Process for increasing solubility of drug

• US 4,732,915 A
• Filed: 06/23/1986
• Issued: 03/22/1988
• Est. Priority Date: 11/02/1983
• Status: Expired due to Fees

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Ayer, Atul, Theeuwes, Felix, Wong, Patrick S. L.
• Primary Examiner(s): Rose, Shep K.
• Application Number:
  US06/877,068
• Time in Patent Office: 638 Days
• Field of Search: 424/19-22, 514/569, 514/567
• US Class Current: 514/567
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

An osmotic system is disclosed for the delivery of haloperidol at a controlled rate over a prolonged period of time.

Claims

1. A process for increasing the solubility of haloperidol in aqueous and biological fluids, which process consists of blending haloperidol with maleic acid, and which blend is useful for the controlled delivery of a therapeutically effective amount of haloperidol by a delivery system.

2. A process for increasing the solubility of haloperidol in aqueous and biological fluids, which process consists of mixing haloperidol with malic acid, and which mixture is useful for the controlled delivery of a therapeutically effective amount of haloperidol by a delivery system.

3. A process for increasing the solubility of haloperidol in aqueous and biological fluids for improving its delivery at a controlled rate from an osmotic delivery device, which process consists of mixing haloperidol with citric acid thereby improving its delivery at a controlled rate from an osmotic device.

4. A composition useful for dispensing from a delivery system, the composition consisting of haloperidol and maleic acid.

5. A composition consisting of haloperidol and malic acid, said composition useful for dispensing haloperidol at a controlled rate from a drug delivery system.

6. A composition consisting of haloperidol and citric acid, said composition useful for delivering haloperidol at a controlled rate by a drug delivery system into a biological fluid environment.

7. A process for increasing the solubility of haloperidol in the presence of aqueous and biological fluids, which process consists of forming a composition consisting of haloperidol and dihydroxysuccinic acid, and wherein the amount of haloperidol to dihyroxysuccinic acid is 1 part to 3 parts by weight up to 1 part to 100 parts by weight.

8. A process for increasing the solubility of the beneficial drug 4-[4-(chlorophenyl)-4-hydroxy-1-peperidinyl]-1-(4-fluorophenyl)-1-butanone in the presence of aqueous and biological fluids, which process consists of forming a composition consisting of said beneficial drug and succinic acid, and at least one member selected from the group consisting of citric acid, maleic acid and malic acid, and wherein the ratio of beneficial drug to total acid is 1 part to 3 parts by weight to 1 part to 100 parts by weight.