• Title/Summary/Keyword: 약물용출

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키토산의 고형분산체에의한 약물전달체계의 개발

  • 김태호;이승진;김길수;서성훈;김동현
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.344-344
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    • 1994
  • 모델약물로 acetaminophen을 사용하여 우리나라에 자원이 풍부한 키토산을 약물전달체계에 응용하려고 시도하였다. 키토산 분산체는 단순혼합물과는 다른 형태였으며 용출지연을 나타냈다. 요출거동의 차이는 약물의 물성보다는 polycation인 키토산의 막형성능과 pH에 좌우되었으며 polyanion인 polyacrvlate을 첨가한경우는 막형성능은 저조했으나 겔형성이 뛰어나 키토산 단독보다 용출이 지연되었다 키토산의 아미노기와 shiff's base를 형성하는 수종의 aldellyde는 키토산분산막과 chitosan-polyacrylate분산막을 강하게 경화시켜 용출을 저하시켰다. 특히 가교제의 농도와 양, 막과 반응하는 시간과 방법에 따라 막의 물리적특성 및 용출거동이 큰영향을 받았다.

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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.

Off-pump Coronary Artery Bypass Surgery Versus Drug Eluting Stent for Multi-vessel Coronary Artery Disease (다혈관 관상동맥질환에서의 심폐바이패스를 사용하지 않은 관상동맥우회술과 약물용출 스텐트시술)

  • Lee, Jae-Hang;Kim, Ki-Bong;Cho, Kwang-Ree;Park, Jin-Shik;Kang, Hyun-Jae;Koo, Bon-Kwon;Kim, Hyo-Soo;Sohn, Dae-Won;Oh, Byung-Hee;Park, Young-Bae
    • Journal of Chest Surgery
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    • v.41 no.2
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    • pp.202-209
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    • 2008
  • Background: The introduction of Drug Eluting Stents (DES) decreased the number of patients referred for coronary artery bypass grafting (CABG). The impact of DES on CABG (Step 1) was studied and compared with the 1-year outcome after CABG with DES (Step 2). Material and Method: Surgical results for patients who underwent off-pump CABG (OPCAB) before the introduction of DES(n=298) were compared with those who underwent OPCAB after the introduction of DES (n=288) (Step 1). Postoperative 30-day and 1-year results were also compared between the patients who underwent percutaneous coronary intervention (PCI) using DES (n=220) and those who underwent OPCAB (n=255) (Step 2). Result: Since the introduction of DES, the ratio of CABG versus PCI decreased. In the CABG group, the number of high risk patients such as elderly patients (age 62 vs. 64, p=0.023), those with chronic renal failure (4% vs. 9%, p=0.021), calcification of the ascending aorta (9% vs. 15%, p=0.043), or frequency of urgent or emergent operations (12% vs. 22%, p=0.002) increased. However, there were no differences in the cardiac death and graft patency rates between the two groups (step 1). During the one-year follow up period, the rate of target vessel revascularization (12.3% vs. 2.4%, p<0.001) and major adverse cardiac events (MACE: death, myocardial infarct, TVR) were higher in the DES than the CABG group (13.6% vs 4.3%) (stage 2). Conclusion: Introduction of DES decreased the number of patients referred for surgery, and increased the comorbidity in patients who underwent CABG. DES increased the rate of target vessel revascularization, and the occurrence of MACE during the 1-year follow-up. However, there was no difference in the incidence of myocardial infarction and cardiac death between the two groups.

