• Title/Summary/Keyword: 서방성

Search Result 138, Processing Time 0.023 seconds

Effect of Food on Pharmacokinetics and Pharmacodynamics of Fenofibric Acid after a Single Oral Dose of Fenofibrate Sustained-Release Capsule (식단에 따르는 페노피브레이트 서방성 캡슐의 1회 경구 투여 후 약물동태학 및 약물동력학의 평가)

  • Yun, Hwi-yeol;Kim, Joung-hyun;Lee, Eun Joo;Chung, Soo Youn;Choi, Sun-oK;Kim, Hyung Kee;Kwon, Jun-tack;Kang, Wonku;Kwon, Kwang-il
    • Korean Journal of Clinical Pharmacy
    • /
    • v.15 no.1
    • /
    • pp.34-40
    • /
    • 2005
  • We examined the effects of food on pharmacokinetic and pharmacodynamic properties of fenofibrate released from sustained-release(SR) capsule as therapy for hypolipidemia. Twenty-four healthy volunteers were used in $3{\times}3$ crossover pharmacokinetic and pharmacodynamic study; Additional six volunteers were used as a control group (i.e., no fenofibrate administration). A single dose of fenofibrate (SR capsule, 250 mg) was administered on three occasions: after overnight fasting, after consumption of a standard breakfast, and after a high-fat breakfast. Serial blood samples were collected for the next 72 hours. Plasma fenofibric acid concentrations were measured by high performance liquid chromatography, and pharmacokinetic parameters were calculated using ADAPT II program. Plsama triglyceride concentrations were measured by blood chemistry analyzer (CH-100). The pharmacokinetic parameters were significantly affected by food intake. The high-fat breakfast affected the rate of absorption of fenofibrate more than did the standard breakfast and fasted conditions. Plasma concentrations of triglyceride at 24 hours decreased significantly after the administration of fenofibrate compared with the concentration at 0 hours(P<0.05). In healthy volunteers, the bioavailability of fenofibrate was greater when administered via sustained-release capsules immediately after the consumption of food than after fasting condition.

  • PDF

새로운 nucleoside계 항암제, ara-CDP-DL-PCA.Na(BR-28702-2)의 약효연구 및 급성독성 시험.

  • 백우현;신원섭;채희상;노정구;강부연;차신우
    • Proceedings of the Korean Society of Applied Pharmacology
    • /
    • 1994.04a
    • /
    • pp.169-169
    • /
    • 1994
  • 항암 및 면역조절작용을 가지고 있으며 그 자체가 서방성 prodrug으로서 약효를 나타낼것으로 기대되는 ara-C와 etherphospholipid의 conjugate인 ara-CDP-DL-PCA.2Na, ara-CDP-DL-PBA.2Na, 및 ara-CDP-DL-PMA.2Na 3종의 BR-8702-2의 micellar soultion을 투여시료로 하여 제암력 평가를 실시하였다. DBA/2J 마우스(평균 체중 25g, 수컷)에 L$_{1210}$임파성 백혈병 세포를 이식한 후, 24시간 후 약물을 복강내에 투여하는 실험계 에서 400mg/kg/day, 단회투여 및 80 혹은 100mg/kg/day, 1~5일간 투여로 ILS%값이 229~543으로 우수한 제암력을 보였다. 또한 BDF$_1$ mice(15~20g)의 axillary region에 3㎣의 Lewis Lung Tumor를 피하로 이식한후 약물투여를 통한 제암효과를 관찰하였다. 100, 200, 300mg/kg/day의 단회 투여계 에서는 수명연장 효과가 없었다. 한편, 20, 40, 60mg/kg/day, 1~5일간의 투여계 에서는 ara-CDP-DL-PCA.2Na만이 효과가 있었는데 농도에 역순하여 저농도인 20mg/kg/day, 1~5일간의 투여계에서 가장 효과가 있었으며 그때의 ILS%는 32.3%였고 투여기간중의 체중변화는 거의 보이지 않았다. 한편 NICOM 370 Dynamic Light Scattering을 이용하여 투여시료로한 micellar solution의 입자도를 분석한 결과 ara-CDP-DL-PCA.2Na는 4.2nm size의 것이 99.48%를 차지하고 있었다. ara-CDP-DL-PCA.2Na의 ICR 마우스를 이용한 급성독성 시험에 있어서 경구투여에서의 LD$_{50}$값은 암,수컷 모두 5000mg/kg이상 이었고, 정맥내 투여 에서는 432mg/kg이었다. 실험과정중 생존동물의 일반적 이상소견등은 없었으나 정맥내 투여의 경우에서 체중증가 억제현상이 있었다.

  • PDF

Formulation Design of Sustained-Release Matrix Tablets Containing 4-Aminopyridine (유드라짓과 알긴산 나트륨 매트릭스를 이용한 4-Aminopyridine의 서방성 제제설계)

  • Kim, Jeong-Soo;Kim, Dong-Woo;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
    • /
    • v.35 no.6
    • /
    • pp.453-460
    • /
    • 2005
  • 4-Aminopyridine (AP) is a potassium channel blocker used in the treatment of neurological disorders such as multiple sclerosis and Alzheimer disease. AP‘s window of therapeutic effect appears to correlate with its plasma halflife (3.5 hours). It demonstrates pH-dependent solubility because of a weakly basic drug. In addition, the resulting release from conventional matrix tablets decreases with increasing pH-milieu of the gastrointestinal tract. The aim of this study is to design sustained release matrix tablet containing AP, overcoming this problem. $Eudragit^{\circledR}$ L 100 (EuL) and sodium alginate were used in an effort to achieve pH independent drug release. The effect of sodium alginate and EuL on drug release from matrix tablet was investigated. The drug release behavior from the different tablets was analyzed by $t_{20%},\;t_{40%},\;t_{60%}$, The exponential diffusion coefficient n, kinetic constant K were calculated according to the Korsmeyer-Peppas equation. The drug release from matrix tablets prepared with sodium alginate was decreased with increasing the content of sodium alginate in pH 7.4 while there is no significant difference in pH 1.2. The exponent n values were determined to be approximately 0.5 and 0.8 respectively, in both pH 1.2 and 7.4. These values indicate diffusion-based anomalous mechanism and erosion-based anomalous mechanism, respectively. The drug release from sodium alginate matrix tablets prepared with solid dispersion of EuL containing drug showed a slow drug release in an acidic medium and a more fast drug release in phosphate medium, compared with sodium alginate matrix tablets prepared with physical mixture. These results may be attributed to the gel forming ability of sodium alginate and pH dependent solubility of EuL. Therefore, sustained-release AP matrix tablets using sodium alginate and EuL were successfully prepared.

Preparation and Release Profile of N8f-loaded Polylactide Scaffolds for Tissue Engineered Nerve Regeneration (조직공학적 신경재생을 위한 NGF를 함유한 PLA 담체의 제조 및 방출)

  • 전은경;황혜진;강길선;이일우;이종문
    • Polymer(Korea)
    • /
    • v.25 no.6
    • /
    • pp.893-901
    • /
    • 2001
  • We developed the nerve growth factor (NGF) loaded poly (L - lactide) (PLA) scaffolds by means of emulsion freeze drying method to the possibility for the application of the nerve regeneration of spinal cord disease and the degeneration in Alzheimer's disease. The release amount of NGF from NGF loaded PLA scaffold were analyzed over a 4 week period in vitro at phosphate buffered saline (PBS), pH 7.4, at $37^{\circ}C$. It can be observed the open cell pore structure of porous scaffolds and can be easily controlled the pore structure by the controlling of formulation factors resulting in the controlling of the release rate and the release period. The stability of NGF during the preparation of PLA scaffold was evaluated by comparing the released amounts of total NGF, assayed NGF enzyme - linked immunosorbent assay (ELISA). Released NGF has been found to enhance the neurite sprouting and outgrowth from pheochromocytoma (PC-12) cells. These results suggest that the released NGF from NGF loaded PLA scaffold such as conduit type can be very useful for the nerve regeneration in the neural tissue engineering area.

