• 제목/요약/키워드: Release profile

검색결과 172건 처리시간 0.023초

Preparation of 5-Fluorouracil-Loaded Poly(L-lactide-co-glycolide) Wafer and Evaluation of In Vitro Release Behavior

  • Lee, Jin-Soo;Chae, Gang-Soo;An, Tae-Kun;Gilson Khang;Cho, Sun-Hang;Lee, Hai-Bang
    • Macromolecular Research
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    • 제11권3호
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    • pp.183-188
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    • 2003
  • The controlled delivery of anticancer agents using biodegradable polymeric implant has been developed to solve the problem of penetration of blood brain barrier and severe systemic toxicity. This study was performed to prepare 5-FU-loaded poly (L-lactide-co-glycolide) (PLGA) wafer fabricated microparticles prepared by two different method and to evaluate their release profile for the application of the treatment of brain tumor. 5-FU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). SEM observation of the 5-FU-loaded PLGA microparticles prepared by rotary solvent evaporation method showed that 5-FU was almost surrounded by PLGA and significant reduction of crystallinity of 5-FU was confirmed by XRD. In case of release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by mechanical mixing, the release profile of 5-FU followed near first order release kinetics. In contrast to the above result, release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by rotary solvent evaporation method followed near zero order release kinetics. These results indicate that preparation method of the 5-FU-loaded PLGA microparticles to fabricate into wafers was contributed to drug release profile.

In vitro Retention of Antimicrobial Activity of Ciprofloxacin-incorporated Central Venous Catheters

  • Jeon, Sung-Min;Kim, Mal-Nam
    • 대한의생명과학회지
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    • 제13권3호
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    • pp.175-182
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    • 2007
  • In vitro ciprofloxacin (CFX)-release study and bioassay using microorganisms were performed to estimate the retention of the antimicrobial activity of the CFX-incorporated central venous catheters (CFX-CVCs). The release experiments were carried out under the optional CFX-release conditions to mimic the in vivo environment. The release of CFX experienced an initial burst followed by a slow and steady matrix-diffusion controlled release. The 1.0CP (polyurethane catheter containing 1.0% (w/w) of CFX) under dynamic condition showed a near zero-order CFX release profile, which is beneficial for the long-tenn antimicrobial activity. The modified Kirby-Bauer method was performed employing S. aureus and E. coli to evaluate the retention of antimicrobial activity of the catheters retrieved from the release experiments. The 1.0CP showed the long-term antimicrobial activity (${\geq}\;21$ days) against both S. aureus and E. coli. These results indicate that 1.0CP is useful as a long-tenn indwelling CVC.

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비육우에서 이식형 bovine somatotropin 지속성 제형의 blood profile test (Blood profile test of sustained release formula of implantable bovine somatotropin in steers)

  • 김남중
    • 대한수의학회지
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    • 제49권1호
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    • pp.9-15
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    • 2009
  • The present study was carried out to examine the sustained release effect of the implantable bovine somatotropin (SRI-BST) formula. In the blood profile test in steers, the bovine somatotropin concentration in serum by radioimmunoassay showed the peak concentration on the first day after the implantation of the SRI-BST formula, and concentration proceeded for 5 days (p < 0.05). The insulin-like growth factor-1 concentration showed the peak concentration on the seventh day after implantation of the SRIF-BST formula, and concentration proceeded for 10 days (p < 0.05). The glucose showed the peak concentration on the first day after implantation of the SRI-BST formula, and concentration continued for 3 days (p < 0.05). The blood urea nitrogen showed the lowest concentration on the third day after implantation of the SRI-BST formula, and concentration continued for 7 days (p < 0.05). These results proved that the SRIF-BST formula was the sustained release effects in steers.

저수축제 및 이형제가 벌크몰드컴파운드의 표면형태 및 물성에 미치는 영향 (Effect of the Low Profile Agent and Release Agent on the Surface Morphology and Property of Bulk Mold Compound)

