• Korean Journal of Weed Science
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• v.11 no.1
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• pp.11-18
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• 1991

Seven formulations of oxyfluorfen selected from the previous studies(4. 5) were tesed to evaluate crop injury and herbicidal efficacy on two rice cultivars and several annual and perennial weeds in a greenhouse. Each formulation at two different rates was applied to rice transplanted with 8-, 22- and 32-day old seedlings and to direct-seeded rice. Among the formulations, Elvan, Bentonite B. Chitosan and Coal Slag gave lower injury than a control formulation, Sand-coated oxyluorfen, and they did not have a problem with excessive release if active ingredient at once. Especially, the formulations of Elvan, Chitosan and Bentonite B controlled annual weeds (Echinochloa crus-galli, Monochoria vaginalis, Cyperus difformis., and Scirpus juncoides) and perennial weeds (Sagittaria pygmaea, and Cyperus serotinus). The surface structure of the formulations indicate the different possibilities of releasing of oxyfluorfen by different cracking and hole sizes, namely retention capacity.

• 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.

• 대한임상약리학회:학술대회논문집
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• 1997.12a
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• pp.36-37
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• 1997

• Biotechnology and Bioprocess Engineering:BBE
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• v.11 no.6
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• pp.526-529
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• 2006

The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to $10\;{\mu}m$, and that of the EPS-LIMs was about $100\;{\mu}m$. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.

• Archives of Pharmacal Research
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• v.27 no.7
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• pp.763-768
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• 2004

To investigate the feasibility of developing a new quercetin transdermal system, a preformulation study was carried out. Therefore, the effects of vehicles and pressure-sensitive adhesives (PSA) on the in vitro permeation of quercetin across dorsal hairless mouse skin were studied. Among vehicles used, propylene glycol monocaprylate (PGMC) and propylene glycol mono-laurate were found to have relatively high permeation flux from solution formulation (i.e., the permeation fluxes were 17.25$\pm$1.96 and 9.60$\pm$3.87 $\mu\textrm{g}$/$\textrm{cm}^2$/h, respectively). The release rate from PSA formulations followed a matrix-controlled diffusion model and was mainly affected by the amount of PSA and drug loaded. The overall permeation fluxes from PSA formulations were less than 0.30 $\mu\textrm{g}$/$\textrm{cm}^2$/h, which were significantly lower compared to those obtained from solution formulations. The lower permeation fluxes may be due to the decrease of solubility and diffusivity of quercetin in the PSA layer, considering the fact that the highest flux of 0.26 $\mu\textrm{g}$/$\textrm{cm}^2$/h was obtained with the addition of 0.2％ butylated hydroxyanisole in PGMC-diethyl-ene glycol monoethyl ether co-solvents (80-85 ： 15-20, v/v). Taken together, these observations indicate that improvement in the solubility and diffusivity of quercetin is necessary to realize fully the clinically applicable transdermal delivery system for the drug.

• Journal of Pharmaceutical Investigation
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• v.34 no.5
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• pp.363-368
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• 2004

In order to investigate the effect of bovine serum albumin (BSA), as a pore former, on the controlled release of an antibiotic from a biodegradable polymeric device, polycaprolactone (PCL)-cefadroxil matrices were prepared by the solvent casting method. The amount of cefadroxil released from various formulations at $37^{\circ}C$ was measured by HPLC. The duration of antimicrobial activity of matrices against S. aureus was evaluated by measuring the diameters of the inhibition zone. The morphology of the matrices was investigated by scanning electron microscopy (SEM). The release rate and extent of cefadroxil from PCL matrix increased as the loading dose and particle size of BSA/cefadroxil mixture powder increased. Cefadroxil released from the matrix exhibited antibacterial activity for up to 4 days. SEM of the cross-section of matrix showed the typical channel formation after 3 days of release study. Thus, a biodegradable polymeric matrix loaded with antibiotic/BSA mixture can effectively prevent bacterial infection on its surface, thereby bringing about an enhancement of biocompatibility of biomaterials.

