• Title/Summary/Keyword: Release effect

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Effect of Hydrophilic Polymers on the Release of BCNU from BCNU-loaded PLGA Wafer (친수성 고분자가 BCNU 함유 PLGA 웨이퍼로부터 BCNU의 방출에 미치는 효과)

  • 안태군;강희정;문대식;이진수;성하수
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.670-679
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    • 2002
  • 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine) is one of the effective chemotherapeutic agents which has been used clinically for treating malignant glioma. Poly(D,L-lactide-co-glycolide) (PLGA, molecular weight: 20000 g/mole. mole ratio of lactide to glycolide 75 : 15) is a well known biodegradable polymer used as a drug carrier for drug delivery system. In this study, we investigated the BCNU release behaviour of BCNU-loaded PLGA wafers containing poly (N-vinylpyrrolidone) (PVP) or polyethyleneoxide (PEO) and the effect of hydrophilic polymers incoporated in the wafers. BCNU-loaded PLGA microparticles with or without hydrophilic polymers were prepared by a spray drying method and fabricated into wafers by direct compression. Encapsulation efficiency of BCNU-loaded PLGA microparticles containing PVP and PEO was 85 ∼ 97% and crystallinity of BCNU encapsulated in PLGA decreased significantly initial release amount and release rate of BCNU increased with the increasing PVP or PEO amount. Morphological change and mass loss of wafers during the release test were confirmed that hydration and degradation of PLGA would be facilitated with an increase of hydrophilic polymers.

Effect of Self-Myofascial Release on Body Composition, Vascular and Metabolic Functions in Obese Female College Students (자가근막이완 운동이 비만 여자대학생의 신체조성과 혈관 및 대사기능에 미치는 효과)

  • Lee, Jae-Hoon;Kim, Ji-Sun;Oh, Yoo-Seong
    • Journal of the Korean Applied Science and Technology
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    • v.37 no.4
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    • pp.769-777
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    • 2020
  • The purpose of this study was to investigate the effects of 8 weeks Self-Myofascial Release exercise on body composition, vascular and metabolic functions in obese female college students. The subjects were 19 obese female college students (n = 9) who were randomly assigned to an exercise group(n=9) and control group(n=9), with an exception of except 1 abandonment. The Self-Myofascial Release exercise group performed exercises twice a week for 8 weeks and for 40 minutes at one time using a foam roller, and the control group maintained normal life pattern for the same period. Body composition was measured by body weight, body fat percentage, vascular function was measured by pulse wave velocity(PWV), augmentation index(AIx), brachial artery vascular flow-mediated dilation(FMD), and metabolic function was measured by fasting glucose and triglyceride levels. The Self-Myofascial Release exercise with foam roller showed no significant effect on body weight and body fat percentage. The Self-Myofascial Release exercise with foam roller showed no significant effect on heart rate, FMD, PWV but, SBP, CSBP and AIx were significant decreased. The Self-Myofascial Release exercise with foam roller showed no significant effect on fasting glucose and triglyceride levels. In conclusion, 8-week Self-Myofascial Release exercise for obese female college students showed no significant effect on body composition and metabolic function, but improved SBP, CSBP and AIx levels significantly. Therefore, Self-Myofascial Release exercise will be an effective way to improve the vascular function of obese female college students.

Application of Dry Elixir System to Oriental Traditional Medicine: Taste Making of Peonjahwan by Coated Dry Elixir

  • Choi, Han-Gon;Kim, Chong-Kook
    • Archives of Pharmacal Research
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    • v.23 no.1
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    • pp.66-71
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    • 2000
  • Peonjahwan, an oriental traditional medicine composed of crude herbal drugs and animal tissues is bitter and poorly water-soluble. To mask the bitterness of peonjahwan and enhance the release of bilirubin, one of the crude active ingredients of peonjahwan, peonja dry elixir (PDE), was prepared using a spray-dryer after extracting the crude materials in ethanol-water solution. coated peonja dry elixir (CPDE) was then prepared by coating the PDE with Eudragit acrylic resin. Panel assessed bitterness and release test of bilirubin from PDE and CPDE were carried out and compared with peonjahwan alone. PDE was found to have little effect upon the reduction of the bitterness of peonjahwan. However, the bitterness of CPDE was found to reduce to 1/4 of that of peonjahwan due to the encapsulation of crude active ingredients by the dextrin and Eudragit shell (P<0.05). The release rate of bilirubin from PDE and CPDE for 60 min increased about 3.5- and 2.5-fold, respectively, compared to peonjahwan at pH 1.2. It is concluded that CPDE, which masked the bitterness of peonjahwan and enhanced the release of bilirubin, is a preferable delivery system for peonjahwan.

