• Title/Summary/Keyword: PEG base

Search Result 39, Processing Time 0.029 seconds

Formulation of Rectal Supopositories of Omeprazole (오메푸라졸 함유 직장좌제의 제제설계)

  • 이창현;황성주;오세종;이계주
    • YAKHAK HOEJI
    • /
    • v.37 no.4
    • /
    • pp.370-382
    • /
    • 1993
  • In order for formulation of rectal containing OMZ, the OMZ suppositories were prepared using water-soluble base, PEG 4000 base and oil-soluble base, Witepsol H 15. Chemical stability of OMZ in suppositories was increased when Witepsol H 15 was used as a suppository base and arginine was added as a stabilizer. The decomposition of OMZ in suppository bases followed the first-order kinetics and their rate constants were 0.11 day $^{1}(t_{1/2}$=/6.25 days) for Witepsol H 15 suppository and 0.48 day $^{1}(t_{1/2}$=/1.43 days) for PEG 4000 suppository, respectively. On the other hand, the decomposition rate constants of Witepsol suppository and PEG suppository stabilized with arginine were 3.89$\times$10$^{-3}$(t$_{1/2}$=171.1 days) and 8.76$\times$10$^{-3}$ day $^{1}(t_{1/2}=79.9 days), respectively. Shelf-lives of the Witepsol and PEG suppositories stabilized with arginine were t$_{90%}$=291.8 days and t$_{90%}$=282.1 days at $35^{\circ}C$ and 75% RH, respectively. The dissolution test of OMZ suppositories was performed by rotating dialysis cell(RDC) method and the release rate constant was calculated by the simplified Higuchi's equation, Q'=K' t$^{1/2}$. Dissolution of OMZ from suppositories was augmented as arginine was added, particle size of OMZ was reduced and a suitable surfactant such as SLS was added. RDC method was more appropriate and available than Paddle method to evaluate the dissolution rate of lipophilic-base suppositoies. Arginine was found to be a very useful exipient for the enhancement of stability and dissolution of OMZ in suppositories.

  • PDF

Dissoultion and Rectal Absorption of Acetaminophen from Suppositories (아세트아미노펜 좌제의 용출과 직장흡수)

  • 한정선;심창구;김신근
    • YAKHAK HOEJI
    • /
    • v.31 no.5
    • /
    • pp.286-295
    • /
    • 1987
  • The relationship between in vitro release and in vivo bioavailability of acetaminophen from suppositories was investigated. Effect of glycyrrhizin on the drug release and rectal absorption in rats was also examined. Suppositories containing 25mg of acetaminophen were prepared with Wecobee FS (fatty base) or PEG (water-soluble base) bases. The release from the suppositories were determined with USP rotating basket dissolution apparatus and with the suppository release tester. The temperature of the dissolution medium was very critical for the dissolution of acetaminophen from Wecobee FS suppositories. The bioavailability of acetaminophen was calculated from the plasma concentration-time curve after rectal administration of the suppositories to the rats. There were no significant differences in AUC following rectal administration of Wecobee FS and PEG suppositories, but the release and absorption from the Wecobee FS suppositories were faster than those from PEG suppositories. The dissolution rate obtained by the suppository release tester was better correlated with in vivo absorption rate constant than that by the USP dissolution apparatus. It suggests that the partitioning between rectal fluid and suppository base is the rate-limiting step in the rectal absorption of acetaminophen from suppositories. Glycyrrhizin was found not to affect in vitro dissolution and rectal absorption of acetaminophen.

