• 제목/요약/키워드: Oral absorption

검색결과 316건 처리시간 0.026초

그리세오풀빈-페노바르비탈 상호작용 (I) -페노바르비탈 전처리 Rat에 있어서 그리세오풀빈의 생체내 동태- (Griseofulvin-Phenobarbital Interaction (I) -Pharmacokineties of Griseofulvin in Phenobarbital-pretreated Rats-)

  • 고익배;신상철;이용복
    • 약학회지
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    • 제30권6호
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    • pp.288-293
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    • 1986
  • Effects of phenobarbital on the pharmacokinetics of griseofulvin were studied in rats. Phenobarbital was administered orally for five days at the dose of 75mg/kg/day. Absolute bioavailability of oral griseofulvin was significantly(p<0.005) reduced but total clearance(CL$_s$ was not changed by phenobarbital pretreatment. Absorption rate constant(K$_a$ and maximum plasma concentration(C$_{max}$) were significantly(p<0.05) reduced, and time to reach maximum plasma concentration(T$_{max}$) of griseofulvin was significantly(p<0.05) increased by phenobarbital pretreatment. Changed pharmacokinetics of griseofulvin seemed not to be due to induced enzyme activity by phenobarbital but to reduced GI absorption of griseofulvin.

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가토에 있어서 Capsaicin의 흡수 및 배설에 관한 연구 (Study on the Absorption and Excretion of Capsaicin in Rabbits)

  • 김낙두;박찬용
    • 약학회지
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    • 제25권3호
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    • pp.101-108
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    • 1981
  • Quantitative determination of capsaicin in biological fluid was investigated. The pharmacokinetic study of capsaicin in rabbits was performed by high-pressure liquid chromatography, equipped with a microparticulate reversed-phase column and a fixed wavelength detector. Elution was carried out using methanolwater(70:30). It allows the quantitative determination at 8-400 ng level. When single dose of capsaicin(4mg/kg) was given to rabbits intravenously, the elimination phase was extremely short with average half-life to 17.35 minute. Urine excretion of capsaicin itself during first 2 hours after intravenous administration (4mg/kg) was 0.004-0.04% of the administered amount. The maximum plasma concentration of capsaicin after oral administration (300mg/kg) was $4{\times}10^{-7}$g/ml at 40 minutes. The $LD_{50}$ of capsaicin in mouse was 0.40mg/kg (i.v.) and 47.2 mg/kg (p.o.) which was determined by Litchfield and Wilcoxon's method, suggesting that the gastrointestinal absorption of capsaicin is poor.

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아프타성 구내염 치료용 구강 패취의 설계 : 약물층 (Design of Oral Patches for the Treatment of Aphthous Stomatitis : Drug Layer)

  • 이규현;박은석;지상철
    • Journal of Pharmaceutical Investigation
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    • 제25권4호
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    • pp.339-345
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    • 1995
  • For the effective treatment of aphthous stomatitis, the matrix type mucoadhesive patches containing triamcinolone acetonide have been formulated. The drug layer was obtained by drying the polymer gel which was prepared with carbomer 934P, ammoniomethacrylate copolymer, titanium dioxide and polyethylene glycol 400. The effects of the content of additives on physical characteristics of the polymer gel and the drug layer were evaluated. The addition of carbomer increased the yield point and the zero-shear viscosity of polymer gel as well as the thickness, the water absorption ratio, the adhesive time and $T_{50%}$ of drug layer. The adhesive time and the water absorption ratio of drug layer were also improved by the addition of ammoniomethacrylate copolymer, but the addition of titanium dioxide had decreased the zero-shear viscosity of polymer gel and the adhesive time of drug layer.

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병태 동물에서 암피실린의 생물약제학적 연구 (A Biopharmaceutical Study on Ampicillin in Pathological Animals)

  • 이진환
    • 약학회지
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    • 제22권4호
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    • pp.226-232
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    • 1978
  • It was to investigate the absorption, excretion, protein binding of ampicillin in the pathological animals pretreated with carbon tetrachloride and mercuric chloride. The absorption of ampicillin was not affected in rats with damaged liver and kidney as compared with that of normal rats. The blood level of ampicillin after oral administration was increased significantly in rabbits with damaged kidney and liver. The blood level of ampicillin in rabbit with damaged kidney was more increased than that in rabbits with damaged liver. In severly damaged rabbits, it was more increased than that of mildly damaged rabbits. Urinary excretion of ampicillin in pathological animals was more inhibited than that of ampicillin in normals. Hepatic excretion of ampicillin was accelerated in rabbits with damaged kidney. However, in rabbits with damaged liver, it was inhibited as compared with that in normals. Protein binding of ampicillin was slightly enhanced by the various concentration of carbon tetrachloride and mercuric chloride, respectively. The results suggest that the increase of blood level of ampicillin in pathological animals was due to the inhibition of renal excretion.

