Patches, formulations, and associated methods for transdermal delivery of alprazolam and other drugs
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A01N-043/62
A61K-031/55
C07D-513/00
C07D-515/00
C07D-487/12
A61K-009/70
A61K-031/485
A61K-031/519
A61K-031/5517
A61K-009/00
A61K-047/10
출원번호
US-0340246
(2008-12-19)
등록번호
US-8927537
(2015-01-06)
발명자
/ 주소
Sharma, Sanjay
Warner, Kevin S.
Zhang, Jie
Yan, Guang
출원인 / 주소
Nuvo Research Inc.
대리인 / 주소
Thorpe North & Western LLP
인용정보
피인용 횟수 :
0인용 특허 :
5
초록▼
The present invention is drawn to transdermal drug formulations, transdermal patches incorporating such formulations, as well as associated methods. The formulations can include about 0.3 wt % to about 5 wt % of a drug, such as alprazolam, about 4 wt % to about 30 wt % water, about 10 wt % to about
The present invention is drawn to transdermal drug formulations, transdermal patches incorporating such formulations, as well as associated methods. The formulations can include about 0.3 wt % to about 5 wt % of a drug, such as alprazolam, about 4 wt % to about 30 wt % water, about 10 wt % to about 40 wt % glycerol, about 0.5 wt % to about 6 wt % oleyl alcohol. Other co-solvents and/or additives can be present to achieve a 100 wt % formulation.
대표청구항▼
1. A formulation for transdermal delivery of a drug, comprising from about 0.3 wt % to about 5 wt % of alprazolam,from about 4 wt % to about 30 wt % water,from about 10 wt % to about 40 wt % glycerol, andfrom about 0.5 wt % to about 6 wt % oleyl alcohol,wherein the alprazolam in the formulation has
1. A formulation for transdermal delivery of a drug, comprising from about 0.3 wt % to about 5 wt % of alprazolam,from about 4 wt % to about 30 wt % water,from about 10 wt % to about 40 wt % glycerol, andfrom about 0.5 wt % to about 6 wt % oleyl alcohol,wherein the alprazolam in the formulation has a degradation rate of less than 5% per year at 25° C. 2. A formulation as in claim 1, further comprising from about 20 wt % to about 85 wt % of additional solvent. 3. A formulation as in claim 1, wherein alprazolam comprises about 0.5 wt % to about 3 wt % of the formulation. 4. A formulation as in claim 1, wherein alprazolam comprises about 0.8 wt % to about 1.8 wt % of the formulation. 5. A formulation as in claim 1, wherein alprazolam comprises about 1.0 wt % to about 1.5 wt % of the formulation. 6. A formulation as in claim 1, wherein water comprises about 5 wt % to about 25 wt % of the formulation. 7. A formulation as in claim 1, wherein water comprises about 6 wt % to about 15 wt % of the formulation. 8. A formulation as in claim 1, wherein glycerol comprises about 15 wt % to 37 wt % about of the formulation. 9. A formulation as in claim 1, wherein glycerol comprises about 20 wt % to about 35 wt % of the formulation. 10. A formulation as in claim 1, wherein the oleyl alcohol comprises about 1 wt % to about 5 wt % of the formulation. 11. A formulation as in claim 1, wherein the oleyl alcohol comprises about 2 wt % to about 4 wt % of the formulation. 12. A formulation as in claim 2, wherein the additional solvent includes propylene glycol. 13. A formulation as in claim 1, wherein the formulation has a pH of 7.0 to 10. 14. A formulation as in claim 1, wherein the formulation includes a compound selected from the group consisting of BHT and EDTA. 15. A formulation as in claim 1, wherein the formulation includes a skin irritation reduction agent selected from the group consisting of corticosteroids and anti-inflammatory agents. 16. A formulation as in claim 1, wherein the formulation has a viscosity of about 20,000 to centipoise to about 200,000 centipoise. 17. A formulation as in claim 1, incorporated in a transdermal patch. 