Critical properties of lactide-co-glycolide polymers for the use in microparticle preparation by the Aerosol Solvent Extraction System

被引:30
作者
Engwicht, A
Girreser, U
Müller, BW
机构
[1] Univ Kiel, Dept Pharmaceut & Biopharmaceut, D-24105 Kiel, Germany
[2] Univ Kiel, Dept Pharmaceut Chem, D-24105 Kiel, Germany
关键词
polylactide-co-glycolide; microparticles; supercritical fluids; NMR; powder diffraction; thermal analysis;
D O I
10.1016/S0378-5173(99)00127-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The Aerosol Solvent Extraction System (ASES) process uses supercritical carbon dioxide for the production of microparticles. Since the critical temperature for this gas is at 304 K, polymers that are used in this process must fulfil certain requirements in crystallinity, and thermal behavior. This can be achieved by the use of blocked copolymers and thus the presence of semicrystalline microdomains in the polymers. However, changing the sequences of the comonomers dilactide and lactide often leads to polymers of low solubility due to long glycolide blocks. In this study, the critical properties of two blocked co-polymers were investigated, such as the blocked structure itself by H-1-NMR and C-13-NMR, the thermal behavior by differential scanning calorimetry (DSC), and the crystallinity by powder diffraction. The impact of these properties on microparticles formed by those polymers was also object of these studies. Additionally, two different model drugs, albumin and estriolm were embedded to investigate the impact of different polymer properties on drug content and release. (C) 1999 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:61 / 72
页数:12
相关论文
共 8 条
  • [1] BRAUN S, 1996, 100 MORE BASIC NMR E, P234
  • [2] ENGWICHT A, 1998, IN PRESS NMR SPECTRO
  • [3] HARLAND RS, 1993, EUR J PHARM BIOPHARM, V39, P229
  • [4] KRICHELDORF HR, 1987, MAKROMOL CHEM, V188, P1861
  • [5] Synthesis, characterization, and hydrolytic degradation of PLA/PEO/PLA triblock copolymers with long poly(L-lactic acid) blocks
    Li, SM
    Rashkov, I
    Espartero, JL
    Manolova, N
    Vert, M
    [J]. MACROMOLECULES, 1996, 29 (01) : 57 - 62
  • [6] Muller B. W., 1991, US Patent, Patent No. [US5043280A, 5043280]
  • [7] RAFLER G, 1996, Patent No. 0573024
  • [8] TICE T R, 1985, Journal of Controlled Release, V2, P343, DOI 10.1016/0168-3659(85)90056-2