports that marked antineoplastic activity was observed when given i.p., indicates that BR-28702-2 would act as a depot system to release active moieties. Further works. therefore, need to be done to characterize active metabolites.

폴록사머를 이용한 디클로페낙 고형 좌제의 개발

용철순,오유경,김정애,김용일,박상만,양준호,이종달,최한곤 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.2

To develop a poloxamer-based solid suppository with poloxamer mixtures, the melting points of various formulations composed of P 124 and P 188 were investigated. To investigate the effect of poloxamer to the dissolution and dissolution mechanism of diclofenac sodium from the suppository the dissolution of diclofenac sodium delivered by the poloxamer-based suppository was performed. Furthermore, to investigate the mucoadhesive property of the poloxamer-based solid suppository, the identification test in the rectum was carried out after its rectal administration in rats. The poloxamer mixtures composed of P 124 and P 188 were homogeneous. Very small amounts of P 188 affected the melting points of poloxamer mixtures. In particular, the poloxamer mixture [P 124/P 188 (97/3%)] with the melting point of about 32℃ was a solid form at room temperature and instantly melted at physiological temperature. Furthermore, very small amounts of P 188 in the poloxamer-based suppository hardly affected the dissolution rates of diclofenac sodium from the suppository. Dissolution mechanism analysis showed the dissolution of diclofenac sodium was proportional to the time. At 4 h after administration, the blue color of poloxamer-based suppository [diclofenac sodium/poloxamer mixture (2.5/97.5%)] with the P 124/P 188 ratio of (97/3%) and blue lake in the rectum was faded. However, the position of suppository in the rectum did not significantly change with time. Thus, it retained in the rectum for at least 4 h. Our results indicated that the poloxamer-based solid suppository with P 124 and P 188 would be a candidate of rectal dosage from for diclofenac sodium.

수용성 고분자물질-단백질 접합체의 합성 및 응용

용철순,손영택 영남대학교 약품개발연구소 1994 영남대학교 약품개발연구소 연구업적집 Vol.4 No.-

Since the advent of recombinant DNA technology coupled with other biotechnology a variety of therapeutically effective proteins and peptides have been extensively invesitigated and many of them are now on clinical trial. They, however, suffer from some problems such as immunogenicity, antigenicity, instability and short half-life in circulation due to their proteinous natures. These draw-backs can be overcome successfully by conjugating proteins and peptides with hydrophilic polymers such as polyethylene glycol (PEG), albumin or dextran. The resulting soluble conjugates showed reduced antigenicity and immunogenicity, increased circulatory half-life, enhanced stability against proteolytic degradation. Comparing with the unmodified proteins and peptides, the therapeutic potential of conjugates is greatly enhanced. Clinical applications of these conjugates have shown promising results for the future use.

헬리코박터 파이로리 균 진단용 ^13C-요소 캅셀의 개발

용철순,김용일,김지만,강성훈,권기철,이종달,김종국,사홍기,최한곤 영남대학교 약품개발연구소 2002 영남대학교 약품개발연구소 연구업적집 Vol.11 No.-

The purpose of this study was to develop a new ^13C-urea-containing capsule for diagnosis of H.pylori. The urea-containing capsules were prepared with various diluents such as polyethylene glycol (PEG), microcrystaline cellulose, sodium lauryl sulfate and citric acid. The dissolution test, ^13C-urea breath test and stability test were then performed on the capsules. Microcrystalline cellulose and sodium lauryl sulfate retarded the initial dissolution rates of urea. However, PEG increased the initial dissolution rates of urea. Furthermore, two formulae composed of PEG,[^13C-urea/PEG (38/1.9 mg/cap)] and [^13C-urea/PEG (38/1.9/1.9 mg/cap)] had the maximum DOB value. about 16 at 20 min, while the formula composed of only 38 mg ^13C-urea had the maximum DOB value at 30 min. The results indicated that PEG improved the sensitivity of ^13C-urea in the human volunteers. The capsule [^13C-urea/PEG (38/1.9 mg/cap)] was stable for at least six months in 25 and 37℃. Thus, a PEG-containing capsule, [^13C-urea/PEG (38/1.9 mg/cap)] would be a more economical, sensitive and stable perparation for diagnosis of H. pylori.