Immediate Drug Release Enhancement of Nateglinide Using Fumaric Acid (푸마르산을 이용한 나테글리니드 함유 속방출형 제형의 약물방출 개선에 관한 연구)

  • Lee, Sung-Hoon
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.18 no.1
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    • pp.506-512
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    • 2017
  • The purpose of this study was to improve release rate and bioavailability of nateglinide formulation. Polymorphism selection and particle size control were performed to enhance formulation dissolution rate, and a pH modifier was included in the formulation to overcome pH-dependent solubility of nateglinide. The enhanced dissolution rate was characterized by using a dissolution test. The results showed that H-type raw material had a higher dissolution rate than that of B-type raw material. There was 6.2% difference in dissolution between the two materials at 60 min. With regard to particle size, raw material with a $1.13{\mu}m$ particle size showed a 20% faster release rate than that of raw material with a $2.28{\mu}m$ particle size. Furthermore, fumaric acid was included in formulation as a pH modifier. That addition produced a greater than 50% improvement in dissolution rate. In conclusion, dissolution rate of nateglinide can be enhanced by optimizing its polymorphism and particle size; moreover, a synergistic effect on the enhancement of dissolution rate is obtained by including fumaric acid, a pH modifier, in the formulation.

Changes in Drug Elution Concentration and Physical Characteristics of Soft Contact Lenses Depending on the Initiator and Crosslinker (개시제와 교차결합제 농도의 변화에 따른 소프트콘택트렌즈의 물리적 성질과 약물용출 농도의 변화)

  • Park, Hyun-Ju;Lee, Hyun Mee
    • Journal of Korean Ophthalmic Optics Society
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    • v.19 no.2
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    • pp.145-151
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    • 2014
  • Purpose: The material properties of contact lenses were measured by varying the amounts of an initiator and a cross-linking agent that are the basis for the manufacture of contact lenses, and the drug delivery effects depending on the material properties of contact lenses were compared. Methods: Contact lens samples were manufactured using HEMA by varying the concentration of the cross-linking agent and the initiator. To investigate the changes in physical characteristics depending on the material properties, the results of the experiments on the amount of drug elution, water content, refractive index, and the amount of protein adsorption were compared. Results: For the contact lenses manufactured by varying the amount of the initiator, the water content hardly changed, and the refractive index also hardly changed. The amount of drug elution was not much affected by the changes in the initiator, but the amount of elution increased as the water content increased. The amount of protein adsorption was hardly affected by the changes in the initiator, but the amount of adsorption increased as the water content decreased. Conclusions: The changes in the properties were hardly affected by the changes in the amount of the initiator, but were significantly affected by the changes in the amount of the cross-linking agent. As the amount of the cross-linking agent increased, the water content decreased, while the refractive index increased. Also, when the water content increased, the amount of drug elution increased, while the amount of protein adsorption decreased.

Effect of Particle Size of HPMC on Dissolution Rate of Venlafaxine HCl and Carbamazepine Sustained Release Tablet (HPMC의 입도에 따른 염산벤라팍신 및 카바마제핀 서방성 정제의 용출 특성)

  • Cha, Jae-Uk;Cha, Ja-Hyun;Hong, Jun-Kee;Lee, Sung-Wan;Ko, Won-Hwa;Beak, Hyun-Ho
    • Polymer(Korea)
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    • v.36 no.3
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    • pp.332-337
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    • 2012
  • The primary objective of this work is to find the properties of sustained release dissolution pattern depending on solubility of drugs, so venlafaxine HCl and carbamazepine tablets were made by using polymer wich various particle size. Hydroxy propyl methyl cellulose (HPMC) has been utilized in this study as an excipient that is one of the most widely used polymers for an oral sustained release formulation, and drug release pattern was strongly influenced by swelling rate depending on particle size of HPMC. Scanning electron microscope (SEM) was employed to investigate the surface of tablets with various HPMC particle size, and differential scanning calorimeter (DSC) was employed to investigate the crystallization of drugs in tablets. The release model equation was applied to analyze the main mechanism of drug release pattern. The results demonstrate that drug release pattern is controlled by the drug solubility and HPMC particle size.

