• Title/Summary/Keyword: T-curve

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Effect of Solubilizing and Microemulsifying Excipients in Polyethylene Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole

  • Heo, Min-Young;Piao, Zong-Zhu;Kim, Tae-Wan;Cao, Qing-Ri;Kim, Ae-Ra;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • v.28 no.5
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    • pp.604-611
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    • 2005
  • Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

In Vitro and In Vivo Studies of Different Liposomes Containing Topotecan

  • Hao, Yan-Li;Deng, Ying-Jie;Chen, Yan;Wang, Xiu-Min;Zhong, Hai-Jun;Suo, Xu-Bin
    • Archives of Pharmacal Research
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    • v.28 no.5
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    • pp.626-635
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    • 2005
  • Liposome as a carrier of topotecan (TPT), a promising anticancer drug, has been reported in attempt to improve the stability and antitumor activity of TPT. However, the biodistr ibution pattern of TPT liposome in vivo and PEG-modified liposome containing TPT have not been studied systemically. In this paper, the in vitro stability and in vivo biodistribution behavior of several liposomes containing TPT with different lipid compositions and PEG-modification were studied. Compared with the 'fluid' liposome (S-Lip) composed of soybean phosphatidylcholine (SPC), the 'solid' liposome (H-Lip) composed of hydrogenated soybean phosphatidylcholine HSPC decreased the leaking efficiency of TPT from liposome and enhanced the stability of liposome in fetal bovine serum (FBS) or human blood plasma (HBP). The results of biodistribution studies in S$_{180}$ tumor-bearing mice showed that liposomal encapsulation increased the concentrations of total TPT and the ratio of lactone form in plasma. Compared with free TPT, S-Lip and H-Lip resulted in 5- and 19- fold increase in the area under the curve (AUC$_{0\rightarrow\propto}$), respectively. PEG- modified H-Lip (H-PEG) showed 3.7-fold increase in AUC$_{0\rightarrow\propto}$ compared with H-Lip, but there was no significant increase in t$_{1/2}$ and AUC$_{0\rightarrow\propto}$ for PEG-modified S-Lip (S-PEG) compared with S-Lip. Moreover, the liposomal encapsulation changed the biodistribution behavior, and H-Lip and H-PEG dramatically increased the accumulation of TPT in tumor, and the relative tumor uptake ratios were 3.4 and 4.3 compared with free drug, respectively. There was also a marked increase in the distribution of TPT in lung when the drug was encapsulated into H-Lip and H-PEG. Moreover, H-PEG decreased the accumulation of TPT in bore marrow compared with unmodified H-Lip. All these results indicated that the membrane fluidity of liposome has an important effect on in vitro stability and in vivo biodistribution pattern of liposomes containing TPT, and PEG-modified 'solid' liposome may be an efficient carrier of TPT.

이성체쌍의 열중성자포획단면적비 측정

  • Park, Hy-Eil;Kim, Heon-Jun;Lee, Chul
    • Nuclear Engineering and Technology
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    • v.4 no.4
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    • pp.340-344
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    • 1972
  • Isomeric ratios were measured for the capture of thermal neutron by $^{79}$ Br, $^{80}$ Se, $^{103}$ Rh, $^{115}$ In and $^{133}$ Cs as well as those of epi-cadmium neutron by $^{79}$ Br, $^{80}$ Se and $^{l33}$Cs. The measurements were performed by analysing decay curves obtained by ${\gamma}$-ray spectrometry after irradiation. The counting efficiency curve was determined by using the calibrated standard sources with overall uncertainties of about 1%. Isomeric ratios, given in $\sigma$ high spin/($\sigma$ high spin + $\sigma$ low spin), of $^{80, 80m}$Br, $^{81,81m}$Se, $^{014, 104m}$Rh, $^{116,116m}$In and $^{134, 134m}$Cs produced by thermal neutron activation were found to be 0.21$\pm$0.01, 0.14$\pm$0.02, 0.12$\pm$0.02, 0.69$\pm$0.07 and 0.058$\pm$0.004, respectively, Those values of $^{80, 80m}$Br, $^{81,81m}$Se, and $^{134, 134m}$Cs Produced by epi-cadmium neutron were found to be 0.19$\pm$0.02, 0.29$\pm$0.02 and 0.074$\pm$0.011, respectively. The experimental values obtained were compared with the theoretical values deduced from the statistical model. There were the general agreements between the theory and the experiment.t.

