• 제목/요약/키워드: Dissolution enhancement

검색결과 50건 처리시간 0.024초

시클로덱스트린과 소염진통제 간의 포접복합체에 관한 연구(I): 2-히드록시프로필-${\beta}$-시클로덱스트린에 의한 이부프로펜의 용출 증가 (Inclusion Complex of Analgesic and Antiinflammatory agents with Cyclodextrins (I): Enhancement of Dissolution of Ibuprofen by $2-Hydroxypropyl-{\beta}-cyclodextrin$)

  • 오인준;박정규;이용복;신상철
    • Journal of Pharmaceutical Investigation
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    • 제23권1호
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    • pp.11-18
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    • 1993
  • Inclusion complex of ibuprofen with $2-Hydroxypropyl-{\beta}-cyclodextrin\;(HP-{\beta}-CD)$ in aqueous solution and in the solid state was evaluated by the solubility method and the instrumental analysis such as infrared spectroscopy, thermal analysis and x-ray diffractometry. The aqueous solubility of ibuprofen was increased linearly with the increase in the concentration of $HP-{\beta}-CD$, showing an $A_L$ type phase solubility diagram. The results showed that the dissolution rate of ibuprofen was significantly increased by complexation with $HP-{\beta}-CD$. $Ibuprofen-HP-{\beta}-CD$ complex enhanced the mean plasma concentration levels and the area under plasma concentration-time curve after oral administration compared to those of the drug alone. It is concluded that the complex of ibuprofen with $HP-{\beta}-CD$ increases the dissolution rate and improves the bioavailability of the ibuprofen by the formation of a water-soluble complex.

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Enhancement of Dissolution from Pharmaceutical Preparation of Hydrophobic Drugs ( I ) -Characteristics of Sulpiride-Polyethylene Glycol Coprecipitates-

  • Ku, Young-Soon
    • Journal of Pharmaceutical Investigation
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    • 제12권4호
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    • pp.145-152
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    • 1982
  • Data from IR spectroscopy and X-ray diffractometry were used for the characterization of sulpiride polyethylene glycol coprecipitates related with polymorphism of sulpiride. Sulpiride Form II transformed to Form I during coprecipitating with polyethylene glycol and the transformation rate is increased in proportion to molecular size of polyethylene glycol and the content of polyethylene glycol in coprecipitate.

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

  • 이창현;황성주;오세종;이계주
    • 약학회지
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    • 제37권4호
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    • pp.370-382
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    • 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.

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담즙산염과 2-히드록시프로필-${\beta}$-시클로덱스트린을 이용한 아토르바스타틴칼슘의 용출 및 십이지장 점막 투과 증진 (Enhanced Dissolution and Duodenal Permeation of Atorvastatin Calcium Using Bile Salt and 2-Hydroxypropyl-${\beta}$-Cyclodextrin)

  • 최지원;전인구
    • 약학회지
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    • 제56권3호
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    • pp.164-172
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    • 2012
  • This study was aimed to increase the solubility, dissolution and permeation rates of atorvastatin calcium (ATC) using bile salt and/or 2-hydroxypropyl-${\beta}$-cyclodextrin ($HP{\beta}CD$). From solubility studies, sodium deoxycholate (SDC) among bile salts studied was found to have the highest solubilizing effect on ATC ($4.4{\pm}0.4$ mg/ml), and the order of increasing solubility was SDC>sod. cholate>sod. glycocholate>sod. taurodeoxycholate>sod. taurocholate>conjugated bile acid. ATC solid dispersions were prepared at various ratios of drug to SDC and/or $HP{\beta}CD$, and evaluated by differential scanning calorimetry (DSC), dissolution studies and dissolution-permeation studies. DSC curves showed amorphous state of ATC in the physical mixture and solid dispersion. Dissolution rates of ATC-SDC solid dispersions and physical mixture were markedly increased at pH 6.8, but decreased at pH 1.2 with greater proportions of SDC due to the precipitation of SDC, compared with that of drug alone. On the other hand, dissolution rates of ATC-$HP{\beta}CD$ solid dispersion and physical mixture at pH 1.2 were varied with the ratio of drug to carriers. From duodenal permeation studies, it was found that fluxes of ATC (donor dose: 0.5 mg/3.5 ml) in the presence of 25 mM sodium glycocholate, SDC, sod. cholate and sod. taurocholate $(5.7{\pm}0.9$, $5.6{\pm}0.9$, $4.8{\pm}0.7$ and $4.6{\pm}0.9\;{\mu}g/cm^2/hr$, respectively) were enhanced, compared with drug alone ($3.4{\pm}0.9\;{\mu}g/cm^2/hr$). In the dissolution-permeation studies, 1 : 9 : 10 (w/w) ATC-SDC-$HP{\beta}CD$ solid dispersion increased the flux 2.2 times, compared with 1 : 5 : 4 (w/w) ATC-lactose-corn starch mixture as control. In conclusion, solid dispersions with bile salt and $HP{\beta}CD$ were found to be an effective means for increasing the dissolution and permeation rates of ATC.