  • 김성룡;권기준
    • 접착 및 계면
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    • 제12권4호
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    • pp.144-150
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    • 2011
  • 폴리스티렌을 저수축제로 사용하고 Zn-stearate를 이형제로 사용하여 함량변화에 따라 벌크 몰드컴파운드의 표면형태 및 기계적 물성에 미치는 영향을 고찰하였다. XPS, 접촉각 측정기 등을 이용하여 표면과 깊이 방향에 대한 원소함량과 접촉각을 측정하였고, 표면형태는 FESEM을 이용하여 관찰하였으며, 표면조도 측정은 AFM을 이용하였다. 저수축제를 첨가하지 않은 경우에 비교하여 저수축제를 9.0 wt% 첨가하였을 경우에는 체적수축률은 0.35%에서 0.05%로 감소하였으며, 표면조도는 $0.27{\mu}m$에서 $0.12{\mu}m$로 감소하였다. 이형제의 함량을 1.8 wt%에서 3.6 wt%로 증가시켰을 경우에는 이형제가 주로 표면에 존재하고 표면조도를 증가시키는 것을 확인하였다. 저수축제의 함량을 5.0 wt%에서 9.0 wt%로 증가시킴에 따라 굴곡탄성율과 충격강도가 약 30% 감소하였다.

Preparation and In vitro Release Characteristics of Hydrophilic Albumin Microspheres Containing Methotrexate and Methotrexate-Human Serum Albumin Conjugates

  • Hwang, Sung-Joo;Lee, Myung-Gulll;Kim, Chong-Kook
    • Archives of Pharmacal Research
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    • 제15권2호
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    • pp.162-168
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    • 1992
  • Release characteristics of five different types of hydrophilic albumin microspheres (HAM) containing different ratios of methotrexate-albumin (MTX-HSA) conjugates to free MTX: 1 : 0 (HAMC), 3 :1 (HAMC 3F), 1 :1 (HAMCF), 1:3 (HAMCF3) and 0 : 1 (HAMF) were investigated in the absence or presence of protease using dissolution tester. In all the HAMs studied except HAMC, the MTX was released bi-exponentially in the absence of protease; an initial fast release period up to approximately 6h, and thereafter the release rate was very much slower. The fast release of MTX from the HAMs (such as HAMC3F, HAMCF, HAMCF3 and HAMF) at the initial phase in probably due to the release of "physically associated" MTX from the core of the HAMs. The initial rate constants were 7.2, 8.7, 8.5 and 5.9 times greater than the second rate constants for HAMF, HAMCF3, HAMCF and HAMC3F, respectively. MTX release from HAMC was very slow and mono-phasic. It was at most 2.2% of the total entrapped amount by 24 h. The protease accelerated the release of MTX from the HAMs. The percentages of MTX released from HAMs up to 24 h were 100, 89.0, 75.0, 66.0 and 61.0% for HAMF, HAMCF3, HAMCF, HAMC3F and HAMC, respectively in the presence of protease and the corresponding values in the absence of protease were 30.2 19.0, 10.0, 6.5 and 2.2%, respectively. In vitro release of MTX in the presence of protease varied according to the ratios of MTX-HSA conjugates to MTX; the data set from HAMF, HAMCF3 and HAMCF fits better to monophasic first-order profile more adequately than to zero-order profile, that of HAMC3 monophasic first-order, and that of HAMC to bi-phasic zero-order. Above results suggested that zero-order release rate can be achieved by adjusting the ratio of MTX-HSA conjugates to MTX in the preparation of HAMs such as HAMC3F.as HAMC3F.

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니페디핀 삼투성 과립 시스템의 제조와 약물 방출 특성 (Preparation and Release Characterization of Osmotic Granule Nifedipine Delivery System)

  • 정성찬;조영호;이수영;이봉;김문석;강길선;이해방
    • Journal of Pharmaceutical Investigation
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    • 제36권1호
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    • pp.11-17
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    • 2006
  • The objective of this study was to confirm the effect of the type of dissolution media and paddle speed on nifedipine (ND) release profile from osmotic granule and the storage stability. Osmotic granule was manufactured by fluidized bed coating method. At each coating step, morphology of osmotic granule was differed. The size of osmotic granule was $750\;{\mu}m$ at 3 wt% membrane thickness. ND release was changed in diverse dissolution media, paddle speed. ND release is governed by not only osmotic pressure but diffusion from osmotic granule. ND release from osmotic granule decreased as storage period increased. These may be caused by liquid excipient which has low molecular weight. Storage stability of osmotic granule could be improved by removing liquid excipient from semipermeable membrane.

