US4764378A
Expired / Lapsed
US
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Buccal drug dosage form
Assignee: Actavis Laboratories UT Inc
•
Filing: 1986-02-10
•
Granted: 1988-08-16
•
Expires: 2006-02-10
Abstract
Abstract Buccal dosage forms for transmucosal administration of drugs comprise a pharmaceutical compound dispersed in an erodible matrix comprising from about 20 to about 75 percent by weight of a low molecular weight polyethylene glycol component, from about 2 to about 65 percent by weight of a medium or high molecular weight polyethylene glycol component, from about 1% to about 40% percent by weight of an auxiliary high molecular weight polymer. Preferred auxiliary high molecular weight polymers are polyethylene oxide and polyvinylpyrrolidone which improve the molding properties of the matrix and provide water-activated adhesive properties to the compositions to provide a buccal dosage form.
Inventors
- 👤 Alec D. Keith
- 👤 Wallace C. Snipes
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 20:41
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0053; A61K9/006; A61K9/20; A61K9/2004; A61K9/2013; A61K9/2022; A61K9/2027; A61K9/2031
Claims Analysis
Total Claims: 46
Claim 1
Independent Claim
161 words
An injection molded, cast, or otherwise solidified buccal or transmucosal oral mucosa adherent dosage form having dimensions which fit into the buccal cavity or under the tongue of a user thereof comprising a pharmaceutical ingredient selected from a pharmaceutical compound, a pharmaceutically acceptable salt, and derivatives thereof adapted to be dispensed typically over a period of 10-30 minutes through transmucosal absorption directly into the bloodstream, said pharmaceutical ingredient being dispersed in a non-crystalline, solidified polymeric matrix which adheres to oral mucosa after being activated by water or saliva comprising, from about 20 to about 75 percent by weight of a polyethylene glycol component having a low molecular weight of from about 100-4000, from about 2 to about 54 percent by weight of a polyethylene glycol component having a medium to high molecular weight of from about 6000-20,000, and from about 1 to about 40 percent by weight of polyethylene oxide having a high molecular weight of from about 100,000 to 5,000,000.
Claim 2
Dependent Claim
161 words
An injection molded, cast, or otherwise solidified buccal or transmucosal oral mucosa adherent dosage form having dimensions which fit into the buccal cavity or under the tongue of a user thereof comprising a pharmaceutical ingredient selected from a pharmaceutical compound, a pharmaceutically acceptable salt, and derivatives thereof adapted to be dispensed typically over a period of 10-30 minutes through transmucosal absorption directly into the bloodstream, said pharmaceutical ingredient being dispersed in a non-crystalline, solidified polymeric matrix which adheres to oral mucosa after being activated by water or saliva comprising, from about 20 to about 75 percent by weight of a polyethylene glycol component having a low molecular weight of from about 100-4000, from about 2 to about 54 percent by weight of a polyethylene glycol component having a medium to high molecular weight of from about 6000-20,000, and from about 1 to about 40 percent by weight of polyethylene oxide having a high molecular weight of from about 100,000 to 5,000,000.
Claim 3
Dependent Claim
23 words
The dosage form of claim 1 wherein said low molecular weight polyethylene glycol component is a mixture of low molecular weight polyethylene glycols.
Claim 4
Dependent Claim
23 words
The dosage form of claim 2 wherein said mixture of low molecular weight polyethylene glycols comprises PEG 1000, PEG 1450 and PEG 3350.
Claim 5
Dependent Claim
32 words
The dosage form of claim 1 wherein said low molecular weight polyethylene glycol component is present in a proportion of from about 35% to about 65% by weight of the total composition.
Claim 6
Dependent Claim
19 words
The dosage form of claim 1 wherein said medium or high molecular weight polyethylene glycol component comprises PEG 8000.
Claim 7
Dependent Claim
18 words
The dosage form of claim 1 wherein said medium or high molecular weight polyethylene glycol comprises PEG 20,000.
Claim 8
Dependent Claim
25 words
The dosage form of claim 1 wherein said medium or high molecular weight component is a mixture of medium and high molecular weight polyethylene glycols.
Claim 9
Dependent Claim
26 words
The dosage form of claim 7 wherein said mixture of medium and high molecular weight polyethylene glycols is a mixture of PEG 8000 and PEG 20,000.
Claim 10
Dependent Claim
17 words
The dosage form of claim 1 wherein said polyethylene oxide has a molecular weight of about 100,000.
Claim 11
Dependent Claim
17 words
The dosage form of claim 1 wherein said polyethylene oxide has a molecular weight of about 5,000,000.
Claim 12
Dependent Claim
31 words
The dosage form of claim 1 wherein said polyethylene oxide has a molecular weight of about 100,000 and is present in an amount from about 2% to about 10% by weight.