  • PDF

Formulation and Pharmacokinetic Evaluation of Sustained Release Preparation Containing Clebopride Malate (말산클레보프리드 서방성 제제의 제조 및 약물동태학적 평가)

  • Ryou, Hae-Won;Lee, Joo-Han;Chi, Yong-Ha;Hahn, Yang-Hee;Tan, Hyun-Kwang;Lee, Kyu-Heung;Kim, Sang-Lin;Jeon, Seung-Yoon;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
    • /
    • v.30 no.3
    • /
    • pp.179-189
    • /
    • 2000
  • Clebopride malate(Cm) is a new benzamide drug which has a potent central antidopaminergic activity possessing antiemetic and anxiolytic properties. A purpose of this study was to assess the feasibility of formulating sustained release preparation by dispersing a drug in hydrophilic polymeric matrices and double layered tablets(DLT), using HPMC, carbopol, PEO, PVP/VA and other polymers as a rate controlling barrier. The matrix and DLT showed optimum dissolution pattern up to 8 hours and the contents of polymer were optimized at 30% level in this preparation. After an oral administration in beagle dog, Cm concentration was determined by use of GC-ECD and pharmacokinetic parameters were calculated by Vallner's method. The AUC of DLT showed similar results and the duration of action was increased 55% compared to that of regular release dosage form. The calculated absorption rate effectiveness(ARE) and controlled release effectiveness(CRE) for DLT increased 50% compared to that of matrix, the overall effectiveness(E) of this product appears to be about 70%. in vivo effectiveness test, DLT showed significant differences from control on antiemetic action of Cm. In consequence, it was possible to conclude that double layered tablet might be a good candidate for the sustained release dosage forms.

  • PDF

A Study on the Fluidity Retention of Cement Paste Added by Naphthalene Sulfonated Condensate and Polycarboxylic Acid Admixture (나프탈렌술폰산축합물과 폴리카르본산계 혼화제가 첨가된 시멘트 페이스트의 유동성 유지에 관한 연구)

  • 노재성;홍성수;김도수
    • Magazine of the Korea Concrete Institute
    • /
    • v.7 no.5
    • /
    • pp.189-199
    • /
    • 1995
  • Naphthalene sulfonated condensate has been widely used as a superplasticizer for cement and concrete, but the application was limited due to its large slump loss with elapsed time. To complement this demerit of NSF, polycarboxylic acid copolymer from nlaleic anhydride and acryl~c acid(MA) was synthesized to retain the mobility of cement and concrete, and then mixed with NSF. The physical properties, such as fluidity, fluidityretention and rheology, were measured by applying these admixtures to cement paste as a function of elapsed time. And also compressive strength of mortar was measured with curing time. NIv-l and NM-2 containing 10, 20 wt% of MA respectively had a excellent fluidity and a fluidity- retention. In rheological property, the increases of shear stress and viscosity with elapsed time were delayed with the increasing of shear rate in cornparision with NSF only. The marked slump loss of cement paste could be controlled by these admixture. Also the added ainount of admixture and the ratio of water to cement affected these properties.

Controlled Release of Tamsulosin from Enteric Coated Sustained-Release Matrices with Aqueous Microchannels (수성미세채널을 형성하는 서방성 매트릭스 장용정을 이용한 탐스로신의 방출제어)

  • Lee, Ki-Bong;Choi, Sung-Up;Jeon, Hong-Ryeol;Lee, Bong-Sang;Kim, Hyun-Il;Lee, Jae-Hwi;Choi, Young-Wook
    • Journal of Pharmaceutical Investigation
    • /
    • v.34 no.6
    • /
    • pp.471-475
    • /
    • 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.

Formulation of Sustained Release Matrix Tablets Containing Ibudilast with Hydroxypropylmethylcellulose Phthalate and Ethylcellulose (히드록시프로필메칠셀룰로오스 프탈레이트 및 에칠셀룰로오스를 이용한 이부딜라스트 함유 서방성 매트릭스 정제의 개발)

  • Oh, Dong-Hoon;Rhee, Jong-Dal;Ryu, Dong-Sung;Jang, Ki-Young;Im, Jong-Seub;Sung, Jung-Hoon;Han, Myo-Jung;Kwon, Tae-Hyup;Yang, Ho-Joon;Park, Byung-Chul;Lee, Jong-Sook;Yong, Chul-Soon;Choi, Han-Gon
    • Journal of Pharmaceutical Investigation
    • /
    • v.37 no.6
    • /
    • pp.355-358
    • /
    • 2007
  • To develop a sustained-release tablet which had the similar dissolution to commercial ibudilast-loaded sustained-release capsule, the tablets were prepared using hydroxypropylmethylcellulose phthalate (HPMCP), ethylcellulose (EC) and hydroxypropylcellulose (HPC), and dissolution test were carried out with paddle method in KP. The tablet prepared only with HPMCP and EC showed sno similar dissolution pattern to the commercial product. As the ratio of HPMCP/HPC in tablet decreased, the dissolution rate of drug decreased in pH 1.2 but increased in pH 6.8. Furthermore, an ibudilast-loaded sustained-release tablet composed of [ibudilast/EC/HPMCP/HPC (10/10/170/10 mg/tab)] gave similar dissolution to commercial product in pH 1.2 for 3 h and in pH 6.8 for 10 h. Thus, it could be a potential candidate for the substitute of commercial capsule.