헬리코박터 파이로리 균 진단용 ^13C-요소 캅셀의 개발

용철순,김용일,김지만,강성훈,권기철,이종달,김종국,사홍기,최한곤 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.1

The purpose of this study was to develop a new ^13C-urea- containing capsule for diagnosis of H. pylori. The urea-containing capsules were prepared with various diluents such as polyethylene glycol (PEG), microcrystalline cellulose, sodium lauryl sulfate and citric acid. The dissolution test, ^13C-urea breath test and stability test were then performed on the capsules. Microcrystalline cellulose and sodium lauryl sulfate retarded the initial dissolution rates of urea. However, PEG increased the initial dissolution rates of urea. Furthermore, two formulae composed of PEG, [^13C-urea/PEG (38/1.9 mg/cap)] and [^13C-urea/PEG/citric acid (38/1.9/1.9 mg/cap)] had the maximum DOB value, about 16 at 20 mim, while the formula composed of only 38 mg ^13C-urea had the maximum DOB value at 30 min. The results indicated that PEG improved the sensitivity of ^13C-urea in the human volunteers. The capsule [^13C-urea/PEG (38/1.9 mg/cap)] was stable for at least six months in 25 and 37℃. Thus, a PEG-containing capsule, [^13C-urea/PEG (38/1.9 mg/cap)] would be a more economical, sensitive and stable preparation for diagnosis of H. pylori.

프레탈정 (실로스타졸 100mg)에 대한 실로스탄정 (한국유나이티드 제약)의 생물학적 동등성

용철순,이경희,최진석,박병주,정세현,김용일,박상만,유봉규,이종달,최한곤 한국병원약사회 2003 병원약사회지 Vol.20 No.2

Bioequivalence of one cilostazol tablets, the Pletaal^(R)(Korea Otsuka Pharmaceutical Co., Ltd.) and Cilostan^(R)(Korea united Pharmaceutical Co., Ltd.), was evaluated according to the guideline of KFDA. Sixteen normal male volunteers(age 20~30 years old)were divided into two groups and a randomized 2×2 cross-over study was employed. After one tablet containing 100㎎ of cilostazol were orally administered, blood was taken at predetermined time intervals and the concentration of cilostazol in plasma was determined with an HPLC method using UV detector. The pharmacokinetic parameters(C_(max), T_(max) and AUC_(t)) were calculated and ANOVA was utilized for the statistical analysis of parameter. The results showed that the differences in C_(max), T_(max) and AUC_(t) between one tablet were 16.08%, 18.88% and 17.57%, respectively. The powers (1-β) for C_(max), T_(max) and AUC_(t) were 85.03%, 83.92% and 80.12%, respectively. Detectable differences(Δ) and confidence intervals were all less than 20%, and confidence interval of all the parameters were also less than 20% at the significance level(α) of 0.05. All of these parameters met the criteria of KFDA for bioequivalence, indicating that Cilostan^(R) tablet is bioequivalent to Pletaal^(R) tablet.

아세클로페낙 연질캡슬(클란자 에스 연질캡슬)의 개발

용철순,이경희,최진석,박병주,정세현,김용일,박상만,배명수,김귀자,김영식,유창훈,강성룡,유봉규,이종달,최한곤 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.1

To develop and aceclofenac soft capsule, four preparations with various solubilizers were prepared and their dissolution test was carried out. Among four preparations tested, a preparation with ethanolamine was selected a formula of aceclofenac soft capsule (Clanza S^(™), since it showed the fastest dissolution rate. Bioequivalence of aceclofenac tablet, Airtal^(™)(Dae-Woong Pharmaceutical Co., Ltd.) and aceclofenac soft capsule, Clanza S^(™)(Korea United Pharmaceutical Co., Ltd.) was evaluated according to the guideline of KFDA. Fourteen normal male volunteers (age 20-25 years old) were divided into two groups and a randomized 2×2 cross-over study was employed. After oral administration of one tablet or capsule containing 100 ㎎ of aceclofenac, blood ws taken at predetermined time intervals and the concentration of aceclofenac in plasma wa determined with an HPLC method under UV detector. The pharmacokinetic parameters (C_(max), T_(max) and AUC_(t)) were calculated and ANOVA was utilized for the statistical analysis of parameters using logarithmically transformed AUC_(t), C_(max) and T_(max) between Airtal tablet and Clanza soft capsule were 2.89%, 0.18% and 43.0%, 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(1.250(e.g.log(0.81) - log(1.23) and log(0.89) - log(1.14)) for AUC_(t) and C_(max), respectively. Thus, the criteria of the KDFA guidelines for the equivalence was satisfied, indicating that Clanza S^(™) soft capsule is bioequivalent to Airtal^(™) tablet.