  • PDF

Base Inhibitor와 Triblock Copolymer를 이용한 고전도도 Poly (3,4-ethylenedioxythiophene)박막의 제작

  • Choi, Sang-Il;Feng, Ma;Kim, Sung-Soo
    • Proceedings of the Korean Vacuum Society Conference
    • /
    • 2012.08a
    • /
    • pp.349-349
    • /
    • 2012
  • 산화제를 이용 기상중합법을 통해 합성되는 고전도도 Poly (3,4-Ethylenedioxythiophene)(PEDOT) 박막은 OTFT, RFID tag, 또는 연성 디스플레이 같은 분야에 다양한 응용 가능성을 가지고 있으며 이로 인해 최근에 연구가 활발히 진행되고 있다. PEDOT박막의 전극소재로써 가능성은 박막의 중합 정도와 표면 형상에 크게 좌우된다. 특히, Si-웨이퍼 기판 위에 산화제의 균일한 도포 및 산화제 자체의 높은 산도 ($pH{\leq}2$)에 따른 부반응의 억제는 기상중합법을 이용한 PEDOT박막의 합성에 있어 매우 중요하다. PEDOT의 효율적인 중합과 균일한 성장을 위해 산화제에 DUDO 와 PEG-PPG-PEG를 첨가한 혼합 산화제 용액을 제조 기상중합 방법을 통해 PEDOT박막을 제작하였다. 그 결과 산화제만을 사용하여 제작된 박막에 비해 전도도가 최대 3,660 S/cm로 향상된 PEDOT 박막이 합성되었다. 이러한 결과는 PEG-PPG-PEG가 산화제 용액의 균일 도포를 향상시키고 Base Inhibitor로 작용하는 DUDO는 PEDOT 성장 시 중합속도를 조절하고 부반응을 최소화 하여 효율적인 공액 이중 결합의 생성을 촉진한데 주로 기인한다. 따라서 그로인해 조밀하며 마이크로 스케일의 기공이 최소화된 PEDOT박막의 합성이 가능하였다. PEDOT박막의 특성 평가에는 4-point probe, optical microscopy, Field Emission-Scanning Electron Microscope, 등이 사용되었으며 또한 전도도의 향상 원인을 분석하고자 ATR-IR Spectrophotometer를 이용하여 합성된 박막의 작용기를 분석하였다. 이러한 고전도도의 PEDOT 박막이 OTFT의 전극소재로 사용된다면 OTFT소자의 성능 향상에 크게 기여 할 것으로 기대된다.

  • PDF

Rectal Absorption of Omeprazole from Syppositories in Rabbits

  • Eun, Kyong-Hoon;Lee, Yong-Hee;Shim, Chang-Koo
    • Archives of Pharmacal Research
    • /
    • v.18 no.4
    • /
    • pp.219-223
    • /
    • 1995
  • Rectal absorption of opeprazole, a proton pump inhibitor, from suppositories was studied in rabbits. The suppositories were prepared by the conventional melting method with two types of bases, water-soluble polyethylene glycol (PEG) 4000 and oil-soluble Witepsol H15 bases, and administered intractally (ir) to rabbits at a dose of 10 mg omeprazole/kg. The plasma omeprazole concentration-time profiles of the two suppositories were compared with those following intravenous 9iv) administration of the same dose. There were no significant differences between the two suppositories in bioabailabilities and peak plasma concentrations $(C_{max})$. Bioavaiabilities and $C_{max}$ of PEG- and Witpsol suppositories were 30.3 and 33.9%, and 7.0 and $5.6\mug/ml$, resepectively. However, PEG suppository showed significantly (p<0.05) shorter time to reach peak plasma concentration $(T_{max})$ mean absorption time (MAT) and mean residence time in the plasma (MRT) than Witepsol suppository. The $T_{max}$ MRT nad MAT were 25.0, 83.0 and 38.5 min for PEG syppository, but were 90.0, 122.5 and 78.0 min for Wiepsol supposiotory, respectively. These differences between thw two suppositories could be explanined by the difference in the in vitro dissolution rates between the suppositories. The dissolution of omeprazole form PEG suppository was reportedly much faster than that from Witepsol suppository. It suggests that plasma profiles of omeprazole, especially $C_{max}$ MAT and MRT, could be controlled by modifying the in vitro dissolution rate of the drug from the suppositories. Above results suggest that rectal suppository is worth developing as an alternative dosage form of omeprazole to the conventional oral preparations which need sophisticated treatments, such as enterix coating, to prevent acid degradation of the drug in the stomach fluid.

