• Title/Summary/Keyword: sustained-releasing

검색결과 29건 처리시간 0.028초

Induction of fertile estrus without the use of steroid hormones in seasonally anestrous Suffolk ewes

  • Miguel-Cruz, Erika Elizabeth;Mejia-Villanueva, Octavio;Zarco, Luis
    • Asian-Australasian Journal of Animal Sciences
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    • 제32권11호
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    • pp.1673-1685
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    • 2019
  • Objective: To evaluate the efficacy of treatments based on gonadotrophin-releasing hormone (GnRH), GnRH-prostaglandin $F2{\alpha}$ ($PGF2{\alpha}$), and/or intense exposure to novel rams to induce fertile estrus without the use of steroid hormones in seasonally anestrous Suffolk ewes. Methods: In the first experiment, ewes were treated with one injection of GnRH, two injections of GnRH administered 7 days apart, or a sequence of GnRH-$PGF2{\alpha}$-GnRH (GPG). In the second experiment anestrous ewes were exposed, for 36 days starting on the day of weaning, to groups of four rams of three different breeds that were alternated every day. Besides exposure to the male effect (ME), the ewes were injected with saline solution (ME group, n = 20), with GnRH (ME-GnRH group, n = 20) or with a sequence of GnRH-$PGF2{\alpha}$-GnRH (ME-GPG group, n = 20). The rams used for male-effect were fitted with aprons to prevent mating, and ewes detected in estrus were bred to selected fertile rams. Ovarian activity was monitored by progesterone determinations in both experiments. Results: In the first experiment sustained induction of ovarian activity was not achieved and no ewe was detected in estrus. In the second experiment induction of sustained ovarian activity was achieved in all groups. Most of the ewes were detected in estrus, 76.7% of the ewes were mated during a 36-d breeding period and 71.7% of all the ewes became pregnant during that period. No significant differences between groups were found for any of these variables. However, estrus detection efficiency was higher in the ME-GnRH group than in the ME group (p<0.05). Conclusion: An intense male-effect, that included the continuous presence and frequent alternation of several rams of different breeds, was sufficient to induce ovarian activity and fertile estrus in Suffolk ewes during the period of deep anestrus without the use of hormones, although addition of GnRH improved the efficiency of estrus detection.

Contractile and Electrical Responses of Guinea-pig Gastric Smooth Muscle to Bradykinin

  • Kim, Chul-Soo;Jun, Jae-Yeoul;Kim, Sung-Joon;So, In-Suk;Kim, Ki-Whan
    • The Korean Journal of Physiology
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    • 제29권2호
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    • pp.233-241
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    • 1995
  • The nonapeptide bradykinin has been shown to exhibit an array of biological activities including relaxation/contraction of various smooth muscles. In order to investigate the effects of bradykinin on the contractility and the electrical activity of antral circular muscle of guinea-pig stomach, the isometric contraction and membrane potential were recorded. Also, using standard patch clamp technique, the $Ca^{2+}-activated$ K currents were recorded to observe the change in cytosolic $Ca^{2+}$ concentration. $0.4 {\mu}M$ bradykinin induced a triphasic contractile response (transient contraction-transient relaxation-sustained contraction) and this response was unaffected by pretreatment with neural blockers (tetrodotoxin, atropine and guanethidine) or with apamin. Bradykinin induced hyperpolarization of resting membrane potential and enhanced the amplitude of slow waves and spike potentials. The enhancement of spike potentials was blocked by neural blockers. Both the bradykinin-induced contractions and changes in membrane potential were reversed by the selective $B_2$-receptor antagonist $(N{\alpha}-adamantaneacetyl-_{D}-Arg-[Hyp, Thy,_{D}-Phe]-bradykinin)$. In whole-cell patch clamp experiment, we held the membrane potential at -20 mV and spontaneous and transient changes of Ca-activated K currents were recorded. Bradykinin induced a large transient outward current, consistent with a calcium-releasing action of bradykinin front the intracellular calcium pool, because such change was blocked by pretreatment with caffeine. Bradykinin-induced contraction was also blocked by pretreatment with caffeine. From these results, it is suggested that bradykinin induces a calciumrelease and contraction through the $B_{2}$ receptor of guinea-pig gastric smooth muscle. Enhancement of slow wave activity is an indirect action of bradykinin through enteric nerve cells embedded in muscle strip.

