• Applied Biological Chemistry
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• 제35권2호
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• pp.76-81
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• 1992

원제와 무기증량제의 혼합분말을 유용성 점결제 stearly alcohol 혹은 ethyl cellulose로 조립한 KC-7079, isoprothiolane, perfluidone 및 tricyazole 입제를 $25^{\circ}C$ 항온조건하에서 물이 담긴 비이커에 침적하고 일정시간 간격으로 수중 유효성분농도를 분석하여 입제의 용출속도를 측정하였다. 입제의 수중용출속도는 점결제 첨가량에 따른 입제의 수중붕괴성, 사용한 점결제의 종류 및 원제의 물에 대한 용해도에 따라 크게 영향을 받았다. Stearyl alcohol 첨가입제의 수중붕괴성은 제제방법에 따라 달라져서 수중에서 붕괴되지 않고 원형을 유지하기 위한 점결제 첨가량은 sodium dodecylbenzene sulfonate 수용액(0.5%)으로 반죽하여 조립할 때는 8%, methanol로 반죽하여 조립할 때는 3% 이상 요구되었다. Stearyl alcohol을 점결제로 사용한 KC-7079 입제는 점결제 첨가량이 증가할수록 수중붕괴성이 감소하여 유효성분의 초기 용출속도가 크게 감소하였으며, 붕괴하지 않는 입제는 점결제 첨가비가 증가하여도 용출속도가 거의 변하지 않았다. Ethyl cellulose가 0.5% 이상 첨가된 입제는 수중에서 붕괴하지 않았으며, 점결제 첨가비가 증가할수록 유효성분의 용출지연효과가 증가하였다. 또한 용출지연효과는 원제함량이 작은 입제에서 현저하였다. Stearyl alcohol 첨가제제는 KC-7079와 perfluidone의 용출을 지연시킨 반면 ethyl cellulose 첨가제제는 모든 원제에 대하여 용출을 지연시킬 수 있었다. 또한 이들 유용성 점결제로 조립한 입제는 원제의 수용해도가 작을수록 용출지연효과가 뚜렷하였다.

• Journal of Pharmaceutical Investigation
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• 제32권4호
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• pp.321-325
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• 2002

IVIVC (In vitro/in vivo correlation) is useful for predicting in vivo results from in vitro data. The aim of this study was to develop IVIVC of sustained release diltiazem. For this purpose, three types of diltiazem tablets with different in vitro dissolution rates were prepared. An in vitro dissolution testing method comprising of paddle apparatus, 50 rpm, water as dissolution medium was developed. Under these condition, we demonstrated that AUCinf could be predicted by evaluating $d_{70%}$ (time dissolved 70%) in vitro since the in vivo AUCinf was correlated with the in vitro $d_{70%}$ (r=-0.9981).

• 대한의용생체공학회:의공학회지
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• 제10권1호
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• pp.59-66
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• 1989

The Applicability of chitin or chitosan microsphere as means to achieve sustained release of p-aminosalicylic acid(PAS) has been examined. The microsphere of chitin or chitosan containing PAS were prepared by coacervation in acidic aqueous system in range of pH 2.0-4.0. The dissolution test of PAS from polymeric drug system was carried out in vitro test. The dissolution rate of PAS from the microsphere with chitin was significanthly lower than that from the microsphere with chitosan.The dissolution rate of PAS from the microsphere was decreased with increasing of concentration of chitin and chitosan. The sustained release of PAS from the microsphere was more effective at pH 1.2 than pH 6.8.

• 약학회지
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• 제39권2호
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• pp.185-192
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• 1995

Flurbiprofen, one of potent nonsteroidal antiinflammatory drugs, has several systemic side effects due to dose dumping effect following oral administration of its conventional solid dosage forms. To reduce these side effects and to sustain therapeutic concentration of the drug, matrix tablets of flurbiprofen were prepared and evaluated for sustained release from the tablets. The matrix tablets of flurbiprofen were prepared with Eudragit, Pluronic, (anhydrous) lactose and colloidal silicon dioxide employing two different preparation methods, wet granulation and direct compression. The dissolution rates of the tablets were evaluated using KP 2 method. Formulation factors that affected dissolution rates of flurbiprofen were the type and content of Eudragit, the type and content of Pluronic, and the tablet preparation method. Several formulations of the matrix tablets showed dissolution patterns close to the simulated profile using pharmacokinetic parameters of flurbiprofen.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.175-180
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• 1988