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Effect of Purified Green Tea Catechins on Cytosolic Phospholipase $A_2$ and Arachidonic Acid Release in Human Gastrointestinal Cancer Cell Lines

  • Hong, Jung-Il;Yang, Chung-S.
    • Food Science and Biotechnology
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    • v.15 no.5
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    • pp.799-804
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    • 2006
  • Ingestion of green tea has been shown to decrease prostaglandin $E_2$ levels in human colorectum, suggesting that tea constituents modulate arachidonic acid metabolism. In the present study, we investigated the effects of four purified green tea catechins, (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epigallocatechin-3-gallate (EGCG), and (-)-epicatechin-3-gallate (ECG), on the catalytic activity of cytosolic phospholipase $A_2$ ($cPLA_2$) and release of arachidonic acid and its metabolites from intact cells. At $50\;{\mu}M$, EGCG and ECG inhibited $cPLA_2$ activity by 19 and 37%, respectively, whereas EC and EGC were less effective. The inhibitory effects of these catechins on arachidonic acid metabolism in intact cells were much more pronounced. At $10\;{\mu}M$, EGCG and ECG inhibited the release of arachidonic acid and its metabolites by 50-70% in human colon adenocarcinoma cells (HT-29) and human esophageal squamous carcinoma cells (KYSE-190 and 450). EGCG and ECG also inhibited arachidonic acid release induced by A23187, a calcium ionophore, in both HT-29 and KYSE-450 cell lines by 30-50%. The inhibitory effects of green tea catechins on $cPLA_2$ and arachidonic acid release may provide a possible mechanism for the prevention of human gastrointestinal inflammation and cancers.

Inhibitory Effect of Clavicepitaceae on Serotonin Release out of Human Platelets and Human Platelet Aggregation

  • Cho, Hyun-Jeong;Ham, Hye-Seon;Lim, Chang-Ryul;Park, Sun-A;Kang, Hyo-Chan;Ju, Young-Cheol;Park, Hwa-Jin
    • Biomedical Science Letters
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    • v.10 no.1
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    • pp.9-13
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    • 2004
  • We have investigated the effects of hypha-water extracts (HWE), fruit body-water extracts (FWE) and cordycepin from Cordyceps militaris on serotonin release out of human platelets and human platelet aggregation. HWE and FWE inhibited the release of [$^3H$]-serotonin from human platelet stimulated by thrombin (2 U/ml) or collagen (20$\mu$g/ml) in a dose-dependent manner. Furthermore, cordycepin, a major component of Cordyceps militaris, inhibited the human platelet aggregation induced by collagen (10$\mu$g/ml) in a dose-dependent manner. These results suggest that cordycepin containing in HWE and FWE may inhibit the serotonin release by suppressing the collagen-induced human platelet aggregation. Accordingly, our data demonstrate that HWE and FWE containing much cordycepin might have antithrombotic and antimigrainous functions.

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A Novel In Situ Gel Formulation of Ranitidine for Oral Sustained Delivery

  • Xu, Haoping;Shi, Min;Liu, Ying;Jiang, Jinling;Ma, Tao
    • Biomolecules & Therapeutics
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    • v.22 no.2
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    • pp.161-165
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    • 2014
  • The main purpose of this study was to develop a novel, in situ gel system for sustained delivery of ranitidine hydrochloride. Ranitidine in situ gels at 0.2%, 0.5%, and 1.0% gellan gum concentration (w/v) were prepared, respectively, and characterized in terms of preparation, viscosity and in vitro release. The viscosity of the gellan gum formulations in solution increased with increasing concentrations of gellan gum. In vitro study showed that the release of ranitidine from these gels was characterized by an initial phase of high release (burst effect) and translated to the second phase of moderate release. Single photon emission computing tomography technique was used to evaluate the stomach residence time of gel containing $^{99m}Tc$ tracer. The animal experiment suggested in situ gel had feasibility of forming gels in stomach and sustained the ranitidine release from the gels over the period of at least 8 h. In conclusion, the in situ gel system is a promising approach for the oral delivery of ranitidine for the therapeutic effects improvement.

Effect of pH-dependent Solubility on Release Behavior of Alginate-Chitosan Blend Containing Activated Carbon

  • Oh, Ae-Ri;Jin, Dong-Hwee;Yun, Ju-Mi;Lee, Young-Seak;Kim, Hyung-Il
    • Carbon letters
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    • v.10 no.3
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    • pp.208-212
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    • 2009
  • Alginate-chitosan blend containing coconut-based activated carbon was prepared as a drug delivery carrier in order to improve the loading and releasing capacity of the drug. The activated carbon was incorporated as effective adsorbent for drug due to the extremely high surface area and pore volume, high adsorption capacity, micro porous structure and specific surface activity. Alginate-chitosan blend containing coconut-based activated carbon showed the sustained release for a longer period. Alginate-chitosan blend showed higher release of drug as the pH increased and higher release of drug as the content of chitosan decreased due to the pH-dependent solubility of blend components.