Performance Enhancement by Adaptation of Long Term Chronoamperometry in Direct Formic Acid Fuel Cell using Palladium Anode Catalyst

  • Kwon, Yong-Chai;Baik, S.M.;Han, Jong-Hee;Kim, Jin-Soo
    • Bulletin of the Korean Chemical Society
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    • 제33권8호
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    • pp.2539-2545
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    • 2012
  • In the present study, we suggest a new way to reactivate performance of direct formic acid fuel cell (DFAFC) and explain its mechanism by employing electrochemical analyses like chronoamperometry (CA) and cyclic voltammogram (CV). For the evaluation of DFAFC performance, palladium (Pd) and platinum (Pt) are used as anode and cathode catalysts, respectively, and are applied to a Nafion membrane by catalyst-coated membrane spraying. After long DFAFC operation performed at 0.2 and 0.4 V and then CV test, DFAFC performance is better than its initial performance. It is attributed to dissolution of anode Pd into $Pd^{2+}$. By characterizations like TEM, Z-potential, CV and electrochemical impedance spectroscopy, it is evaluated that such dissolved $Pd^{2+}$ ions lead to (1) increase in the electrochemically active surface by reduction in Pd particle size and its improved redistribution and (2) increment in the total oxidation charge by fast reaction rate of the Pd dissolution reaction.

고속 교반을 이용한 기-액 혼합 플라즈마방전 시스템의 성능 향상 (Performance Enhancement of Gas-Liquid Mixed Plasma Discharge System using High Speed Agitation)

  • 박영식
    • 한국환경과학회지
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    • 제26권6호
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    • pp.711-717
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    • 2017
  • Dielectric Barrier Discharge (DBD) plasma is a new technique for use in environmental pollutant degradation, which is characterized by the production of hydroxyl radicals as the primary degradation species. Due to the short lifetime of the chemically active species generated during the plasma reaction, the dissolution of the plasma gas has a significant effect on the reaction performance. The plasma reaction performance can be enhanced by combining the basic plasma reactor with a homogenizer system in which the bubbles are destroyed and turned into micro-bubbles. For this purpose, the improvement of the dissolution of plasma gas was evaluated by measuring the RNO (N-dimethyl-4-nitrosoaniline, an indicator of the generation of OH radicals). Experiments were conducted to evaluate the effects of the diameter, rotation speed, and height of the homogenizer, pore size, and number of the diffuser and the applied voltage on the plasma reaction. The results showed that the RNO removal efficiency of the plasma reactor combined with a homogenizer is two times higher than that of the conventional one. The optimum rotor size and rotation speed of the homogenizer were 15.1 mm, and 19,700 rpm, respectively. Except for the lowest pore size distribution of $10-16{\mu}m$, the pore size of the diffuser showed little effect on RNO removal.

오메프라졸의 제제화 및 평가 (Stability and Dissolution Enhancement of Omeprazole by Pharmacentical Formulation)

  • 지웅길;이계원;전운종
    • Journal of Pharmaceutical Investigation
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    • 제22권4호
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    • pp.281-287
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    • 1992
  • Omeprazole (OMZ) is very unstable in acidic solution, which selectively inhibit the release of the gastric juice in the gastric mucosa, In order to stabilize (OMZ) in oral solid dosage form, the enteric-coated microcapsules and compression-coated OMZ tablets containing lysine or arginine as stabilizer were prepared and their dissolution and stability test were performed. The haif life of OMZ microcapsules containing arginine was 194 days at $30^{\circ}C$ and OMZ was completely released in 60 min. The half-lives of enteric coated and non-coated compression-coated OMZ tablets with lysine were 292 and 95 days at $30^{\circ}C$, respectively. The half-lives of enteric coated and non-coated compression-coated tablets with arginine were 1752 and 293 days at $30^{\circ}C$, respectively, and OMZ were released completely in 20 min in the 2nd fluid of K.P.VI. Consequently, the enteric-coated compression-coated OMZ tablets with arginine as stabilizer provided a good formulation for oral solid dosage form.

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흰쥐에 경구 투여시 히드록시프로필-베타-시클로덱스트린과 니트렌디핀 고체분산에 의한 생체이용률 증가 (Enhancement of Nitrendipine Bioavailability in Rats by its Solid Dispersion with $Hydroxypropyl-{\beta}-Cyclodextrin$ after Oral Administration)

