.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Claims for Patent: 7,470,433

« Back to Dashboard

Claims for Patent: 7,470,433

Title:Formulations for transdermal or transmucosal application
Abstract:The present invention relates generally to formulations for transdermal or transmucosal administration of an active agent such as estradiol. The invention is a substantially malodorous-free and irritation free transdermal formulation which is substantially free of long chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters.
Inventor(s): Carrara; Dario Norberto R. (Oberwil, CH), Grenier; Arnaud (Steinbrunn le Haut, FR), Besse; Celine (Saint Louis, FR), Simes; Stephen M. (Long Grove, IL), Lehman; Leah M. (Green Oaks, IL)
Assignee: Antares Pharma IPL AG (Zug, CH)
Application Number:11/693,988
Patent Claims: 1. A gel formulation for transdermal or transmucosal administration of an active agent, the formulation comprising: at least one active agent comprising estrogen; a gelling agent and a delivery vehicle comprising a C.sub.2 to C.sub.4 alkanol, a polyalcohol, and a permeation enhancer of monoalkyl ether of diethylene glycol present in an amount sufficient to provide permeation enhancement of the active agent through dermal or mucosal surfaces; wherein the formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters in order to avoid undesirable odor and irritation effects caused by such compounds during use of the formulation; provided that a progestin is not present in the formulation.

2. The formulation of claim 1, wherein the amount of estrogen is between about 0.01% to 10% by weight of the formulation and the daily administration of the formulation in an amount of from about 0.625 g to about 2.5 g.

3. The formulation of claim 2, wherein the amount of estrogen is about 0.06% by weight of the formulation and the daily administration of the formulation is made in an amount of about 1.25 g to about 2.5 g.

4. The formulation of claim 1, wherein the estrogen is selected from the group consisting of 17 beta-estradiol, estradiol, estradiol benzoate, estradiol 17 beta-cypionate, estriol, estrone, ethynil estradiol, mestranol, moxestrol, mytatrienediol, polyestradiol phosphate, quinestradiol, quinestrol, and any combination thereof.

5. The formulation of claim 1, wherein the polyalcohol is present in an amount between about 1% and 30% by weight of the vehicle; the alkanol is present in an amount of 5 to 75% by weight of the vehicle, and the permeation enhancer is present in an amount of between about 0.2% and 25% by weight of the vehicle.

6. The formulation of claim 5, wherein the alkanol is present in an amount between about 20 to 65% by weight of the formulation; the polyalcohol is present in an amount between about 1% to 15% by weight of the formulation; and the permeation enhancer is present in an amount between about 1% to 15% by weight of the formulation.

7. The formulation of claim 6, wherein the alkanol is selected from the group consisting of ethanol, isopropanol and n-propanol, and wherein the polyalcohol is polypropylene glycol.

8. The formulation of claim 7, wherein the polyalcohol and permeation enhancer are present in a weight ratio of 1.25:1 to 1.2:1 and the formulation further comprises a gelling agent present in an amount of between 0.05% to about 4% by weight of the formulation, a neutralizing agent present in an amount between about 0.05% and 1% by weight of the formulation, and water present in an amount between about 20% to 65% by weight of the formulation so that the formulation is provided as a gel.

9. The formulation of claim 1, wherein the formulation further comprises at least one of a neutralizing agent, sequestering agent, buffering agent, moisturizing agent, humectant, surfactant, antioxidant, emollient, buffer or a combination thereof.

10. The formulation of claim 9, wherein the gelling agent is selected from the group consisting of carbomer, carboxyethylene, polyacrylic acid, ethylcellulose, hydroxypropylmethylcellulose, ethylhydrooxyethylcellulose, carboxymethylcellulose, hydroxypropylcellulose, hydroxyethylcellulose, natural gums, arabic, xanthan, guar gums, alginates, polyvinylpyrrolidone polymers, polyoxyethylene polyoxypropylene copolymers, chitosan, polyvinyl alcohol, pectin, and veegum; the buffering agent is selected from the group consisting of carbonate buffers, citrate buffers, phosphate buffers, acetate buffers, hydrochloric acid, lactic acid, tartaric acid, diethylamine, triethylamine, diisopropylamine, tetrahydroxypropylethylendiamine, and aminomethylamine; or the sequestering agent is edetic acid.

11. The formulation of claim 1 wherein the active agent is estradiol.

12. The formulation of claim 1 comprising the following composition: 0.01 to 1% by weight of estradiol, 1.2% by weight of carbomer 940, 0.4% by weight of triethanolamine (adjust to pH 5.9), 46.28% by weight of alcohol, 6% by weight of propylene glycol, 5% by weight of diethylene glycol monoethyl ether, 0.06% by weight of disodium EDTA and 100% by weight of ion exchange purified water q. ad.

13. A gel formulation for transdermal or transmucosal administration of an active agent, the formulation comprising: estrogen; a gelling agent; and a delivery vehicle comprising a C.sub.2 to C.sub.4 alkanol, a polyalcohol, and a permeation enhancer of monoalkyl ether of diethylene glycol to provide permeation enhancement of the active agent through dermal or mucosal surfaces, wherein the polyalcohol is propylene glycol and is present in an amount between about 1% and 30% of the vehicle, the permeation enhancer is diethylene glycol monoethyl ether and is present in an amount of between about 0.2% and 25% of the vehicle, the alkanol is ethanol and is present in an amount of 5 to 75% by weight of the vehicle wherein the formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty in order to avoid undesirable odor and irritation effects caused by such compounds during use of the formulation; provided that a progestin is not present in the formulation.

14. The formulation of claim 13, wherein the amount of estrogen is between about 0.01% to 10% by weight of the formulation and the daily administration of the formulation in an amount of from about 0.625 g to about 2.5 g.

15. The formulation of claim 13, wherein the amount of estrogen is about 0.06% by weight of the formulation and the daily administration of the formulation is made in an amount of about 1.25 g to about 2.5 g.

16. The formulation of claim 13, wherein the alkanol is present in an amount between about 20 to 65% of the formulation; the polyalcohol is propylene glycol present in an amount between about 1% to 15% of the formulation; the permeation enhancer is diethylene glycol monoethyl ether present in an amount between about 1% to 15% of the formulation, and further wherein the formulation comprises a gelling agent present in an amount of between 0.05% to about 4% of the formulation, a neutralizing agent present in an amount between about 0.05% and 1% of the formulation, and water present in an amount between about 20% to 65% of the formulation so that the formulation is in the form of a gel.

17. The formulation of claim 13 wherein the active agent is estradiol.

18. The formulation of claim 13 comprising the following composition: 0.01 to 2% by weight of estradiol, 0.05-4% by weight of carbomer, 0.05-1% by weight of triethanolamine (adjust to pH 5.9), 20-65% by weight of alcohol, 1-15% by weight of propylene glycol, 1-15% by weight of diethylene glycol monoethyl ether, 20-65% by weight of ion exchange purified water q. ad.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc