• Title/Summary/Keyword: Drug absorption

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Current Methodologies for Membrane Permeability Assessment

  • Shin, Beom-Soo;Youn, Yu-Seok;Jeong, Seong-Hoon;Park, Eun-Seok;Lee, Mann-Hyung;Yoo, Sun-Dong
    • Journal of Pharmaceutical Investigation
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    • v.40 no.spc
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    • pp.19-31
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    • 2010
  • Orally administrated drugs permeate the biological membrane by various transport mechanisms. The oral absorption potential is closely related to the physicochemical properties of the drug and interaction with the physiological factors surrounding the site of absorption. Assessment of the drug membrane permeability is an integral part of the early stage drug developmental process. Appropriate selection of the permeability screening method at the right stage of drug development process is important in achieving successful developmental outcomes. This review aims at introducing currently available in vitro and in vivo screening methods for the membrane permeability assessment.

Studies on the Drug Absorption in Rat Intestine Effect on Acrid Condiments for the Absorption of Drugs (Rat 소장에서의 의약품(醫藥品)의 흡수(吸收)에 관(關)한 연구(硏究) 의약품(醫藥品)의 흡수(吸收)에 미치는 신미료(辛味料)의 영향(影響))

  • Park, Jung-Yong;Woo, Chong-Hak;Kim, Shin-Keun;Han, Se-Ho
    • Journal of Pharmaceutical Investigation
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    • v.1 no.1
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    • pp.3-12
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    • 1971
  • Many of the studies on absorption and excretion of drugs have been reported in the field of pharmaceutics, but the effect of acrid condiments for the absorption of drugs has not been. Hereupon, the authors investigated them in small intestine canal of rat in situ. In this experiment, aminopyrine, sulfadiazine and salicylic acid appended acrid condiments such as garlic, red pepper and pepper showed more increased absorption than constituted drugs. In particular, pepper showed the most increased than pepper, red pepper and garlic take lower absorption than pepper. When two drugs and over exist at a time, the efficacy is different from each other. Therefore, it is necessary to research of each circumstances administering one drug or compound drugs. We considers that we are abet to get safe and effectivecopound preparations when we studies on the effect. of drug action.

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Drug-drug Interactions between Psychotropic Agents and Other Drugs in Physically Ill Patients - Experience of Consultation-liason in Korea University Hospital - (내외과계 환자의 정신과 약물치료에서 약물-약물 상호작용 - 고려대학교 부속병원의 자문조정의 경험을 통하여 -)

  • Lee, Min Soo;Lee, Heon-Jeong
    • Korean Journal of Biological Psychiatry
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    • v.6 no.1
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    • pp.49-66
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    • 1999
  • Polypharmacotherapy, both psychotropic and nonpsychotropic, is widespread in various situations including psychiatric hospitals and general hospitals. As the clinical practice of using more than one drug at a time increase, the clinician is faced with ever-increasing number of potential drug interactions. Although many interactions have little clinical significances, some may interfere with treatment or even be life-threatening. The objective of this review is evaluation for drug-drug interactions often encountered in psychiatric consultation. Drug interactions can be grouped into two principal subdivisions : pharmacokinetic and pharmacodynamic. These subgroups serve to focus attention on possible sites of interaction as a drug moves from the site of administration and absorption to its site of action. Pharmacokinetic processes are those that include transport to and from the receptor site and consist of absorption, distribution on body tissue, plasma protein binding, metabolism, and excretion. Pharmacodynamic interactions occur at biologically active sites. In psychiatric consultation, these two subdivisions of drug interactions between psychotropic drugs and other drugs are likely to happen. We gathered informations of the drugs used in physically ill patients who are consulted to psychiatric department in Korea University Hospital. And we reviewed the related literatures about the drug-drug interactions between psychotropic drugs and other drugs.