Cross-Linked Starch Microspheres: Effect of Cross-Linking Condition on the Microsphere Characteristics

  • Atyabi, Fatemeh;Manoochehri, Saeed;Moghadam, Shadi H.;Dinarvand, Rassoul
    • Archives of Pharmacal Research
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    • v.29 no.12
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    • pp.1179-1186
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    • 2006
  • Cross-linked starch microspheres were prepared using different kinds of cross-linking agents. The influence of several parameters on morphology, size, swelling ratio and drug release rate from these microspheres were evaluated. These parameters included cross-linker type, concentration and the duration of cross-linking reaction. Microspheres cross-linked with glutaraldehyde had smooth surface compared with those prepared with epichlorhydrine or formaldehyde. The particle size increased with increasing the cross-linking time and increasing the drug loading. Swelling ratio of the particles was a function of cross-linker type but not the concentration or time of cross-linking. Drug release from starch microspheres was measured in phosphate buffer and also in phosphate buffer containing a-amylase. Results showed that microspheres cross-linked with epichlorhydrine released all their drug content in the first 30 minutes. However, cross-linking of the starch microspheres with glutaraldehyde or formaldehyde decreased drug release rate. SEM and drug release studies showed that cross-linked starch microspheres were susceptible to the enzymatic degradation under the influence of alpha-amylase. Changing the enzyme concentration from 5000 to 10,000 IU/L, increased drug release rate but higher concentration of enzyme (20,000 IU/L) caused no more acceleration.

Effects of Traditional Drugs on $CCl_4-induced$ Cytotoxicity in Primary Cultured Rat Hepatocytes (수종의 전통약제가 일차 배양 간세포에서 $CCl_4$ 유발 세포독성에 미치는 영향)

  • Kim, Young-Sook;Park, Ki-Hyun
    • Korean Journal of Pharmacognosy
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    • v.25 no.4 s.99
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    • pp.388-394
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    • 1994
  • 80% Methanol extracts of 44 traditional drugs used for the treatment of liver diseases or tonic effects were screened for anti-hepatotoxic activity by in vitro assay using $CCl_4-induced$ cytotoxicity in primary cultured rat hepatocytes. $CCl_4-induced$ cytotoxicity was evaluated by determination of LDH, GOT or GPT activity in the medium. Rehmaniae Radix Preparata and Gelantina nigra inhibited the release of LDH, GOT or GPT from $CCl_4-treated$ hepatocytes. Gibotii Rhizoma and Eucommiae Cortex showed inhibitory effect on release of LDH from normal hepatocytes as well as $CCl_4-treated$ hepatocytes. Eucommiae Cortex and Lili Bulbus decreased release of GOT and LDH from normal hepatocytes, respectively. Astragali Radix inhibited release of GPT in $CCl_4-treated$ hepatocytes. Phlomidis Radix, Imperatae Rhizoma, Cistanchis Herba, Broussonetiae Fructus, Asparagi Tuber, Trigonellae Semen and Polgonati Rhizoma inhibited release of LDH from $CCl_4-treated$ hepatocytes. Among 44 traditional drugs, most of them released LDH, GOT or GPT at the dose of 1 mg/ml in normal hepatocytes, and Drynariae Rhizoma, Acanthopanacis Cortex, Longanae Arillus, Atratylodis Rhizoma and Ecliptae Herba increased $CCl_4-induced$ cytotoxicity.

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Effects of Socheongryongtang-ga-seoggo and Prescription D on Airway Mucin Secretion (소청룡탕가석고(小靑龍湯加石膏) 및 ${\ll}$석실비록${\gg}$소치법방(小治法方)이 호흡기 점액의 분비에 미치는 영향)

  • Kim, Ho;Seo, Un-Kyo
    • The Journal of Internal Korean Medicine
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    • v.27 no.4
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    • pp.895-904
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    • 2006
  • Objectives : In the present study, the author intended to investigate whether two oriental medical prescriptions named Socheongryongtang-ga-seoggo (SCTS) and Prescription D (P-D) significantly affect mucin release from cultured hamster tracheal surface epithelial (HTSE) cells. Materials and Methods : Confluent HTSE cells were metabolically radiolabeled with 3H-glucosamine for 24 hrs and chased for 30 min in the presence of SCTS or P-D to assess the effect of each agent on 3H-mucin release. Possible cytotoxicities of each agent were assessed by measuring lactate dehydrogenase (LDH) release. Also, the effects of SCTS and P-D on contractility of isolated tracheal smooth muscle were investigated. Results : SCTS did not affect mucin release from cultured HTSE cells, without cytotoxicity. However, P-D significantly increased mucin release from cultured HTSE cells. with significant cytotoxicity. SCTS inhibited Ach-induced contraction of isolated tracheal smooth muscle. P-D also inhibited Ach-induced contraction of isolated tracheal smooth muscle. Conclusions : The author suggests that the effects of SCTS and P-D with their components should be further investigated and it is valuable to find, from oriental medical prescriptions, novel agents which might regulate mucin secretion from airway goblet cells.

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