적혈구를 이용한 약물 수송

용철순,박경아 영남대학교 약품개발연구소 1992 영남대학교 약품개발연구소 연구업적집 Vol.2 No.-

The use of erythrocyte as drug carrier has been reviewed. Carrier erythrocytes have proven to offer many advantages for delivery of therapeutic agents, especially in the treatment of inherited enzyme deficiency and cancer. Carrier erythrocytes are biodegradable and nonimmunogenic. Encapsulated drugs may be protected from premature degradation, inactivation and excretion. Carrier erythrocytes may be used as a slow-release system. Targeting of encapsulated drugs directly to a site of action is another possibility. Methods for encapsulating drugs into erythrocytes, the fate of carrier erythrocytes in vivo, the strategies of targeting carrier erythrocytes to special organs and in vivo applications of erythrocytes have been discussed. The encapsulation of drugs in erythrocytes has shown attractive possibilites in future use.

치수유래 구심성 신경섬유의 삼차신경 감각핵군에서의 연접특성

배용철,이은희,최민기,홍수형,김현정,남순현,김영진 대한소아치과학회 2001 大韓小兒齒科學會誌 Vol.28 No.2

일차연접부위에서 악안면 영역에서 유래하는 유해자극의 전달 및 처리기전을 이해하고자 horseradish pe개xidase를 치수지배 구심성 신경섬유를 표식한 후 연수후각에서 미세구조 및 연절 양상을 분석하여 다음과 같은 결과를 얻었다. 표식종말은 소수의 큰 치밀소포가 관찰되는 종말 (S형) 및 다수의 치밀소포를 함유하는 종말 (LDCV형)등 2종류로 분류할 수 있었다. S형 및 LDCV형 표식종말의 연접양식은 유사하였으며, 다수의 표식종말이 1개 혹은 2개의 neurofile과 연접을 이루어 대단히 단순한 연접양상을 보였다. 표식종말은 가지돌기체 보다는 다수의 가지돌기가시와 연접을 이루는 빈도가 높았다. 표식종말이 세포체 및 이에 인접한 근심부 가지돌기와 연접하는 경우는 드물었으며, 소수의 표식종말에서 p-ending과 연접하는 경우를 보였다. 표식종말의 체적, 표면적, 사립체의 체적, neurofile과 접하는 면적, 활성부위의 면적, 단위표식종말당 연접소포의 수 및 연접소포의 밀도등은 넓은 범위의 계측치를 나타내었으며, 이는 5명 및 LDCV형 표식종말 사이에 유의한 차이가 없었다. 이상의 결과로 미루어보아 연수후각에서 치수유래 구심성 신경섬유 종말의 연접양식은 고유의 특징을 보이며 이는 신경회로의 기능과 밀접한 상관관계를 가지는 것으로 판단되었다. Little is known about processing mechanism of pain sensation of the oral cavity at the 1st synapse of trigeminal sensory nuclei. Serial ultrathin sections of tooth pulp afferent terminals, identified by the transganglionic transport of 1% wheatgerm agglutinin conjugated horseradish peroxidase, were investigated wih electron microscope. Quantitative ultrastructural analysis was performed on digitizing tablet connected to Macintoshi personal computer (software: NIH Image 1.60, NIH, Bethesda, MD). Labeled boutons could be classified into two types by the shapes of containing vesicles : S bouton which contained mainly spherical vesicles (Dia. 45-55 nm) and few large dense cored vesicles (Dia. 80-120nm), and LDCV bouton, which contained spherical vesicles as well as large number of large dense coredd vesicles. Most of the parameters on the ultrastruotural characteristic and synaptic organization of labeled boutons were similar between S and LDCV boutons, except shapes of containing vesicles. Majority of the labeled boutons showed simple synaptic arrangement. The labeled bouton were frequency presynaptic to dendritic spine, and to a lesser extent, dendritic shaft. They rarely synapsed with soma and adjacent proximal dendrite. A small proportion of labeled boutons made synaptic contacts with presynaptic pleomorphic vesicless containing endings and synaptic triad. Morphometric parameters of labeled boutons including volume and surface area, total apposed area, mitochondrial volume, active zone area, vesicle number and density showed wide variation and theme were not significantly different between S and LDCV boutons. The present study revealed characteristic features on ultrastructure and synaptic connection of pulpal afferents which may involved in transmission of oral pain sensation.