마이크로캅셀화에 의한 조절방출제제 개발 I: 유드라짓 마이크로캅셀화에 의한 $\beta$-락탐계 항생제의 방출제어

  • Ji, Woong-Gil;Han, Gun;Jung, Yeon-Bok
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.64-64
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    • 1992
  • 1. Eudragit RS, RL, E, S 및 L을 이용하여 유중건조법으로 제조한 $\beta$-락탐계 항생제 (Amoxicillin, Cephalexin) 마이크로캅셀 모두가 구상 성형성과 정립성이 양호한 결과를 얻었다. 2. 분리 분산제 (aluminium tristearate)의 양을 고정시켰을 때에는 일정한 입자 분포도를 가지는 마이크로캅셀을 얻을 수 있었고, 양을 증가시켰을 때에는 입자 크기는 작아 졌으며, 용출율은 증가하였다. 3. Eudragit RS 및 S 마이크로캅셀제제로부터의 약물용출은 저조하였고, Eudragit RL 및 L 제제로부터의 약물용출은 양호하였다. 따라서 Eudragit RS/RL 마이크로캅셀제제에서는 Eudragit RL의 양을 증가시킬수록 약물의 용출율이 증가하였으며, Eudragit S/L 마이크로캅셀제제에서는 Eudragit L의 양을 증가시킬수록 약물의 용출율이 증가하였다. 약물방출 실험결과, Amoxicillin 함유Eudragit RS/RL (25/75) 마이크로캅셀, cephalxin함유 Eudragit RS/RL (75/25) 마이크로캅셀 및 Eudragit S/L (75/25) 마이크로캅셀제제는 유용한 제제로 펑가되었다. 또한 수용성 고분자인 polyethylene glycol을 혼합하어 제조하는 것에 의해 방출조절성 마이크로캅셀의 제조가 가능하였다. 유중건조법을 이용하여 본 연구방법으로 저조한 마이크로캅셀제제는 투어횟수를 줄일 수 있을 뿐만 아니라 생체에 대해 안전하고 재현성에 확보되는 유용한 제제로 판단된다. 앞으로 연구를 계속 수행하여, 특히 약물의 물리화학적 성질 및 생제내 투어 후의 생물약제학적 펑가를 엄격히 하므로써 안정성이 심히 문제시되는 다용 약물계열에 대한 조절방출성제제의 개발을 기대할 수 있다.은 해리항수의 역수이므로 해리항수가 적을수록 $\beta$ 수용체에 대한 친화력이 큰 약물이다. 시사되었으며, 이 조직에서 또한 5-$HT_2$와 5-$HT_3$ 수용체의 존재를 확인하고 각각의 기능을 분명히 했다.가 수월하게 하였고 메모리를 동적으로 관리할 수 있게 하였다. 또한 기존의 smpl에 디버깅용 함수 및 설비(facility) 제어용 함수를 추가하여 시뮬레이션 프로그램 작성을 용이하게 하였다. 예를 들면 who_server(), who_queue(), pop_Q(), push_Q(), pop_server(), push_server(), we(), wf(), printfct() 같은 함수들이다. 또한 동시에 발생되는 사건들의 순서를 조종하기 위해, 동시에 발생할 수 있는 각각의 사건에 우선순위를 두어 이 우선 순위에 의하여 사건 리스트(event list)에서 자동적으로 사건들의 순서가 결정되도록 확장하였으며, 설비 제어방식에 있어서도 FIFO, LIFO, 우선 순위 방식등을 선택할 수 있도록 확장하였다. SIMPLE는 자료구조 및 프로그램이 공개되어 있으므로 프로그래머가 원하는 기능을 쉽게 추가할 수 있는 장점도 있다. 아울러 SMPLE에서 새로이 추가된 자료구조와 함수 및 설비제어 방식등을 활용하여 실제 중형급 시스템에 대한 시뮬레이션 구현과 시스템 분석의 예를 보인다._3$", chain segment, with the activation energy of carriers from the shallow trap with 0.4[eV], in he amorphous regions.의 증발산율은 우기의 기상자료를 이용하여 구한 결과 0.05 - 0.10 mm/hr 의 범위로서 이로 인한 강우손실량은 큰 의미가 없음

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Predictive Factors of Major Adverse Cardiac Events after Drug-Eluting Balloon Angioplasty for In-Stent Restenosis Lesion (스텐트 내 재협착 병변에서 약물용출 풍선확장술 후 주요 심장사건 발생의 예측인자)