  • 용철순
    • Journal of Pharmaceutical Investigation
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    • 제27권4호
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    • pp.295-301
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    • 1997
  • Nitrendipine, a slightly soluble calcium channel blocking agent forms a solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$, which exhibits better dissolution characteristics than the uncomplexed drug. The dissolution rate of nitrendipine was markedly increased in solid dispersion system in pharmacopeial disintegration media at pH 1.2 and pH 6.8. Four different dosage forms of nitrendipine were administered to rats: (a) nitrendipine in the solution of PEG 400; (b) nitrendipine solid dispersion system with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 by solvent evaporation method and administered in capsule form; (c) physical mixture of nitrendipine with $hydroxypropyl-{\beta}-cyclodextrin$ in a molar ratio of 1:2 and administered in capsule form; (d) nitrendipine alone administered in capsule form. Relative bioavailability after the oral administration of various dosage forms to rats with a dose of 10 mg/kg equivalent to nitrendipine was compared with that of nitrendipine in the solution of PEG 400. The AUC of solid dispersion was significantly bigger than that of nitrendipine powder. $T_{max}$ of solid dispersion was significantly shorter and $C_{max}$ was higher than that of nitrendipine powder. These results indicate that the bioavailability of nitrendipine could be improved markedly by inclusion complexation. An interesting correlation also appears to exist between the in vitro dissolution data and the area under the plasma concentration-time curves.

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Effect of Solubilizing and Microemulsifying Excipients in Polyethylene Glycol 6000 Solid Dispersion on Enhanced Dissolution and Bioavailability of Ketoconazole

  • Heo, Min-Young;Piao, Zong-Zhu;Kim, Tae-Wan;Cao, Qing-Ri;Kim, Ae-Ra;Lee, Beom-Jin
    • Archives of Pharmacal Research
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    • 제28권5호
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    • pp.604-611
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    • 2005
  • Polyethylene glycol (PEG) 6000-based solid dispersions (SDs), by incorporating various pharmaceutical excipients or microemulsion systems, were prepared using a fusion method, t o compare the dissolution rates and bioavailabilities in rats. The amorphous structure of the drug in SDs was also characterized by powder X-ray diffractometry (XRD) and differential scanning calorimetry (DSC). The ketoconazole (KT), as an antifungal agent, was selected as a model drug. The dissolution rate of KT increased when solubilizing excipients were incorporated into the PEG-based SDs. When hydrophilic and lipophilic excipients were combined and incorporated into PEG-based SDs, a remarkable enhancement of the dissolution rate was observed. The PEG-based SDs, incorporating a self microemulsifying drug delivery system (SMEDDS) or microemulsion (ME), were also useful at improving the dissolution rate by forming a microemulsion or dispersible particles within the aqueous medium. However, due to the limited solubilization capacity, these PEG-based SDs showed dissolution rates, below 50% in this study, under sink conditions. The PEG-based SD, with no pharmaceutical excipients incorporated, increased the maximum plasma concentration (C$_{max}$) and area under the plasma concentration curve (AUC$_{0-6h}$) two-fold compared to the drug only. The bioavailability was more pronounced in the cases of solubilizing and microemulsifying PEG-based SDs. The thermograms of the PEG-based SDs showed the characteristic peak of the carrier matrix around 60$^{\circ}C$, without a drug peak, indicating that the drug had changed into an amorphous structure. The diffraction pattern of the pure drug showed the drug to be highly crystalline in nature, as indicated by numerous distinctive peaks. The lack of the numerous distinctive peaks of the drug in the PEG-based SDs demonstrated that a high concentration of the drug molecules was dissolved in the solid-state carrier matrix of the amorphous structure. The utilization of oils, fatty acid and surfactant, or their mixtures, in PEG-based SD could be a useful tool to enhance the dissolution and bioavailability of poorly water-soluble drugs by forming solubilizing and microemulsifying systems when exposed to gastrointestinal fluid.

CZ 방법에 의해 성장된 실리콘에서 산소 석출물의 성장/감소에 관한 모델 및 해석 (Modeling and Analysis for the Growth/Dissolution of Oxygen Precipitation in CZ-grown Silicon)

  • 고봉균;곽계달
    • 전자공학회논문지D
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    • 제35D권10호
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    • pp.29-38
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    • 1998
  • 본 논문에서는 CZ 방법으로 성장된 실리콘에서 임의의 열처리 과정 또는 VLSI 공정중에 발생하는 산소석출물(oxygen precipitates)의 성장 및 감소에 대한 모델을 유도하고 수치해석법으로 시뮬레이션을 수행하여 모델에 대한 타당성을 검증하였다. 확산제한 성장법칙(diffusion-limited growth law)과 DBET(detailed balance equilibrium theory)를 이용하여 산소 석출물의 성장률과 감소율을 유도하고 이를 CREs(chemical rate equations)와 PFE (Fokker-Planck equation)이 결합된 식에 적용하여 수치해석법으로 풀었다. 또한 어닐링 분위기에 따라 표면에서 일어나는 현상을 달리 고려해야 하는데, 특히 O₂가스 분위기에서는 산화막이 성장되는 조건을 고려해야 하므로 산화막 성장 모델과 산소 용해도 증가등의 영향을 고려하였다. 이 방법으로 기존의 결과보다 더 정확하게 깊이에 따른 산소 농도의 분포와 산소 석출물의 밀도분포 함수를 계산할 수 있었다.

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