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Cooking Properties of Dry Noodles Prepared from HRW-WW and HRW-ASW Wheat Flour Blends (미국밀과 호주밀의 제면성 비교)

  • Shin, Sung-Young;Kim, Sung-Kon
    • Korean Journal of Food Science and Technology
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    • v.25 no.3
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    • pp.232-237
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    • 1993
  • The rheological properties of hard red winter, western white and Australian standard white wheat flours and of HRW-WW and HRW-ASW wheat flour blends having the same protein content were studied. Cooking properties of dry noodles prepared from HRW-WW and HRW-ASW wheat flour blends were also investigated. The noodles were prepared with salt and alkaline reagent. The salt and alkaline concentrations used were 1.7% and 0.17%. respectively, based on the weight of wheat flour. The alkaline reagent was an equal mixture of sodium carbonate and potassium carbonate. The HRW-ASW wheat flour blend had higher farinograph absorption and slightly stronger curve than HRW-WW wheat flour blend. Salt decreased the absorption of wheat flours by 2 and of wheat flour blends by 1%. However, alkaline reagent essentially had no effort on farinograph absorption. Salt and alkaline reagent strengthened the dough of wheat floors and wheat flour blends, with the former being more effective. No significant differences in pasting properties between HRW-WW and HRW-ASW wheat flour blends by amylograph were observed. There were no significant differences in rate of increase of weight or volume between noodles prepared from HRW-WW and HRW-ASW wheat flour blends. Alkaline reagent did not affect the weight gain of noodles hut lowered the volume gain. Breaking force of dry noodles and cutting force of cooked noodles were similar between the two noodles. Alkaline reagent increased both the breaking and cutting forces of noodles. Sensory evaluation revealed that the noodles prepared from HRW-WW and HRW-ASW wheat flour blends were slightly different. but not different from each other by preference test.

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Formation of TiO(OH)$_2$ Ultrafine Particles by Reverse Micelle (역마이셀에 의한 TiO(OH)$_2$ 미세분말 제조)

  • 장화익;강석원;이광래
    • Journal of the Korean Ceramic Society
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    • v.35 no.6
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    • pp.594-602
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    • 1998
  • Titanium hydroxide (TiO({{{{ {OH }_{2 } }})) fine particles were produced by the reverse micelle technique. For the formation of titanium hydroxide (TiO({{{{ {OH }_{2 } }})) particles with the technique reversed micellar solution was prepared by solubilizing water into organic solvent (isooctane) with a surfactant and titanium alkoxide (tetraisopropyl orthotitanate) diluted with isopropyl alcohol was added to the reversed micellar solution. The hdrolyzed species (TiO({{{{ {OH }_{2 } }})) was formed by the hydrolysis of titanium alkoxide and titanium dioxide is then formed by the condensation of the hydrolyzed species. There are several process variables such as surfactants concentration of surface cosurfactant hydrolysis temperature and pH. In this work the ef-fects of process variables on paticle shapes particle size distribution and paticle agglomeration were bi-nodal for an anionic surfactant(AOT) in the whole range of temperature pH and surfactant concentration of this experiment. The addition of ethanol as a cosurfactant resulted in narrow particle size distribution of the experiment. The additiono of ethanol as a cosurfactant resulted in narrow particle size distribution and 0.12${\mu}{\textrm}{m}$ of smaller average particle diameter. FT-IR spectrum of particles shows the absorption peak of Ti-OH bonding and Ti-O bonding. An exothermic peak around 41$0^{\circ}C$ in TGA-DTA curve shows that crys- tallized anatase phase appears and completely transits to anatase around 45$0^{\circ}C$.

