• Journal of Pharmaceutical Investigation
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• 제34권5호
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• pp.401-406
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• 2004

To develop an intravenous delivery system of all-trans retinoic acid (ATRA) for the cancer therapy, poly(L-lactic acid) nanoparticles were prepared and characterized. Emulsification-solvent evaporation method was chosen to prepare submicron sized nanoparticles. Spherical nanoparticles less than 200 nm in diameter with narrow size distribution were prepared, and the entrapment efficiency of drug was more than 95%. The endothermic peak at $183^{\circ}C$ and X-ray crystallographic peak of ATRA appeared in the nanoparticle system, suggesting the inhibition of crystallization of ATRA by polymer adsorption during the precipitation process. ATRA was released at $37^{\circ}C$ for 60 days and the release rate was dependent on the concentration of drug incorporated in the nanoparticles. While ATRA was unstable in the light, it was very stable at $4^{\circ}C$. These results suggest the usefulness of PLA nanoparticles as a sustained and prolonged release carrier for ATRA.

• Journal of Pharmaceutical Investigation
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• 제31권4호
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• pp.257-263
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• 2001

The microspheres have been developed as a new drug delivery system. Although many particulate drug carriers, such as liposome, niosome and emulsion, have been introduced, injectable and biodegradable microspheres appears to be a particularly ideal delivery system because the local anesthesia is not necessary for the insertion of large implants and for the removal of the device after the drug release is finished. Biodegradable microspheres with nicotine and triamcinolone acetonide are prepared and evaluated. As biodegradible polymers, PLA (M.W. 15,000, PLA-0015), PLGA (M.W. 17,000, RG 502) and PLGA (M.W. 8,600, RG 502H) are used. This study attempted to prepare and evaluate the nicotine and triamcinolone acetonide-incorporated microspheres, which were prepared by two methods, solvent-evaporation and spray-drying methods. The microspheres, as a disperse system for injections, were evaluated by particle size, size distribution, entrapment efficiency, and in vitro drug release patterns. The differences of preparation method, partition coefficient, types of polymer, and preparation conditions of microspheres influence the particle size, entrapment efficiency, and in vitro drug release patterns.

• Journal of Pharmaceutical Investigation
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• 제35권6호
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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.

• Journal of Pharmaceutical Investigation
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• 제37권2호
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• pp.101-106
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• 2007

Venlafaxine, 1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl] cyclohexanol hydrochloride is a novel, nontricyclic antidepressant. venlafaxine is a unique antidepressant that differs structurally from other currently available. The aim ot the study was to formulate sustained-release venlafaxine granules and assess their formulation variables. It consists of two layers, venlafaxine drug layer and sustained release coating layer and manufactured by fluidized bed process. The sustained release of drug could be increased by double-control rising various components in venlafaxine drug layer and sustained-release layer. The drug-containing granules were coated with cellulose acetate, cetyl alcohol and Eudragit RS along with plastisizer such as dibuthyl sebacate as an nano-pore former The release oi venlafaxine depended on the type of Eudragit such as RS, and RL used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for venlafaxine could be designed with satisfying drug release profile approved.

• 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.

• Archives of Pharmacal Research
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• 제28권3호
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• pp.364-369
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• 2005

HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values, pH-sensitive values, water vapor permeability, tensile strength and Tg, were investigated, and found to show good film forming properties. The pH­sensitive values were 3.0 to 3.7. In vitro results demonstrate that HPMCAM could completely suppress drug release within 2h in a simulated gastric fluid (pH 1.2) and rapidly release the drug in a simulated pathological duodenal fluid (pH 3.4). These results indicate that HPMCAM might be a useful material for a duodenum-specific drug delivery system.

• Journal of Pharmaceutical Investigation
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• 제35권6호
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• pp.471-481
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• 2005

In Korea, generic drug and bioequivalence test are the hot issues since a new medical system of separation of dispensary from medical practice was started in 2000. The KFDA(Korea FDA) had revised several times ${\ulcorner}Guidance\;for\;bioequivalence\;test{\lrcorner}$. In vitro dissolution test has been extensively used as a quality control tool for solid oral dosage forms. In an effort to minimize unnecessary human testing, in vitro/in vivo correlations (IVIVC) between in vitro dissolution and in vivo bioavailability are increasingly becoming an integral part on extended release drug product development. The recently published US guidance, ${\ulcorner}Extended\;release\;oral\;dosage\;forms\;:\;development,\;evaluation,\;and\;application\;of\;in\;vitro/in\;vivo\;correlations{\lrcorner}$ will be helpful for us to make our own guideline.

• 대한화학회지
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• 제37권5호
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• pp.527-536
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• 1993

Chitin을 강알칼리로 탈아세틸화시켜 합성한 chitosan을 증류수에 팽윤시킨 다음 글리세린을 가하여 교반하였다. 이 고분자 용액에 약물인 silver sulfadiazine을 가하여 경피흡수용 고분자 matrix을 제조하였다. 이렇게 제조된 고분자 matrix로부터 약물의 방출거동과 고분자 matrix 변수와의 상관관계 등을 조사함으로써 지속적이고 조절된 경피흡수제형으로서의 사용 가능성과 특성을 조사하였다. 고분자 matrix 내의 약물의 함유량과 matrix의 두께가 증가할수록 약물의 방출시간은 더 지연되었다. 그러나 글리세린의 함유량이 증가함에 따라 약물의 방출시간은 오히려 감소하였다. 약물의 함유량, 글리세린의 함유량 및 matrix의 두께가 증가할수록 겉보기 방출속도상수(K)값도 증가하였다.이상과 같이 chitosan은 의약의 방출조절형제제로서 가능성을 나타냈으며, 약물로 사용된 silver sulfadiazine의 방출거동은 Higuchi model에 따른 확산으로 생각되었다.

• 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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• 제38권2호
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• pp.105-110
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• 2008

Indapamide (4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoyl-benz-amide) is an oral antihypertensive diuretic agent indicated for the treatment of hypertensive. The diuretic and natriuretic effects are mainly due to the structure of o-chlorobenzenesulfonamide. The objective of this study was to formulate sustained release indapamide granules and assess their formulation variables. Granules were prepared by fluid bed coating method and consist of drug layer and membrane layer. The granules were coated with HPC and ethyl cellulose along with plasticizer dibuthyl sebacate. The release of indapamide depended on the type of Eudragit such as RS and NE 30 D used in the formulation controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for indapamide could be designed with satisfying drug release profile approved.