  • PDF

Structural and thermal characteristics of photocrosslinked silk fibroin - PEG hydrogel

  • Jo, You-Young;Lee, Kwang-Gill;Bragg, John C.;Lin, Chien-Chi;Kweon, HaeYong
    • International Journal of Industrial Entomology and Biomaterials
    • /
    • v.32 no.1
    • /
    • pp.35-40
    • /
    • 2016
  • Hydrogels are crosslinked hydrophilic matrices for a variety of biomedical applications. Silk fibroin (SF), one of typical natural biomaterials, has been explored as base material for hydrogel. Photocrosslinked SF hydrogel containing poly(ethylene glycol) (PEG) was formulated through visible light initiated thiol-acrylate photopolymerization. The morphological, structural and thermal properties of SF - PEG hydrogel was investigated through scanning electron microscopy, X-ray diffractometry, thermogravimetry, and differential scanning calorimetry. The morphology of SF hydrogel showed dot and uneven surface with network cross-section. X-ray diffraction curves showed that the specific diffraction peaks of PEG were not changed by the intensity of the peaks were affected by sonication. Thermo-degradation behavior of SF - PEG hydrogel sonicated was significantly affected and became complex pattern compared to unsonicated ones. However, the melting endothermic temperature of SF - PEG hydrogel was not changed but the crystalline enthalpy was decreased by gelation and sonication.

Base Inhibitor를 이용한 고전도도의 PEDOT박막의 제작

  • Lee, Joon-Woo;Choi, Byoung-Blk;Choi, Sang-Il;Kim, Sung-Soo
    • Proceedings of the Korean Vacuum Society Conference
    • /
    • 2012.02a
    • /
    • pp.442-442
    • /
    • 2012
  • PEDOT[Poly(3,4-Ethylenedioxythiophene)]박막의 제작은 산화촉매제를 이용한 기상중합(Vapor Phase Polymerization)방법을 통해 최근 활발히 연구되어 지고 있다. 기상중합된 PEDOT박막의 특성은 박막의 중합의 정도와 성장 형상에 따라 그 특성이 크게 좌우된다. PEODT박막의 효율적인 중합에 있어 산화촉매제의 균일한 도포는 매우 중요하다. PEDOT의 효율적인 중합과 균일도포를 위해 산화촉매제에 DUDO와 PEG-PPG-PEG를 첨가한 혼합용액을 제작 VPP방법을 통해 PEDOT박막의 제작을 시도하였다. 그 결과 spin-coating 시 산화촉매 혼합용액의 균일한 도포가 관찰 되었으며 산화촉매제만 사용하여 제작된 박막에 비해 전도도와 막질이 향상된 PEDOT박막이 제작되었다. 이러한 결과는 산화촉매용액에 첨가된 PEG-PPG-PEG와 DUDO의 영향으로 PEG-PPG-PEG는 oxdiant용액의 균일 도포를 도왔으며 Inhibitor로 작용하는 DUDO는 PEDOT성장에 있어 불균일 결정성장을 억제하여 조밀한 PEDOT 박막 성장을 도운 것으로 생각된다. PEDOT 박막의 특성평가에는 Field Emission-Scanning Electron Microscopy, 4-Pointprobe, Optical microscopy 등이 사용되었다. 이러한 고전도도의 PEDOT박막을 OTFT의 전극소재로 사용한다면 OTFT소자의 성능 향상에있어 크게 기여 할 것으로 기대된다.

