• Journal of Pharmaceutical Investigation
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• v.41 no.4
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• pp.217-225
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• 2011

The aim of this work was to prepare porous osmotic pump tablets for controlled delivery of Aceclofenac. Aceclofenac solid dispersion was prepared to improve the solubility by using the drug - carrier (Mannitol) ratio of 1:1. The osmotic pump tablets were prepared using the solid dispersed product of Aceclofenac. The formulation contains potassium chloride as osmotic agent, cellulose acetate as semipermeable membrane, poly ethylene glycol (PEG 4000) as pore former and sodium lauryl sulphate (SLS) as solubility enhancer. The formulations were designed by the general factors such as osmotic agent and pore former. All formulations were evaluated for various physical parameters and, the in vitro release studies were conducted as per USP. The drug release kinetic studies such as zero order, first order, and Higuchi and Korsmeyer peppas were determined and compared. All the formulations gave more controlled release compared to the marketed tablet studied. Numerical optimization techniques were applied to found out the best formulation by considering the parameter of in vitro drug release kinetics and dissolution profile standards. It was concluded that the porous osmotic pump tablets (F7) composed of Aceclofenac solid dispersion/Potassium chloride/Lactose/Sodium lauryl sulphate/Magnesium Stearate (400/40/95/10/5, mg/tab) and coating composition with Cellulose acetate/ PEG 4000 (60/40 %w/w) is the most satisfactory formulation. The porous osmotic pump tablets provide prolonged, controlled, and gastrointestinal environment-independent drug release.

• The Korean Journal of Pesticide Science
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• v.8 no.4
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• pp.319-324
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• 2004

Pesticide formulations for controlled release were pepared with hollow silica microspheres. The hollow microsphere, which was obtained through calcination for the core removed after silica coating, showed maximum impregnation of benfuracarb up to 2.7 times of its mass in comparison with those obtained through the other core removal method. The release test of the pesticide formulation, when used with ESO(Epoxidized Soybean Oil) as a binder, showed ideal release pattern with steady release rate from the day 10 to 30 retaining the benfuracarb concentration in the water around 1.65 ppm.

• 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.

• Journal of Pharmaceutical Investigation
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• v.28 no.3
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• pp.177-183
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• 1998

Low toxicity, reverse thermal gelation and high drug loading capabilities suggest that poloxamer 407 gels have great potential as a topical drug delivery system. 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 skin irritancy due to its acidic pH. Poloxamer gels of different polymer contents were formulated to overcome the problem and compared to the cream type formulations of either w/o/w multiple emulsion cream or o/w type emulsion cream. 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 solutions. Drug release from w/o/w multiple emulsion cream was controlled by oil membrane, showing the apparent zero order release kinetics. The KA release from the poloxamer gels was also controlled by the gel matrix, showing that drug release increased linearly as KA contents increase, but decreased exponentially as the polymer contents increase. In the skin irritancy test, the primary irritancy index(PII) of poloxamer gel base was lower than those of multiple emulsion cream base and o/w cream. Depending on KA contents or polymer contents in the gel. PH values in poloxamer gels were ranged from 1.3 to 2.0, which are interpreted as low or negligible irritation on skin. There was a good correlation between the log value of flux in drug release and PII value in skin irritation. It was possible to conclude that the poloxamer gels containing KA might be a good candidate for an antimelanogenic topical delivery system by virtue of the controlled release of the drug and the reduced skin irritancy.

• Korean Journal of Weed Science
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• v.11 no.3
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• pp.159-166
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• 1991

Seven oxyfluorfen formulations were tested for control of 8 weed species and rice injury under four different water depths with various ages of rice seedlings. Among formulations tested, rice injury was slight by formulations of Elvan, Coal Slag, Chitosan and Bentonite B under 0 cm or shallow water depths, and by those of Elvan and Coal Slag under deep water conditions. Weed control was high by Bentonite A and B, and Chitosan, and was low by Elvan. Coal Slag and Sand coated oxyfluorfen, if the target weeds of oxyfluorfen are annual species, further development of Elvan, coal slag, chitosan and Bentonite A would be controlled to increase control efficacy or to decrease rice injury.

