• Title/Summary/Keyword: drug release

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Formulation and Evaluation of Controlled Release Patch Containing Naproxen (나프록센 함유 방출제어형 패취의 제제설계 및 평가)

  • Rhee, Gye-Ju;Hong, Seok-Cheon;Hwang, Sung-Joo
    • Journal of Pharmaceutical Investigation
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    • v.29 no.4
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    • pp.343-348
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    • 1999
  • The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

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Drug Release from Thermo-Responsive Self-assembled Polymeric Micelles Composed of Cholic Acid and Poly(N-isopropylacrylamide)

  • Kim, In-Sook;Jeong, Young-Il;Lee, Yun-Ho;Kim, Sung-Ho
    • Archives of Pharmacal Research
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    • v.23 no.4
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    • pp.367-373
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    • 2000
  • Cholic acid, conjugated with amine-terminated poly(W-isopropylacrylamide) (abbreviated as CA/ATPNIPAAm), was synthesized by a N, N'-dicyclohexyl carbodiimide (DCC)-mediated coupling reaction. Self-assembled CA/ATPNIPAAm micelles were prepared by a diafiltration method in aqueous media. The CA/ATPNIPAAm micelles exhibited a lower critical solution temperature (LCST) at $31.5^{\circ}C$. Micelle sizes measured by photon correlation spectroscopy (PCS) were approximately 31.6 $\times$$\times$ 5.8 nm. The CA/ATPNIPAAm micelles were spherical and their thermal size transition was observed by transmission electron microscope (TEM). A fluorescence probe technique was used for determining the micelle formation behavior of CA/ATPNIPAAm in aqueous solutions using Pyrene as a hydrophobic Probe. The critical micelle concentration (CMC) was evaluated as $8.9{\times}0^{-2}$ g/L. A drug release study was performed using indomethacin (IN) as a hydrophobic model drug. The release kinetics of IN from the CA/ATPNIPAAm micelles revealed a thermo-sensitivity by the unique character of poly(N-isopropylacrylamide) i.e. the release rate was higher at $25^{\circ}C$ than at $37^{\circ}C$.

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Rectal Absorption of Acetaminophen from Polyethylene Glycol and Witepsol Suppositories (아세트아미노펜의 Polyethylene glycol 및 Witepsol 좌제의 직장흡수 - 병원제제를 목적으로 한 아세트아미노펜좌제의 조제 및 유용성 검토-)

  • Lee, Hye Suk;Jin, Sun Kyung;Choi, Jung Hwa;Ku, Young Soon
    • Korean Journal of Clinical Pharmacy
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    • v.8 no.2
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    • pp.143-146
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    • 1998
  • Acetaminophen (APAP) suppositories with active ingredients, i.e., polyethylene glycol (PEG), Witepsol H-15 (WH), were prepared for hospital use and investigated on their drug release characteristics and pharmacokinetics. WH was employed as oil-soluble base with an aim of reducing fragility and mucosa irritancy that are common drawbacks found in PEG suppositories. Also hollow type suppository was tried as compared with conventional type suppository. Drug release tests revealed that in most formulations, more than $80\%$ of loaded APAP were released within 20 minutes, except for APAP-WH hollow type suppositories. Significant differences in the plasma concentration profile were observed among four type suppositories. $T_{max}$ of APAP-PEG and APAP-WH suppositories were 90 and 60 minutes, respectively, in hollow types. APAP-WH hollow type suppositories demonstrated fast absorption rates of APAP as compared with those of APAP-PEG suppositories. No burst effect was observed from APAP-WH suppository in contrast to APAP conventional type suppository, whereas AUCs of all the suppositories were similar. APAP-WH hollow type suppository may be an useful dosage form for hospital use.