  • PDF

Synthesis and Hydrolysis of Ketoprofen Prodrug Conjugated to Poly(Ethylene Glycol) (케토프로펜-폴리에틸렌글리콜 전구약물의 합성 및 가수분해)

  • Lee, Se-Hee;Kim, Hee-Doo;Oh, Seaung-Youl
    • Journal of Pharmaceutical Investigation
    • /
    • v.33 no.1
    • /
    • pp.37-43
    • /
    • 2003
  • The objective of this study is to prepare ketoprofen (KP) - poly(ethylene glycol) (PEG) conjugates and to investigate their degradation kinetics. KP-PEG conjugates were synthesized from KP and PEG methy1ester by esterification in the presence of DCC. The KP-PEG conjugates (KPEG) were characterized by IR and $^{1}H-NMR$ spectroscopy. The hydrolysis of KPEG with time was studied using HPLC by simultaneous quantification of KP and KPEG. The hydrolysis rate constant was high at low and high pHs, and showed minimum at pH 4 and 5. As the size of KPEG increases, hydrolysis rate increased. The slope of degradation rate profile suggests that catalytic reaction seems to occur by specific acid/base catalysis. These results suggest that KPEG could be used as a prodrug for KP, which releases KP slowly in the body.

Effects of Suppository Bases on Bioavailability of Aspirin Suppositories (좌제기제가 아스피린 좌제의 생체내이용율에 미치는 영향)

  • Kim, Yong-Hyun;Lee, Jin-Hwan;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
    • /
    • v.18 no.2
    • /
    • pp.61-67
    • /
    • 1988
  • The influence of different suppository bases on the dissolution, and the bioavailability of aspirin suppositories in rabbits and humans was investigated using Witepsol H15 (WIT), WIT-Tween 80 (TWE), WIT-sodium lauryl sulfate (SLS), polyethylene glycol (PEG), hollow WIT (WIT-HOLL) and capsule incorporated into WIT (WIT-CAP). The results obtained were as follows: 1) Dissolution rates of aspirin suppositories with different bases in distilled water were faster in the order of WIT-TWE >WIT-SLS >PEG >WIT-HOLL >WIT >WIT-CAP. 2) The maximum blood levels $(C_{max})$ of aspirin in rabbits and humans were highest in WIT-TWE and WIT-SLS bases, but $C_{max}$ from WIT base was lower than that in oral administration of aspirin suspension. 3) The times reaching the maximum blood levels $(T_{max})$ in rabbits were 1 hr for oral administration, 1.5-2.5 hr for WIT-TWE, WIT-SLS, PEG, and WIT bases, and 2.5-4.0 hr for WIT-HOLL and WIT-CAP bases, but $T_{max}$ in humans were 1 hr for oral administration and WIT-TWE base, and 2-4 hr for WIT and WIT-HOLL bases. 4) Relative bioavailability (RBA) of aspirin suppositories in rabbits was higher in WIT-SLS, WIT-TWE and PEG bases than that in oral administration, and RBA of aspirin suppositories in humans was higher in the order of WIT-TWE >PEG >WIT-HOLL >oral >WIT bases tested. 5) Good correlation between dissolution rates and $C_{max}$ was obtained: y = 0.60x+32.23 (r = 0.96) for rabbits, and y = 0.60x+35.74 (r = 0.97) for humans.

  • PDF

Pharmacokinetics of Omeprazole from Rectal Suppositories (오메프라졸 함유 직장좌제의 약물속도론적 연구)

  • 이창현;황성주;권광일;이계주
    • YAKHAK HOEJI
    • /
    • v.37 no.5
    • /
    • pp.427-436
    • /
    • 1993
  • The pharmacokinetics and relationship between in vitro dissolution and in vivo fraction absorbed were investigated after intravenous(iv) injection of omeprazole(OMZ), oral administration of OMZ capsules and rectal administration of 8 types of suppositories. The plasma concentration of OMZ (C$_{p}$)-time (t) curve after iv. administration fitted a two-compartment open model and the equation which best fitted the pharmacokinetics of OMZ was $C_{p}$ = 13.936 $e^{-8.78t}$+2.973 $e^{-0.716t}$. The bioavailabilities of OMZ in Witepsol H15 base (Supp-2) and PEG 4000 base (Supp-6) suppositories were 40.7% and 33.4%, respectively, which are higher(p<0.001) than 13% of oral administration of capsule. The avoidance fractions of the first-pass metabolism for Supp-2 and Supp-6 suppositiories were 31.8% and 23.4%, respectively, suggesting that the rectal application of OMZ may be a more adequate route of administration than oral one.

  • PDF