• Title/Summary/Keyword: Release effect

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Studies on the Enzyme-releasing Mechanism of Aminoglycosides from Pancreas (Aminoglycosides의 취효소 분비항진기전에 관한 연구)

  • Shim, Ho-Shik;Kim, Kyung-Hwan;Hong, Sa-Suk
    • The Korean Journal of Pharmacology
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    • v.19 no.1
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    • pp.71-76
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    • 1983
  • Aminoglycoside antibiotics are reported to enhance the amylase release from isolated slices of pancreas in vitro and the mode of action of aminoglycosides on amylase release is considered different from those of acetylcholine or cholecystokinin(CCK), i.e., electronmicroscopically intact zymogen granules are appeared in the lumen of pancreatic acini by treatment of aminoglycosides. It is known that atropine blocks the secretagogue effect of acetylcholine, and phenoxybenzamine is reported to block the effects of CCK or its analogue caerulein. Present study was undertaken to investigate the mode of action of aminoglycosides on the amylase release using atropine, phenoxybenzamine and propranolol as a membrane stabilizing agent in slices of chicken pancreas. The results are summarized as follows : 1) Streptomycin and kanamycin increased the amylase release significantly from slices of chicken pancreas. 2) The effect of streptomycin was inhibited by atropine but not by phenoxybenzamine or propranolol. 3) The amylase release by acetylcholine was blocked by atropine tut the effect of cholecystokinin octapeptide(CCK-8) was not influenced by atropine, phenoxybenzamine or propranolol. 4) Pretreatment of streptomycin enhanced the secretagogue effect of acetylcholine or CCK-8. From these results it is suggested that amylase releasing effects of aminoglycosides are mediated in part by cholinergic stimulation and in part by membrane alteration and these effects are enhanced by acetylcholine or cholecystokinin.

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Inclusion Complex of Analgesic and antiinflammatory Agents with Cyclodextrins (II) : Effect of $2-Hydroxypropyl-{\beta}-cyclodextrin$ on the Release of Ibuprofen Suppository (시클로덱스트린과 소염진통제간의 포접복합체에 관한 연구 (II) : 2-히드록시프로필-${\beta}$-시클로덱스트린이 이부프로펜 좌제의 방출에 미치는 영향)

  • Oh, In-Joon;Lee, Mi-Young;Lee, Yong-Bok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • v.27 no.3
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    • pp.165-171
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    • 1997
  • Ibuprofen, a nonsteroidal antiinflammatory, analgesic and antipyretic drug, has several limitations in clinical application because of low solubility in water and gastrointestinal irritation. Effect of ibuprofen/$2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP{\beta}CD)$ inclusion compound on release of suppository was investigated. Complex formation was confirmed by $^{1}H-\;and\;^{13}C-NMR$ spectroscopy. The release of ibuprofen from suppository base in vitro was significantly increased by the complexation with $HP{\beta}CD$. The release of ibuprofen from hydrophilic base was faster than that from hydrophobic base. In vivo studies, the release rate of ibuprofen from suppository was accelerated after rectal administration in complex form. This results suggested that ibuprofen/$HP{\beta}CD$ complex can be practically used for suppository to have faster effect of ibuprofen with reduced side effect.

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FURTHER PURIFIED GINSENG EXTRACT FRACTION (D-O-ANA) FOR INSULIN RELEASE AND ITS MODE OF ACTION COMPARED WITH THE ISOLATED RESIDUAL COMPONENTS (인삼성분 D-O-ANa이 인슐린 분비에 미치는 영향 및 작용기전에 관한연구)

  • KIMURA Masayasu;SUZUKI Jun;WAKI Isami;KIMURA Ikuko;TANAKA Osamu;MATSU-URA Hiromichi
    • Proceedings of the Ginseng society Conference
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    • 1984.09a
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    • pp.191-197
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    • 1984
  • A further purified fraction (D-O-ANa) was obtained from DPG 3-2 fraction of Ginseng Radix by complete removal of saponins, nucleosides, nucleic acid bases, amino acids, and sugars. D-O-ANa - induced insulin release was investigated to compare with that of DPG 3-2 and other isolated components. Among the sub fractions of DPG 3-2, D-O-ANa exhibited the most potent release of insulin with or without high concentrations of glucose, and it particularly enhanced the second phase of glucose-induced insulin release. DGP 3-2 potentiated significantly the glucose-induced insulin release from the isolated islets of diabetic mice at increasing concentrations of extracellular calcium ions (0.16 - 2.5 mM). A definite relationship was found between calcium $(^{45}Ca)$ uptake and insulin release. Ginsenoside $(G)-Rb_1\;and\;G-Rg_1$ did not enhance the glucose-induced insulin release. The effect of ginseng saponins was blocked by glucose (16.7 mM), being distinctly different from the glucose-potentiated effect of DPG 3-2. The insulin release effect of $G-Rg_1$ was unaffected by the presence or absence of extracellular $Ca^{2+}$ and theophylline. Adenosine also increased insulin release from isolated islets, but had no effect on perfused rat pancreas. Arginine stimulated insulin release less evidently than D-O-ANa, though arginineand adenosine-induced glucagon releases were more remarkable. In conclusion, D-O-ANa appears to be a major fraction in insulin release activity of ginseng and its mode of action may be related to $Ca^{2+}$ ion uptake. This physiological mechanism was distinct from that of the abnormal release induced by ginseng saponins.

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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
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    • v.35 no.6
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    • pp.453-460
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    • 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.