The role and effect of aluminum tristearate in microencapsulation were investigated based on the dispersion system of ethambutol hydrochloride in acetone-liquid paraffin. Eudragit RS was used as a wall-forming material. Eudragit RS microcapsules prepared using aluminum tristearate were uniform, free-flowing particles. The phase diagram of ethambutol hydrochloride-Eudragit RS-aluminum tristearate indicated that spherical microcapsules ranging from 250 to 1400 ${\mu}m$ in diameter could be prepared only in a very limited region. Instrumental analysis using an energy dispersive-type X-ray microanalyser and a scanning electron microscope showed that aluminum tristearate was localized near the surface of microcapsules. From these results, it was presumed that aluminum tristearate reduced the phase tension between Eudragit microcapsules and liquid paraffin. The dissolution rates of ethambutol hydrochloride from Eudragit RS microcapsules were consideraly lower than those from ethambutol hydrochloride powders and decreased as the amount of aluminum tristearate decreased.

• 한국식품과학회지
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• 제44권3호
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• pp.274-279
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• 2012

본 연구에서는 널리 사용되는 수용성 비타민인 비타민 C의 지속성 특성을 발현시키기 위해 HPMC를 사용하여 정제를 제조하였다. 먼저 비타민 C 지속성 정제의 효과적인 용출실험을 진행하기 위해서 용출 용매에 비타민 C의 산화를 방지할 수 있는 항산화제를 첨가함으로써 수분에 의한 비타민 C의 분해를 방지하였다. 비타민 C 지속성 정제의 용출 거동을 확인하기 위해 "대한약전 9개정"과 "경구용의약품의 용출규격 설정 가이드라인"의 용출시험법과 "건강기능식품이 기준 및 규격 고시전문(제2009-153호)"에 근거하여 함량시험과 시간별 용출률을 분석하였다. 분석된 용출 거동은 zero-order release model과 Korsmeyer-Peppas model에 의해 겔 내에서의 활성 성분의 확산과 겔층의 소실로 인한 이의 유리 메카니즘이 분석되었다(37,38). 비타민 C 지속성 정제에 사용된 지속성 HPMC의 사용량이 증가할수록 위장관 운동의 영향에 관계없는 zero-order release의 용출 거동에 가까워짐을 확인하였다. 이는 정제에 사용된 HPMC의 사용량이 높을수록 물을 흡수하여 초기에 겔을 형성하는 속도가 빨라져 용출 속도가 감소함을 보여준다. 점도에 따른 차이는 비타민 C의 높은 수용성 성질 때문에 차이를 보이지 않았으나, 난용성 유효 성분을 적용한 처방에서는 수화능과 겔 형성능에 따라 점도별로 차이가 날 것으로 사료된다. 이는 Korsmeyer-Peppas model에 의한 메커니즘 분석에서 비타민 C의 겔 내 활성 성분의 확산이 겔 층의 소실로 인한 유리보다 다소 우세한 것으로 설명될 수 있다. 이러한 결과를 바탕으로 비타민 C는 수분에 대한 안정성이 부족함에도 지속성 정제로의 개발 및 용출분석이 가능하며, 지속성 고분자로 사용된 HPMC의 사용량에 따라 용출 거동을 조절할 수 있어 1일 2회 내지 1일 1회 요법의 비타민 C 지속성 정제의 제제화와 안정적인 용출분석을 수행할 수 있다. 건강기능식품에 고시된 비타민 C의 정량법인 HPLC법 및 본 연구를 통해 차이가 없음이 확인된 UV spectrophotometer를 사용한 평가방법을 통해 보다 편리하게 수행할 수 있다.

