• Journal of Pharmaceutical Investigation
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• v.35 no.6
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• pp.445-451
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• 2005

As a selective ${\alpha}_{1A}-adrenoreceptor$ antagonist, tamsulosin has been used clinically for urinary obstructed patients with benign prostatic hyperplasia. The single and multi-layered pellets containing tamsulosin hydrochloride were prepared in an effort to control the drug release, avoiding dose-dependent side effects of tamsulosin hydrochloride upon oral administration. The drug release from multi-layered pellets was substantially controlled, compared with single layered pellets. The drug release from coated pellets with single or multi layer was affected by the nature of coating agent, the percentage of coating level and the presence of hydrophilic material in coating layer. In conclusion, the controlled release oral delivery system using multi-layered pellet is very useful for tamsulosin hydrochloride, resulting in improvement of patient compliance and therapeutic drug levels for a longer period of time.

• The Korean Journal of Physiology and Pharmacology
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• v.8 no.6
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• pp.329-333
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• 2004

In this study, we investigated whether TNF-alpha, IL-1beta, CTMA (carboxymethyl trimethylammonium) and LPD (Lup-20[29]-ene-3beta,28-diol) affect mucin release from airway goblet cells and compared the activities of these agents with the inhibitory action of PLL and the stimulatory action of ATP on mucin release. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H-glucosamine$ for 24 h and chased for 30 min in the presence of varying concentrations of each agent to assess the effects on $^3H-mucin$ release. The results were as follows: TNF-alpha, CTMA and LPD increased mucin release at the highest concentration, but IL-1beta did not. We conclude that CTMA and LPD can stimulate mucin release by directly acting on airway mucin-secreting cells, and suggest that these agents should be further investigated for the possible use as mild expectorants during the treatment of chronic airway diseases.

• YAKHAK HOEJI
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• v.32 no.1
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• pp.26-39
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• 1988

Eudragit $RS^{\circledR}$ polymer was used as a wall material for the microencapsulation of aspirin by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene (PIB) in cyclohexane, and microcapsules obtained were evaluated by particle size analysis, scanning electron microscopy (SEM), drug release and drug stability test. With PIB as a coacervation inducing agent, smooth and tight microcapsules with less aggregation were obtained. Below 1 : 0.3 core-wall ratio, it was possible to coat individual particle. Variation of production conditions showed that increasing the proportion of wall material, particle size and wall thickness of microcapsules and the concentration of paraffin wax in cyclohexane as a sealant sustained drug release rates effectively. SEM confirmed that larger microcapsules after drug release did not rupture into smaller particles but contained a few small pores on the surface. Aspirin release from Eudragit $RS^{\circledR}$ coated microcapsules was independent of the pH of medium, and the mechanism of drug release from non-sealed and sealed microcapsules appeared to fit Higuchi matrix model kinetics. Aspirin in the mixture of aspirin microcapsules and sodium bicarbonate was by far more stable than that in the mixture of pure aspirin and sodium bicarbonate.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.294.2-295
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• 2003

Gentisic acid, a skin-whitening agent, is known to possess tyrosinase inhibition activity. In order to develop an effective skin-whitening agent, hydroquinone derivatives in which the carboxylic acid moiety of gentisic acid was replaced with various functional groups, were selected and evaluated for their ability to inhibit tyrosinase activity as well as to inhibit melanin release. (omitted)

• Journal of Dental Rehabilitation and Applied Science
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• v.35 no.2
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• pp.81-89
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• 2019

Purpose: This study aimed to investigate the correlation between the solubility and the amount of fluoride release when a resin surface coating agent is applied to RMGIC. Materials and Methods: To measure the fluoride release and solubility, Fuji II $LC^{(R)}$and $Filtek^{TM}$ Z350XT without a surface coating, Fuji II $LC^{(R)}$ with G coat $plus^{TM}$ and Fuji II $LC^{(R)}$ with $Permaseal^{(R)}$ were prepared. And the amount of fluoride release and solubility were measured. Results: There was no significant difference in the daily fluoride release between the surface coating agents. The cumulative fluoride release was significantly different between the groups using RMGIC at 56 days (P < 0.05). In the solubility measurement, RMGIC without surface coating was significantly different only on the 7th day compared to the other three groups (P < 0.05). Conclusion: Surface coating agents can prevent the degradation of properties by the initial solvent in RMGIC. Therefore, fluoride is preserved inside the restorative material and the effect of surface coating after the addition is reduced, so that the effect on fluoride release and storage is also reduced.

