• Title/Summary/Keyword: VIVO

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Correlation between in vitro release and in vivo bioavailability of Propranolol.HCI from Poly(vinyl alcohol) Hydrogel Suppositories (폴리비닐알코올 하이드로겔 좌제로부터 프로프라놀롤의 in vitro 방출과 in vivo 생체이용률간의 상관성)

  • Kim, Ho-Jeong;Ku, Young-Soon
    • Journal of Pharmaceutical Investigation
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    • v.28 no.4
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    • pp.275-282
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    • 1998
  • In order to develop a desirable in vitro release which correlates well with in vivo bioavailability, hollow type suppository containing Propranolol HCl(PPH) powder in the cavity and conventional type suppository with dispersed PPH in the base were prepared. Polyvinyl alcohol (PVA) hydrogel as a base and PPH as a model drug were used for the preparation of suppository. The rates of drug release from the suppositories were studied by Paddle method, Muranish method, Dialysis tubing method and Rotating dialysis cell method. The release profiles from suppositories using the four different release tests were compared. After a rectal administration in rat, the mean $C_{max}$ of hollow type suppository was significantly lower than that of conventional type, but $T_{max}$, $AUC_{0{\to}12}$ and MRT of hollow type were significantly higher 1.6 times, 1.2 times and 1.9 times than those of conventional type, respectively. The computer program was used to simulate plasma concentration from in vitro released amounts of drug and in vivo pharmacokinetic parameters. Based on comparison of the simulated bioavailability from computer program with experimental bioavailability in rat we have found out in vitro release test which correlates well with in vivo bioavailability. Our results have shown the best correlation between in vitro release and in vivo bioavailability in PPH-PVA hydrogel hollow type suppository for the paddle method and conventional type suppository for the rotating dialysis cell method. In this work we propose that PPH-PVA hydrogel suppository shows in vitro-in vivo correlation. This data should help to optimize the formulation of the drug and provide a basis for quality control procedures.

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Tectorigenin Promotes Osteoblast Differentiation and in vivo Bone Healing, but Suppresses Osteoclast Differentiation and in vivo Bone Resorption

  • Lee, So-Youn;Kim, Gyu-Tae;Yun, Hyung-Mun;Kim, Youn-Chul;Kwon, Il- Keun;Kim, Eun-Cheol
    • Molecules and Cells
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    • v.41 no.5
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    • pp.476-485
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    • 2018
  • Although tectorigenin (TG), a major compound in the rhizome of Belamcanda chinensis, is conventionally used for the treatment of inflammatory diseases, its effects on osteogenesis and osteoclastogenesis have not been reported. The objective of this study was to investigate the effects and possible underlying mechanism of TG on in vitro osteoblastic differentiation and in vivo bone formation, as well as in vitro osteoclast differentiation and in vivo bone resorption. TG promoted the osteogenic differentiation of primary osteoblasts and periodontal ligament cells. Moreover, TG upregulated the expression of the BMP2, BMP4, and Smad-4 genes, and enhanced the expression of Runx2 and Osterix. In vivo studies involving mouse calvarial bone defects with ${\mu}CT$ and histologic analysis revealed that TG significantly increased new bone formation. Furthermore, TG treatment inhibited osteoclast differentiation and the mRNA levels of osteoclast markers. In vivo studies of mice demonstrated that TG caused the marked attenuation of bone resorption. These results collectively demonstrated that TG stimulated osteogenic differentiation in vitro, increased in vivo bone regeneration, inhibited osteoclast differentiation in vitro, and suppressed inflammatory bone loss in vivo. These novel findings suggest that TG may be useful for bone regeneration and treatment of bone diseases.

Evaluation of different media for ex vivo porcine lung culture model

  • Yang, Myeon-Sik;Zhou, Zixiong;Khatun, Amina;Nazki, Salik;Jeong, Chang Gi;Kim, Won Il;Lee, Sang Myeong;Kang, Seog-Jin;Lim, Chae Woong;Kim, Bumseok
    • Korean Journal of Veterinary Service
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    • v.41 no.4
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    • pp.263-269
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    • 2018
  • Developing drugs targeting respiratory pathogen is essential to control respiratory diseases. Many experiments have been performed under in vivo situation. However, in vivo experiments have economical and ethical issues. The objective of this study was to determine the possibility of developing an ex vivo lung culture system with possible application for respiratory infection studies. After isolating lungs from naïve pigs, agarose-inflated lung tissues were prepared and sliced manually. These sliced lung tissues were then subsequently placed on 24-well plates. Eight different combinations of media were used to determine the optimum ex vivo lung culture condition. In addition, lung tissues were infected with porcine reproductive and respiratory syndrome (PRRS) virus at a titer of $1{\times}10^4\;TCID_{50}/mL$. Virus growth was confirmed by titration in MARC-145 cells at 2, 4, 6 days post infection (dpi). We found that ex vivo lung culture in physiological environment was not media specific based on histopathology and cytotoxicity. However, under virus-infected condition, thickened alveolar walls in the lung tissues and stable virus titers at 2, 4, 6 dpi were shown in F12K medium suggesting that it was useful for tissue maintenance and virus infection using PRRS virus infected lung tissues. The present study shows the possibility of using porcine ex vivo lung model for respiratory infection studies.

