• Journal of Pharmaceutical Investigation
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• v.18 no.1
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• pp.23-30
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• 1988

The sustained-release micropellets containing rifampicin were prepared by spray congealing micropelleting technique using gelatin as the embedding matrix, and hardened by treating with the formalin-isopropanol mixture. Dissolution of rifampicin from micropellets was significantly retarded, and greatly dependent on formalin concentration, hardening time and pH of the dissolution medium. It was found that this prolongation was more distinguished in pH 1.2 dissolution medium rather than pH 7.4, which might be attributed to the swelling characteristics of gelatin used in the dissolution medium. In-vitro dissolution kinetics indicated that the drug release followed the first-order process.

• Journal of Acupuncture Research
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• v.23 no.5
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• pp.167-175
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• 2006

Objectives : We studied the effects of Radix Asteris herbal acupuncture solution (RAHAS) on the type I hypersensitivity. Methods : In vivo, we measured compound 48/80 induced active systemic anaphylactic shock, anti-DNP IgE induced passive cutaneous anaphylaxis (PCA) and acetic acid induced microvascular permeability using ICR mice. In vitro, we showed effects on cytotoxicity and ${\beta}$-hexosaminidase release from RBL-2H3 cells. Results : In vivo, RAHAS pretreatments at $BL_{13}$ and optional points inhibited active systemic anaphylactic shock induced by compound 48/80 and microvascular permeability increased by acetic acid. PCA was only inhibited by RAHAS pretreatments at $BL_{13}$. In vitro, RAHAS treatments inhibited ${\beta}$-hexosaminidase release. Conclusion : These results suggest that RAHAS may be beneficial in the prevention of type I hypersensitive inflammatory response.

• Korean Journal of Acupuncture
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• v.23 no.3
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• pp.111-122
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• 2006

Objectives : We studied the effects of Scutellariae Radix pharmacopuncture solution (SRHAS) on the type 1 hypersensitivity. Methods : In vivo, we measured compound 48/80-induced active systemic anaphylactic shock using ICR mice and anti-DNP IgE-induced passive cutaneous anaphylaxis (PCA) using Sprague Dawley rats. In vitro, we showed effects on cytotoxicity and ${\beta}-hexosaminidase$ release from RBL-2H3 cells. Results : In vivo, SRHAS pretreatments (100% or 50%) at BL13 inhibited active systemic anaphylactic shock induced by compound 48/80. PCA was only inhibited by pretreatments of SRHAS at optional points. In vitro, $0.1{\sim}2%$ SRHAS treatments did not affect cell viability while ${\beta}$-hexosaminidase release was significantly inhibited. Conclusions : These results suggest that SRHAS may be beneficial in the inhibition of type I hypersensitive inflammatory response.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.408-413
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• 1998

To establish prediabetes in vitro/ model concerning the etiology of Insulin Dependent Diabetes Mellitus (IDDM) in cellular level we have designed experimental prediabefic model in pancreatic beta cells. RINm5F, HIT-T15 and isolated rat islets were chosen as pancreatic beta cells. Since interleukin-$1{\beta}$-induced beta cell cytotoxicity has been implicated in the autoimmune cytotoxicity of IDDM, we used inteleukin-$1{\beta}$ as diabetogenic agent. For establishment of prediabetic in vitro model, the degree of beta cell deterioration was determined by cell proliferation, insulin release and morphological appearance. Cell proliferation, insulin release and morphology were changed dose-dependently in condition that inteleuldn-$1{\beta}$ was exposured to pancreatic beta cells. The concentration and exposure time of interleukin-$1{\beta}$ to set up prediabetic model in beta cell lines and isolated rat islets were 100${\sim}$1000U/ml, 48hr. And 25${\sim}$100U/ml, 48hr, respectively.

• Journal of Pharmaceutical Investigation
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• v.39 no.1
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• pp.59-63
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• 2009

Soybean phosphatidylcholine microparticles loaded with cyclosporin A (CsA) were prepared by the modified emulsion solvent diffusion and ionic gelation method, in which chitosan on the surface of the microparticles was crosslinked with various concentrations of tripolyphosphate (TPP). The morphology of the particles was characterized by scanning electron microscopy (SEM). The change of particle size and zeta-potential by chitosan on the surface of the lipid microparticles were systematically observed. The encapsulation efficiency and loading capacity of CsA in the particles were determined by high performance liquid chromatography (HPLC). In vitro release kinetics was studied using the dialysis method. In the results, the mean particle size and the zeta-potential of lipid microparticles increased when the attached chitosan was cross-linked (from 2.5 to 6.2 ${\mu}m$ and from -37.0 to +93.0 mV, respectively). The cyclosporin A-loaded lipid microparticles appeared discrete and spherical particles with smooth surfaces. The encapsulation efficiency of CsA was between 79% and 90% while the loading capacity was between 41% and 56%. In vitro release study showed that the crosslinkage of chitosan by TPP significantly delayed the release of CsA from the particles in a concentration-dependent manner. Thus, the release of CsA from the lipid microparticles could be controlled by tripolyphosphate used as a cross-linking agent.