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Comparative Bioavailability of Ipriflavone by Pharmaceutical Preparation Types (제제헝태에 따른 이프리플라본의 생체이용률 비교)

  • Jeong, Je-Kyo;Khang, Gil-Son;Rhee, John M.;Shin, Ho-Chul;Lee, Hai-Bang
    • Journal of Pharmaceutical Investigation
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    • 제30권1호
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    • pp.21-26
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    • 2000
  • Bioavailability of ipriflavone (3-phenyl-7-isopropoxy-4H-I-benzopyran-4-one, IP), an antiosteoporotic drug with poor water-solubility, was studied for various types of pharmaceutical preparation in SD rats. The IP preparation types included (1) intact IP, (2) freezer milled IP (FIP), (3) freezer milled IP physically mixed with freezer milled poly-N-vinylpyrrolidone (PVP) (FIP+FPVP) and (4) spray-dried IP with PVP (SIP). Upon oral administration, SIP showed significantly higher absorption and elimination half-lives and the lag time $(t_{lag})$ than those of FIP+FPVP (approximately 2-fold). These results may be due to a sustained releasing effect of IP in the gastrointestinal tract by spray-drying with PVP. The $C_{max}$ of SIP was about 2 and 10 times higher than those of FIP+FPVP and FIP, respectively. The AUC of SIP was about 6 times higher than that of FIP+FPVP and 60 times that of FIP. Scanning electron microscopy (SEM) showed that SIP consisted of the finest particle size and minimal aggregation than other IP preparations. It is concluded that the IP formula prepared by the spray-drying method with PVP is the most effective approach to the improvement of bioavailability of IP.

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Effect of PNF Leg Flexion Pattern on Muscle Activity of Ipsilateral Trunk and Leg with and without Abdominal Drawing-in Maneuver (PNF 다리 굽힘 패턴 시 복부 드로잉-인 기법 동시적용이 동측 몸통과 다리의 근활성도에 미치는 효과)

  • Ahn, Su-Hong;Lee, Su-Kyong;Jo, Hyun-Dai
    • PNF and Movement
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    • 제18권1호
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    • pp.35-44
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    • 2020
  • Purpose: The purpose of this study was to investigate the effect of the simultaneous abdominal drawing-in maneuver (ADIM) on the muscle activity of the ipsilateral trunk and leg during proprioceptive neuromuscular facilitation (PNF) leg flexion, adduction, and external rotation with knee flexion (D1) patterns. Methods: The participants were 20 healthy adult males and females (18 males and 2 females). The maneuvers were performed by a physical therapist who fully understands the PNF leg patterns (D1) and their application in clinical practice. The participants were trained and allowed to practice for 15 minutes prior to applying ADIM, to ensure adequate learning as evidenced by the pressure biofeedback unit. In this study, we measured the muscle activity of the trunk and leg when the PNF leg pattern (D1) was performed by the physical therapist either sustaining or releasing the ADIM. Muscle activity was measured on the right transverse abdominis muscle (TRA), the external abdominal oblique muscle (EO), the internal abdominal oblique muscle (IO), the erector spinae muscle (ES), the vastus medialis oblique muscle (VMO), the vastus lateralis oblique muscle (VLO), and the tibialis anterior muscle (TA) and compared using the mean values from averaging three repeated measurements. Results: The muscle activity of the transversus abdominis, the external abdominal oblique, the internal abdominal oblique, the vastus medialis oblique, and the vastus lateralis oblique was significantly greater (p < 0.05), and the muscle activity of the erector spinae was significantly less (p < 0.05) during PNF leg pattern (D1) when the ADIM contraction was sustained compared to when it was not. Conclusion: These results suggest that sustaining ADIM during PNF leg pattern (D1) training increases the trunk and leg muscle activity, resulting in more effective training.

Algorithms for Determining Korea Meteorological Administration (KMA)'s Official Typhoon Best Tracks in the National Typhoon Center (기상청 국가태풍센터의 태풍 베스트트랙 생산체계 소개)

  • Kim, Jinyeon;Hwang, Seung-On;Kim, Seong-Su;Oh, Imyong;Ham, Dong-Ju
    • Atmosphere
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    • 제32권4호
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    • pp.381-394
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    • 2022
  • The Korea Meteorological Administration (KMA) National Typhoon Center has been officially releasing reanalyzed best tracks for the previous year's northwest Pacific typhoons since 2015. However, while most typhoon researchers are aware of the data released by other institutions, such as the Joint Typhoon Warning Center (JTWC) and the Regional Specialized Meteorological Center (RSMC) Tokyo, they are often unfamiliar with the KMA products. In this technical note, we describe the best track data released by KMA, and the algorithms that are used to generate it. We hope that this will increase the usefulness of the data to typhoon researchers, and help raise awareness of the product. The best track reanalysis process is initiated when the necessary database of observations-which includes satellite, synoptic, ocean, and radar observations-has become complete for the required year. Three categories of best track information-position (track), intensity (maximum sustained winds and central pressure), and size (radii of high-wind areas)-are estimated based on scientific processes. These estimates are then examined by typhoon forecasters and other internal and external experts, and issued as an official product when final approval has been given.

