# US 10,500,196 B2 · Transdermal and/or topical delivery systems composed of doxylamine succinate and pyridoxine hydrochloride in combination, or alone

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- Number: US 10,500,196 B2
- Document ID: US10500196B2
- Status: Granted
- Kind: B2
- Application number: 15/228,382
- Filed: 2016-08-04
- Published: 2017-02-23
- Granted: 2019-12-10
- Earliest claimed: 2015-08-17
- Assignees: Alpha To Omega Pharmaceutical Consultants, Inc.
- Applicants: Aequus Pharmaceuticals Inc.
- Inventors: Fotios M. Plakogiannis; Donald McAfee; Tamanna Lather; Marina Borovinskaya
- Web page: https://patentgrep.com/patent/US10500196B2

## CPC

- A61K 31/4415: Pyridoxine, i.e. Vitamin B6 (pyridoxal phosphate A61K31/675)
- 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 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 31/4402: only substituted in position 2, e.g. pheniramine, bisacodyl
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- A61K 47/38: Cellulose; Derivatives thereof
- 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

Pharmaceutical compositions for simultaneous transdermal delivery of Doxylamine and Pyridoxine comprising Doxylamine or its salts, Pyridoxine or its salts or its active metabolites and a vehicle system wherein pharmaceutical compositions are liquid formulations, semisolid formulations and polymer matrices. Further pharmaceutical compositions can be incorporated into transdermal delivery systems or transdermal patches. The invention provides a method for treatment of nausea and vomiting in general, and for pregnant women in particular by continuous and simultaneous transdermal delivery of Doxylamine and Pyridoxine. This is to be accomplished through topical application of pharmaceutical compositions or by application of a transdermal delivery system or transdermal patch to the surface of the skin wherein the duration of application is once in a day, once every two days, once every three days, once every four days, once every five days, once every six days, or once in a week.

## Claims

### Claim 1

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine Succinate,
5-20 wt % Pyridoxine Hydrochloride,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 2

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine Succinate,
5-20 wt % Pyridoxine Hydrochloride,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-30 wt % glycerine,
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 3

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine Succinate,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 4

A transdermal pharmaceutical composition as a semisolid formulation, wherein the semisolid formulation comprises:
5-20 wt % Doxylamine Succinate,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-30 wt % glycerine,
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 5

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine free base,
5-20 wt % Pyridoxine free base,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 6

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine free base,
5-20 wt % Pyridoxine free base,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-30 wt % glycerine,
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 7

A transdermal pharmaceutical composition as a semisolid formulation wherein the semisolid formulation comprises:
5-20 wt % Doxylamine free base,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 8

A transdermal pharmaceutical composition as a semisolid formulation, wherein the semisolid formulation comprises:
5-20 wt % Doxylamine free base,
5-45 wt % dimethylsulfoxide,
1-30 wt % hexylene glycol,
1-40 wt % diethylene glycol monoethyl ether,
1-25 wt % propylene glycol monolaurate type (II),
1-30 wt % glycerine,
1-50 wt % water,
1-10 wt % hydroxypropyl cellulose, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 9 (depends on 1)

The transdermal pharmaceutical composition of claim 1, wherein the semisolid formulation comprises:
Doxylamine Succinate about 9.00 wt %,
Pyridoxine HCl about 8.25 wt %,
Dimethyl Sulfoxide, about 30.25 wt %,
Hexylene Glycol about 10.0 wt %,
diethylene glycol monoethyl ether about 17.25 wt %,
Water about 17.75 wt %,
propylene glycol monolaurate type (II) about 4.0 wt %,
hydroxypropyl cellulose about 3.5 wt %, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.

### Claim 10 (depends on 5)

The transdermal pharmaceutical composition of claim 5, wherein the semisolid formulation comprises:
Doxylamine Free Base about 9.00 wt %,
Pyridoxine Free Base about 8.25 wt %,
Dimethyl Sulfoxide, about 30.25 wt %,
Hexylene Glycol about 10.0 wt %,
diethylene glycol monoethyl ether about 17.25 wt %,
Water about 17.75 wt %,
propylene glycol monolaurate type (II) about 4.0 wt %,
hydroxypropyl cellulose about 3.5 wt %, and
hydrochloric acid and/or sodium hydroxide to adjust the pH to between 4-7, wherein the transdermal pharmaceutical composition is in a reservoir patch.