United States Patent:  6,056,975

Assignee:  BASF Corporation (Mount Olive, NJ)

Filed:  September 18, 1998

Disclosed are thyroid hormone preparations useful in pharmaceutical applications. These preparations are disclosed to contain thyroxine drugs in combination with an inorganic salt, a carbohydrate having a molecular weight of greater than 500, and glycine. The preparations are also disclosed to have a free water content less than 4.5% by weight of the preparation. Also provided are compositions containing a reduced carbohydrate, a water soluble polysaccharide, or galactose. The preparations have improved stability wherein they are provided as being stable to the extent that substantially no potency loss is measured when the preparation is stored at 40^oC. and 75% relative humidity for 3 months.

SUMMARY OF THE INVENTION

The present invention is directed to providing an improved, stable, solid dosage form of thyroid hormone pharmaceutical preparations. The preparations contain an effective amount of a thyroid drug, at least one excipient, such as a diluent or bulker, which excipient is an inorganic salt, a carbohydrate having a molecule weight of greater than 500, or glycine.

An embodiment of the present invention is directed to a stable solid dosage form of a thyroid hormone preparation containing a water soluble polysaccharide. A further embodiment of the invention contains a reduced carbohydrate (e.g. typical reduction of ketoses and aldehydes), preferably mannitol. Also contemplated by the present invention is a preparation containing galactose.

The preparation preferably has a free water content of less than 4.5% by weight and a pH greater than 7 (one gram of the preparation mixed with one milliliter of water). Such preparations are stable to the extent that when subjected to stability testing at 40^oC. and 75% RH for 3 months, substantially no potency loss can be measured (e.g. the potency loss is less than about 10%). It is preferred that the stability of the preparations of the present invention, when tested at 40^oC. and 75% RH for 1 month, be such as to result in a potency loss of less than about 3-5%.

Claim 1 of 38 Claims

1. A stable, solid dosage form pharmaceutical preparation suitable for the treatment of thyroid disorders, said preparation comprising:

an effective amount of a thryoxine drug; and a water soluble glucose polymer;

said preparation being stable to the extent that substantially no potency loss is measured when the preparation is stored at 40^oC. and 75% relative humidity for 3 months.

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