Solvent system enhancing the solubility of pharmaceuticals for encapsulation

  • US 5,071,643 A
  • Filed: 10/09/1987
  • Issued: 12/10/1991
  • Est. Priority Date: 10/17/1986
  • Status: Expired due to Term
First Claim
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1. A pharmaceutically acceptable highly concentrated solution of an acidic pharmaceutical agent suitable for filling softgels or for two-piece encapsulation or for tablet formation for subsequent oral administration, comprising the acidic pharmaceutical agent and a solvent system, the solvent system comprising 10% to 80% polyethylene glycol by weight of the solvent system, 1% to 20% water by weight of the solvent system and a hydroxide species, the hydroxide species being capable of dissociating in the solvent system into pharmaceutically acceptable cations and hydroxide ions, the hydroxide species being present in an amount such that between 0.1 and less than one mole of hydroxide ions per mole of acidic groups in the acidic pharmaceutical agent is present in the solution, the hydroxide species partially ionizing the acidic pharmaceutical agent such that the acidic pharmaceutical agent is present in a dissolved state in the solution as both a free acid and a cationic salt in a total amount of 20% to 80% by weight of the solution.

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