천연물 항암제의 유도체 개발

  • 심영기
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.212-212
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    • 1994
  • 본 연구소에서 분리하여 항암활성을 측정한바 있는 Sesquiterpene lactone계열의 KR-53170이 in vitro에 비해 in vivo에서 상대적으로 낮은 효력을 보이는데 착안 그 유도체들을 합성함으로써 in vivo stability 및 efficacy를 개선하고자 하였다. 합성된 물질의 in vivo activity는 human tumor cell중에서 A549(폐암), SK-OV-3(난소암1, SK-MEL-2(피부암), XF-498(중추신경계암), HCT-15(직장암)의 5개 암세포를 이용하여 ED$_{50}$($\mu\textrm{g}$/ml )를 측정하였으며 대조물질로는 KR-53170과 Cisplatin이 사용되었다. 그 결과 HR-53170의 terminal methyl ketone이 carboxylic acid로 변환된 CW-251001과 이것의 methyl ester인 CW-251002, ethyl ester인 CW-251003, 그리고 morpheline과 수용성으로 N-methylpiperazine, N-methyl-N'-aminopiperazine, 4-Piperidinopiperidine을 결합시켜서 합성한 CW-251011, CW-251012, CW-251013, CW-251014가 in vitro에서 어느 정도 활성을 유지하였다. 특히 이들중 CW-251001, CW-251012, CW-251013, CW-2s1014는 물에 대한 용해도가 상당히 개선되어 in vivo 활성검색을 위한 후보물질로 고려되었다. 하지만 이들중 CW-251001은 in vivo에서 낮은 농도에서는 활성이 거의 없었으며 놓은 농도에서는 독성을 나타내었다.

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Assay of In Vivo Chromium with a Hollow-fiber Dialysis Sensor

  • Ly, Suw-Young;Yoo, Hai-Soo;Jung, Min-Ki;Ko, Kwang-Hee;Kim, Byung-Jin;Lee, Ki-Chul;Choi, Byung-Min
    • Toxicological Research
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    • v.26 no.3
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    • pp.233-236
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    • 2010
  • The analytical in vivo chromium ion was searched for using a voltammetric hollow-fiber dialysis sensor via square wave stripping voltammetry (SW), cyclic voltammetry (CV), and chronoamperometry. Under optimum parameters, the analytical results indicated linear working ranges of 50~400 mg/l CV and $10{\sim}80\;{\mu}g/l$ SW within a 30-sec accumulation time. The analytical detection limit (S/N) was $6.0\;{\mu}g/l$. The developed method can be applied to in vivo tissues and in ex vivo toxicity assay, as well as to other materials that require chromium analysis.

Isolation and in vivo Activities of Antifungal Compounds from Myxococcus sp. JW154 (Myxobacteria). (점액세균 Myxococcus sp. JW154로 부터 항균물질의 분리 및 식물병원균에 대한 in vivo 활성)

  • 안종웅;김병섭
    • Microbiology and Biotechnology Letters
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    • v.30 no.2
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    • pp.162-166
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    • 2002
  • Two bithiazole-type antibiotics were isolated from the culture broth of a Myxococcus species which isolated from the marine sediment off the coast of Cheju Island, Korea. The structures of these metabolites were determined as KR025 and melithiazole F, previously reported bithiazoles, using combined spectroscopic methods. Both compounds showed an antifungal activity. In in vivo tests, these compounds exhibited potent controlling activities against tomato late blight, wheat leaf rust, and barley powdery mildew with control values more than 80% at a concentraton of 20 $\mu\textrm{g}$/ml.

