• Title/Summary/Keyword: in vitro release

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Effects of Allergy Related Drugs on Rat Peritioneal Mast Cells in Hyaluronidase Activity and Histamine Release (수종의 알레르기 관련 약물이 흰쥐의 복강내 비만세포에서 Hyaluronidase 및 히스타민 유리에 미치는 영향)

  • Yoo, Shin-Ae;Kim, Ku-Ja;Hah, Jong-Sik
    • The Korean Journal of Physiology
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    • v.22 no.2
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    • pp.259-272
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    • 1988
  • Type I allergic reaction and it's related clinical manifestations are known to occur by the effects of various chemical mediators. These chemical mediators are released from circulating basophils and tissue mast cells, which become 'sensitized' through the binding of antigens and antibodies of the IgE type to their cell surface receptors. Efforts to elucidate the mechanism of the release of these mediators, especially that of histamine, have been persued for years. The mechanism is not yet clarified at the present time. Recent reports of hyaluronidase, an enzyme known to be involved in the tissue inflammatory process, as possible participant in type I allergic reaction, initiated this study. Relationships between the hyaluronidase activity and histamine release from the sensitized rat peritoneal mast cells were investigated. Also anti-allergic agents, tranilast and disodium cromoglycate, along with known histamine releasers, morphine and compound 48/80, were used to observe the inhibitory and stimulatory effects of these substances on the hyaluronidase activity as well as histamine release from the rat mast cells. The results obtained are summarized as follows: 1) Hyaluronidase activity and histamine release from sensitiaed rat peritoneal mast cells started to increase on the 4th day of postsensitization. Hyaluronidase activity reached it's peak value on the 7th day of postsensitization and that of histamine release on the 14th day of postsensitization. 2) Hyaluronidase activity and histamine release from sensitized rat peritoneal mast cells, pre-treated with tranilast revealed significant decrease in comparison with those of non-treated cells. 3) Hyaluronidase activity and histamine release from sensitized rat peritoneal mast cells, pre-treated with tranilast, followed by morphine injection, revealed significant increase in comparison with those of tranilast treated cells. 4) In vitro study of hyaluronidase activity and histamine release from un-sensitized rat peritoneal mast cells, using morphine and compound 48/80 as activators, revealed significant increase compared to those of non-activator used cells. 5) In vitro study of hyaluronidase activity and histamine release from un-sensitized rat peritoneal mast cells, pre-treated with tranilast and disodium cromoglycate, using confound 48/80 and morphine as activators revealed significant decrease in comparison with those of tranilast and disodium cromoglycate treated cells. From above results, participation of enzyme hyaluronidase in the process of histamine release from sensitized rat pertioneal mast cells, could be suggested. It was also quite evident that the clinically used anti-allergic agents, tranilast and disodium cromoglycate, have significant inhibitory function on the hyaluronidase activity and histamine release from sensitized rat peritoneal mast cells, while morphine significantly increased the hyaluronidase activity and histamine release from sensitized rat peritoneal mast cells.

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Injectable Sustained Release Gel as a Local Drug Delivery for Periodontal Diseases (치주질환치료를 위한 국소적용 서방출성 리오겔)

  • Kim, Ki-jun;Shin, Young-hee
    • YAKHAK HOEJI
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    • v.60 no.1
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    • pp.46-50
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    • 2016
  • The purpose of this study was the development of sustained-release lyogel of chlorhexidine in the treatment of periodontal diseases. A sustained-release chlorhexidine lyogel (CHX-G) was formulated, based on Eudragit$^{(R)}$ (1~3%), polyvinyl pyrrolidone (PVP) (0~10%), triacetin (20~40%), hydroxy ethyl cellulose (HEC) (1%) and glycerin. In vitro studies were performed to determine the release rate of chlorhexidine from CHX-Gs using dialysis tube. Our results suggest that the release rate of chlorhexidine from lyogel could be controlled by changing the lyogel compositions.