Effect of Crosslinking Agent Structure on Drug Release and Antibacterial Effect of Contact Lenses (교차결합제 구조가 콘택트렌즈의 약물용출 및 항균효과에 미치는 영향)

  • Lee, Pil-Heon;Lee, Hyun Mee
    • Journal of the Korean Chemical Society
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    • v.65 no.5
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    • pp.320-326
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    • 2021
  • This study investigated the effect of the structure of the crosslinking agent used in contact lens polymerization on the physical properties and drug dissolution of contact lenses.es Contact lenses were manufactured using 0.3% and 3% of 4 types of crosslinking agents, respectively, and ofloxacin was used as the drug. Contact lenses using hydrophilic crosslinking agents improved water contents and wettability, and the more hydrophilic functional groups, the greater the effect. Contact lenses with a high concentration of crosslinking agent had a low concentration of eluted drug and a longer release time. The cross-linking agent structure of contact lenses had an effect on improving the performance of contact lenses and controlling drug release.

Inhibitory Effect of Anaphylaxis by WK101 and Mechanism of Action (WK101에 의한 아나필락시의 억제효과와 작용기전)

  • 이영미;김형룡
    • YAKHAK HOEJI
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    • v.39 no.6
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    • pp.616-621
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    • 1995
  • The effect of WK101 on compound 48/80-induced anaphylaxis was studied in rat. WK101 was found to exhibit a inhibitory activity on the compound 48/80-induced anaphylaxis. WK101 also inhibited the serum histamine release induced in anaphylaxis by compound 48/80. The effect of WK101 on the histamine release from rat peritoneal mast cells was studied. WK101 ($10^{3}-1mg/ml$) inhibited the histamine release induced by compound 48/80($5{\;}\mu\textrm{g}/ml$) in rat peritoneal mast cells. To clarify the mechanism of these inhibitons, we investigated the effects of WK101 on cAMP and intracellular calcium content of rat peritoneal mast cell. The content of cAMP in mast cells, when WK101 was added, was increased transiently, and was significantly increased more 53 fold at 10 sec than that of basal cells. Moreover, WK101 inhibited intracellular calcium release induced by compoound 48/80. This results suggest that WK101 may be useful for the prevention and treatment of allergy-related disease.

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A Study on the PAS Release Therapy used by Myofascial Release (근막 이완술을 이용한 파스 이완술에 관한 고찰)

  • Park Ji-Whan
    • The Journal of Korean Physical Therapy
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    • v.11 no.3
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    • pp.107-113
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    • 1999
  • The purpose of study on the PAS release therapy used by myofascial release was to Introduce for clinical therapists whose want to relict pain on myofascia or soft tissue lesion patients by pas. According to review the earlier studies for a myofascial pain syndrome, myofascial release is not only to decrease muscle tone but also the effect of pas therapy has to facilitate a circulation of the human energy called Ki, so PAS release which was combined therapy pattern would be Possible relief Pain in the musculoskeletal lesion's Patients. Therefore I would be suggested to physical therapists in domestic the PAS release therapy used by myofascial release.

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Effect of Diethylphthalate on the Release of Salicylic Acid from Ethylcellulose Films (소수성 가소제 Diethylphthalate가 Ethylcellulose 필름으로부터의 살리씰산 방출에 미치는 영향)

  • 이승용;신상철;이민화;심창구
    • YAKHAK HOEJI
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    • v.28 no.3
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    • pp.169-177
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    • 1984
  • Release characteristics of salicylic acid from ethylcellulose(EC) films containing varying ratio of dieththylphthalate (DEP) were studied. Mathematical analysis of the release data showed that the release behavior actually conforms with the Higuchi's diffusion-controlled model. The release rate constants(k) were independent from the film thickness and the pH of release medium, but were proportional to the concentration of salicylic acid itself. The logarithm of the release rate constant (log k) increased as the concentration of DEP was increased. In conclusion, hydrophobic plastisizer DEP seemed to be very useful in controlling release rate constant of slightly soluble drugs as like salicylic acid without changing it's release characteristics.

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Effect of slow-release fertilizers on yield of chiness cabbage and spinash (비료의 시용이 배추와 시금치의 수량에 미치는 영향)

  • 완효성
    • Korean Journal of Organic Agriculture
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    • v.4 no.2
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    • pp.86-96
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    • 1995
  • This experiment was carried out to investigate the effect of slow-release fertilizers on yield of chinese cabbage and spinach. Fertilizers were treated with CDU, MEISTER, Jobi Gohyungbokhapbiryo, Kyungki Wonyebokbi 1ho, kyungkibokbi Nojeok, Kyungki Jeonjakgohyungbokbi, Traditional manuring, and No manuring. Yields of chinese cabbage were increased with slow-release fertilizers, and CDU was more effective to the head than to the out-leaf, especially. Spinach was increased with slow-release fertilizers, also. However, analysis of chemical components of plants and soil were no difference. It was very effective to increase yields of chinese cabbage and spinach, to reduce in number of supplementary manuring and laboring.

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One-zone heat release analysis for IDI diesel engine (IDI 디젤기관의 단일영역 열발생량 계산)

  • Lee, S.Y.;Kim, G.B.;Choi, S.H.;Jeon, C.H.;Chang, Y.J.;Chun, K.M.
    • Proceedings of the KSME Conference
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    • 2001.11b
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    • pp.830-836
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    • 2001
  • An one-zone heat release analysis was studied for a 4 cylinder indirect diesel engine. The object of the study is to calculate the heat release accurately including the effect of specific heat ratio, heat transfer and crevice volume and to find out combustion characteristics of an indirect diesel engine cosidering the effect of both pressure in the main and swirl chambers. The integrated gross heat release values were close to the measured fuel energy at various full load operating conditions.

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