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카르보폴-젤라틴의 상분리법을 이용한 Acyclovir 마이크로캅셀 현탁액의 제조 및 생물학적 평가 (Biological Evaluation of Acyclovir Microcapsule Suspension Prepared by Carbopol-Gelatin Coacervation)

  • 조진호;한양희;이정우;최영욱
    • Journal of Pharmaceutical Investigation
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    • 제23권3호
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    • pp.139-144
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    • 1993
  • Microencapsulation of acyclovir, an effective antiviral agent which acts as a specific inhibitor of herpes DNA polymerase, by carbopol-gelatin complex coacervation has been carried out to develop an oral controlled release preparation, which could improve the absorption characteristics in GI tract. After dissolving carbopol and gelatin separately in distilled water at $40^{\circ}C$, gelatin solution was mixed with carbopol solution while stirring at the same temperature. The pH of the mixture was lowered gradually by dropwise addition of 10% HCI with continuous stirring, and then, at pH 3.5, positively charged gelatin molecules were attracted to negatively charged carbopol. These coacervation processes were observed by optical microscopy during preparation. Plasma concentrations of acyclovir in rats after an oral administration of microcapsule suspension were assayed by HPLC, and pharmacokinetic parameters were calculated based on the model-independent analyses. Two standard formulations, oral solution and intravenous bolus injection, were used as references to compare the bioavailability. It has been revealed that $C_{max}$, $T_{max}$, and MRT of microcapsule suspension were greater than those of oral solution, which results in about two-fold increases in bioavailability. Therefore, in conclusion, the carbopol-gelatin microcapsule of acyclovir might be evaluated as an effective oral controlled release preparation which could increase the bioavailability of acyclovir.

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Volumetric quantification of bone-implant contact using micro-computed tomography analysis based on region-based segmentation

  • Kang, Sung-Won;Lee, Woo-Jin;Choi, Soon-Chul;Lee, Sam-Sun;Heo, Min-Suk;Huh, Kyung-Hoe;Kim, Tae-Il;Yi, Won-Jin
    • Imaging Science in Dentistry
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    • 제45권1호
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    • pp.7-13
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    • 2015
  • Purpose: We have developed a new method of segmenting the areas of absorbable implants and bone using region-based segmentation of micro-computed tomography (micro-CT) images, which allowed us to quantify volumetric bone-implant contact (VBIC) and volumetric absorption (VA). Materials and Methods: The simple threshold technique generally used in micro-CT analysis cannot be used to segment the areas of absorbable implants and bone. Instead, a region-based segmentation method, a region-labeling method, and subsequent morphological operations were successively applied to micro-CT images. The three-dimensional VBIC and VA of the absorbable implant were then calculated over the entire volume of the implant. Two-dimensional (2D) bone-implant contact (BIC) and bone area (BA) were also measured based on the conventional histomorphometric method. Results: VA and VBIC increased significantly with as the healing period increased (p<0.05). VBIC values were significantly correlated with VA values (p<0.05) and with 2D BIC values (p<0.05). Conclusion: It is possible to quantify VBIC and VA for absorbable implants using micro-CT analysis using a region-based segmentation method.

Effects of fibrin glue on bone formation in combination with deproteinized bone xenografts in humans

  • Kim, Moon-Su;Kim, Su-Gwan;Lim, Sung-Chul;Kim, Hak-Kyun;Moon, Seong-Young
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제34권1호
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    • pp.19-27
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    • 2008
  • Thirty-six sinus grafts were performed in 34 patients with an alveolar crest bone height in the posterior maxilla of 3 to 5 mm before grafting. The sinuses were grafted using Bio-Oss alone or mixed with fibrin glue. Group 1 was the control group and included 25 patients who received a xenograft mixed in saline. Group 2 comprised 9 patients who received a xenograft and fibrin glue. The study was further subdivided at the time of 9 months. This histologic study evaluated by hematoxylin-eosin (H&E) and histomorphometric analysis whether fibrin glue in combination with Bio-Oss enhances bone regeneration in sinus floor elevation in humans. The new bone formation was better in Group 2 than in Group 1, but the difference was not significant. The absorption of the graft material was faster in Group 2 than in Group 1, in the short term, but better in Group 1 over the long term, although the difference was not significant. Lamellar bone was formed earlier in Group 1 compared to Group 2, but the difference was not significant. Overall, the surgery site stabilized earlier with new bone formation in Group 2 than in Group 1, but the difference was not significant. Combining a fibrin sealant and Bio-Oss could lead to improved scaffolds for bone tissue engineering based on the synergistic effects of the biomaterials. Therefore, Bio-Oss or Bio-Oss plus Tisseel may be used depending on the situation.

