• Title/Summary/Keyword: Release Layer

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Pharmacokinetics of Acebrophylline Containing Double-layered Sustained Release Tablet in Mini Pigs (미니피그를 이용한 아세브로필린 이중정의 약동학적 평가 (아세브로필린 이중정 개발))

  • Kim, Kang Min;Ko, Chan Young;Kang, Jae Seon
    • YAKHAK HOEJI
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    • v.57 no.6
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    • pp.442-447
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    • 2013
  • The aim of the present study was to improve commercial twice-a-day Acebrophylline formulation to once-a-day new formulation to improve patient compliances. To develop the double-layered tablet, the sustained release layer was prepared using Eudragit$^{(R)}$ L100-55 and Carnauba wax. The sustained release layer has shown delayed release rates in pH 1.2 which comparable to that of performed in pH 6.8 buffer. In the comparative pharmacokinetic study with commercialized Surfolase$^{(R)}$, the present double-layered Acebrophylline tablet has shown similar pharmacokinetic parameters of AUC, $C_{max}$ and $T_{max}$ values.

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.

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.

A Formulation Study for the Controled Release Rate of Diltiazem. HCl using the Multiple Drug Release System (다중약물방출시스템을 이용한 염산딜티아젬의 방출속도 조절에 관한 연구)

  • Kim, Hak-Hyung;Oh, Jin-Hwan;Han, Kun
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.157-163
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    • 2005
  • The pellets with multiple drug release system (MDRS) of Diltiazem. HCl which consist of immediate drug release layer, drug reservoir layer and controlled release rate membrane, were prepared by using CF-Coater. As main factors for more effective MDRS of Diltiazem. HCl, ethylcellulose was used for the controlling drug release rate, and diethylphthalate was used for plasticizer, respectively. In vitro evaluation study was performed by comparative dissolution test between our test MDRS and reference Diltiazem. HCl preparation. The physical tests were performed using FT-IR and SEM. In vivo evaluation was also performed by observing the behavior of a plasma drug concentration after oral administration. The bioavailability was determined by analyzing the blood sample after oral administration to healthy, male volunteers once a day. As a result, there were no significant differences in bioequivalence parameters $(AUC_{\infty},\;C_{max},\;t_{1/2})$ between two systems. It might be concluded that our MDRS of Diltiazem. HCl could be an alternative delivery system to reference drug preparation.

Controlled Release of Tamsulosin from Nanopore-Forming Granules (미세 다공성 과립을 이용한 탐스로신의 방출제어)

  • Seo, Seong-Mi;Lee, Hyun-Suk;Lee, Jae-Hwi;Lee, Ha-Young;Lee, Bong;Lee, Hai-Bang;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.36 no.1
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    • pp.39-44
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    • 2006
  • Tamsulosin or a salt thereof such as its hydrochloride salt has been known to have an adrenaline ${\alpha}$ receptor blocking action for urethra and prostate areas. It has been widely used as a drug which lowers the prostate pressure and improves urinary disturbance accompanied by prostate-grand enlargement, thus for the treatment of prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is essentially required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin granules and assess their formulation variables. We designed entric coated sustained-release tamsulosin granules for this purpose. Nano-pores in the outer controlled release membrane were needed in order to obtain initial tamsulosin release even in an acidic environment such as gastric region. In our sustained release osmotic granule system, hydroxypropylmethylcellulose in a drug-containing layer was used as a rate controller. The drug-containing granules were coated with hydroxypropylmethylcellulose phthalate (HPMCP) and Eudragit, along with glycerol triacetate as an aqueous nano-pore former. The release of tamsulosin depended heavily on the type of Eudragit such as RS, RL, NE 30D, used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the Korean Food and Drug Administration.