Swelling and Drug Release Characteristics of PVP Hydrogel Polymerized by $\gamma$-Irradiation Method (김마선 조사법으로 합성한 PVP하이드로겔의 팽윤과 약물방출특성)

  • 심창구;오정숙;신병철
    • YAKHAK HOEJI
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    • 제37권5호
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    • pp.511-519
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    • 1993
  • The short and variabke transit of drug throught GI tracj and the inter-and intra-subject variations of the transit restrict the sustained drug absorption after oral adminstration. These restrictions may be solved by retaining the dosage forms in the stomach. Then the dosage form will act as a platform which releases the drug slowly and makes the GI absorption occur for a long time. In this study, as the platforms, PVP hydrogels were synthesized by chemical and y-irradiation method in the cylindrical test tube. The chemical method means the synthesis of the hydrogel by heating the mixed solution of N-vinyl-2-pyrrolidone [monomer], acrylated albumin [crosslinking agent], 2, 2'-agobis(2-methylpropionitrile) [initiator] and proxyphylline [drug] at $65^{\circ}C$ for 5 hr. The $\gamma$-irradiation method means the synthesis of the hydrogel by irradiation with $^{60}$ Co $\gamma$-ray of the mixed solution of the monomer, acrylated albumin, and flurbiprofen [drug] at room temperature with total 0.2 Mrad for 3 hr. Our intention is to design the hydrogel tablet (diameter : 1.20 cm, thickness : 0.60 cm) which swells in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the period of drug release. After releasing drug, the hydrogel should be degraded by the enzymeatic digestion in the stomach, or by hydrolysis and eventually solubilized. Thus, in votro tests were performed to examine the factors that affect swelling and drug release from the PVP hydrogels. Experimental results show that the hydrogels swell to a size larger than the diameter of the pylorus(l.3$\pm$0.7 cm) and the hydrogel prepared by the chemical method is digested by pepsin. But the hydrogel prepared by the $\gamma$-irradiation method was not digested by the pepsin and just collapsed with time. Thus, the swelling of the hydrogel synthesized by $\gamma$-irradiation was independent albumin acrylation time and pepsin concentration. But drug content and radiation dose affected the swelling and drug release kinetics of the hydrogel. Drug release from the hydrigels was prolonged up to about 24 hr. Therefore, it was concluded that by adjusting these factors, the albumin-crosslinked PVP hydrogel synthesized by $\gamma$-irradiation method is expected to be retained in the stomach for up to 60hr and be a potential platform of drugs for long-term GI absorption.

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Preparation and Characterization of Deoxycholic Acid-Conjugated Low Molecular Weight Water-Soluble Chitosan Nanoparticles for Hydrophobic Antifungal Agent Carrier (소수성 항진균제 전달체로 응용하기 위한 데옥시콜릭산이 결합된 저분자량 수용성 키토산 나노입자의 제조와 특성)

  • Choi, Chang-Yong;Jung, Hyun;Nam, Joung-Pyo;Park, Yoon-Kyung;Jang, Mi-Kyeong;Nah, Jae-Woon
    • Polymer(Korea)
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    • 제33권4호
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    • pp.389-395
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    • 2009
  • To develop the carrier of hydrophobic antifungal agents based on low molecular weight water-soluble chitosan (LMWSC), LMWSC was chemically modified with deoxycholic acid (DA) which is one of the bile acid as a hydrophobic group. The nanoparticles (WSCDA) using DA conjugated LMWSC were characterized using dynamic light scattering (DLS) and transmittance electron microscope (TEM). The particle size of WSCDA ranged from 250 to 350 nm and increased with the number of DA substitution. The loaded itraconazole as an antifungal agent WSCDA nanoparticles (WSCDA-ITCN) were prepared by solvent evaporation method. The drug content and the loading efficiency were investigated approximately $9{\sim}10%$ and $61{\sim}68%$ by UV spectrophotometer, respectively. The release of drug from nanoparticles was slow and showed sustained release characteristics. Based on the results of release study that the higher DA contents in WSCDA, the slower the releasing rate, the WSCDA-ITCN could be used as an excellent antifungal agent.

