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

Hwang, Sung-Joo   (College of Pharmacy. Chungnam National University  ); Lee, Myung-Gulll   (College of Pharmacy, Seoul National University  ); Kim, Chong-Kook   (College of Pharmacy, Seoul National University  );
  • 초록

    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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  • 주제어

    Hydrophilic albumin microspheres  . methotrexate  . methotrexate-human serum albumin conjugates  . in virto drug release  . drug release by protease  . zero-order release  .

 저자의 다른 논문

  • 황성주 (72)

    • 1. 1990 Preparation of Substained-Release Microspheres of Phenylpropanolamine HCI and Their Release Characteristics Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 13 (4): 293~297    
    • 2. 1991 Microencapsulation of Isoprinosine with Ethylcellulose Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 14 (4): 298~304    
    • 3. 1993 치아 연마용 인산일수소칼슘의 합성 및 물리화학적 성질 약학회지 = Yakhak hoeji 37 (1): 66~75    
    • 4. 1993 오메프라졸과 Hydroxypropyl-$\beta$-cyclodextrin의 포접화합물의 형성과 특성 약학회지 = Yakhak hoeji 37 (4): 331~340    
    • 5. 1993 오메푸라졸 함유 직장좌제의 제제설계 약학회지 = Yakhak hoeji 37 (4): 370~382    
    • 6. 1993 오메프라졸 함유 직장좌제의 약물속도론적 연구 약학회지 = Yakhak hoeji 37 (5): 427~436    
    • 7. 1994 이온교환수지를 이용한 새로운 오메프라졸 복합체 개발 약학회지 = Yakhak hoeji 38 (3): 250~264    
    • 8. 1995 비이온성 미셀용액과 수중유형 마이크로에멀젼계의 특성 및 수단 IV의 가용화 약학회지 = Yakhak hoeji 39 (5): 495~505    
    • 9. 1997 설린닥의 경구용 지속성 제제설계 및 용출특성 약학회지 = Yakhak hoeji 41 (1): 48~59    
    • 10. 1997 설린닥의 경구용 지속성 제제설계 및 생체이용율 약학회지 = Yakhak hoeji 41 (1): 60~73    
  • Lee, Myung-Gulll (0)

  • Kim, Chong-Kook (188)

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