Solvent system for enhancing the solubility of pharmaceutical agents
AssigneeBanner Life Sciences LLC
InventorsNachiappan Chidambaram, Aqeel Fatmi
Life of this patent
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Abstract
Liquid and semi-solid pharmaceutical compositions, which can be administered in liquid form or can be used for preparing capsules, are described herein. The composition comprises the salt of one ore more active agents, polyethylene glycol, 0.2-1.0 mole equivalents of a de-ionizing agent per mole of active agent, and water. The pH of the composition is adjusted within the range of 2.5-7.5. The de-ionizing agent causes partial de-ionization (neutralization) of the salt of the active agent resulting in enhanced bioavailability of salts of weakly acidic, basic or amphoteric active agents as well as lesser amounts of polyethylene glycol (PEG) esters.
Claims46
A pharmaceutical composition comprising
- (a) a salt of one or more either acidic or basic pharmaceutically active agents;
- and
- (b) a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the pharmaceutically active agents, which at least partially neutralizes the pharmaceutically active agents;
- and
- (c) polyethylene glycol;
- wherein when the salt is a salt of a weak acid and a strong base, the deionizing agent is a hydrogen ion species and when the salt is a salt of a weak base and a strong acid, the deionizing agent is a hydroxide ion species;
- and
- wherein the one or more pharmaceutically active agents are not amphoteric.
(canceled)
A method of making a softgel capsule comprising a fill material comprising
- (a) a salt of one or more either acidic or basic pharmaceutically active agents;
- and
- (b) a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the pharmaceutically active agent(s), which at least partially neutralizes the pharmaceutically active agent(s);
- and
- (c) polyethylene glycol;
- wherein, when the salt is a salt of a weak acid and a strong base, the deionizing agent is a hydrogen ion species and when the salt is a salt of a weak base and a strong acid, the deionizing agent is a hydroxide ion species;
- and
- wherein the one or more pharmaceutically active agents are not amphoteric;
- comprising the steps of:
- (a) mixing a salt of one or more acidic or basic pharmaceutically active agents, a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the pharmaceutically active agent(s), which at least partially neutralizes the pharmaceutically active agent(s), and polyethylene glycol at an appropriate temperature;
- and
- (b) encapsulating the mixture in a softgel capsule.
(canceled)
A softgel capsule comprising a fill material wherein the fill material comprises
- (a) a salt of one or more either acidic or basic pharmaceutically active agents;
- and
- (b) a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the pharmaceutically active agent(s), which at least partially neutralizes the pharmaceutically active agent(s);
- and
- (c) polyethylene glycol;
- wherein, when the salt is a salt of a weak acid and a strong base, the deionizing agent is a hydrogen ion species and when the salt is a salt of a weak base and a strong acid, the deionizing agent is a hydroxide ion species;
- and
- wherein the one or more pharmaceutically active agents are not amphoteric.
(canceled)
A softgel capsule comprising a fill material comprising
- from about 10% to about 80% by weight polyethylene glycol having a molecular weight between 300 and 1500, about 10% to about 50% by weight naproxen sodium, and about 0.2 to about 1.0 moles of a deionizing agent per mole of naproxen sodium, which at least partially neutralizes the naproxen sodium
- wherein the deionizing agent is a hydrogen ion species.
A pharmaceutical composition prepared by a method comprising
- (a) mixing a salt of one or more either acidic or basic pharmaceutically active agents;
- (b) a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the salt of the pharmaceutically active agent(s), which at least partially neutralizes the salt of pharmaceutically active agent(s);
- and
- (c) polyethylene glycol;
- wherein when the salt is a salt of a weak acid and a strong base, the deionizing agent is a hydrogen ion species, and when the salt is the salt of a weak base and a strong acid, the deionizing agent is a hydroxide ion species, and
- wherein the one or more pharmaceutically active agents are not amphoteric.
A softgel capsule prepared by a method comprising
- (a) producing a fill material by mixing
- (i) a salt of one or more either acidic or basic pharmaceutically active agents;
- (ii) a deionizing agent in an amount from about 0.2 to about 1.0 mole equivalents per mole of the pharmaceutically active agent(s) to cause partial deionization of the salt of the pharmaceutically active agent(s);
- and
- (iii) polyethylene glycol;
- (b) encapsulating the mixture in a softgel capsule;
- wherein when the salt is a salt of a weak acid and a strong base, the deionizing agent is a hydrogen ion species, and when the salt is the salt of a weak base and a strong acid, the deionizing agent is a hydroxide ion species;
- and
- wherein the one or more pharmaceutically active agents are not amphoteric.
Dependencies are inferred from the claim text.