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.

• Polymer(Korea)
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• v.26 no.5
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• pp.691-700
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• 2002

Interstitial therapy using biodegradable polymeric device loaded with anticancer agent can deliver the drug to the tumor site at high concentration, resulting in an increase of therapeutic efficacy. 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine) is most commonly used as chemotherapeutic agent for brain tumors. The design of implantable device is regarded as an important factor lot the efficient delivery of antitumor agent to targeting site. In order to control the release profile of drug, the release pattern of BCNU with the changes of various dimension and additives was investigated. The PLGA wafers containing 3.85, 10, 20 and 30% of BCNU were prepared in various shape (diameter of 3, 5 and 10 mm, thickness of 0.5, 1 and 2 mm) by direct compression method. In vitro drug release profile of BCNU-loaded PLGA wafers could be controlled by changing the dimension of wafers such as initial drug content, weight, diameter, thickness, volume and surface area of wafers, as well as PLGA molecular weight and additives. Drug release from BCNU-loaded PLGA wafers was facilitated with an increase of BCNU-loading amount or presence of poly(N-vinylpyrrolidone)(PVP) or sodium chloride (NaCl). The effects of various geometric factors and additives on the BCNU release pattern were confirmed by the investigation of mass loss and morphology of BCNU-loaded PLGA wafers.

• Journal of Adhesion and Interface
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• v.9 no.2
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• pp.8-15
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• 2008

Microcapsules have been widely used in cosmetics and pharmacology as controlled delivery devices of various active materials. Chitosan is the second most plentiful natural biopolymer with biocompatibility and nontoxicity. The chitosan microcapsules were prepared by the water-in-oil (W/O) emulsion method using glutaraldehyde as a crosslinking agent. Span80 was used as an emulsifier, and mineral oil was used as a medium material. Perfectly spherical microcapsules were obtained in the size range of $2{\sim}10{\mu}m$. The effects of emulsifier concentration and stirring speed on the average particle size and distribution were investigated. Encapsulation and release behavior of the microcapsules with different amount of the crosslinking agent (glutaraldehyde), different chitosan contents and different emulsifier concentration conditions were also investigated. The release rate of riboflavin was controlled by the crosslinking density of the chitosan and amount of emulsifier in the preparation of the microcapsule.

• Membrane Journal
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• v.15 no.4
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• pp.281-288
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• 2005

The hyaluronic acid (HA) with excellent biocompatibility can be combined with lactide, the ester dimer of polylactide, with good biodegradability to produce biocompatible materials applicable to drug delivery system. By freeze drying method, HA and lactide were crosslinked with crosslinking agent, 1-ethyl-3-(3-dimethyl aminopropyl) carbodiimide. Degree of lactide and EDC reaction was determined by the analysis of nuclear magnetic resonance (NMR) spectroscopy. The degree of lactide and EDC reaction increased and swelling ratio decreased as the mole ratio of lactide to HA or crosslinking agent concentration increased or reaction temperature decreased. The drug release experiment result from membranes having different degree of lactide reaction showed that drug release rate reduced in proportion to the degree of lactide reaction. The drug release experiment result from drugs having different hyrodphobicity showed that the more hydrophobic drug was released more slowly.

• Biomolecules & Therapeutics
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• v.13 no.4
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• pp.251-255
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• 2005

In the present study, we tried to investigate whether protein kinase C (PKC) activator, phorbol 12-Myristate 13-Acetate (PMA), and PKC inhibitors, $G\"{o}-6976$, Ro-31-8220 and rottlerin significantly affect basal mucin relesed from cultured airway goblet cells. Confluent primary hamster tracheal surface epithelial (HTSE) cells were metabolically radiolabeled with $^3H$-glucosamine for 24 hr and chased for 30 min in the presence of each agent to assess the effects on $^3H$-mucin release. The results were as follows: (1) PMA increased mucin release from cultured HTSE cells, during 30 min of treatment period; (2) However, $G\"{o}-6976$, Ro-31-8220 and rottlerin did not significantly affect mucin release, during 30 min of treatment period. This finding suggests, at least in part, that PKC might playa minor role in the signaling pathways involved in basal - physiological or constitutive - mucin release from airway goblet cells, although further studies are needed.