• KSBB Journal
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• v.17 no.1
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• pp.33-37
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• 2002

To improve in vitro release kinetic of G-CSF in PLGA microsphere, G-CSF was PEGylated with methoxy polyethylene glycol-aldehyde (mPEG-aldehyde, MW 5000). The majority of G-CSF was mono-PEGylated and it was characterized using SDS-PAGE, HPLC, and peptide mapping. The PLGA microencapsulation with the native, or PEGylated G-CSF was performed using W/O/w method, where the encapsulation efficiency was high. For the high loading of G-CSF to microsphere, G-CSF and PEGylated G-CSF were concentrated and then verified the protein stability using native gel and gel filtration chromatography. In comparison with native G-CSF, PEGylated G-CSF was released during the extended period and its maximum amount of released G-CSF was also increased.

• Biotechnology and Bioprocess Engineering:BBE
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• v.9 no.3
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• pp.179-183
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• 2004

A biocompatible polyelectrolyte complex multilayer (PECML) film consisting of poly-L-lysine (PLL) as a polycation and hyaluronic acid (HA) as a polyanion was developed to test its use for surface modification to prevent cell attachment and protein drug delivery. The formation of PECML through the electrostatic interaction of HA and PLL was confirmed by contact angle measurement, ESCA analysis, and HA content analysis. HA content increased rapidly up to 8 cycles for HA/PLL deposition and then slightly increased with an increasing number of deposition cycle. In vitro release of PLL in the PECML continued up to 4 days and ca. 25% of HA remained on the chitosan-coated cover glass after in vitro release test for 7 days. From the results, PECML of HA and PLL appeared to be stable for about 4 days. The surface modification of the chitosan-coated cover glass with PECML resulted in drastically reduced peripheral blood mononuclear cell (PBMC) attachment. Concerned with its use for protein drug delivery, we confirmed that bovine serum albumin (BSA) as a model protein could be incorporated into the PECML and its release might be triggered by the degradation of HA with hyaluronidase.

• YAKHAK HOEJI
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• v.20 no.1
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• pp.63-69
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• 1976

Prednisolone tablet product design problem was structured as constrained optimization problem and subsequently solved by multiple regression analysis and Lagrangian method of optimixation. Prednisolone was the drug chosen and anhydrous lactose and corn starch were the adjuvants. The effect of anhydrous lactose and corn starch concentrations on tablet hardness, volume, disintegration time and in vitro release rate was studied. The concentrations of anhydrous lactose and corn starch used in this experiment were 30-60 percent and 5-30 percent, respectively. A full second-order (quadratic) model with all possible two-factor interactions was employed. To obtain the values of anhydrous lactose and corn starch which miniumize the in vitro : release time (t$_{60%}$) subject to the constraint on tablet hardness, disintegration time and volume, we solved the Lagrange function. Multiple correlation coefficients for the regression models were correlated at less than 0.05 level and it was found that the optimum concentrations of anhydrous lactose and corn starch were 45 percent and 21 percent, respectively.

• Bulletin of the Korean Chemical Society
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• v.34 no.6
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• pp.1800-1808
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• 2013

Dual-responsive amphiphilic block copolymers were synthesized by combining enzymatic ring-opening polymerization (eROP) of ${\varepsilon}$-caprolactone (CL) and ATRP of N,N-dimethylamino-2-ethyl methacrylate (DMAEMA). The obtained block copolymers were characterized by gel permeation chromatography (GPC), $^1H$ NMR and FTIR-IR. The critical micelle concentration (CMC) of copolymer was determined by fluorescence spectra, it can be found that with hydrophilic block (PDMAEMA) increasing, CMC value of the polymer sample increased accordingly, and the CMC value was 0.012 mg/mL, 0.025 mg/mL and 0.037 mg/mL for $PCL_{50}$-b-$PDMAEMA_{68}$, $PCL_{50}$-b-$PDMAEMA_{89}$, $PCL_{50}$-b-$PDMAEMA_{112}$, $PCL_{50}$-b-$PDMAEMA_{89}$ was chosen as drug carrier to study in vitro release profile of anti-cancer drug (taxol). The temperature and pH dependence of the values of hydrodynamic diameter (Dh) of micelles, and self-assembly of the resulting block copolymers in water were evaluated by dynamic light scattering (DLS). The result showed that with the temperature increasing and pH decreasing, the Dh decreased. Drug-loaded nanoparticles were fabricated using paclitaxel as model. Transmission electron microscopy (TEM) and atomic force microscopy (AFM) had been explored to study the morphology of the hollow micelles and the nanoparticles, revealing well-dispersed spheres with the average diameters both around 80 nm. In vitro release kinetics of paclitaxel from the nanoparticles was also investigated in different conditions (pH and temperature, etc.), revealing that the drug release was triggered by temperature changes upon the lower critical solution temperature (LCST) at pH 7.4, and at $37^{\circ}C$ by an increase of pH.

• Parasites, Hosts and Diseases
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• v.52 no.3
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• pp.317-319
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• 2014

The oocyst wall is severed by means of mechanical injury or chemical agents. This study reports the percentage of in vitro sporocyst release following mechanical shaking in the presence of varying sizes of glass beads. Glass beads measured 0.5, 1, and 3 mm in diameter and were shaken with the oocysts for different times ranging from 5 sec to 5 min. Approximately 80% of sporocysts were released with 5 min of shaking in the presence of 3 mm glass beads, as well as 30 sec with 0.5 mm beads and 1 mm glass beads. The release of sporocysts of E. tenella was most efficient using 1 mm glass beads and treatment times of 30 sec to 1 min. Therefore, the use of 1 mm glass beads with 30 sec to 1 min of agitation is recommended in order to maximize sporocyst release and recovery and to improve the yield of viable sporozoites for use in biochemical, tissue culture, and immunological applications of coccidia.