Effect of Intermittent Versus Continuous Infusion of Progesterone on LHRH Release In Viuo from the Rat Mediobasal Hypothalamus

  • 김경진
    • The Korean Journal of Zoology
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    • v.32 no.4
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    • pp.329-338
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    • 1989
  • Present study examined the effect of intermittent versus continuous infusion of progesterone(P) on LHRH release in uiuo from the mediobasal hvpothalamus of ovariectomiEed, estradiol-primed adult rats bearing push-pull cannulae. Three experimental groups were studied: 1) control (perfusion medium only),2) intermittent perfusion of P (10-min on,20-min off, and 3) continuous perfusion of p. p (10 ng/mll was directly infused into the MBH following a 3 hr basal collection. Perfusates were collected at 10 min intents린s on ice and LHRH release was measured by LHRH radioimmunoassav. Cycle detector analysis revealed that the spontaneous HRH output in the control group was pulsatile over a 7 hr push-pull perfusion period. The mean basal LHRH release, pulse amplitude and pl서se period were 0.68 $\pm$ 0.03 ps110 min, 1.15 $\pm$0.08 pg and 60 $\pm$ 9 min, respectivelv. Intermi구eat perfusion of P clearly stimulated the mean LHRH release (pre-P vs post-P: 1.14 $\pm$ 0.18 vs 1.99 $\pm$ 0.53 pg) without changes in LHRH pulse frequency. In contrast to intermittent infusion of p, continuous administration of P faithed to modify LHRH release, since the mean LHRH release and pulse amplitude between pre-P and post-P perfusion urere similar. The in vitro study clearly showed that intermittent, but not continuous administration of P is effective in stimulating LHRH release. Therefore, it appears that rhythmic secretion of P mal be the erective signal for activating the neural LHRH apparatus.

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A Release Test for Gels Containing Ketoprofen (겔제제로부터 케토프로펜의 방출특성 시험법)

  • Kim, Ho-Jeong;Yun, Mi-Ok;Lee, Su-Jung;Choi, Hyun-Chul;Kim, Ji-Young;Kim, In-Wha;Shim, Chang-Koo;Kang, Shin-Jung
    • Journal of Pharmaceutical Investigation
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    • v.32 no.2
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    • pp.103-106
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    • 2002
  • A method that describes the determination of the in vitro release of ketoprofen from gels was suggested. The experimental system of the method consists of a Franz diffusion cell, which contains a pH 7.4 phosphate buffer as a receptor medium, and a $70\;{\mu}m$ mesh woven nylon membrane as a diffusion barrier. Under the given condition of the system, the diffusion of ketoprofen across the membrane was rapid enough that the apparent release profile of ketoprofen obtained from the present method could represent the release of the drug from gel preparations. The release of ketoprofen in the present method was reproducible, and the rate increased in proportion to the concentration of ketoprofen in the gel. These suggest that the present method is applicable to the quality evaluation of gel preparations containing ketoprofen.

Neuroendocrine Study of the Korean Native Cattle: Pulsatile LHRH Release from Hypothalamic Tissues Superfused in vitor (한우의 신경내분비학적 연구 : 시상하부의 체외배양 조직에서 맥동적 LHRH분비 양상에 관하여)

  • 김경진;유선경;안혜영;이병주;강해묵;조완규
    • The Korean Journal of Zoology
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    • v.32 no.3
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    • pp.275-280
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    • 1989
  • Present study examined the endogenous release of luteinizing hormone releasing hormone (LHRH) from superiused hypothalamic sBces derived from Korean native cattie (KNC). In addition, the in vitro secretory pattern of LHRH release in '(NC was compared with that in imported cattle such as Holstein cow. The median eminences (ME) of hypothalamic tissues were disseded out, sliced and quici'ly placed in ice-cold superfilsion chamber. Superhision chambers containing ME slices were maintained in a constant temperature water-bath at 37$^{\circ}C$. Effluents were colleded on ice at 10 min intervals for a 4 hr superfusion period, and kept -2$0^{\circ}C$ prior to LHRH radloimmunoassay. LHRH release was analyzed by the PULSAR algorithm. The spontaneous release of LHRH from both cows was episodic during a 4 hr superhision period. The mean LHRH release, pulse amplitude and pulse interval m KNC were 11.08 $\pm$ 1.50 pg/min/mg x 10-$^2$, 21.43 1 7.28 pg/mg x 10-$^2$, and 39.42 $\pm$ 3.08 min, which were quite similar to those observed in Holstein cows. The basic charaderistics of the LHRH pulse generator of '(NC appears important for a better understanding about the endocrine function of KNC.

