• Journal of Pharmaceutical Investigation
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• 제41권4호
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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.

• 농약과학회지
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• 제8권4호
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• pp.319-324
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• 2004

실리카 중공 미세구를 이용하여 방출 조절형 입제 농약을 제조합에 있어 실리카 중공 미세구 제조시 핵 제거 방법으로 열분해법을 사용하면 benfuracarb를 실리카 중공 미세구 중량의 2.67배까지 함침이 가능하였다. 이렇게 제조된 방출 조절형 입제 농약을 수중 방출 실험한 결과, 점결제로 ESO를 사용하였을 때 일정한 benfuracarb 방출 속도를 유지하여 10일부터 용액 중의 benfuracarb의 농도를 1.65 ppm 정도를 30일까지 유지되었다.

• Journal of Pharmaceutical Investigation
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• 제28권2호
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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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• 제28권3호
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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.

• 한국잡초학회지
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• 제11권3호
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• pp.159-166
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• 1991

필자(筆者)들의 전보(前報)에서와 동일(同一)한 Oxyfluorfen 6제형(劑型)을 동일(同一)한 초자실(硝子室)에서 4수준의 관개수심 조건을 부여하여 서로 다른 묘령의 벼와 8종의 주요 논잡초종에 대한 약해 반응 및 약효 차이를 비교 검토하였다. 공시 제형 가운데 Elvan. Coal slag, Chitosan 및 Bentonite B 제형은 비담수 및 천수조건에서, 그리고 Elvan, Coal slag는 심수조건에서 약해가 경미하였고, 제초효과는 Bentonite A 및 B. Chitosan이 전반적으로 높았고, Elvan, Coal slag는 Sand coating과 함께 낮은 경향이었다. 그러나, Oxyfluorfen의 제초대상을 일년생으로 제한하여 판단할 경우에는 제초 효과면에서 제형간 차이가 크지 않았으므로 상대적으로 약해가 경미하였던 Elvan, Coal slag, Chitosan 및 Bentonite B제형을 보완 개발하거나 약해 약효간의 유사관계가 분명하였던 Elvan 및 Bentonite A형의 최초 방출 속도를 보완개발 함이 기대된다.

• 한국환경농학회지
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• 제14권3호
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• pp.289-295
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• 1995

시설원예작물(施設園藝作物)을 가해(加害)하는 짓딧물을 효율적(效率的)으로 방제(防除)하기 위하여 살충제(殺蟲劑)인 imidacloprid를 유효성분(有效成分)으로 하고 저밀도(低密度) 포리에틸렌과 초산(醋酸)비닐을 고분자(高分子) 매체(媒體)로 하여 방출조절형(放出調節型) 살충성(殺蟲性) 농약제제(農藥製劑)를 제조(製造)하고 그 이화학적(理化學的) 특성(特性) 및 약효(藥效)를 조사(調査)한 결과(結果)는 다음과 같다. 1. 시제품(試製品)중 농약주성분(農藥主成分)의 제제율(製劑率)은 90% 이상으로 대부분의 농약(農藥)이 합성수지(合成樹脂)에 함유(含有)되어 있었다. 2. 농약주성분(農藥主成分)의 수중용출양상(水中溶出樣相)은 합성수지(合成樹脂)의 혼합비율(混合比率)에 따라 큰 차이를 보여 저밀도(低密度) 포리에틸렌의 함량(含量)이 높을수록 용출속도(溶出速度)는 완만(緩慢)하였다. 3. 시제품(試製品)중 농약주성분(農藥主成分)의 경시분해(經時分解)는 처리초기(處理初期)에는 적었으나 처리(處理)90일 후에는 분해율(分解率)이 10% 이상으로 높았으며 유효기간은 1년으로 평가된다. 4. 토양(土壤)중 농약잔류양상(農藥殘留樣相)은 기존(旣存)의 입제(粒劑)와 크게 달라 장기간에 걸쳐 일정수준이 유지되었으며 수중용출시험(水中溶出試驗)의 결과(結果)와 밀접한 연관성을 보였다. 5. 장미와 국화진딧물에 대한 효과(效果)는 우수하였고 120후에까지 약효(藥效)가 지속(持續)되었으며 1회의 처리로 기존 진딧물약의 다수 살포작업을 절약할 수 있어 새로운 농약제형(農藥劑型)으로서의 개발가능성이 제시되었다.

• Journal of Microbiology and Biotechnology
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• 제9권1호
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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.

• 농약과학회지
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• 제2권1호
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• pp.53-58
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• 1998

Dicamba의 부작용을 최소화하고, 약효지속효과를 증진하며, 유효성분의 용출속도를 조절할 수 있는 전분을 중합매체로 한 방출조절형 dicamba 입제를 제조하여 기존의 dicamba 액제와 용탈, 토양잔류 및 휘산을 비교하였다. 이들 방출조절형 dicamba 입제는 dicamba 액제에 비하여 약 50% 이상 용탈이 감소되었으며, 토양잔류는 양토에 처리된 dicamba 입제의 토양중 반감기가 $50{\sim}51$일 이었으며, 사양토에 처리하였을때는 $50{\sim}58$일 이었다. 한편 양토 및 사양토에 처리된 dicamba 액제는 각각 24일과 22일 이었다. 또한 dicamba의 휘산성은 방출조절형 dicamba 입제가 dicamba 액제에 비하여 약 10배의 휘산억제효과가 있었다.

• Journal of Pharmaceutical Investigation
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• 제40권spc호
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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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• 제13권2호
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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.