Alginate와 Kaoline을 이용(利用)한 방출조절제(放出調節劑)의 14C-Butachlor 용출특성(溶出特性) (Release Profile of 14C-Butachlor from Controlled Release Formulation Prepared with Alginate-Kaoline Matrix)

  • 오병열
    • 한국잡초학회지
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    • 제10권2호
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    • pp.122-129
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    • 1990
  • Alginate와 Kaoline을 저장매체(貯藏媒體)로 사용(使用)하여 제제(製劑)한 Butachlor[N-(butoxymethyl)-2-chloro-2', 6'-diethylacetamlide] 방출조절제(放出調節劑)의 특성(特性) 및 주성분(主成分) 용출양상(溶出樣相)을 암조건(暗條件)과 일광노출(日光露出) 조건하(條件下)에서 zeolite 흡착형립제(吸着型粒劑)와 비교시험(比較試驗)하였다. Calcium alginate-Kaoline 저장체(貯藏體)에의 butachior제제율(製劑率)은 91.8%이상(以上)이었고 제품(製品)의 수율(收率)은 kaoline의 첨가량(添加量)이 증가(增加)할수록 감소(減少)하였다. 방출조절제(放出調節劑)의 수중(水中) 주성분(主成分) 용출속도(溶出速度)는 시험조건(試驗條件)에 관계(關係)없이 zeolite흡착형립체(吸着型粒劑)보다 완만(緩慢)하였고 kaoline의 함량(含量)이 증가(增加)할수록 그 속도(速度)는 현저(顯著)하게 감소(減少)하였다. 일광노출조건(日光露出條件)에서 수증기(水蒸氣)와의 공증류(共蒸溜)에 의(依)한 용출주성분(溶出主性成分)의 감소율(減少率)은 kaoline의 함량(含量)이 증가(增加)할수록 저하(低下)되는 경향(傾向)을 보였다.

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Postulated release profile of recombinant human bone morphogenetic protein-2 (rhBMP-2) from demineralized dentin matrix

  • Um, In-Woong;Ku, Jeong-Kui;Lee, Bu Kyu;Yun, Pil-Young;Lee, Jeong Keun;Nam, Jeong-Hun
    • Journal of the Korean Association of Oral and Maxillofacial Surgeons
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    • 제45권3호
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    • pp.123-128
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    • 2019
  • Demineralized dentin matrix (DDM) has been used as a recombinant human bone morphogenetic protein-2 (rhBMP-2) carrier in many clinical trials. To optimize the clinical safety and efficacy of rhBMP-2 with DDM, efforts have been made to improve the delivery of rhBMP-2 by 1) lowering the administered dose, 2) localizing the protein, and 3) prolonging its retention time at the action site as well as the bone forming capacity of the carrier itself. The release profile of rhBMP-2 that is associated with endogenous BMP in dentin has been postulated according to the type of incorporation, which is attributed to the loosened interfibrillar space and nanoporous dentinal tubule pores. Physically adsorbed and modified, physically entrapped rhBMP-2 is sequentially released from the DDM surface during the early stage of implantation. As DDM degradation progresses, the loosened interfibrillar space and enlarged dentinal tubules release the entrapped rhBMP-2. Finally, the endogenous BMP in dentin is released with osteoclastic dentin resorption. According to the postulated release profile, DDM can therefore be used in a controlled manner as a sequential delivery scaffold for rhBMP-2, thus sustaining the rhBMP-2 concentration for a prolonged period due to localization. In addition, we attempted to determine how to lower the rhBMP-2 concentration to 0.2 mg/mL, which is lower than the approved 1.5 mg/mL.

압축코팅법에 의한 3단계 약물방출형 지속성제제의 제조 및 용출특성 (Preparation and Dissolution Characteristics of the Compression-Coated Controlled Release Tablet Exhibiting Three-step Release)

  • 김철수;권혁노;차봉진;권종원;양중익;민신홍
    • Journal of Pharmaceutical Investigation
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    • 제22권2호
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    • pp.133-137
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    • 1992
  • A novel oral controlled release tablet which may offer more uniform drug level in the body than simple zero-order was developed. The tablet is composed of three layers; outer film layer, middle part compression-coated hydroxypropylmethylcellulose (HPMC) matrix layer, and inner core layer. Each layer contains nicardipine HCl as a model drug. In vitro dissolution test showed that the tablet released the drug in clear three steps; a rapid initial release, followed by a constant rate of release, and then a second phase of fast release of drug. The dissolution characteristics could be modified easily by changing the grade of HPMC, thickness of matrix layer, content of methylcellulose in matrix layer, content of active ingredient in each layer. The pH of dissolution medium did not affect the release profile. This three-step release system is expected to raise the blood concentration rapidly to effective level and to maintain effective blood level longer than simple slow-release systems.

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

  • 이계주;홍석천;황성주
    • Journal of Pharmaceutical Investigation
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    • 제29권4호
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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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