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Ginsenoside Rg1 Stimulates Nitric Oxide Release in Pulmonary Artery Endothelial Cells in Culture

  • Kim, Hye-Young
    • BMB Reports
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    • v.28 no.4
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    • pp.301-305
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    • 1995
  • Considering the stimulatory effects of ginsenosides from Panax ginseng C. A. Meyer on the release of nitric oxide from bovine aortic endothelial cells in vitro and vasodilatation of rabbit pulmonary artery in vivo, the present study is designed to investigate the mechanism of nitric oxide release by ginsenosides in calf pulmonary artery endothelial cells, Nitric oxide release was determined in endothelial cells treated with ginsenosides and compared with those of the receptor-dependent agonists, bradykinin and ADP and the receptor-independent calcium ionophore $A_{23187}$. The results showed that total saponin and ginsenoside $Rg_1$, not $Rb_1$, stimulated nitric oxide release measured as conversion to L-citrulline. The nitric oxide releasing properties of total saponin and ginsenoside $Rg_1$ were different; total saponin stimulated only conversion to L-citrulline, like $A_{23187}$, while ginsenoside $Rg_1$ stimulated both L-arginine transport and conversion to L-citrulline, as bradykinin or ADP did.

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Preparation of BCNU-loaded PLGA Wafers and In Vitro Release Behavior (BCNU 함유 PLGA 웨이퍼의 제조와 생체외 방출거동)

  • 성하수;문대식;강길선;이정식;이해방
    • Polymer(Korea)
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    • v.26 no.1
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    • pp.128-138
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    • 2002
  • 1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU, Carmustine)-loaded poly(D, L-lactide-co-glycolide) (PLGA, lactide/glycolide mole ratio 75 : 25) microparticles were prepared and fabricated into wafers in an attempt to study the possibility for the treatment of malignant glioma by direct inserting the wafers to the tumor or the cavity remained after surgical resection of the tumor. SEM observation of the microparticles prepared by spray drying method revealed that the microparticles were spherical, i. e. microspheres. Significant reduction of the crystallinity of BCNU encapsulated in PLGA was confirmed by X-ray diffraction and differential scanning calorimetry analyses of the BCNU-loaded PLGA microparticles. Release pattern of BCNU was dependent on several preparation parameters, such as the molecular weight and concentration of PLGA, and initial BCNU loading amount, etc. In vitro release of BCNU was prolonged over 8 weeks with close to zero-order release pattern after initial burst effect. Observations of morphological change of wafers and pH change of release media during release test period confirmed that hydration and degradation of PLGA would be facilitated with an increase of BCNU-loading amount.

The Relationship of in vitro Dissolution and Intestinal Membrane Permeability with in vivo Bioavailability (시험관내 용출 및 장관막 투과도와 생체이용률과의 상관성)

  • 서수경;손수정;박인숙;최기환;김순선;유태무;조혜영;이용복;김동섭
    • YAKHAK HOEJI
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    • v.44 no.5
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    • pp.424-431
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    • 2000
  • A biopharmaceutics drug classification system for correlation between in vitro dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and extent of drug absorption. The objective of this study was to assess whether in vitro dissolution profiles of immediate-release beta-blocker tablets can be correlated with intestinal membrane permeability and/or in vivo bioavailability In vitro dissolution of the beta-blocker tablets was examined using KP VII Apparatus II methods at various pH. Intestinal membrane permeability was determined in vitro using the diffusion chamber method. Bioavailablity parameters were cited from literatures. The dissolution profiles did not accurately represent the in vivo bioavailablity However there were good correlations between intestinal membrane permeability and log P (noctanol/buffer). The correlations obtained in this study indicated that in vitro diffusion chamber method could be used to predict intestinal absorption in vivo.