Claim 13
Dependent Claim
10 words
The dosage form of claim 1 additionally comprising a plasticizer.
Claim 14
Dependent Claim
12 words
The dosage form of claim 12 wherein said plasticizer is propylene glycol.
Claim 15
Dependent Claim
20 words
The dosage form of claim 12 wherein said plasticizer is present in a proportion of about 3 percent by weight.
Claim 16
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is nitroglycerin.
Claim 17
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is scopolamine.
Claim 18
Dependent Claim
13 words
The dosage form of claim 1 wherein said pharmaceutical compound is an estrogen.
Claim 19
Dependent Claim
19 words
The dosage form of claim 17 wherein said estrogen is selected from the group consisting of 17-beta-estradiol and ethinylestradiol.
Claim 20
Dependent Claim
24 words
The dosage form of claim 17 wherein said estrogen is present in proportion of from about 0.02 percent to about 0.05 percent by weight.
Claim 21
Dependent Claim
13 words
The dosage form of claim 1 wherein said pharmaceutical compound is a progestin.
Claim 22
Dependent Claim
11 words
The dosage form of claim 20 wherein said progestin is norethindrone.
Claim 23
Dependent Claim
25 words
The dosage form of claim 20 wherein said progestin is present in a proportion of from about 1.0 percent to about 5.0 percent by weight.
Claim 24
Dependent Claim
19 words
The dosage form of claim 1 wherein said pharmaceutical compound is a mixture of an estrogen and a progestin.
Claim 25
Dependent Claim
44 words
The dosage form of claim 33 wherein said estrogen is present in a proportion of from about 0.02 percent to about 0.05 percent by weight and said progestin is present in a proportion of from about 1.0 percent to about 5.0 percent by weight.
Claim 26
Dependent Claim
36 words
The dosage form of claim 23 wherein said estrogen is ethinylestradiol present in a proportion of about 0.02 percent by weight and said progestin is norethindrone present in a proportion of about 2.0 percent by weight.
Claim 27
Dependent Claim
36 words
The dosage form of claim 23 wherein said estrogen is 17-beta-estradiol present in a proportion of about 0.2 percent by weight and said progestin is norethindrone present in a proportion of about 2.0 percent by weight.
Claim 28
Dependent Claim
14 words
The dosage form of claim 1 wherein said pharmaceutical compound is gonadotropin releasing hormone.
Claim 29
Dependent Claim
14 words
The dosage form of claim 1 wherein said pharmaceutical compound is human growth hormone.
Claim 30
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is insulin.
Claim 31
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is phenylephrine.
Claim 32
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is desmopressin.
Claim 33
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is oxytocin.
Claim 34
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is vasopressin.
Claim 35
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is nicotine.
Claim 36
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is verapamil.
Claim 37
Dependent Claim
13 words
The dosage form of claim 1 wherein said pharmaceutical compound is isosorbide dinitrate.
Claim 38
Dependent Claim
12 words
The dosage form of claim 1 wherein said pharmaceutical compound is oxymetazoline.
Claim 39
Dependent Claim
33 words
The dosage form of claim 1 having the following composition ______________________________________
PEG 1450 11.0% by weight
PEG 3350 25.0% by weight
PEG 8000 59.0% by weight
PEO (MW 5,000,000)
5.0% by weight
______________________________________
Claim 40
Dependent Claim
15 words
The dosage form of claim 1 wherein said dosage form is a buccal dosage form.
Claim 41
Dependent Claim
15 words
The dosage form of claim 1 wherein said dosage form is an oral dosage form.
Claim 42
Dependent Claim
26 words
The dosage form of claim 1 wherein said dosage form is selected from the group consisting of a lozenge, a lamella, a disk, and a wafer.
Claim 43
Dependent Claim
49 words
The dosage form of claim 1 wherein said dosage form is a buccal dosage form having a length of from about 5 mm to about 10 mm, a width of from about 2 mm to about 10 mm and a thickness of from about 0.2 mm to 3 mm.
Claim 44
Dependent Claim
18 words
The dosage form of claim 42 wherein said thickness is from about 0.5 mm to about 1.5 mm.
Claim 45
Dependent Claim
22 words
The dosage form of claim 1 wherein the total weight of said dosage is from about 10 mg to about 150 mg.
Claim 46
Dependent Claim
23 words
The dosage form of claim 1 wherein the total weight of said dosage form is from about 50 mg to about 100 mg.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-08-16 | 1992-02-15 | 1992-08-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-16 | 1996-02-15 | 1996-08-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-16 | 2000-02-15 | 2000-08-16 | $7700.00 | Window Closed / Lapsed |