• Korean Journal of Environmental Agriculture
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• v.14 no.3
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• pp.289-295
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• 1995

This study was carried out to develop a controlled-release insecticide formulation for the control of rose aphid (Macrosiphum ibarae) in rose and cotton aphid (Myzus persicae) in chrysanthemum (Dendranthema grandiflorum var. Meibung) in greenhouse. Imidacloprid[1-(6-chloro-3-pyridylmethyl)-N-nitroimidazolidin-2-ylideneamine] was chosen as a toxicant. Two synthetic polymers, low density polyethylene(LDPE) and ethylene vinyl acetate(EVA), were used as polymer matrices. The tested plastic sheet formulations were prepared by heat-aided extrusion procedures after mixing imidacloprid technical and the polymers of three different combinations, and physicochemical properties as well as efficacy of the formulations were investigated. The amounts of imidacloprid recovered and incorporated in the formulations were recorded over 90% and 80%, respectively. Release of the active ingredient from the formulations was remarkably affected by mixing rates of polymers. The active ingredient in the formulations was chemically unstable with over 10% degradation rates after 90 day storage at $50{\pm}2^{\circ}C$. The residual amounts of imidacloprid in the soil treated with the formulations were paralleled with the release pattern of the formulations. Efficacy of the formulations on rose and cotton aphid was maintained over 90% even 120days after treatment under greenhouse.

• Journal of Microbiology and Biotechnology
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• v.9 no.1
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• pp.50-55
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• 1999

To develop a new form of controlled release dosage for administering for indomethacin (IND), two formulations of IND-loaded nanoparticles were designed based on polysaccharide (guar) derivatives. Nanoparticles prepared by the dialysis method were characterized with respect to morphology, size distribution, drug content, and in vitro drug release. Morphological studies by scanning electron microscopy (SEM) indicated that guar acetate (GA) nanoparticles were spherical in shape and had a smooth surface. The particle size distributions of formulation I (40mg of GA) and formulation II (80mg of GA) were shown to be $250.78\pm185.13nm$ and $718\pm145.90nm$ in distilled water ($20$^{\circ}C$), respectively. The drug loading efficiencies of nanoparticles were approximately 26% and 31% for formulations I and II, respectively. The differential scanning calorimetry (DSC) results indicated that the IND was perfectly distributed within GA nanoparticles. We also found, from the X-ray diffractometry analysis, that a decrease in the degree of crystallinity of the drug occurred in the nanoparticles. No changes between the original IND and the released IND from GA nanoparticles were detected by FT-IR. Using guar acetate, it is possible to design nanoparticles which allow the controlled release of IND over an extended period of time.

• The Korean Journal of Pesticide Science
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• v.2 no.1
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• pp.53-58
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• 1998

In order to minimize harmful side effects, extend weed control performance, and control the releasing rate of the active ingredient, dicamba controlled release granular formulations were prepared with starch as matrix. Leaching, soil residue, and volatilization of the granules were compared with dicamba soluble concentrate formulation (SL). Leaching of dicamba through the soil applied with the granules could be reduced more than 50% as compared with that of dicamba SL. The half life of dicamba in loamy soil treated with the granules was 50 to 51 days, while that in sand loamy soil was 50 to 58 days. Whereas, the half life of dicamba in loamy and sand loamy soil applied with dicamba SL was 24 and 22 days, respectively. Volatilization of dicamba from the granules was 10 times less than that of dicamba SL.

• Journal of Pharmaceutical Investigation
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• v.40 no.spc
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• pp.103-112
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• 2010

Pellets, which are multiple-unit dosage systems, have the several therapeutic advantages over single-unit dosage systems in oral drug delivery. This review focuses on the current status and explores extrusion-spheronization technique with special attention to controlled-release application of pellets including coated pellets for delayed release formulations, coated pellets for colon delivery, coated pellets for sustained drug delivery, sustained-release matrix pellets, pellets compressed into tablets, bioadhesive pellets, floating pellets, and pelletization with solubilization techniques.

• Archives of Pharmacal Research
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• v.13 no.2
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• pp.151-160
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• 1990

In order to develop a controlled-release oral drug delivery system (DDS) which sustains the plasma acetaminophen (AAP) concentration for a certain period of time, microporous membrane-coated tablets were prepared and evaluated in vitro. Firstly, highly water-soluble core tablet of AAP were prepared with various formulations by wet granulation and compression technique. Then the core tablets were coated with polyvinychloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of core tablets and coating suspensions on the pharmaceutical characteristics such as drug release kinetics and membrane stability of the coated tablets was investigated in vitro. AAP was released from the coated tablets as a zero-order rate in a pH-independent manner. This independency of AAP release to pH change from 1.2 to 7.2 is favorable for the controlled oral drug delivery, since it will produce a constant drug release in the stomach and intestine regardless of the pH change in the GI tract. Drug release could be extended upto 10 h according to the coating condition. The release rate could be controlled by changing the formula compositions of the core tablets and coating suspensions, coat weight per each tablet, and especially PVC/sucrose ratio and particle size of the sucrose in the coating suspension. The coated tablets prepared in this study had a fairly good pharmaceutical characteristics in vitro, however, overall evaluation of the coated tablet should await in vivo absorption study in man.