# US 5,707,873 A · Method of accessing mixed lipid transport properties of a drug

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 5,707,873 A
- Document ID: US5707873A
- Status: Granted
- Kind: A
- Application number: 08/449,225
- Filed: 1995-05-24
- Granted: 1998-01-13
- Earliest claimed: 1990-08-13
- Inventors: David W. Yesair
- Web page: https://patentgrep.com/patent/US5707873A

## CPC

- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A method of assessing the mixed lipid transport properties of a drug is provided. The method includes providing a mixed lipid composition which incorporates a drug in colloidal particles, applying the particles to a size exclusion chromatography column, eluting free drug and drug incorporated into mixed lipid particles from the column, and determining the elution profiles of the free drug and the drug incorporated into mixed lipid particles. Drugs which elute with the mixed lipid particles are considered to have stable transport properties when incorporated into the mixed lipid particles.

## Claims

### Claim 1

A method of assessing the mixed lipid transport properties of a drug in a mixed lipid composition comprising the steps of:
a. providing a mixed lipid composition comprising:
i. at least one non-esterified fatty acid;
ii. at least one monoglyceride which is a monoester of glycerol and a fatty acid;
iii. lysophosphatidylcholine; and
iv. said drug;
wherein the molar ratio of said at least one non-esterified fatty acid to said at least one monoglyceride is from about 2:1 to about 1:2, and the amount of said lysophosphatidylcholine is from about 1.0 mole percent to about 30.0 mole percent of the total lipid formulation;
b. placing the mixed lipid composition of at least one non-esterified fatty acid, at least one monoglyceride, lysophosphatidylcholine and drug in an aqueous environment containing bicarbonate;
c. subjecting said mixed lipid composition to shearing forces sufficient to cause formation of mixed lipid-bicarbonate colloidal particles which incorporate the drug;
d. applying said particles to a size exclusion chromatography column;
e. eluting said particles from said size exclusion chromatography column; and
f. determining the elution profiles of the free drug and the drug incorporated into the particles; wherein drags eluting with said particles are considered to be stably transportable in the mixed lipid composition.

### Claim 2 (depends on 1)

The method of claim 1, wherein a fatty acid moiety of the lysophosphatidylcholine has 14-18 carbon atoms.

### Claim 3 (depends on 1)

The method of claim 1, wherein the at least one non-esterified fatty acid has 14-18 carbon atoms.

### Claim 4 (depends on 1)

The method of claim 1 wherein the at least one monoglyceride has 14-18 carbon atoms.

### Claim 5 (depends on 1)

The method of claim 1, wherein a fatty acid moiety of the lysophosphatidylcholine has 14-18 carbon atoms, the at least one non-esterified fatty acid has 14-18 carbon atoms and the at least one monoglyceride has 14-18 carbon atoms.

### Claim 6 (depends on 1)

The method of claim 1, wherein the mixed lipid composition includes an unsaturated fatty acid selected from the group consisting dan unsaturated fatty acid of the lysophosphatidylcholine, an unsaturated fatty acid of the at least one non-esterified fatty acid, and an unsaturated fatty acid of the at least one monoglyceride.

### Claim 7 (depends on 1)

The method of claim 1, wherein a biologically compatible surfactant is added to the aqueous environment containing bicarbonate.

### Claim 8 (depends on 1)

The method of claim 1 comprising the addition of bile salts to said aqueous environment before applying said shearing forces, wherein the molar ratio of said bile salts to said lysophosphatidylcholine is at least 10:1.

### Claim 9 (depends on 8)

The method of claim 8, wherein a biologically compatible surfactant is added to the aqueous environment containing bicarbonate and bile salt.