• 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.

• Journal of Pharmaceutical Investigation
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• 제19권3호
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• pp.145-154
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• 1989

Methyl methacrylate-butyl methacrylate copolymer (MMBM)-povidone (PVP) films were investigated as a potential topical drug delivery system for the controlled release of econazole nitrate as a model drug. The effect of changes in film composition, drug concentration, film thickness, pH and temperature of release medium on the in vitro release of econazole nitrate were studied. The release rate constant was found to be increased with increasing povidone content in dry films. Drug release followed zero-order kinetics in the initial stage and then release rate increased gradually with time, espicially in the films having larger proportions of PVP. The release rate was found to be dependent on drug content, film thickness, the pH and temperature of release medium. Antimicrobial test showed that microbial growth was inhibited markedly with increasing proportions of PVP in films. Also drug content and film thickness affected the antimicrobial activity.

• Journal of Pharmaceutical Investigation
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• 제21권4호
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• pp.237-245
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• 1991

Matrix type silicone rubber devices were designed for long-term implantable drug delivery system. Release controlling agents (RCA), i.e., polypropylene glycol, polyethylene glycol, were employed to control drug release from the devices. The release rate of drug from RCA dispersed silicone matrices was mainly dependent on hydrophilicity-hydrophobicity of drug and RCA. In the case of hydrophilic drug, the release from the RCA dispersed matrix was regulated by swelling kinetics. Especially when the relatively hydrophobic polypropylene glycol was used, swelling control mechanism induced zero-order release kinetics. Whereas, the release of hydrophobic drug was resulted from partition mechanism. The effect of RCA was to increase drug diffusivity.

• Journal of Pharmaceutical Investigation
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• 제41권6호
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• pp.347-354
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• 2011

Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.

• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.89-95
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• 1990

Ethylcellulose-PEG 4000 film coated on core tablets was investigated as a potential drug delivery system for the controlled release of chlorpheniramine maleate (CPM). The kinetic analysis of the release data indicated that CPM release followed a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The effect of the film composition, CPM concentration, plasticizer concentration and CPM solubility on the release characteristics were examined. The release rate constant increased as CPM concentration increased. It also increased as the PEG 4000 content in the film increased above 10%(w/w), however, it decreased as the PEG 4000 content increased in the concentration range below 10%(w/w). The release rate constant was not affected by the coated weight on the core tablet. The film-coated tablets which contain CPM only in the coated film layer seemed to be a potential oral drug delivery system for the controlled release of CPM.

• 대한기계학회논문집B
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• 제36권5호
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• pp.545-551
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• 2012

마이크로 유체구조를 기반으로 하는 약물전달장치는 마이크로 유체 채널형상의 간단한 변형만으로 약물분출량을 쉽게 조절할 수 있는 장점이 있다. 그러나 디바이스 제작에 사용된 생분해성 고분자 85/15poly(lactic-co-glycolic acid) (85/15PLGA)의 소수성 기질 때문에 약물전달 장치내부로의 release medium의 유입이 원활하게 이루어지지 않으며 그 결과, 디바이스의 임플랜트 후 초기의 약물 분출에 영향을 줄 것으로 예상된다. 따라서 surfactant인 polyethylene-glycol600 (PEG600)과 Tween80을 이용하여 micro-channel의 표면처리를 한 디바이스와 surfactant를 사용하지 않은 디바이스를 각각 제작하여 약물 전달 실험을 하였으며, 이를 바탕으로 마이크로 유체 채널의 기하학적 형상에 따른 국소 마취제의 일종인 bupivacaine HCl(BHCl)의 분출속도제어를 입증하였다.

• Archives of Pharmacal Research
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• 제23권4호
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• pp.385-390
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• 2000

To demonstrate the effect of formulation conditions on the controlled release of protein from poly(lactide-co-glycolide) (PLGA) microspheres for use as a parenteral drug carrier, ovalbumin (OVA) microspheres were prepared using the W/O/W multiple emulsion solvent evaporation and extraction method. Methylene chloride or ethyl acetate was applied as an organic phase and poly(vinyl alcohol) as a secondary emulsion stabilizer. Low loading efficiencies of less than 20％ were observed and the in vitro release of OVA showed a burst effect in all batches of different microspheres, followed by a gradual release over the next 6 weeks. Formulation processes affected the size and morphology, drug content, and the controlled release of OVA from PLGA microspheres.

• Archives of Pharmacal Research
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• 제12권2호
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• 공업화학
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• 제34권2호
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• pp.161-169
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• 2023

본 연구는 allbanggae starch (ABS), polyvinyl alcohol (PVA), alginic acid (SA)를 이용하여 naproxen (NP) 각인 starch 기반 다층 바이오소재를 제조하고, 물리화학적 특성과 약물 방출 제어 효과를 조사하였다. 또한, FE-SEM과 FT-IR 분석에 의해 제조한 다층 바이오소재의 특성을 조사하였다. 약물 방출 제어 효과와 경피 약물 전달 시스템의 적용 가능성을 확인하기 위해 NP 각인 다층 바이오소재로부터 NP 방출 특성을 사람의 체온인 36.5 ℃에서 다양한 pH buffer solution과 인공 피부를 이용하여 확인하였다. NP는 낮은 pH보다 높은 pH에서 1.3배 더 빠른 방출을 나타냈고, single-layer 바이오소재에서보다 multi-layer 바이오소재에서 약 4.0배 느린 방출이 일어남을 확인하였다. 인공 피부 방출에서도 동일하게 single-layer 바이오소재보다 multi-layer 바이오소재에서 약 4.0배 더 느린 약물 방출 결과를 나타내었다. 또한, double-layer와 triple-layer 바이오소재 모두 12시간 동안 지속적으로 NP가 방출되었음을 확인 하였다. NP 방출 mechanism을 규명하기 위해 수학적 모델링에 적용하여 비교했을 때, pH buffer solution에서의 방출은 Fickian diffusion mechanism, 인공 피부 방출은 empirical mechanism에 적합한 것을 확인하였다.

• Journal of Pharmaceutical Investigation
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• 제19권2호
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• pp.99-107
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• 1989

In order to develop a pediatric liquid preparation with sustained release properties, dextromethorphan hydrobromide (DEXT) was complexed with strong cation exchange resin (CG 120) and the-complex was coated with Eudragit RS using a phase separation method by non-solvent addition. The effect of pH, ionic strength of the release medium and drug/resin ratio on the release rate of DEXT was studied. The release rate of free drug from the uncoated complex, and coated complexes with 9.5 and 18.5% Eudragit RS in artificial gastric juice were measured. The release rate from the uncoated complex was faster with higher pH, higher ionic strength of the release medium and higher drug/resin ratio. The release rate from the coated complex could be controlled by the amount of coating material, and the surface after release did not rupture into.