• Title/Summary/Keyword: Sustained-release

Search Result 354, Processing Time 0.022 seconds

Sustained release granular formulation with oil-soluble binder (유용성 점결제를 이용한 수중용출지연입제의 제제)

  • Yu, Ju-Hyun;Lee, Byung-Hoi;Cho, Kwang-Yun
    • Applied Biological Chemistry
    • /
    • v.35 no.2
    • /
    • pp.76-81
    • /
    • 1992
  • The technicals of KC-7079, isoprothiolane, perfluidone and tricyclazole were granulated with a mixture of inorganic carrier and oil-soluble binder, that is, stearly alcohol or ethyl cellulose. The concentration of the released active ingredient from the granules was analyzed at several days intervals after immersion of these granules in water at $25^{\circ}C$. At the content of stearyl alcohol less than $80g\;kg^{-1}$, the granule kneaded with stearyl alcohol mixture and water disintegrated in water. But the granule kneaded with methanol disintegrated in water at the content of stearyl alcohol less than $30g\;kg^{-1}$. The less the KC-7079-stearyl alcohol granule disintegrated, the slower the release rate of KC-7079 was. No matter how was increased the stearyl alcohol content, the release rate of KC-7079 granule which did not disintegrate was not significantly changed. The sustained releasing effect of the granules was little in the other three pesticides of which the water solubility was higher than of KC-7079(21 ppm). The granule made of ethyl cellulose did not disintegrate even at $5g\;kg^{-1}$ of ethyl cellulose. With the increase of ethyl cellulose content and the decrease of active ingredient in the granules, the sustaining effect of the granules on releasing acitive ingredient was increased. The lower the water solubility of pesticide was, the release rate tended to be sustained except perfluidone.

  • PDF

In vitro/In vivo Correlation of Sustained Release Diltiazem (딜티아젬서방정을 이용한 In vitro/In vivo 상관성)

  • Choi, Myoeng-Sin;Kang, Chan-Soon;Choi, Bo-Kyung;Hong, Chong-Hui;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
    • /
    • v.32 no.4
    • /
    • pp.321-325
    • /
    • 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).

Dissolution properties of Chitin or Chitosan Microsphere Containing p-Aminosalicylic Acid (p-Aminosalicylic acid를 포함하고 있는 Chitin, Chitosan-Microsphere의 용출특성)

  • 임정수;김공수
    • Journal of Biomedical Engineering Research
    • /
    • v.10 no.1
    • /
    • pp.59-66
    • /
    • 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.

  • PDF

Formulation of Sustained-Release Tablets of Flurbiprofen (서방출성 플루르비프로펜 정제의 제제설계)

  • 이상철;박은석;지상철
    • YAKHAK HOEJI
    • /
    • v.39 no.2
    • /
    • pp.185-192
    • /
    • 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.

  • PDF

Effects of Aluminum Tristearate in the Preparation of Sustained Release Ethambutol Hydrochloride Microcapsules (지속 방출형 염산에탐부톨 마이크로캅셀의 제조에 있어서 스테아린산알루미늄의 효과)

  • Yoo, Bong-Shin
    • Journal of Pharmaceutical Investigation
    • /
    • v.18 no.4
    • /
    • pp.175-180
    • /
    • 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.

  • PDF

Dissolution Profile Analysis of Hydroxypropyl Methylcellulose-based Vitamin C Tablets (Hydroxypropyl methylcellulose를 활용한 비타민 C 지속성 정제의 용출 특성 분석)

  • Cha, Ja-Hyun;Hong, Jun-Kee;Lee, Sung-Wan;Cha, Jae-Uk;Ko, Won-Hwa;Baek, Hyon-Ho;Park, Hyun-Jin
    • Korean Journal of Food Science and Technology
    • /
    • v.44 no.3
    • /
    • pp.274-279
    • /
    • 2012
  • The objective of this study was to develop oral matrix tablets for the sustained release of vitamin C. In this study hydroxypropyl methylcellulose (HPMC) has been utilized as an excipient, as it is one of the most widely used polymers, for use during long periods of time in formations. The vitamin C tablet formulation depends on the molecular weight and concentration of sustained-delivery in HPMC. Anti-oxidants have been added as a dissolution medium in order to prevent vitamin C degradation in water. The dissolution test was carried out in a distilled water medium, and the release model equation was applied to analyze the vitamin C release pattern. The results demonstrated that the release and lasting power of vitamin C tablets, containing HPMC, lasted for more than 12 h.

Fire Characteristics of Composites for Interior Panels Using Cone calorimeter (콘칼로리미터를 이용한 내장판용 복합재료의 화재특성)

  • 이철규;정우성;이덕희
    • Journal of the Korean Society for Railway
    • /
    • v.7 no.1
    • /
    • pp.55-59
    • /
    • 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.

Controlled Release of Silymarin from Chitosan Carrier (Chitosan을 이용한 Silymarin의 방출 제어)

  • Ho, Byuong-Kyun;Park, Kyung-Ock;Kang, Chin-Yang;Seo, Seong-Hoon
    • Journal of Pharmaceutical Investigation
    • /
    • v.25 no.1
    • /
    • pp.37-46
    • /
    • 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.

  • PDF

Sustained Release of PLGylated G-CSF from PLGA Microsphere (PLGA 미립구로부터 PLGylated G-CSF의 서방성 방출)

  • 정경환;임형권;이시욱;강관엽;박태관
    • KSBB Journal
    • /
    • v.17 no.1
    • /
    • pp.33-37
    • /
    • 2002
  • To improve in vitro release kinetic of G-CSF in PLGA microsphere, G-CSF was PEGylated with methoxy polyethylene glycol-aldehyde (mPEG-aldehyde, MW 5000). The majority of G-CSF was mono-PEGylated and it was characterized using SDS-PAGE, HPLC, and peptide mapping. The PLGA microencapsulation with the native, or PEGylated G-CSF was performed using W/O/w method, where the encapsulation efficiency was high. For the high loading of G-CSF to microsphere, G-CSF and PEGylated G-CSF were concentrated and then verified the protein stability using native gel and gel filtration chromatography. In comparison with native G-CSF, PEGylated G-CSF was released during the extended period and its maximum amount of released G-CSF was also increased.

Surfactant-Free Microspheres of Poly(${\varepsilon}-caprolactone$)/Poly(ethylene glycol)/Poly(${\varepsilon}-caprolactone$) Triblock Copolymers as a Protein Carrier

  • Sun, Sang-Wook;Jeong, Young-Il;Kim, Sung-Ho
    • Archives of Pharmacal Research
    • /
    • v.26 no.6
    • /
    • pp.504-510
    • /
    • 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.