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Fabrication and Evaluation of Active Drug Delivery System Using Polypyrrole (폴리피롤을 이용한 능동형 약물전달시스템의 제작 및 평가)

  • Lee, Sang-Jo;Lee, Seung-Ki;Pak, James Jung-Ho
    • Journal of Sensor Science and Technology
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    • v.13 no.1
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    • pp.47-55
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    • 2004
  • This paper presents drug release properties of active drug delivery system (DDS) using volume change of polypyrrole (PPy). The incorporation of various chemical substances into the PPy and controlling its release with the externally applied voltage to the PPy are possible. In order to confirm possibility for drug delivery system qualitatively, indicator(phenol red) was examined as a dopant of PPy. The applied voltage to the PPy electrode was set to -2 V and this negative voltage makes the anionic indicator released in saline solution. After qualitative analysis, in order to confirm quantitative drug release characteristic of PPy, salicylate which is one of the aspirin substance was used as a dopant of PPy. As a result, the salicylate release characteristics with time was thoroughly investigated while varying the electrode area, polymerization time, the applied voltage for drug release. Based on these quantitative results, a preliminary experiment was carried out to check the feasibility of the PPy applicable to the neuronal system.

Development of Evaluation Method for Drug Release Propreties in Drug Eluting Stent (약물방출스텐트의 약물 방출 특성 평가 방법 개발)

  • Song, J.M.;Baek, H.;Lee, S.Y.;Jang, D.H.;Seo, M.Y.;Park, G.J.;Maeng, Eun-Ho
    • Journal of Biomedical Engineering Research
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    • v.34 no.2
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    • pp.69-72
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    • 2013
  • The goal of this study is to develop test method for evaluating the drug eluting properties of drug eluting stents (DES). PBS and the detergent solutions, presented by each DES manufacturer, were used for drug release of DES coated with paclitaxel, zotarolimus and everolimus. The drugs which are coating DES were not released by PBS but released by the detergent solutions, finally paclitaxel 83.38%, zotarolimus 103.85% and everolimus 115.78%. It seems that the use of the detergents is necessary in order to release the drugs because those drugs are extremely hydrophobic. In conclusion, using of detergent solutions presented by each manufacturer were suitable for evaluating the drug eluting property of drug eluting stent.

Preparation and Dissolution Profiles of Controled Release Formulations Containing Tamsulosin Hydrochloride (염산 탐스로신을 함유하는 방출제어형 제제의 제조 및 용출거동)

  • Yun, Jae-Nam;Kim, Jeong-Soo;Kim, Dong-Woo;Lee, Gye-Won;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.35 no.6
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    • pp.445-451
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    • 2005
  • As a selective ${\alpha}_{1A}-adrenoreceptor$ antagonist, tamsulosin has been used clinically for urinary obstructed patients with benign prostatic hyperplasia. The single and multi-layered pellets containing tamsulosin hydrochloride were prepared in an effort to control the drug release, avoiding dose-dependent side effects of tamsulosin hydrochloride upon oral administration. The drug release from multi-layered pellets was substantially controlled, compared with single layered pellets. The drug release from coated pellets with single or multi layer was affected by the nature of coating agent, the percentage of coating level and the presence of hydrophilic material in coating layer. In conclusion, the controlled release oral delivery system using multi-layered pellet is very useful for tamsulosin hydrochloride, resulting in improvement of patient compliance and therapeutic drug levels for a longer period of time.

Swelling Behavior and Drug Release of Poly(vinyl alcohol) Hydrogel Cross-Linked with Poly(acrylic acid)

  • Byun, Hong-Sik;Hong, Byung-Pyo;Nam, Sang-Yong;Jung, Sun-Young;Rhim, Ji-Won;Lee, Sang-Bong;Moon, Go-Young
    • Macromolecular Research
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    • v.16 no.3
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    • pp.189-193
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    • 2008
  • Thermal cross-linking method of poly(vinyl alcohol) (PVA) using poly(acrylic acid) (PAA) was carried out on PVA/PAA hydrogels. The level of gelation was measured in the PVA/PAA hydrogels with various PAA contents. The swelling behavior at various pHs showed that the swelling kinetics and water contents of the PVA/PAA hydrogels reached equilibrium after 30 h, and the time to reach the equilibrium state decreased with increasing PAA content in the hydrogel. The water content increased with increasing pH of the buffer solution. The permeation and release of the drug were tested using indomethacin as a model drug. The permeated and released amounts of the drug increased with decreasing the PAA content because of the low free volume in the hydrogel due to the higher cross-linking density. The kinetic profile of drug release at various pHs showed that all samples reached the equilibrium state within the 5 h.

Effect of Crosslinking Agent Structure on Drug Release and Antibacterial Effect of Contact Lenses (교차결합제 구조가 콘택트렌즈의 약물용출 및 항균효과에 미치는 영향)

  • Lee, Pil-Heon;Lee, Hyun Mee
    • Journal of the Korean Chemical Society
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    • v.65 no.5
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    • pp.320-326
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    • 2021
  • This study investigated the effect of the structure of the crosslinking agent used in contact lens polymerization on the physical properties and drug dissolution of contact lenses.es Contact lenses were manufactured using 0.3% and 3% of 4 types of crosslinking agents, respectively, and ofloxacin was used as the drug. Contact lenses using hydrophilic crosslinking agents improved water contents and wettability, and the more hydrophilic functional groups, the greater the effect. Contact lenses with a high concentration of crosslinking agent had a low concentration of eluted drug and a longer release time. The cross-linking agent structure of contact lenses had an effect on improving the performance of contact lenses and controlling drug release.

Controlled Release of Doxazosin in Multi-layered Pellet Using Polymer Blending (고분자 블렌딩을 이용하여 제조된 독사조신 다중층 펠렛의 약물방출제어)

  • Youn, Ju-Yong;Park, Sang-Wook;Lee, Soo-Young;Kim, Moon-Suk;Lee, Bong;Khang, Gil-Son;Lee, Hai-Bang
    • Polymer(Korea)
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    • v.32 no.4
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    • pp.322-327
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    • 2008
  • In this study, a multi-layered pellet was composed of a seed layer including a water-swellable agent and a drug layer containing doxazosin as a model drug, a porous membrane and a castor oil layer to control drug release. The pellet is prepared by a fluidized bed coating method. To confirm drug release from polymer blending in multi-layered pellet system, it is prepared by containing different ratio such as hydroxypropylmethylcellulose (HPMC) : ethyl cellulose (EC) in drug layer and cellulose acetate(CA) : Eudragit RS in membrane. Also, to confirm the effect of oil in drug release, castor oil is coated. As a result, we observed regularly spherical pellet with diameter of $1500{\mu}m$. Release pattern of drug is confirmed by dissolution tester in aqueous media. The more the ratio of EC in drug layer, CA in membrane, and castor oil layer in pellet, the less the drug release is observed. Formation and the amount of pores in membrane is observed by SEM.

The Effect of Drug Release from Osmotic Pellet Related to the Various Ratio of $Eudragit^{(R)}$ RL and RS ($Eudragit^{(R)}$ RL과 RS의 비에 따른 삼투정 펠렛의 약물방출에 미치는 영향)

  • Youn, Ju-Yong;Ku, Jeong;Lee, Soo-Young;Kim, Byung-Soo;Kim, Moon-Suk;Lee, Bong;Khang, Gil-Son;Lee, Hai-Bang
    • Polymer(Korea)
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    • v.31 no.4
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    • pp.329-334
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    • 2007
  • Osmotic pellet system, which is one of the oral drug delivery systems, has been developed to improve manufacturing process, reduce product cost and other problems of osmotic tablet systems. Osmotic pellet is consisted of water swellable seed layer, drug layer, and membrane layer. Among them, the membrane layer plays an important role in a control of the drug release. In this work, we examined the effect of ratio for Eudragit RL and RS on the drug release behavior. Osmotic pellet with nifedipine as a model drug was easily obtained in a good yield by fluidized bed coater. Osmotic pellet showed round morphology with a range of size $1300{\sim}1500\;{\mu}m$. In the experiment of nifedipine release, the release amount increased with the increase of the ratio of Eudragit. This is due to the fact that Eudragit RL contains more hydrophilic quaternary ammonium group than Eudragit RS. Additionally, the release amount was retarded with increasing the membrane thickness. There are no differences in the release amount measured at the different pH 1.2, 6.5, 6.8, and 7.2. In conclusion, it was found that the drug release from osmotic pellets depended on the composition ratio and coating thickness of membrane layer.