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Studies on Color and Rheological Properties in Strawberry Jam (딸기쨈의 색깔과 물성에 관한 연구)

  • Lee, Jong Hyeouk;Chang, Kyu Seob;Yoon, Han Kyo
    • Korean Journal of Agricultural Science
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    • v.14 no.1
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    • pp.134-143
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    • 1987
  • In order to observe the strawberry as the raw materials and to compare the color of strawberry's products, Hunter L,a,b tristimulate color values were measured physically by color difference meter. Food textural properties of strawberry were measured by Rheo textural meter for rheological properties of strawberry jam. According to results obtained, it showed that Hunter L,a,b tristimulus color values were affected by ripening time of strawberry and Hunter color values changed regularly on different pH. Deformation of red color pigment Hunter color values changed linearlly on different pH, therefore red color pigment of elderberry showed to be used as a food color agent. The first peak of strawberry in TPA curve was high as cherry, grape and pineapple Strawberry jam showed pseudoplastic characteristic and time dependence.

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A Comparison Study with the Vatiation of Isocenter and Collimator in Stereotactic Radiosurgery (방사선 수술시 Isocenter, 콜리메이터 변수에 따른 선량 분포 비교연구)

  • 오승종;박정훈;곽철은;이형구;최보영;이태규;김문찬;서태석
    • Progress in Medical Physics
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    • v.13 no.3
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    • pp.129-134
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    • 2002
  • The radiosurgery is planned that prescribed dose was irradiated to tumor for obtaining expected remedial value in stereotactic radiosurgery. The planning for many irregular tumor shape requires long computation time and skilled planners. Due to the rapid development in computer power recently, many optimization methods using computer has been proposed, although the practical method is still trial and error type of plan. In this study, many beam variables were considered and many tumor shapes were assumed cylinderical ideal models. Then, beam variables that covered the target within 50% isodose curve were searched, the result was compared and analysed. The beam variables considered were isocenter separation distance, number of isocenters and collimator size. Dose distributions obtained with these variables were analysed by dose volume histogram(DVH) and dose profile at orthogonal plane. According to the results compared, the use of more isocenters than specified isocenter dosen't improve DVH and dose profile but only increases complexity of plan. The best result of DVH and dose profile are obtainedwhen isocenter separation was 1.0-1.2 in using same number of isocenter.

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Analysis of Bioconversion Components of Fermentation Hwangryunhaedok-tang (발효 황련해독탕의 생물 전환 성분분석)

  • Lee, Kwang Jin;Lee, BoHyoung;Jung, Pil Mun;Lian, Chun;Ma, Jin Yeul
    • YAKHAK HOEJI
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    • v.57 no.4
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    • pp.293-298
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    • 2013
  • Hwangryunhaedok-tang (HRT) is a traditional herbal medicine, which has been known as a useful prescription for anti-biotic, anti-inflammatory, anti-oxidative and immunosuppressive activity. In this study, the variation in the amount of eight bioactive components of Hwangryunhaedok-tang (HRT) and its fermentation HRT with Lactobacillus casei KFRI 127, Lactobacillus curvatus KFRI 166 and Lactobacillus confuses KFRI 227 was investigated via high-performance liquid chromatography coupled with diode array detection (HPLC-DAD). Simultaneous qualitative and quantitative analysis of eight bioactive components; geniposide, genipin, baicalin, wogonoside, palmatine, berberine, baicalein and wogonin was achieved by comparing their retention times ($t_R$) and UV spectra with those of the standard components. All calibration curve of standard components showed good linearity ($r^2$ >0.979). As a result, the geniposide amount was $15.52{\pm}0.19{\mu}/mg$ that as a main components in HRT. The wogonoside was decreased by 29.28~58.35% with Lactobacillus casei KFRI 127 and L. confuses KFRI 227 ($3.17{\pm}0.31{\mu}g/mg$ and $3.55{\pm}0.13{\mu}g/mg$) compared with the original HRT ($5.02{\pm}0.14{\mu}g/mg$). Otherwise wogonin was increased by 16.28~41.86% with Lactobacillus casei KFRI 127 and L. confuses KFRI 227 ($0.61{\pm}0.01{\mu}g/mg$ and $0.50{\pm}0.02{\mu}g/mg$) compared with the original HRT($0.43{\pm}0.00{\mu}g/mg$). HRT fermented with L. casei KFRI 127 and L. confuses KFRI 227 were evaluated as creating the changes in wogonoside to that aglycon wogonine. In the fermented HRT using Lactobacillus acidophilus KFRI 166, the genipin was only detected, among 3 species of fermentation strains. Thus, these results considered that the strains 166 were exhibited the remarkable changes in genipin.