Effect of Gongjindan, a Polyherbal Formula on the Pharmacokinetics Profiles of Sorafenib in Male SD Rats (1) - Single Oral Combination Treatment of Sorafenib 50mg/kg with Gongjindan 100mg/kg within 5min -

  • ;;;;;;구세광;이영준
    • 대한예방한의학회지
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    • 제18권2호
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    • pp.89-100
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    • 2014
  • Objective : The co-administration effects of Gongjindan (GJD) on the pharmacokinetics (PK) of sorafenib were observed as a process of the comprehensive and integrative medicine. Methods : After sorafenib treatment, GJD was administered within 5 min. The plasma were collected at 30min before administration, 30min, 1, 2, 3, 4, 6, 8 and 24hrs after end of GJD treatment, and plasma concentrations of sorafenib were analyzed using LC-MS/MS methods. PK parameters of sorafenib ($T_{max}$, $C_{max}$, AUC, $t_{1/2}$ and $MRT_{inf}$) were analysis as compared with sorafenib single administered rats. Results : The absorption of sorafenib were significantly increased at 30min, 1, 6 and 6hrs after co-administration with GJD as compared with sorafenib single treated rats. Accordingly, the $AUC_{0-t}$ (47.20%) of sorafenib was significantly increased but $t_{1/2}$ (-30.63%) and $MRT_{inf}$ (-34.11%) in co-administered rats were non-significantly decreased. These findings are considered as direct evidences that GJD increased the oral bioavailability of sorafenib through increase of the absorption, when they co-administered within 5min. Conclusion : Based on the results, co-administration of GJD increased the oral bioavailability of sorafenib through increase of the gastrointestinal absorption. It is considered that the more detail pharmacokinetic studies should be tested to conclude the effects of GJD on the pharmacokinetics of sorafenib, when they were co-administered, like the effects after co-administration with reasonable intervals considering the $T_{max}$ of sorafenib (about 3.5hr-intervals) and after repeated co-administrations.Hence, concomitant uses of GJD with sorafenib may require close monitoring for potential drug interactions.

수온과 세균 감염이 나일 틸라피아(Oreochromis niloticus)의 oxolinic acid 흡수와 배설에 미치는 영향 (Effect of Temperature and Bacterial Infection on the Absorption and Elimination of Oxolinic Acid in Nile tilapia (Oreochromis niloticus))

  • 김명석;박성우;허민도;정현도
    • 한국수산과학회지
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    • 제31권5호
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    • pp.677-684
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    • 1998
  • Oxolinic acid (OA)를 경구 (80 mg/kg body weight)와 약욕 (20mg/$\ell$)의 방법으로 각기 다른 생리적 상태에 있는 나일 틸라피아 (Oreochromis niloticus)에 투여한 후 어류의 각 장기 내에 분포하는 OA의 농도를 bioassay 법으로 분석함으로써 어류의 생리적 상태가 OA 흡수, 분포 및 배설에 미치는 영향을 조사하였다. 사육수의 온도를 $15^{\circ}C$$25^{\circ}C$로 한 실험구에 OA를 경구로 투여한 후 약물의 흡수와 배설을 비교해 보면, $15^{\circ}C$ 실험구에서의 약물 흡수와 배설속도는 $25^{\circ}C$ 실험구보다 느렸지만 각장기 내 최고농도는 $25^{\circ}C$ 실험구와 유의성 있는 차이를 보이지 않았다. 그러나 OA를 약욕법으로 투여하는 경우 흡수 및 배설속도 모두 온도차에 의한 명확한 차이를 보여 주었다. 약물투여의 실질적인 목표가 되는 병어에서의 약물분포를 분석하기 위하여 E. tarda에 인위감염된 어류에 OA를 경구와 약욕의 방법으로 투여하였을 때 각조직 내의 약물 분포 및 농도의 변화는 건강어에 대비하여 구별됨을 확인하였다.

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조피볼락, Sebastes schlegeli에 경구투여된 oxolinic acid의 약물동태에 미치는 수온의 영향 (Effects of temperature on pharmacokinetics of oxolinic acid in black rockfish, Sebastes schlegeli following oral administration)

  • 정승희;김진우;서정수;지보영;박명애
    • 한국어병학회지
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    • 제23권2호
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    • pp.221-227
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    • 2010
  • Oxolinic acid를 사육수온($13{\pm}1.5^{\circ}C$, $23{\pm}1.5^{\circ}C$)에 따라서 조피볼락(평균체중 500 g)에 60 mg/kg의 농도로 1회 경구 투여한 다음, 경시적인 혈청내 잔류농도를 분석하였다. $23{\pm}1.5^{\circ}C$의 경우 투여 후 30시간째($0.60{\mu}g/ml$)에 최대혈중농도에 도달하였다. $13{\pm}1.5^{\circ}C$의 경우 투여 후 10시간째($2.22{\mu}g/ml$) 최대혈중농도에 도달하였다. OA의 조피볼락 혈중내 흡수양상과 소실정도는 사육수온에 크게 영향을 받았다. Two-compartment model로 해석하여 WinNonlin program을 이용, 약물동태학적 매개변수(parameter)를 조사하였다. $23{\pm}1.5^{\circ}C$의 경우, 혈장농도-시간곡선하 면적(AUC)은 $42.16{\mu}g{\cdot}h/ml$, 혈중최고농도의 도달시간(Tmax)은 26.13 h, 혈중최고농도(Cmax)는 $0.43{\mu}g/ml$, 예상약물소실시간(Et)은 230시간으로 계산되었다. $13{\pm}1.5^{\circ}C$의 경우, AUC는 $131.98{\mu}g{\cdot}h/ml$, Tmax는 8.81 h, Cmax는 $2.04{\mu}g/ml$, Et는 492시간으로 계산되었다.