ENHANCED INTESTINAL-ABSORPTION OF AN RGD PEPTIDE FROM WATER-IN-OIL MICROEMULSIONS OF DIFFERENT COMPOSITION AND PARTICLE-SIZE

被引：67

作者：

CONSTANTINIDES, PP ^{[1
]}

LANCASTER, CM ^{[1
]}

MARCELLO, J ^{[1
]}

CHIOSSONE, DC ^{[1
]}

ORNER, D ^{[1
]}

HIDALGO, I ^{[1
]}

SMITH, PL ^{[1
]}

SARKAHIAN, AB ^{[1
]}

YIV, SH ^{[1
]}

OWEN, AJ ^{[1
]}

机构：

[1] IBAH INC,BIOPHARM DRUG DELIVERY SERV,ASTON,PA 19014

来源：

JOURNAL OF CONTROLLED RELEASE | 1995年 / 34卷 / 02期

关键词：

WATER-IN-OIL MICROEMULSION; LIPID COMPOSITION; PARTICLE SIZE; INTESTINAL ABSORPTION; FIBRINOGEN RECEPTOR ANTAGONIST; PHARMACOKINETICS;

D O I：

10.1016/0168-3659(94)00129-I

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The fibrinogen receptor antagonist SK and F 106760 is a water-soluble tetrapeptide (M(r) 634) with very low oil/water partitioning and membrane permeability. Thus, the intraduodenal bioavailability of this peptide in the rat from a saline formulation was found to be less than 1%. Upon formulation, however, in w/o microemulsions of different composition and particle size, the intraduodenal bioavailability of SK and F 106760 was increased up to 29% depending on the microemulsion composition. There was no apparent correlation between the particle size of microemulsions (mean droplet diameter of 0.010-1.0 mu m) and enhanced absorption. None of the investigated microemulsions induced gross changes in gastrointestinal mucosa at a dosing volume of 3.3 ml/kg. Lipids containing medium-chain fatty acids play a major role on the observed absorption enhancement. These findings further support the use of microemulsion formulations for oral drug/peptide delivery, provided however, that development issues with these systems are properly addressed.

引用

页码：109 / 116

页数：8

共 29 条

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