Effect of rice seed dressing with imidacloprid WS on early occurring rice insect pests (본답 초기해충의 생력방제를 위한 imidacloprid의 종자분의 효과)

  • Choi, Byung-Ryul;Yoo, Jae-Ki;Lee, Sang-Guei;Lee, Jeong-Oon
    • The Korean Journal of Pesticide Science
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    • 제2권1호
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    • pp.85-90
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    • 1998
  • A series of experiments were carried out to determine the effect of seed dressing application of chemicals on the early occurring rice insect pests. The number of small brown planthopper adults per 3hills in seed-dressing plot of Imidacloprid WS (Im WS) was 1.6 and its control efficacy was over 90%, compared with that of untreated plot. Rice water weevil was observed in the density of 8.8 larvae per 5 hills seed-dressed Im WS plots(showing 95.5% of control efficacy). Control efficacy of Im WS and Im GR against adult weevils lasted for 26 days after treatment and was higher than that of Carbofuran GR. Rates of injured stems by rice stem maggot and injured leaves by rice leaf miner were 3% and 3.7% in Im WS treatment plot respectively. Seed germination rate after seed dressing with recommended dosage (3 g/seed kg) of Im WS was 71 % on the 1st day and increased on 5th day up to that of untreated seed. The residual amount of Im in seed dressing plot was 0.11 ppm in rice roots and 0.05 ppm in leaves on the 40th day after treatment. Residual effect of Im WSI sustained for 50 days with over 95% insecticidal effect for the rice water weevil and over 90% for the brown planthopper. Quantity of the chemical applied in the field was calculated as 0.084 kg a.i./ha in seed dressing and 0.3 kg a.i./ha in seed box treatment, respectively It took 1 hour to treat insecticide by seed dressing, 2.5 hours by seed box applying, and 3.6 hours by water surface releasing per 990 $m^2$.

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Studies on the Mechanism of Contraction by Substance P in Rabbit Ileum (Substance P에 의한 가토 회장평활근의 수축기전에 대한 연구)

  • Jo, Se-Hun;Jung, Jin-Sup;Lee, Sang-Ho
    • The Korean Journal of Physiology
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    • 제18권2호
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    • pp.151-162
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    • 1984
  • The mechanism of the contractile response of longitudial muscle of rabbit ileum to substance P (SP) has been investigated. The contractions in rabbit ileum under various conditions were recorded isometrically The following results were obtained. 1) The contractions by SP increased according to concentrations. SP·induced contraction was not sustained but faded rapidly at $10^{-7}M$. The response to the commutative addition of SP was decreased in comparison to the response to separate administration of each concentration . 2) The response to $10^{-8}M$ SP after 5 min application cf $10^{-7}M$ SP was increased with increasing the time interval between the administration of $10^{-7}$ and $10^{-8}M$ SP. 3) The treatment of rabbit ileum by $10^{-7}M$ SP for 5 min didn't decrease the response to $10^{-6}M$ acetylcholine. 4) $10^{-6}M$ atropine had no effect of the contractile response to $10^{-7}M$ SP. The response to $10^{-7}M$ SP was normal or subnormal in the presence of 3 mM tetraethylammonium(TEA). 5) 100k solution, $10^{-4}M$ ouabain, and Na-free solution inhibited the response to $10^{-8}M$ SP and 3 mM TEA completely, and to $10^{-7}M$ SP incompletely. 3 mM TEA induced a considerable contraction in K-free solution, but $10^{-8}M$ SP didn't induce the contraction. $10^{-6}M$ norepinephrine decreased the contractile responses to SP and TEA. 6) The contractile response to $10^{-7}M$ SP was dependent on the extracellular $Ca^{2+}$ concentrations to 1.8 mM. 7) The contractile response to $10^{-7}M$ SP remained 15% of the maximal response after bathing the ileum in a Ca-free solution for 2.5 min. 8) The responsiveness to SP was completely lost within 10 min of bathing in Ca-free solution, but was restored by the exposure to $Ca^{2+}$. The restorative effect of $Ca^{2+}$ depended on the concentration of $Ca^{2+}$, and on time for which the tissue exposed to this $Ca^{2+}$ concentration. These results suggest that there are two mechanisms of the action by which the low concentrations of substance P causes the contraction of intestinal smooth muscle: the reduction of K conductance and a mechanism dependent on the extracellular $Ca^{2+}$, and that high concentration of SP may elicit a contraction by releasing $Ca^{2+}$ from an intracellular store, which is not as sensitive to removal of extracellular $Ca^{2+}$ or as easily accessible to EGTA as the extracellular space of the muscle. The location of this store is not known; it may be associated with the internal side of the cell membrane.

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