  • Lee, Doo Hwan;Kim, In Soo;Kong, Chang gi;Han, Jae Bok
    • Journal of the Korean Society of Radiology
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    • v.14 no.2
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    • pp.179-191
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    • 2020
  • The aim of this study was to investigate the predictors of major adverse cardiac events (MACE) in patients with drug-eluting balloon (DEB) for in-stent restenosis (ISR) lesion. Total of 257 patients who developed ISR on follow-up coronary angiography (66.1 ± 10.1years, 172 males) in Chonnam National University Hospital between October 2012 and January 2017 were enrolled. We divided the patients into two groups; group I (MACE group; n= 35) and group II (No MACE group; n= 222). A multivariate logistic regression analysis revealed that type IV ISR (HR=4.179, 95% C.I.=1.851-9.437 p= 0.001), lesion length > 25 mm (HR=8.773, 95% C.I.=1.898-40.546 p=0.005), number of ISR recurrence > 2 (HR=4.693, 95% C.I.=1.259-17.490 p= 0.021) were independent factors for MACE after DEB in ISR lesions.

새로운 오메프라졸염의 개발 및 제제화 연구

  • 이계주;이기명;이창현;우종수
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1994.04a
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    • pp.329-329
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    • 1994
  • OMZ과 HP-$\beta$-CD 포접화합물의 유형은 $A_{L}$ type의 가용성 복합체이며, CD, UV, IR, DSC, XRD pattern 및 $^1$H-NMR 방법으로 측정한 포접화합물의 결함형태는 OMZ의 benzimidazole부분이 HP-$\beta$-CD 공동에 포접된 형태이었고, OMZ과 HP-$\beta$-CD의 결합조성몰비는 1:1, 안정도 상수는 약 34 M$^{-1}$이었다. 또한 cholestyramine 수지와 OMZ 복합체는 방출양상이 신속하였다. OMZ-cholestyramine 수지염은 안정성이 양호하고 용출율이 우수한복합체로 경구용 재제를 개발할 수 있었으며, 용출시험 및 산 저항성이 양호하고 pellet의 제조에 있어서 core의 제조는 정제수 : 에탄올(7: 3) 결합액을 이용하여 lactose를 주로 사용하고 기타 PEG 6000, sorbitol, Avicel PH101, sodium lauryl sulfate 및 무수 PVP K-30을 적절히 배합하여 제조하고, 장용코팅의 내산성은 90.5% 이었으며, 소장에서의 용출경향이 85%이상이 10분 이내에 용출되어 규정에 적합하였다.

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Release Behavior of Olmesartan Medoxomil from Solid Dispersion Prepared by PVP Addition (PVP 첨가에 의해 제조된 올메사탄 메독소밀 고체분산체의 방출패턴 연구)

  • Oh, Seung-Chang;Lee, Cheon Jung;Lee, Hyun Gu;Park, Jin Young;Jeong, Hyun Ki;Kim, Young-Lae;Lim, Dong-Kwon;Lee, Dongwon;Khang, Gilson
    • Polymer(Korea)
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    • v.39 no.1
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    • pp.33-39
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    • 2015
  • Olmesartan affiliated to biopharmaceutics classification system class 2 is a poorly water soluble drug. For this reason, olmesartan showed a low bioavailability and a lot of difficulties in the process of designing the pharmaceutical formulation. We prepared the solid dispersions of olmesartan. We confirmed the dissolution rate of drug which was prepared by manufacturing. The pharmaceutical formulation of solid dispersions was designed by using PVP as water soluble polymer. We analyzed morphological feature of solid dispersion by employing a scanning electron microscope. Then, the crystalline property of solid dispersion was confirmed through X-ray diffraction and differential scanning calorimeter. Also, the chemical change of solid dispersion was confirmed by the Fourier transform infrared spectroscopy. In vitro dissolution test was used to analyze the dissolution rate of solid dispersion. The prepared solid dissolution olmesartan confirmed the dissolution rate in the pH 1.2. It was compared with olmetec and improved dissolution rate through solid dispersion.