Comparative Research on Global Policy in ICT Accessibility for Vulnerable Groups -Focusing on Implementation of Legislative System- (취약계층을 위한 정보통신 접근성 정책에 대한 국가 간 비교 연구 -관련제도 중심으로-)

  • Kim, Jung-Yeon;Park, Sung-Woo;Kang, Byung-Gwon;Son, Chang-Yong;Jung, Bong-Keun
    • 재활복지
    • /
    • v.20 no.1
    • /
    • pp.131-150
    • /
    • 2016
  • This study aims to compare global policies on ICT accessibility and to suggest possible solutions that help to enhance ICT accessibility for socially disadvantaged groups. The results indicated that related laws and standards in Korea are relatively well established than Asian countries' whereas they need improvements when compared to the US or the UK. Particularly, in spite of rapid development in information communication technology industry, incorporating the definition of newly developed technologies into existing laws related to ICT accessibility seemed slow that caused reluctancy of related parties to address accessibility issues the new technologies create. In addition, Korean government seems less effortful to develop policies and standards apart from web and mobile application accessibility. In order to resolve the problems, firstly, the period or process of enacting and amending laws can be shorten. Next, a government affiliated research institute can be established to do research and develop ICT accessibility related to user scenarios so that effective policies and standards could be readily provided. Even though other possible solutions can be suggested, what is more important than that is that any interested parties should sustainably make efforts to provide equal opportunities for the underserved populations.

Therapeutic comparison between low-dose sustained-release theophylline dry syrup and capsule in children with mild persistent asthma (유소아 경증 지속성 천식에서 저용량 서방형 테오필린 건조시럽과 캡슐 제형의 치료 효과 비교)

  • Lee, Hyun Seung;Lee, Hae Kyung;Kwon, Hi Jeong;Kim, Jeong Hee;Rha, Yeong Ho;Kim, Jin Tack;Kim, Young Ho;Lee, Hae Rhan;Pyun, Bok Yang
    • Clinical and Experimental Pediatrics
    • /
    • v.50 no.3
    • /
    • pp.284-291
    • /
    • 2007
  • Purpose : Theophylline has recently been reported to have concurrent anti-inflammatory effects at low therapeutic plasma concentrations which are below the doses at which significants, clinically useful bronchodilatation is evident. Sustained-release formulation in capsule and dry syrup forms were developed to reduce its adverse effects and improve its clinical effects. We compared the therapeutic effects of theophylline dry syrup and capsules in children with mild asthma. Methods : Ninety children with mild asthma were randomized to receive either theophylline dry syrup (n=44) or theophylline capsules (n=46); 4 mg per kilogram of body weight, twice a day, for 12 weeks. Baseline and serial measurements of daytime and nighttime asthma symptom score were performed. Compliance scores, drug swallowing scores, and drug usability scores were measured every 4 weeks. Each scoring was rated on a scale of 0-4. Serum theophylline concentration were measured at 4 and at 12 weeks. To examine the anti-inflammatory effect of theophylline on asthma, Serum eosinophilic cationic protein as a marker of airway inflammation caused by eosinophil was measured 12 weeks pre- and post-administration. Results : The daytime and nighttime asthma symptom scores of the two groups after 4 weeks significantly improved over the baseline score. Daytime and nighttime asthma symptom scores in the dry syrup group were statistically lower at all time points except for the nighttime symptom scores at 4 weeks. Compliance scores, drug swallowing scores, and drug usability scores in the dry syrup group were significantly higher at the end time point. Only in the dry syrup group was the serum ECP at the end time point statistically lower than baseline. Conclusion : Low-dose sustained-release theophylline may be safe and effective in bronchial asthma and this effect may be mediated by its anti-inflammatory action mechanisms. Especially, when used in children with asthma, dry syrup formulation is recommended because of its higher compliance than capsule formulation.