• Title/Summary/Keyword: in vitro release

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Effects of Hyeongbangpaedok-san (HBPDS) on Allergic Contact Dermatitis (ACD) induced by DNFB in Mice (형방패독산(荊防敗毒散)이 DNFB로 유발된 생쥐의 알레르기접촉피부염에 미치는 영향)

  • Park, Geun-Hee;Lim, Tae-Hyung;Park, Hye-Sun
    • Journal of Sasang Constitutional Medicine
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    • v.26 no.2
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    • pp.180-193
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    • 2014
  • Objectives The present study was carried out to investigate effects of HBPDS on allergic contact dermatitis (ACD) induced by 2,4-Dinitro-1-fluorobenzene (DNFB) in mice. Methods In this experiment, effects of HBPDS on body weights, skin thicknesses, skin weights, histopathological changes, clinical aspects, erythema index, melanin index, production levels of cytokines in ACD mice were investigated. In addition, effects on proliferation rates, release of ${\beta}$-hexosaminidase and histamine were also investigated in vitro. Results & Conclusions 1) HBPDS inhibited enlargement of skin thickness and weight significantly (P < 0.05). 2) HBPDS treatment prevented spongiosis, edema and immune cell infiltrations. 3) Erythema, desquamation and keratosis were diminished by oral administration of HBPDS. 4) Production levels of TNF-alpha and IFN-gamma in serum were decreased by HBPDS treatment in vivo. 5) More than 200 ${\mu}g/ml$ of HBPDS treatment decreased ${\beta}$-hexosaminidase release and more than 400 ${\mu}g/ml$ of HBPDS treatment also decreased histamine release in vitro.

The Microencapsulated Ascorbic Acid Release in vitro and Its Effect on Iron Bioavailability

  • Lee, Jun-Beum;Ahn, Joung-Jwa;Lee, Jong-Hwi;Kwak, Hae-Soo
    • Archives of Pharmacal Research
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    • v.26 no.10
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    • pp.874-879
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    • 2003
  • The present study was carried out to examine the stability of microencapsulated ascorbic acid in simulated-gastric and intestinal situation in vitro and the effect of microencapsulated ascorbic acid on iron bioavailability. Coating materials used were polyglycerol monostearate (PGMS) and medium-chain triacylglycerol (MCT), and core materials were L-ascorbic acid and ferric ammonium sulfate. When ascorbic acid was microencapsulated by MCT, the release of ascorbic acid was 6.3% at pH 5 and 1.32% at pH 2 in simulated-gastric fluids during 60 min. When ascorbic acid was microencapsulated by PGMS, the more ascorbic acid was released in the range of 9.5 to 16.0%. Comparatively, ascorbic acid release increased significantly as 94.7% and 83.8% coated by MCT and PGMS, respectively, for 60 min incubation in simulated-intestinal fluid. In the subsequent study, we tested whether ascorbic acid enhanced the iron bioavailability or not. In results, serum iron content and transferring saturation increased dramatically when subjects consumed milks containing both encapsulated iron and encapsulated ascorbic acid, compared with those when consumed uncapsulated iron or encapsulated iron without ascorbic acid. Therefore, the present data indicated that microencapsulated ascorbic acid with both PGMS and MCT were effective means for fortifying ascorbic acid into milk and for enhancing the iron bioavailability.

Injectable Gel Type Formulation of Hydrated Egg Phosphatidylcholine and Hyaluronate for Local Drug Delivery

  • Kim, Sang-Gyun;Chung, Hesson;Lee, In-Hyun;Kang, Seung-Back;Kwon, Ick-Chan;Sung, Ha-Chin;Jeong, Seo-Young
    • Journal of Pharmaceutical Investigation
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    • v.32 no.3
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    • pp.165-172
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    • 2002
  • Injectable gel composed of egg phosphatidylcholine (egg PC), hyaluronate (HA) and water was formulated for local drug delivery. The lamellar liquid crystalline structure of the egg PC/water system did not change by adding HA in the formulation. However, egg PC/HA/water gel was more resistant to erosion than the egg PC/water gel. The egg PC/HA/water and egg PC/water gels containing model drugs, tetracycline and sudan IV were prepared to perform in vitro and in vivo drug release experiments. In vitro release of tetracycline was sustained in the gel type formulations. The release rate of hydrophobic sudan IV was extremely slow. More than 99% of sudan IV remained inside the gel after 5 days. In vivo release of drugs from the air pouch model in Balb/c mice shows that lipophilic sudan IV remained for more than 10 days whereas tetracycline remained for 1 day in the pouch. The compatibility of the gels was also examined by histopathology. The gels did not cause any adverse inflammatory effect in the air pouch.