In Vivo Measurements of Blood Flow in a Chicken Embryo Using Micro PIV Technique (유정란 배아 혈액유동의 in vivo 계측)

  • Yeo Chang-Sub;Han Kyu-Yeon;Lee Sang-Joon
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.30 no.4 s.247
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    • pp.314-319
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    • 2006
  • To analyze in-vivo blood flow characteristics in a chicken embryo, in-vivo experiment was carried out using micro-PIV technique. Because endothelial cells in blood vessels are subject to shear stress of blood flow, it is important to get velocity field information of the placental blood flow. Instantaneous velocity fields of an extraembryonic blood vessel using a high-speed camera and intravital microscope. The flow images of RBCs were obtained with a spatial resolution of $20\times20{\mu}m$ in the whole blood vessels. The mean velocity field data confirm that the blood flow does show non-Newtonian fluid characteristic. The blood in a branched vessel merged smoothly without any flow separation into the main blood vessel with the presence of a slight bump. This in-vivo micro-PIV measurement technique can be used as a powerful tool in various blood flow researches.

ULTRASTRUCTURAL COMPARISON OF BOVINE BLASTOCYSTS DEVELOPED IN VIVO AND IN VITRO

  • Ohboshi, S.;Nakamichi, R.;Hanada, K.;Zhao, J.;Hattori, M.;Fujihara, N.;Umetsu, R.
    • Asian-Australasian Journal of Animal Sciences
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    • v.8 no.6
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    • pp.599-605
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    • 1995
  • The ultrastructures of in vitro-derived bovine blastocysts have been compared with those of blastocysts obtained from a superovulated cow. In vivo blastocysts obtained from the uterus showed well-differentiated features, while in vitro-derived embryos, which were developed from in vitro fertilized ovum, showed insufficient cellular organizations. In vitro-derived embryos contained many undefined cellular organizations in the perivitelline spaces compared with in vivo-derived blastocysts. Other features of in vivo and in vitro blastocysts were characterized by differential development of microvilli projection into blastocoele from the surface of the trophoblast cells. The conceivable reason for the difference between in vivo and in vitro developments of bovine embryos is that it is likely that in vitro culture system adopted in the present experiment may not be sufficient for better embryonic development.

Anticoagulation Activity Pattern and In vivo Test of Extract from Eugenia caryophyllata (정향 추출물의 항응고 활성양식 및 In vivo Test)

  • 이종임;이현순;전우진;유광원;신동훈;홍범식;조홍연;양한철
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.29 no.3
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    • pp.543-548
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    • 2000
  • EC-2B와 EC-2C 획분은 정향(Eugenia caryophyllata)의 알칼리 추출물로부터 에탄올 침전, cetavlon 처리 및 한외여과를 거쳐 분획하였다. EC-2B 획분은 APTT에서 항응고 활성을 가지는 반면, EC-2C 획분은 APTT와 TT 모두에서 항응고 활성을 가지고 있으며 EC-2B와 EC-2C에서 모두 혈소판 응집억제능을 관찰할 수 있었다. EC-2B와 EC-2C 획분의 경구투여에서 두 획분 모두 독성이 없었으며 EC-2B 획문은 1,000 mg/kg (mouse, intravenours)에서도 독성이 없었으나, EC-2C 획분은 LD50 322 mg/kg 정도의 독성을 가지고 있었다. 두 획분의 in vivo 성에서의 항응고 활성을 60% 생존율을 갖는 dose로 표시한 결과 EC-2B는 131 mg/kgdlsep 비해 EC-2C는 58 mg/kg로 활성의 차이가 in vitro에서 보다 크게 나타났다. 이 두획분을 sulfation시킨 후 활성의 변화를 ex vivo를 통해 확인한 결과 두 획분 모두 활성이 증가하였으며 특히 EC-2B 획분의 활성이 급격히 증가하였다.

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A Study on the Source of Reductants for Nitrate Reduction in Rice (Oryza sativa cv. Tongil) Roots (벼(Oryza sativa cv. Tongil) 뿌리에 있어서 Nitrate 환원에 필요한 환원력의 공급원에 관한 연구)

  • Chang, Nam-Kee;Choe, Hong-Gwan
    • The Korean Journal of Ecology
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    • v.7 no.2
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    • pp.85-90
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    • 1983
  • There was a decrease in nitrate reductase activity (NRA) measured in vivo in rice roots (Oryza sativa cv. Tongil) grown in anaerobic culture solution. But it was reversed by addition of malonate to the in vivo nitrate reduction assay medium. Malonate increased the in vivo NRA during 2-5 hours incubation and decreased it in longer incubation hours. In vivo NRA was stimulated by addition of NaHCO3 to the assay medium, but not by Na2CO3. The stimulation of NRA by NaHCO3 was not observed in shoot removed rice roots. It is suggested that CO2 from NaHCO3 is carboxylated by phosphoenol pyruvate carboxylase, results in increasing the malate contents in the roots, and stimulates the in vivo NRA. NADH needed in nitrate reduction is supported by malate oxidation. In rice roots, it seems probable that malate oxidation in the mitochondria is more important to nitrate reduction than malae oxidation in cytoplasm.

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