Formulations for coated microprojections containing non-volatile counterions
First Claim
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1. A composition comprising a formulation of a pharmaceutically active agent, a volatile counterion and a non-volatile counterion, wherein said pharmaceutically active agent is hPTH(1-34) present as uncharged species and as charged species and wherein said non-volatile counterion is present in an amount sufficient to achieve a molar ratio between said uncharged species and charged species of about 1 uncharged species to at least 100 charged species;
- wherein said formulation has increased pH stability and solubility when dried, and wherein said composition is applied to a transdermal delivery device having stratum corneum-piercing microprojections;
wherein said composition achieves an increase in delivery of the pharmaceutically active agent compared to a composition comprising a formulation without said non-volatile counterion.
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Abstract
The invention provides for a formulation for coating one or more microprojections which reduces or minimizes the loss of counterions from the coating in order to achieve a pH-stabilized formulation.
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Citations
15 Claims
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1. A composition comprising a formulation of a pharmaceutically active agent, a volatile counterion and a non-volatile counterion, wherein said pharmaceutically active agent is hPTH(1-34) present as uncharged species and as charged species and wherein said non-volatile counterion is present in an amount sufficient to achieve a molar ratio between said uncharged species and charged species of about 1 uncharged species to at least 100 charged species;
- wherein said formulation has increased pH stability and solubility when dried, and wherein said composition is applied to a transdermal delivery device having stratum corneum-piercing microprojections;
wherein said composition achieves an increase in delivery of the pharmaceutically active agent compared to a composition comprising a formulation without said non-volatile counterion. - View Dependent Claims (2, 3, 4, 5, 6, 8, 9, 10, 11)
- wherein said formulation has increased pH stability and solubility when dried, and wherein said composition is applied to a transdermal delivery device having stratum corneum-piercing microprojections;
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7. A composition comprising a formulation of a pharmaceutically active agent, a volatile counterion and a non-volatile counterion, wherein said pharmaceutically active agent is hPTH (1-34) present as uncharged species and as charged species;
- wherein said pharmaceutically active agent has a positive charge at the pH of the formulation and said non-volatile counterion comprises a strong acid; and
wherein said formulation has increased pH stability and solubility when dried.
- wherein said pharmaceutically active agent has a positive charge at the pH of the formulation and said non-volatile counterion comprises a strong acid; and
- 12. A composition comprising a formulation of hPTH(1-34), a volatile counterion and a non-volatile counterion from a weak or strong acid, wherein said non-volatile counterion is present in an amount sufficient to achieve a molar ratio of about 1 uncharged hPTH species to at least about 100 charged hPTH species, wherein said composition achieves an increase in delivery of said hPTH when applied to a transdermal delivery device having stratum corneum-piercing microprojections compared to a composition comprising a formulation without said non-volatile counterion.
Specification