Preparation and Evaluation of Meloxicam-loaded Poly(D,L-lactic acid) Microspheres (멜록시캄 함유 poly (D,L-lactic acid) 미소립자의 제조 및 평가)

  • Im, Jong-Seob;Oh, Dong-Hoon;Li, Dong-Xun;Sung, Jung-Hoon;Yoo, Bong-Kyu;Kim, Jung-Ae;Woo, Jong-Soo;Lee, Yong-Bok;Kim, Se-Mi;Choi, Han-Gon;Yong, Chul-Soon
    • Journal of Pharmaceutical Investigation
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    • v.38 no.1
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    • pp.63-72
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    • 2008
  • Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

Evaluation of In-Vitro Dissolution and In-Vivo Absorption for Two Different Film-Coated Pellets of Clarithromycin

  • Zhang Xiang-rong;Chen Xiao-yan;Hu Lian-Dong;Tang Xing;Li San-Ming;Zhong Da-fang
    • Archives of Pharmacal Research
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    • v.28 no.8
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    • pp.977-982
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    • 2005
  • The aim of this study was to compare two formulations of film-coated pellets containing c1arithromycin after single oral dose study in healthy male volunteers. Two formulations with different coating polymers were prepared: formulation-1 (F-1) was prepared by incorporating three kinds of pH-dependent gradient-release coated pellets into capsules and formulation-2 (F-2) was prepared by coated with an insoluble semiosmotic film. Release profiles of filmcoated pellets were evaluated using paddle method under different conditions. Pharmacokinetic profiles of these formulations were obtained in three healthy male volunteers and compared to commercially available immediate release (IR) tablets. The relative bioavailability based on the $AUC_{0-24h}$ was found to be $96.2\%\;and\;58.7\%$ for F-1 and F-2 compared with IR, and the $T_{max}$ was delayed.

In vitro Immunomodulating Effects of PALMIWON (팔미원의 in vitro 면역조절 작용)

  • Lee, Ihn-Soon;Rhee, In-Ja
    • YAKHAK HOEJI
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    • v.40 no.6
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    • pp.684-689
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    • 1996
  • PALMIWON is composed of 8 oriental herbs which has been known to show some pharmacological effects in kidney, blood vessels and immune systems, and used for the treatment of kid ney disease, hypertension, nervous disease and diabetic mellitus in the Orient for a long time. Based on our previous report that PALMIWON showed different effects on immune cells and ${\beta}$-cells, the immunoreactivity of ICSA (Islet Cell Surface Antibody) with ${\beta}$-cell (RINm5F) and the cell proliferation and function of interleukin-1${\beta}$ damaged ${\beta}$-cells in the presence of PALMIWON were examined. It was observed that PALMIWON significantly inhibited the immunoreactivity of ICSA with ${\beta}$-cell, and markedly increased cell proliferation and insulin release of interleukin-1${\beta}$ damaged ${\beta}$-cells.

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A Study on the Melanin Synthesis Inhibition and Whitening Effect of Bombysis Corpus (백강잠의 멜라닌 생성 억제와 미백효과에 관한 연구)

  • Oh, Han-Cheol;Lim, Kyu-Sang;Hwang, Chung-Yeon;Youn, In-Hwan;Kim, Nam-Kwen
    • The Journal of Korean Medicine Ophthalmology and Otolaryngology and Dermatology
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    • v.20 no.3
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    • pp.1-13
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    • 2007
  • Objective : This study was performed to assess the whitening effect of Bombysis Corpus on melanin synthesis. Methods : The whitening effects of Bombysis Corpus were examined by in vitro melanin production assay. We assessed inhibitory effects of Bombysis Corpus on melanin-release from B16F10, on melanin production in B16F10, on mushroom tyrosinase activity in vitro, on tyrosinase activity in B16F10, effect of Bombysis Corpus on the expression tyrosinase, TRP-1, PKA, ERK-1 ERK-2, AKT-1, MITF in B16F10. Results : 1. Bombysis Corpus inhibited melanin-release, melanin production in B16F10. 2. Bombysis Corpus inhibited tyrosinase activity in vitro and in B16F10. 3. Bombysis Corpus suppressed the expression of tyrosinase, TRP-1 in B16F10. 4. Bombysis Corpus suppressed the expression of PKA in B16F10. 5. Bombysis Corpus suppressed the expression of ERK-1, ERK-2, AKT-1 in B16F10. 6. Bombysis Corpus suppressed the expression of MITF in B16F10. Conclusion : The study shows that Bombysis Corpus inhibited melanin production on the melanogenesis.

