Novel composition for the transdermal administration of drugs

• US 20010023261A1
• Filed: 12/12/2000
• Published: 09/20/2001
• Est. Priority Date: 01/27/1997
• Status: Abandoned Application

• Current Assignee: LG Chem Limited (LG Corporation)
• Original Assignee: LG Chem Limited (LG Corporation)
• Inventors: Choi, Mi-Suk, Choi, Jong-Kun, Ryoo, Je-Phil
• Application Number:
  US09/746,448
• Publication Number:
  US 20010023261A1
• Time in Patent Office: Days
• US Class Current: 514/772
• CPC Class Codes: A61K 31/568 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
• CPC Class Codes: A61K 31/569 substituted in position 17 alpha, e.g. ethisterone
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: 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
• CPC Class Codes: 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
• CPC Class Codes: A61K 9/7061 Polyacrylates

Abstract

A composition for the transdermal administration of a drug, comprising: 0.05 to 50 wt % of the drug based on the total weight of the composition; 1 to 30 wt % of an absorption promoter consisting of a diethylene glycol ether and a sorbitan ester in a weight ratio ranging from 1:4 to 4:1, based on the total weight of the composition; and a pharmaceutically acceptable adhesive matrix.

Claims

1. A composition for the transdermal administration of a drug, comprising:

0.05 to 50 wt % of the drug based on the total weight of the composition;

1 to 30 wt % of an absorption promoter consisting of a diethylene glycol ether and a sorbitan ester in a weight ratio ranging from 1;

4 to 4;

1, based on the total weight of the composition; and

a pharmaceutically acceptable adhesive matrix.

2. The composition of

claim 1

, wherein the weight ratio of the diethylene glycol ether and the sorbitan ester ranges from 1:

2 to 2;

1.

3. The composition of

claim 1

, wherein the diethylene glycol ether is diethylene glycol monoethyl ether, diethylene glycol monomethyl ether or a mixture thereof.

4. The composition of

claim 1

, wherein the sorbitan ester is sorbitan monolaurate, sorbitan monooleate or a mixture thereof.

5. The composition of

claim 1

, wherein the amount of the drug ranges from 0.1 to 20 wt % based on the total weight of the composition.

6. The composition of

claim 1

, wherein the drug is an estrogen, progestogen, androgen, non-steroidal anti-inflammatory drug or a mixture thereof.

7. The composition of

claim 6

, wherein the amount of the androgen ranges from 1 to 10 wt % based on the total weight of the composition.

8. The composition of

claim 6

, wherein the amount of the non-steroidal anti-inflammatory drug ranges from 1 to 10 wt % based on the total weight of the composition.

9. The composition of

claim 6

, wherein the drug consists of 0.05 to 5 wt % of estrogen and 1 to 10 wt % of progestogen, each based on the total weight of the composition.

10. The composition of

claim 6

, wherein the estrogen is estradiol, ethynyl estradiol or estradiol ester.

11. The composition of

claim 6

, wherein the progestogen is norethisterone, norethisterone acetate, medroxyprogesterone acetate, desogestrel, gestaten or levonorgestrel.

12. The composition of

claim 6

, wherein the androgen is testosterone, testosterone propionate, testosterone enanthate, testosterone cypionate, methyltestosterone or dehydroepiandrosterone.

13. The composition of

claim 6

, wherein the non-steroidal anti-inflammatory drug is ketoprofen, flurbiprofen, methylsalicylate, salicylic acid, ibuprofen, indomethacin, diclofenac sodium, flufenamic acid, naproxen, mefenamic acid, fenoprofen, fenclofenac, piroxicam or a mixture thereof.

14. The composition of

claim 1

, wherein the amount of the absorption promoter ranges from 5 to 25 wt % based on the total weight of the composition.

15. The composition of

claim 1

, wherein the adhesive matrix is a polyacrylate adhesive, polyisobutylene or silicon rubber.

16. A transdermal formulation for the transdermal administration of a drug, comprising:

a protective backing layer;

a drug reservoir layer containing the composition of

claim 1

, which is placed on the protective backing layer, one side of which is laminated on the protective backing layer; and

a removable peel layer attached to the other side of the drug reservoir layer.

17. The formulation of

claim 16

, which further comprises a supplementary adhesive layer.