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

  • Lee, Kyu-Hyun;Park, Eun-Seok;Chi, Sang-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.25 no.4
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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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A Biopharmaceutical Study on Rifampicin-Polyvinylpyrrolidone Coprecipitate (Rifampicin-Polyvinylpyrrolidone 공침물에 관한 생물약제학적 연구)

  • 김영일
    • YAKHAK HOEJI
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    • v.23 no.2
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    • pp.81-94
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    • 1979
  • Rifampicin-polyvinylpyrrolidone coprecipitates were prepared by the solvent method to increase the solubility and dissolution rate, thereby improving absorption of rifampicin. It was found that the solubility and dissolution rate were greater with the 1 : 5 (w/w) coprecipitate than with the pure drug, physical mixtures or coprecipitates of any other ratio of the two components. The blood concentration data in non-fasted rats showed that the extent of absorption of rifampicin were significantly enhanced following the oral administration of the 1 : 5 coprecipitate; The area under the serum concentration curve (0-8hr) was 1.3 times greater with the 1 : 5 coprecipitate than with the pure drug. The blood concentration reached its peak (4. 38$\pm$1.36mcg/ml) within two hours in the case of oral administration of the 1 : 5 coprecipitate and, on the other hand, it reached the maximum (3.77$\pm$0.90mcg/ml) after four hours of oral administration of the pure drug. It was observed that there was no significant difference between the 1 : 5 coprecipitate and the pure drug in the extent and rate of absorption of rifampicin when fasted rats were used. When the 1 : 5 coprecipitate was orally administered to human subjects 20 minutes after meal, it was found that the blood concentration reached the maximum after one hour; in the case of the pure drug, it reached its peak after four hours.

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Percutaneous Absorption Characteristics of Tacrine in Alzheimer-type Dementia Treatment (Alzheimer형 치매치료제인 Tacrine의 경피 투과 특성 연구)

  • Lee, Han-Seob
    • Journal of the Korean Applied Science and Technology
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    • v.29 no.4
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    • pp.552-560
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    • 2012
  • Drug delivery technologies are patent protected formulation technologies that modify drug release profile, absorption, distribution, and elimination for the benefit of improving product efficacy and safety, as well as patient convenience and compliance. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stop if the drug dosage lead to side effect. Polysaccharide, such as karaya gum and locust bean gum(LBG)/water-soluble chitosan oligomer(WSCO) were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers, tacrine contents. Among these polysaccharide, the permeation rate of karaya gum matrix was fastest in tacrine such as lipophilic drug in vitro. We used glycerin, PEG 400, and PEG 800 as enhancers. Therefore, transdermal absorption of tacrine could be improved by changing vehicle composition or by using penetration enhancers. Especially it would be anticipated that the high permeation efficacy could be obtained by using vehicle that has enhancing effect for itself and by adding enhancers to it.

Swelling and Proxyphylline Release Kinetics of Enzyme-Digestible Swelling Hydrogel Tablet (효소 소화성 하이드로겔 정제의 팽윤 및 프록시필린 방출 특성)

  • Shim, Chang-Koo;Lee, Young-Mee;Yeo, So-Hyeon
    • YAKHAK HOEJI
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    • v.36 no.3
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    • pp.212-219
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    • 1992
  • Although oral route is the most convenient route for drug administration, the short and variable transit of drug through GI tract restricts the sustained drug absorption after oral administration. Thus, for sustained absorption of drugs, it is desirable to prolong the GI transit time by retaining the dosage forms in the stomach. In this study, the enzyme-digestible swelling hydrogel was synthesized by heating the mixed solution of N-vinyl-2-pyrrolidone[monomer], acrylated albumin[crosslinking agent] and proxyphylline[drug] at $65^{\circ}C$ for 10 hours in the cylindrical test tube. The resultant hydrogel tablet (diameter; 0.77 cm, thickness; 0.47 cm) was designed to swell in the gastric fluid after oral administration to such a size that passing through the pylorus could be inhibited during the drug release. After releasing drug, the hydrogel was expected to be degraded by pepsin, an enzyme in the stomach, and eventually solubilized. Actually, the hydrogel synthesized in the study swelled to a size larger than the diameter of the pylorus ($1.3{\pm}0.7$ cm) and slowly digested in the presence of pepsin. Drug release from the hydrogel was prolonged up to about 12 hours. The swelling kinetics was dependent on albumin acrylation time, drug content and gel thickness. Particularly the gel thickness was the most important factor that influences on drug release. By adjusting these factors, the albumin-crosslinked hydrogel was expected to be retained in the stomach for up to 60 hours and used as a potential platform of drugs for long-term GI absorption.

