Formulations for coated microprojections having controlled solubility
First Claim
1. A composition for coating a transdermal delivery device having stratum corneum-piercing microprojections comprising a formulation of a biologically active agent, a non-volatile counterion and a volatile counterion, wherein said non-volatile counterion causes the formation of a first species of said biologically active agent that has improved solubility when said formulation is dried and wherein said volatile counterion causes the formation of a second species of said biologically active agent that has reduced solubility when said formulation is dried.
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Abstract
The invention provides for a formulation for coating one or more microprojections using a non-volatile counterion to improve solubility of a biologically active agent. The invention also includes formulations having a volatile counterion to reduce the solubility of a portion of the biologically active agent.
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Citations
64 Claims
- 1. A composition for coating a transdermal delivery device having stratum corneum-piercing microprojections comprising a formulation of a biologically active agent, a non-volatile counterion and a volatile counterion, wherein said non-volatile counterion causes the formation of a first species of said biologically active agent that has improved solubility when said formulation is dried and wherein said volatile counterion causes the formation of a second species of said biologically active agent that has reduced solubility when said formulation is dried.
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6. The composition of claim 6, wherein said non-volatile weak acid has an acidic pKa and a property selected from the group consisting of a melting point higher than about 50°
- C. and a boiling point higher than about 170°
C. at atmospheric pressure. - View Dependent Claims (7)
- C. and a boiling point higher than about 170°
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54. A method for transdermally delivering a biologically active agent comprising the steps of:
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providing a transdermal delivery device having at least one stratum corneum-piercing microprojection, the microprojection including a biocompatible coating comprising a dried formulation of said biologically active agent, a non-volatile counterion and a volatile counterion, wherein said non-volatile counterion causes the formation of a first species of the biologically active agent that has improved solubility when said formulation is dried and said volatile counterion causes the formation of a second species of said biologically active agent that has reduced solubility when said formulation is dried; and
applying said delivery device to a patient to deliver said biologically active agent. - View Dependent Claims (55, 56, 57, 58, 59, 60, 61, 62, 63)
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64. A method for applying a biocompatible coating to a transdermal delivery device that has a least one stratum corneum-piercing microprojection comprising the steps of:
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providing a formulation of a biologically active agent, a non-volatile counterion, and a volatile counterion, wherein said non-volatile counterion causes the formation of a first species of said biologically active agent that has improved solubility when the formulation is dried and wherein said volatile counterion causes the formation of a second species of said biologically active agent that has reduced solubility when said formulation is dried;
applying said formulation to said microprojection; and
drying said formulation.
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Specification