• Journal of Pharmaceutical Investigation
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• v.41 no.5
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• pp.263-272
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• 2011

Tablet dosage forms have been preferred over other formulations for the oral drug administration due to their low manufacturing costs and ease of administrations, especially controlled-release applications. Controlled-release tablets are oral dosage forms from which the active pharmaceutical ingredient (API) is released over an intended or extended period of time upon ingestion. This may allow a decrease in the dosing frequency and a reduction in peak plasma concentrations and hence improves patient compliance while reducing the risk of undesirable side effects. Conventional singlelayered matrix tablets have been extensively utilized to deliver APIs into the body. However, these conventional single-layered matrix tablets present suboptimal delivery properties, such as non-linear drug delivery profiles which may cause higher side effects. Recently, a multi-layered technology has been developed to overcome or eliminate the limitations of the singlelayered tablet with more flexibility. This technology can give a good opportunity in formulating new products and help pharmaceutical companies enhancing their life cycle management. In this review, a brief overview on the multi-layered tablets is given focusing on the various tablet designs, manufacturing issues and drug release profiles.

• Journal of Pharmaceutical Investigation
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• v.30 no.2
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• pp.93-98
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• 2000

In order to evaluate the effect of fabrication methods on the controlled release of an antibiotic from a polymeric device, two types of polyurethane-cefadroxil matrix were prepared by the solvent casting method or the freeze drying method, using bovine serum albumin as a pore former. The amount of cefadroxil released from various formulations at $37^{\circ}C$ was measured by HPLC. The duration of antimicrobial activity of matrices against S. aureus was evaluated by measuring the diameters of the inhibition zone. The morphology of the matrices was investigated by scanning electron microscopy (SEM). Changing the fabrication method could alter the release rate of cefadroxil from the matrix. The matrix fabricated by the freeze drying method had more porous inner structure and showed higher release rate than that prepared by the solvent casting method. However, the duration of antimicrobial activity was shorter when the matrix was fabricated by the freeze drying method.

• The Korean Journal of Pesticide Science
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• v.3 no.1
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• pp.37-45
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• 1999

Dicamba (3,6-dichloro-o-anisic acid) granular formulations for controlled release (DGFCRs) were prepared with biodegradable polymers, corn starch and pregelatinized starch, to minimize harmful side effects, extend weed control performance, and control the releasing rate of the active ingredient. Physico-chemical properties and biological activity of DGFCRs were studied. Six different granules were formulated by applying two processes, granulation and extrusion. Formulation efficiencies of active ingredient (A.I.) in the granules prepared by granulating and extruding were $90.0{\sim}96.3%$. Incorporation ratios of A.I. in the granules prepared by granulating and extruding showed $89.5{\sim}94.5%$ and $46.7{\sim}82.0%$, respectively. The highest swellability was DG-2 formulation prepared with corn starch. Whereas, the lowest floatability in water was DG-2 formulation, while the highest one was DG-1 formulation prepared with pregelatinized starch, Miragel 463. The degradation rates of dicamba in the granules under the elevated temperature of $50^{\circ}C$ were less than 5% for DG-1 and DG-2 formulations even after 90 days, meanwhile, those of DE-1 formulations prepared with pregelatinized starch, Mirasperse, were more than 5%. The release rates of A.I. from the granules into water under a static condition were about 100% after 2 weeks. Weeding effects of the granules on broad leaf weeds tested in greenhouse were more than 90% after 30 days.

• Biomolecules & Therapeutics
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• v.19 no.2
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• pp.248-254
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• 2011

Biotransformation of pharmacologically inactive lactone prodrug simvastatin (SV) into pharmacologically active simvastatin ${\beta}$-hydroxy acid (SVA) exhibits inter-species differences due to variations in amount and activity of esterase enzymes. In this study, we investigated the pharmacokinetics (PK) of SV and its metabolite SVA following oral doses of SV from controlled-release (CR) tablets and immediate-release (IR) tablets in rodent and canine animal models that features different esterase activity. In rat PK study, no SV was detected in plasma for both formulations due to rapid hydrolysis of SV into SVA by plasma esterase. Besides, no significant differences in PK parameters of SV or SVA were observed between both species. In dog PK study, the relative oral bioavailability of CR tablets in terms of SV was 72.3% compared to IR tablets. Regarding formulation differences in dogs, CR tablets exhibited significantly lower $C_{max}$ (p<0.05), and higher $T_{max}$ (p<0.01) and MRT (p<0.01) for both SV and SVA compared to IR tablets. Accordingly, CR tablets of SV with prolonged drug release profiles in both species might be a potential candidate for a more effective delivery of SV with reduced side effects. Besides, similar PK parameters of SV and SVA in both species despite variation in enzyme activities suggested involvement of equally potent biotransformation pathways in these animal species.