18. A transdermal patch for transdermal delivery of alprazolam, comprising: a transdermal drug formulation incorporated into a transdermal patch, said transdermal drug formulation comprising from about 0.3 wt % to about 5 wt % alprazolam, from about 4 wt % to about 30 wt % water, from about 10 wt % to about 40 wt % glycerol, from about 0.5 wt % to about 6 wt % oleyl alcohol, and optionally from about 20 wt % to about 85 wt % of additional solvent, wherein the alprazolam in the formulation has a degradation rate of less than 5% per year at 25° C. 19. A transdermal patch as in claim 18, wherein the patch has a formulation-skin contact area of from 2 cm2 to 100 cm2. 20. A transdermal patch as in claim 18, wherein the patch has a formulation-skin contact area of from 5 cm2 to 60 cm2. 21. A patch as in claim 20, wherein each square centimeter of the formulation-skin contact area generates a mean AUC of at least 20 ng·hr/ml when administered to at least 10 human adults for a 72 hour period of time. 22. A transdermal patch as in claim 20, wherein each square centimeter of the formulation-skin contact area generates a mean AUC of at least 34 ng·hr/ml when administered to at least 10 human adults for a 72 hour period of time. 23. A transdermal patch as in claim 20, wherein each square centimeter of the formulation-skin contact area generates a mean AUC of at least 50 ng·hr/ml when administered to at least 10 human adults for a 72 hour period of time. 24. A transdermal patch as in claim 20, wherein the total quantity of alprazolam in said patch per cm2 of the transdermal drug formulation-skin contact area is less than 2 mg/cm2. 25. A transdermal patch as in claim 18, wherein the patch includes a microporous non-rate-limiting membrane. 26. A transdermal patch as in claim 18, wherein the patch is configured to deliver alprazolam therapeutically effective rates for a period of at least 48 hours. 27. A formulation for transdermal delivery of alprazolam, comprising: alprazolam,about 6 wt % to about 15 wt % water,about 20 wt % to about 35 wt % glycerol,about 40% to about 70% propylene glycol, andabout 2 wt % to about 4 wt % oleyl alcoholwherein the alprazolam in the formulation has a degradation rate of less than 5% per year at 25° C. 28. A formulation as in claim 27 incorporated into a transdermal patch. 29. A formulation as in claim 27, said formulation having a pH of 7-10. 30. A formulation as in claim 27, wherein the alprazolam is present at from about 1.0 wt % to about 1.5 wt %. 31. A transdermal patch for transdermal delivery of alprazolam, comprising: a transdermal drug formulation incorporated in a transdermal patch, wherein the transdermal drug formulation comprises about 1.0 wt % to about 1.5 wt % alprazolam, about 6 wt % to about 15 wt % water, about 20 wt % to about 35 wt % glycerol, about 40% to about 70% propylene glycol, from about 2 wt % to about 4 wt % oleyl alcohol, and has a pH of 7-10; wherein each square centimeter of the contact area between said formulation and the skin is capable of generating a mean AUC of at least 50 ng.hr/ml when administered to at least 10 human adults for a 72 hour period of time and wherein the alprazolam in the formulation has a degradation rate of less than 5% per year at 25° C. 32. A method of treating anxiety disorder or panic disorder in a subject, comprising: applying a transdermal drug formulation to a skin surface of a subject, said transdermal formulation comprising from about 0.3 wt % to about 5 wt % alprazolam, from about 4 wt % to about 30 wt % water, from about 10 wt % to about 40 wt % glycerol, and from about 0.5 wt % to about 6 wt % oleyl alcohol and optionally about 20 wt % to about 85 wt % of additional solvent; andmaintaining said transdermal drug formulation in contact with said skin surface for a period of at least 48 hours. 33. A method as in claim 32, wherein the applying step is by applying the transdermal drug formulation to the skin surface by way of a transdermal patch which includes the transdermal drug formulation.
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이 특허에 인용된 특허 (5)
Patel Dinesh C. (Murray UT) Chang Yunik (Lakewood NJ), Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols.
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