Preparation and Dissolution Characteristics of Sustained Release Granules Containing Indapamide (인다파마이드가 함유된 서방형 과립의 제조 및 용출 특성)

  • Park, Ji-Seon;Seo, Hui;Kim, Byung-Jin;Jeong, Sang-Young;Shin, Byung-Cheol;Yuk, Sun-Hong;Hwang, Sung-Joo;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.38 no.2
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    • pp.105-110
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    • 2008
  • Indapamide (4-chloro-N-(2-methyl-1-indolinyl)-3-sulfamoyl-benz-amide) is an oral antihypertensive diuretic agent indicated for the treatment of hypertensive. The diuretic and natriuretic effects are mainly due to the structure of o-chlorobenzenesulfonamide. The objective of this study was to formulate sustained release indapamide granules and assess their formulation variables. Granules were prepared by fluid bed coating method and consist of drug layer and membrane layer. The granules were coated with HPC and ethyl cellulose along with plasticizer dibuthyl sebacate. The release of indapamide depended on the type of Eudragit such as RS and NE 30 D used in the formulation controlled release layer. These results obtained clearly suggest that the sustained release oral delivery system for indapamide could be designed with satisfying drug release profile approved.

A Novel Drug Delivery System Design for Meloxicam

  • Kim, Hyun-Jo;Lee, Il-Kyu
    • Journal of Pharmaceutical Investigation
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    • v.35 no.3
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    • pp.151-155
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    • 2005
  • A drug delivery system(DDS) for practically insoluble meloxicam was developed and evaluated by dissolution study. A novel DDS is two layered system, where the first layer is consisted of gas-forming agent for an immediate release and the second layer is composed of metolose SR(HPMC) for sustained release. This bilayered tablets were manufactured by using manual single punch machine. The results of dissolution study showed an initial burst release followed by sustained release for the experimental period time. From a pharmaceutical point of view, the designed DDS for meloxicam would be informative system in terms of poorly soluble analgesic medicines.

Development and Characterization of Membrane for Local Delivery of Cephalexin

  • Shin, Sang-Chul;Oh, In-Joon;Cho, Seong-Jin
    • Archives of Pharmacal Research
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    • v.19 no.1
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    • pp.1-5
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    • 1996
  • Laminated films composed of drug-containing reservoir layer and drug-free membrane were prepared. Zero-order drug release with lag time was achieved by laminating drug-free film onto the reservoir layer, while burst effect was observed on cast-on film. The rate controlling membrane was either attached to or cast directly into the reservoir. The release rate was independent on the reservoir composition but dependent on the composition of rate-controlling membrane. In growth inhibitory test of cephalexin from Eudragit RS film to Streptococcus Mutans, the disk even after release test for 72 hours showed more bacterial growth inhibition than that of control. Permeation of drug through rat skin was proportional to the HPC fraction in the film. We could control the release of cephalexin from the film by changing the fraction of Eudragit RS, HPC and DEP content. Consequently, Eudragit RS/HPC film was found to be very effective system for local delivery of drugs.

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Analysis of the strain energy release rate for time-dependent delamination in multilayered beams with creep

  • Rizov, Victor I.
    • Advances in materials Research
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    • v.11 no.1
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    • pp.41-57
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    • 2022
  • This paper is focused on delamination analysis of a multilayered inhomogeneous viscoelastic beam subjected to linear creep under constant applied stress. The viscoelastic model that is used to treat the creep consists of consecutively connected units. Each unit consists of one spring and two dashpots. The number of units in the model is arbitrary. The modulus of elasticity of the spring in each unit changes with time. Besides, the modulii of elasticity and the coefficients of viscosity change continuously along the thickness, width and length in each layer since the material is continuously inhomogeneous in each layer of the beam. A time-dependent solution to the strain energy release rate for the delamination is derived. A time-dependent solution to the J-integral is derived too. A parametric analysis of the strain energy release rate is carried-out by applying the solution derived. The influence of various factors such as creep, material inhomogeneity, the change of the modulii of elasticity with time and the number of units in the viscoelastic model on the strain energy release rate are clarified.