LIPID MICROEMULSIONS FOR IMPROVING DRUG DISSOLUTION AND ORAL ABSORPTION - PHYSICAL AND BIOPHARMACEUTICAL ASPECTS

被引:592
作者
CONSTANTINIDES, PP
机构
[1] Pharmaceutical Development, UW 2921 Pharmaceutical Technologies, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania, 19406
关键词
SELF-EMULSIFYING SYSTEMS; MICROEMULSIONS; DRUG DISSOLUTION; MEMBRANE PERMEABILITY; INTESTINAL ABSORPTION; MEDIUM-CHAIN GLYCERIDES; ENHANCER; PEPTIDE DELIVERY;
D O I
10.1023/A:1016268311867
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Purpose. This review highlights the state-of-the-art in pharmaceutical microemulsions with emphasis on self-emulsifying systems, from both a physical and biopharmaceutical perspective. Although these systems have several pharmaceutical applications, this review is primarily focused on their potential for oral drug delivery and intestinal absorption improvement. Methods. Physicochemical characteristics and formulation design based on drug solubility and membrane permeability are discussed. Results. Case studies in which lipid microemulsions have successfully been used to improve drug solubilization/dissolution and/or intestinal absorption of poorly absorbed drugs/peptides are presented. Conclusions. Drug development issues such as commercial viability, mechanisms involved, range of applicability, safety, scale-up and manufacture are outlined, and future research and development efforts to address these issues are discussed.
引用
收藏
页码:1561 / 1572
页数:12
相关论文
共 51 条
  • [1] A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY
    AMIDON, GL
    LENNERNAS, H
    SHAH, VP
    CRISON, JR
    [J]. PHARMACEUTICAL RESEARCH, 1995, 12 (03) : 413 - 420
  • [2] DRUG RELEASE FROM LIPID-BASED DOSAGE FORMS .2.
    ARMSTRONG, NA
    JAMES, KC
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1980, 6 (3-4) : 195 - 204
  • [3] ENTERAL, ORAL, AND RECTAL ABSORPTION OF CEFTRIAXONE USING GLYCERIDE ENHANCERS
    BESKID, G
    UNOWSKY, J
    BEHL, CR
    SIEBELIST, J
    TOSSOUNIAN, JL
    MCGARRY, CM
    SHAH, NH
    CLEELAND, R
    [J]. CHEMOTHERAPY, 1988, 34 (02) : 77 - 84
  • [4] CABAZAT AM, 1980, J COLLOID INTERF SCI, V73, P1
  • [5] SELF-EMULSIFYING DRUG DELIVERY SYSTEMS - FORMULATION AND BIOPHARMACEUTIC EVALUATION OF AN INVESTIGATIONAL LIPOPHILIC COMPOUND
    CHARMAN, SA
    CHARMAN, WN
    ROGGE, MC
    WILSON, TD
    DUTKO, FJ
    POUTON, CW
    [J]. PHARMACEUTICAL RESEARCH, 1992, 9 (01) : 87 - 93
  • [6] CHO YW, 1989, Patent No. 4849227
  • [7] PARTICLE-SIZE DETERMINATION OF PHASE-INVERTED WATER-IN-OIL MICROEMULSIONS UNDER DIFFERENT DILUTION AND STORAGE-CONDITIONS
    CONSTANTINIDES, PP
    YIV, SH
    [J]. INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 115 (02) : 225 - 234
  • [8] ENHANCED INTESTINAL-ABSORPTION OF AN RGD PEPTIDE FROM WATER-IN-OIL MICROEMULSIONS OF DIFFERENT COMPOSITION AND PARTICLE-SIZE
    CONSTANTINIDES, PP
    LANCASTER, CM
    MARCELLO, J
    CHIOSSONE, DC
    ORNER, D
    HIDALGO, I
    SMITH, PL
    SARKAHIAN, AB
    YIV, SH
    OWEN, AJ
    [J]. JOURNAL OF CONTROLLED RELEASE, 1995, 34 (02) : 109 - 116
  • [9] FORMULATION AND INTESTINAL-ABSORPTION ENHANCEMENT EVALUATION OF WATER-IN-OIL MICROEMULSIONS INCORPORATING MEDIUM-CHAIN GLYCERIDES
    CONSTANTINIDES, PP
    SCALART, JP
    LANCASTER, C
    MARCELLO, J
    MARKS, G
    ELLENS, H
    SMITH, PL
    [J]. PHARMACEUTICAL RESEARCH, 1994, 11 (10) : 1385 - 1390
  • [10] CONSTANTINIDES PP, 1994, Patent No. 9408610