Changes of mandibular dental arch during surgical-orthodontic treatment in skeletal class III malocclusion individuals (악교정수술을 받은 III급 부정교합자의 치료 전, 후의 하악치열궁 변화)

  • Nam, Hyung-Jin;Son, Woo-Sung;Park, Soo-Byung;Kim, Seong-Sik
    • The korean journal of orthodontics
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    • v.38 no.4
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    • pp.283-298
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    • 2008
  • Objective: The purpose of this study was to investigate changes in the mandibular dental arch from presurgical orthodontic treatment and orthognathic surgery, and to evaluate the relationships between the pretreatment records and changes of mandibular dental arch in skeletal Class III malocclusion individuals. Methods: Lateral cephalometric radiographs and mandibular study models of 31 adults with skeletal class III malocclusion were taken and measured. All measurements were evaluated statistically by ANOVA, Scheffe's Post Hoc, and paired t-test, and correlation coefficients were evaluated. Results: No significant difference in Mn-LMMC, Mn-LIE, Mn-MnOcc was detected between pretreatment and presurgical groups. Statistically significant but low correlations were demonstrated between the initial arch length discrepancy (ALD) and change in ICW, IPW1 (r = 0.492, 0.615) and change in arch length (r = 0.641). No association was seen between the initial depth of curve of Spee and change in mandibular incisor angle and arch width or arch length. Regression analysis showed that the amount of change for arch length and IPW1 could be explained by 64.0% and 75.8% of the pretreatment variables respectively. Conclusions: This study suggests that orthognathic surgery results can be predictable by measuring the pretreatment records.

Acoustic Characteristics of Sound Field in Partially Opened Rooms -Emphasis on Vertical Coupling of Diffuse and Free Field- (실내공간의 부분적 개방에 따른 음향특성변화 II -확산음장과 자유음장의 수직적 결합을 중심으로-)

  • Jeong, Dae-Up;Choi, Young-Ji
    • Journal of Korean Association for Spatial Structures
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    • v.7 no.5
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    • pp.75-82
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    • 2007
  • The present work measured and analyzed changes in the acoustics of a sound field which has a retractable ceiling. An 1/20 scale model of an openable space was built and measurement was carried out by varying the opened area of a ceiling. The most widely used room acoustic and design parameters, RT, EDT, and D50 were investigated. The results suggest that the use of RT as an acoustic design parameter may not be proper in an openable space and further it is likely to mislead the initial acoustic design of such spaces. It is mainly due to the characteristics of RT in which non-exponential decay processes are linearly fitted. Early decay times were found to be decreased in proportion to increaing the ratio of opened area. D50, an index of speech intelligibility, was effectively shows the influence of openings on the acoustics. It is also found that EDT and D50 at the seats, not directly exposed to the opened part of a ceiling, were almost linearly decreased in proportion to the ratio of opened area, while little influence was found for the opening ratio larger than 40% at the directly exposed seats to the opened part of a ceiling.

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