Convertible microemulsion formulations
AssigneeLDS Technologies, Inc.
InventorsAlbert J. Owen, Seang H. Yiv, Ani B. Sarkahian
Life of this patent
Estimating the term…
Abstract
There is provided a water-in-oil (w/o) micro emulsion which readily converts to an oil-in-water (o/w) emulsion by the addition of aqueous fluid to the w/o microemulsion, whereby an water-soluble biologically-active material in the aqueous phase is released for absorption by the body. The w/o microemulsion contains a preferred high purity short chain monoglyceride surfactant. The w/o microemulsion is particularly useful for storing proteins and the like for ling periods of time at room temperature and above until they are ready for use, at which time the addition of aqueous fluid converts the microemulsion to an o/w emulsion and release the protein.
Claims22
A stable, water-in-oil microemulsion composition suitable for storage and administration of biologically active materials, comprising:
- (a) from about 5 to about 99 volume percent of an oil phase comprising at least one pharmaceutically acceptable oil;
- (b) up to about 60 volume percent of an aqueous phase comprising water;
- (c) a biologically active material having a water:oil partition coefficient greater than 10:1;
- (d) from about 1 to about 70 volume percent of a mixture of surfactants having a combined HLB value of from about 7 to about 14 comprising
- (i) a low HLB surfactant having an HLB below 8, said low HLB surfactant being at least 80 percent by weight of a C.sub.9 monoglyceride, C.sub.10 monoglyceride, C.sub.11 monoglyceride, C.sub.12 monoglyceride, or C.sub.13 monoglyceride, and
- (ii) at least one surfactant having an HLB value above about 8.
A stable, water-in-oil microemulsion composition suitable for storage and administration of biologically active materials, comprising:
- (a) from about 5 to about 99 volume percent of an oil phase comprising at least one pharmaceutically acceptable oil;
- (b) up to about 60 volume percent of an aqueous phase comprising water;
- (c) a biologically active material that is a therapeutic and is a protein or peptide and has a water:oil partition coefficient greater than 10:1;
- (d) from about 1 to about 70 volume percent of a mixture of surfactants having a combined HLB value of greater than about 7, comprising
- (i) a low HLB surfactant having an HLB below 8, said low HLB surfactant being at least 80 percent by weight of a C.sub.9 monoglyceride, C.sub.10 monoglyceride, C.sub.11 monoglyceride, C.sub.12 monoglyceride, or C.sub.13 monoglyceride, and
- (ii) at least one surfactant having an HLB value above about 8, and
- (e) a modifier, present in an amount sufficient to cause the water-in-oil microemulsion to convert to an oil-in-water microemulsion upon the addition of aqueous fluid.
A method of administering to animals a water-in-oil microemulsion composition, comprising:
- (a) providing a water-in-oil microemulsion comprising
- (1) from about 5 to about 99 volume percent of an oil phase comprising at least one pharmaceutically acceptable oil;
- (2) up to about 60 volume percent of an aqueous phase comprising water;
- (3) a biologically active material that is therpeutic and has a water:oil partition coefficient greater than 10:1;
- (4) from about 1 to about 70 volume percent of a mixture of surfactants having a combined HLB value of from about 7 to about 14 comprising
- (i) a low HLB surfactant having an HLB below 8, said low HLB surfactant being at least 80 percent by weight of a C.sub.9 monoglyceride, C.sub.10 monoglyceride, C.sub.11 monoglyceride, C.sub.12 monoglyceride, or C.sub.13 monoglyceride, and
- (ii) at least one surfactant having an HLB value above about 8;
- (b) administering an effective amount of the water-in-oil microemulsion to the body of an animal, wherein the administration is parenterally, enterally, or via any other mucous membrane;
- and
- (c) achieving a therapeutically elective increase in the blood system of said animal of said biologically-active material.
Dependencies are inferred from the claim text.