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Sustained Release of Water-Soluble Blue Dextran from PLGA Nanoparticles (PLGA 나노파티클로부터 수용성 블루 덱스트란의 서방성 방출)

  • Ryu, Sang-Hwa;Hwang, Sung-Joo;Park, Jeong-Sook
    • Journal of Pharmaceutical Investigation
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    • v.36 no.2
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    • pp.109-114
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    • 2006
  • Biodegradable poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles were developed for sustained delivery of water-soluble macromolecules. PLGA nanoparticles were fabricated by spontaneous emulsification solvent diffusion method generating negatively charged particles and heterogeneous size distribution. As a model drug, blue dextran was encapsulated in PLGA nanoparticles. In addition, nanoparticles were also prepared with varying ratio of poloxamer 188 (P188) and poloxamer 407 (P407), and coating with poly(vinyl alcohol) (PVA). Then, the particle size, zeta potential and encapsulation efficiency of nanoparticles containing blue dextran were studied. In vitro release of blue dextran from nanoparticles was also investigated. The surface and morphology of nanoparticles were characterized by scanning electron microscopy (SEM). In case of nanoparticles prepared with PLGA, P407, and different organic solvents, particle size was in the range of $230{\sim}320\;nm$ and zeta potentials of nanoparticles were negative. The SEM images showed that ethyl acetate is suitable for the formulation of PLGA nanoparticles with good appearance. Moreover, ethyl acetate showed higher encapsulation efficiency than other solvents. The addition of P188 to formulation did not affect the particle size of PLGA nanoparticles but altered the release patterns of blue dextran from nanoparticles. However, PVA, as a coating material, altered the particle size with increasing the PVA concentration. The nanoparticles were physically stable in the change of particle size during long-term storage. From the results, the PLGA nanoparticles prepared with various contents of poloxamers and PVA, could modulate the particles size of nanoparticles, in vitro release pattern, and encapsulation of water-soluble macromolecules.

Study on anti-allergic effects of Arctii Fructus herbal acupuncture (우방자약침(牛蒡子藥鍼)의 항(抗)알러지 효과(效果)에 대한 연구(硏究))

  • Jang, Seok-Chang;Song, Choon-Ho
    • Korean Journal of Acupuncture
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    • v.25 no.1
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    • pp.197-211
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    • 2008
  • Objectives : We studied on anti-allergic effects of Arctii Fructus Herbal Acupuncture(AFHA) and Arctii Fructus Herbal Acupuncture Solution(AF). Methods : In vivo, Animals were herbal-acupunctured AFHA at both ST36 three times for 5 days. Then, we investigated compound 48/80-induced active systemic anaphylaxis(ASA) using ICR mice and anti-DNP IgE-induced passive cutaneous anaphylaxis(PCA) using Sprague Dawley rat. In vitro, we measured cell viability, b-hexosaminidase, IL-4 and TNF-a release from RBL-2H3 cells after treatment of AF of various concentrations. Results : In vivo, AFHA pretreatments at both ST36 inhibited compound 48/80-induced ASA. PCA was inhibited by AFHA pretreatments at both ST36. In vitro, AF treatments were not affect on cell viability and inhibited b-hexosaminidase, IL-4 and TNF-a release. Conclusions : These results suggest that AFHA and AF may be beneficial in the inhibition of allergic inflammatory response.

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ffect of Semen Perillae herbal acupuncture on the type 1 hypersensitivity (소자약침(蘇子藥鍼)이 Type 1 Hypersensitivity에 미치는 영향)

  • Song, Se-Hoon;Song, Choon-Ho
    • Korean Journal of Acupuncture
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    • v.25 no.1
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    • pp.213-227
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    • 2008
  • Objectives : We studied on anti-allergic effects of Semen Perillae Herbal Acupuncture(SPHA) and Semen Perillae Herbal Acupuncture Solution(SP). Methods : In vivo, Animals were herbal-acupunctured SPHA at both ST36 three times for 5 days. Then, we investigated compound 48/80-induced active systemic anaphylaxis (ASA) using ICR mice and anti-DNP IgE-induced passive cutaneous anaphylaxis (PCA) using Sprague Dawley rat. In vitro, we measured cell viability, b-hexosaminidase release, IL-4 and TNF-a from RBL-2H3 cells after treatment of SP of various concentrations. Results : In vivo, SPHA pretreatments at both ST36 inhibited compound 48/80-induced ASA. PCA was inhibited by SPHA pretreatments at both ST36 and optional points. In vitro, SP treatments were not affect on cell viability and inhibited b-hexosaminidase release, IL-4 and TNF-a. Conclusions : These results suggest that SPHA and SP may be beneficial in the inhibition of allergic inflammatory response.

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