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Drug Release Characteristics of Biodegradable Polymers for Stent Coating (스텐트 코팅용 생분해성 고분자의 약물 방출 특성)

  • 강혜수;김진설;김동운;강병철;이봉희;김범수
    • KSBB Journal
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    • v.18 no.2
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    • pp.107-110
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    • 2003
  • Biodegradable polymers, poly(lactic-co-glycolic acid) (PLGA), poly(3-hydroxybutyrate) (PHB), and medium chain length polyhydroxyalkanoates (MCL-PHA) containing rose bengal (model drug) were coated onto the surface of stainless steel (stent materials) and their in vitro release characteristics were investigated. Drug release increased with; decreasing PLGA concentration, increasing rose bengal concentration, and Increasing dip-coating duration. The order of drug release from the polymer coating was: PHB > PLGA > MCL-PHA. These results suggest that drug release can be controlled by: changing the concentration and type of polymer, the drug concentration, and the dip-coating duration.

Effects of Polyurethane Coated Urea Supplement on In vitro Ruminal Fermentation, Ammonia Release Dynamics and Lactating Performance of Holstein Dairy Cows Fed a Steam-flaked Corn-based Diet

  • Xin, H.S.;Schaefer, D.M.;Liu, Q.P.;Axe, D.E.;Meng, Q.X.
    • Asian-Australasian Journal of Animal Sciences
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    • v.23 no.4
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    • pp.491-500
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    • 2010
  • Three experiments were conducted to investigate the effects of polyurethane coated urea on in vitro ruminal fermentation, ammonia release dynamics and lactating performance of Holstein dairy cows fed a steam-flaked corn-based diet. In Exp. 1, a dual-flow continuous culture was run to investigate the effect of polyurethane coated urea on nutrient digestibility, rumen fermentation parameters and microbial efficiency. Three treatment diets with isonitrogenous contents (13.0% CP) were prepared: i) feedgrade urea (FGU) diet; ii) polyurethane coated urea (PCU) diet; and iii) isolated soy protein (ISP) diet. Each of the diets consisted of 40% steam-flaked corn meal, 58.5% forages and 1.5% different sources of nitrogen. PCU and FGU diets had significantly lower digestibility of NDF and ADF (p<0.01) than the ISP diet. Nitrogen source had no significant effect (p = 0.62) on CP digestibility. The microbial efficiency (expressed as grams of microbial N/kg organic matter truly digested (OMTD)) in vitro of the PCU diet (13.0 g N/kg OMTD) was significantly higher than the FGU diet (11.3 g N/kg OMTD), but comparable with the ISP diet (14.7 g N/kg OMTD). Exp. 2, an in vitro ruminal fermentation experiment, was conducted to determine the ammonia release dynamics during an 8 h ruminal fermentation. Three treatment diets were based on steam-flaked corn diets commonly fed to lactating cows in China, in which FGU, PCU or soybean meal (SBM) was added to provide 10% of total dietary N. In vitro $NH_3-N$ concentrations were lower (p<0.05) for the PCU diet than the FGU diet, but similar to that for the SBM diet at all time points. In Exp. 3, a lactation trial was performed using 24 lactating Holstein cows to compare the lactating performance and blood urea nitrogen (BUN) concentrations when cows were fed PCU, FGU and SBM diets. Cows consuming the PCU diet had approximately 12.8% more (p = 0.02) dietary dry matter intake than those consuming the FGU diet. Cows fed the PCU diet had higher milk protein content (3.16% vs. 2.94%) and lower milk urea nitrogen (MUN) concentration (13.0 mg/dl vs. 14.4 mg/dl) than those fed the FGU diet. Blood urea nitrogen (BUN) concentration was significantly lower for cows fed the PCU (16.7 mg/dl) and SBM (16.4 mg/dl) diets than the FGU (18.7 mg/dl) diet. Cows fed the PCU diet had less surplus ruminal N than those fed the FGU diet and produced a comparable lactation performance to the SBM diet, suggesting that polyurethane coated urea can partially substitute soybean meal in the dairy cow diet without impairing lactation performance.