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Compositions and methods for drug delivery

Inactive Publication Date: 2002-05-16
HOUZE DAVID +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One drawback with the use of acrylic-based polymers with functional groups is that due to the generally high solubility of the drug in the polymer matrix, a large amount of drug generally must be incorporated into the dermal drug delivery composition to saturate it and provide an adequate flux to the skin of the user.
Another drawback is that the functional groups provide reaction sites for undesirable degradation reactions of the drug with the polymer matrix.
While these blends generally provide good results in terms of controlling the flux and the solubility of the drug within the matrix, polysiloxane adhesives are generally more expensive than acrylic-based adhesives resulting in higher production costs.
Of course, the surface area of the dermal delivery system also affects the delivery of the drug from the system through the skin.
The functionality of one of the acrylic-based polymers is such that it has a high drug solubility or loading requirements.
Since dermal drug delivery compositions made with high proportions of non-functional acrylic-based polymers generally do not have sufficient wear properties, there is an upper limit on the amount of non-functional acrylic-based adhesive incorporated into the composition.
For most drugs, the passage of the drugs through the skin or mucosa will be the rate-limiting step in delivery.

Method used

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  • Compositions and methods for drug delivery
  • Compositions and methods for drug delivery
  • Compositions and methods for drug delivery

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

and Comparative Example 1, the effect of acrylic functionality on haloperidol flux is determined. Haloperidol and other non-polymer components of a dermal delivery system are formulated in the indicated order to provide a masterbatch.

1 Masterbatch (all amounts are in grams) 1. toluene 17.55 2. ethanol 17.80 3. oleic acid 1.50 4. dipropylene glycol 2.51 5. Brij 52 2.04 6. haloperidol 5.00 Total 46.40 grams.

[0113] To the masterbatch the following acrylic-based polymers are added in the amounts indicated (all amounts are in grams of solution, i.e., solids and solvents):

[0114] DT 87-2196 (carboxy functional acrylic PSA, 50% solids) produced by National Starch, Inc.

[0115] HRJ 4483 (non-functional acrylic PSA, 50% solids)-produced by Schenectady, International, Inc.

2TABLE 1 Component Comp. (grams) Ex. 1 Ex. 1 Ex. 2 Ex. 3 Ex. 4 Master-batch 4.63 4.63 4.63 4.65 4.64 DT 87-2196 7.92 6.88 5.87 4.9 3.85 HRJ 4483 -- 1.05 2.05 2.98 4.01

[0116] The blends are drawn down to 20 mil thickness on a si...

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Abstract

A dermal composition for administration of a drug comprising a blend of two or more acrylic-based polymers having differing functionalities so as to modulate the drug solubility in the polymer matrix and the delivery rate of the drug, and methods therefor.

Description

[0001] In accordance with 35 U.S.C. .sctn.119 (e), the benefit of provisional application 60 / 115,927, filed Jan. 14, 1999, is hereby claimed. The entire contents of this provisional application are incorporated herein by reference.[0002] 1. Field of the Invention[0003] The present invention relates to compositions and methods for dermal administration of drugs, their method of making and method of use. In particular, the present invention is directed to a dermal drug delivery matrix system for the dermal application of one or more drugs, which includes a blend of two acrylic-based polymers having differing functionalities and a therapeutically effective amount of one or more drugs.[0004] 2. Description of Related Art[0005] The use of a dermal drug delivery composition, for example a pressure-sensitive adhesive containing a medicament, namely, a drug, as a means for administering therapeutically effective amounts of the medicament is well known. Such known delivery compositions invol...

Claims

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Application Information

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IPC IPC(8): A61K8/02A61K8/81A61K9/00A61K9/70A61Q19/00
CPCA61K8/0208A61K8/8147A61K8/8152A61K9/7061A61Q19/00A61K31/445A61K2800/54A61K2800/594A61K31/4439
Inventor HOUZE, DAVIDMANTELLE, JUANKANIOS, DAVID
Owner HOUZE DAVID