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Studies on Excipients for oral dosage forms of currently marketed drug products

  • Kang, Shin-Jung;Choi, Hyun-Ceol;Kim, Ho-Jeong;Park, Sang-Aeh;Kim, Ji-Sun;Kim, Tae-Hee
    • Proceedings of the PSK Conference
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    • 2003.04a
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    • pp.303.1-303.1
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    • 2003
  • Excipients of the drug products can sometimes affect the rate and extent of drug absorption. The changes in components or composition of them can also affect the pharmacological activity. So the quantity of excipients to be changed, the new excipients and atypically large amount of commonly used excipients should be considered as bioequivalence studies. (omitted)

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Controlled Release of Propranolol Hydrochloride(PPH) from PPH-Solid Dispersion System-Polyvinyl Alcohol Hydrogel Hollow Type Suppository (염산 프로프라놀롤-고체 분산계-폴리비닐알코올 하이드로겔 중공좌제로부터의 약물방출)

  • Chung, Jeen-Hoon;Lee, Jeong-Yeon;Ku, Young-Soon
    • Journal of Pharmaceutical Investigation
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    • v.26 no.4
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    • pp.299-308
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    • 1996
  • In order to develop the controlled release of a drug from the suppsitories, in vitro drug release and in vivo absorption in rabbits were investigated. Various suppository forms with hollow cavities, into which drugs in the form of fine powder or solid dispersion system(SDS) could be placed, were utilized. The polyvinyl alcohol(PVA) hydrogel as a base, and propranolol HCl(PPH) as a model drug were employed. In vitro drug dissolution studies showed that the dissolved amounts(%) of PPH from PPH-methylcellulose(MC)-SDS and PPH-ethylcellulose(EC)-SDS reached 100% and 63% in 4.5-hours, respectively. In the relative strength test for PVA hydrogel, PVA hydrogel became harder and more rigid when the number of freezing-thawing cycles and the ratio of PVA 2000 were increased. In vitro drug release profile revealed that the release rate(%) of PPH from PPH-EC-SDS and PPH-MC-SDS hollow type suppositories were sustained. The release amount(%) of PPH from PPH-EC-SDS hollow type suppositories was not affected by storage time, but since the use of hydrophilic MC made PPH diffuse into the hydrogel after it absorbed the water of base, the various release patterns were appeared as the storage time went by. In vivo absorption experiments with rabbits showed that PPH-EC-SDS(PPH : EC=1:3) hollow type suppository delayed the absorption of PPH, significantly. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH powder hollow type suppository were $196.37{\pm}5.63\;ng/ml$, 1105.26 ng/ml/min and 8.66 min, respectively. The $C_{max}$, $AUC_{0{\rightarrow}8}$ and MRT of PPH-EC-SDS(PPH : EC=1:3) were $91.30{\pm]14.14\;ng/ml$, 554.69 ng/ml/min, 235.99 min, respectively.

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Evaluating the absorption loading technique to acrylic resin for drug delivery

  • Al-Kaabi, Arshad F.;Hamid, Mohammed A.
    • Advances in materials Research
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    • v.11 no.2
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    • pp.165-170
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    • 2022
  • Acrylic resin or polymethylmethacrylate (PMMA) is one of the most attractive materials to be used for dental appliances manufacturing. It has been introduced as a biomaterial during the last century. This study aims to evaluate the compounds absorption and release through acrylic resin to be used for drug delivery as well. The study specimens were 10 pieces of heat-cured clear acrylic resin with dimensions of 10 × 10 × 2 mm. The specimens were dipped in methylene blue solution at a powder-water ratio of 1:20 for 5 days. The samples were removed and dipped in 5 ml distilled water vials for 24 hours. Then the specimens were replaced into new 5 ml vials and the process lasted for 4 days. The extracted solutions were analyzed by the visible light spectroscopy for absorbance. The statistical results showed a gradual increase in stain release from day 1 to day 4 with a significant difference between day 1 and day 4 solutions. The study showed that PMMA resin is able to absorb and release some compounds constantly and the absorption drug-loading technique is applicable to this material.