• 한국철도학회논문집
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• 제7권1호
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• pp.55-59
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• 2004

Composite materials were used widely due to merit of light weight, low maintenance cost and easy installation. But it is the cause of enormous casualties to men and properties because of weak about the fire. Particularly, it is more serious in case of subway train installed composite materials. For this reason, experimental comparison has been done fur measuring heat release rate(H.R.R) and smoke production rate(S.P.R) of interior panels of electric motor car using cone calorimeter. A high radiative heat flux of 50kW/㎡ was used to bum out all materials and to simulate the condition of fully developed fire case in the tests. It was observed that Heat Release Rate and Smoke Production Rate curves were dependent on the kinds of the interior materials. From the heat release rate curves, the sustained ignition time, peak heat release rate and total heat release rate were deduced, These data are useful in classifying the materials by calculating two parameters describing the possibility to flashover.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.37-46
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• 1995

The experiment was designed to investigate the sustained release dosage form of silymarin (SL) from chitosan (CS) carrier. Solid dispersed system was prepared by mixing the drug with chitosan. This solid dispersed system was cross-linked by glutaraldehyde, formaldehyde, acetaldehyde and butylaldehyde, respectively. The dissolution rates of these preparations were compared with each other in vitro. The silymarin was mired with anionic alginate gel and bead was prepared by dropping this mixture to cationic chitosan solution including calcium chloride. Chitosan encapsulated alginate bead after drying in the oven was investigated for the dissolution rate. The dissolution rate of SL-CS mixture was delayed with increase in the amounts of CS and the concentration of aldehyde. The effect on the delay of dissolution rate was in the increasing order of formaldehyde, glutaraldehyde, acetaldehyde, butylaldehyde. The dissolution rate of chitosan encapsulated alginate bead was parallel with the concentration of chitosan in diluted hydrochloric acid solution and delayed with increase in the concentration of chitosan in phosphate buffer solution.

• KSBB Journal
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• 제17권1호
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• pp.33-37
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• 2002

PLGA 미립구로부터 G-CSF의 방출 거동 양상을 향상 시키기 위하여 G-CSF를 분자량 5000인 methoxy polyethylene glycol-aldehyde로 PEGylation 시켰다. 대부분의 G-CSF는 mono-PEGylation 되었으며, 이를 SDS-PAGE, HPLC, 및 펩타이드 지도 분석을 통해 확인하였다. W/O/W 방법을 사용하여 G-CSF 및 PEGylated G-CSF의 PLGA 미립구를 제조하였으며, 이때 봉입율은 높은 상태였다. 미립구내로 더 많은 G-CSF를 봉입하기 위하여 액상의 G-CSF 및 PEGylated G-CSF을 농축하였고 native gel과 gel filtration 크로마토 그래피를 통하여 단백질이 안정함을 확인하였다. 이렇게 제조한 PLGA 봉입체의 in vitro 방출 거동을 조사한 결과 PEGylated G-CSF는 native G-CSF에 비하여 더 오랜 시간 동안 방출이 지속되었고 최대 방출량도 증가하였다.

• Archives of Pharmacal Research
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• 제26권6호
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• pp.504-510
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• 2003

The aim of this study is to prepare biodegradable microspheres without the use of surfactants or emulsifiers for a novel sustained delivery carriers of protein drugs. A poly($\varepsilon$-caprolactone)/poly(ethylene glycol)/poly($\varepsilon$-caprolactone) (CEC) triblock copolymer was synthesized by the ring-opening of $\varepsilon$-caprolactone with dihydroxy poly (ethylene glycol) to prepare surfactant-free microspheres. When dichloromethane (DCM) or ethyl formate (EF) was used as a solvent, the formation of microspheres did not occur. Although the microspheres could be formed prior to lyophilization under certain conditions, the morphology of microspheres was not maintained during the filtration and lyophilization process. Surfactant-free microspheres were only formed when ethyl acetate (EA) was used as the organic solvent and showed good spherical micro-spheres although the surfaces appeared irregular. The content of the protein in the micro-sphere was lower than expected, probably because of the presence of water channels and pores. The protein release kinetics showed a burst release until 2 days and after that sustained release pattern was showed. Therefore, these observations indicated that the formation of microsphere without the use of surfactant is feasible, and, this the improved process, the protein is readily incorporated in the microsphere.