# US 9,750,813 B2 · Use of heptyl glucoside as skin penetration enhancer in transdermal pharmaceutical compositions

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- Number: US 9,750,813 B2
- Document ID: US9750813B2
- Status: Granted
- Kind: B2
- Application number: 14/682,419
- Filed: 2015-04-09
- Published: 2016-10-13
- Granted: 2017-09-05
- Earliest claimed: 2015-04-09
- Assignees: Professional Compounding Centers of America (PCCA)
- Applicants: Daniel Banov
- Inventors: Daniel Banov
- Web page: https://patentgrep.com/patent/US9750813B2

## CPC

- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 31/565: not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61P 5/00: Drugs for disorders of the endocrine system
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present disclosure refers to heptyl glucoside included, as a natural solubilizer and as a skin penetration enhancer, in transdermal pharmaceutical compositions. Heptyl glucoside is a natural alkyl glycoside and a hydrotrope that improves solubility of active pharmaceutical ingredients (APIs), thereby enhancing skin permeability to APIs. Transdermal pharmaceutical compositions including heptyl glucoside allow lower APIs dosage requirements. Heptyl glucoside can be combined with at least one API and suitable ingredients to formulate transdermal pharmaceutical compositions with improved skin permeability, thereby promoting percutaneous absorption of APIs. Transdermal pharmaceutical compositions including heptyl glucoside can be formulated in a plurality of dosage forms, such as, a liquid, cream, paste, gel, lotion, patch (e.g., matrix and reservoir), tape, film former (e.g., plaster), and the like.

## Claims

### Claim 1

A composition to be used for skin permeation, the composition comprising a combination of: 20% w/w heptyl glucoside; 1-10% w/w of a steroidal hormone; and an olive oil ester, wherein the heptyl glucoside is used as a natural solubilizer and as a skin permeation enhancer.

### Claim 2 (depends on 1)

The composition of claim 1, wherein the steroidal hormone is present at 1% w/w.

### Claim 3 (depends on 1)

The composition of claim 1, wherein the steroidal hormone is estradiol.

### Claim 4 (depends on 1)

The composition of claim 1, wherein the steroidal hormone is estriol.

### Claim 5 (depends on 1)

The composition of claim 1, wherein the oil ester is present at 79% w/w.

### Claim 6 (depends on 1)

The composition of claim 1, wherein the oil ester is Olive Oil Glycereth-8 Ester.

### Claim 7

A composition to be used for skin permeation, the composition comprising a combination of: 20% w/w heptyl glucoside; 1-10% w/w of a steroidal hormone; and an olive oil glycereth-8 ester, wherein the heptyl glucoside is used as a natural solubilizer and as a skin permeation enhancer.

### Claim 8 (depends on 7)

The composition of claim 7, wherein the steroidal hormone is present at 1% w/w.

### Claim 9 (depends on 7)

The composition of claim 7, wherein the composition is in a form selected from the group consisting of a liquid, cream, paste, gel, lotion, patch, tape, film former, and combinations thereof.