Solid formulations of therapeutic proteins for gastrointestinal

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 3, 530303, 530324, 530399, 424409, 424465, 424498, A61K 3800

Patent

active

054242894

ABSTRACT:
The present invention is directed to a pharmaceutical formulation of a therapeutic polypeptide together with a permeation-enhancing mixture of sodium salicylate and an oil to provide enhanced absorption of the polypeptide through the wall of the gastrointestinal tract, and particularly of the colon, after oral administration, the amount of oil being from about 10 wt % to about 30 wt %, preferably from about 15 wt % to about 25 wt %, of the total formulation and the amount of sodium salicylate being from about 70 wt % to about 90 wt %, preferably from about 75 wt % to about 85 wt %, of the total formulation. The polypeptide may be non-lyophilized. The pharmaceutical formulation is characterized as a solid, which provides a convenient and improved format for handling and storage and for the preparation of oral dosage forms (such as pills, capsules and delivery vessels) containing a homogeneous mixture of ingredients.

REFERENCES:
patent: 3950521 (1976-04-01), Higuchi
patent: 4639435 (1987-01-01), Fujii
patent: 4702918 (1987-10-01), Ushimaru
Illustrated Stedman's Medical Dictionary, 24th ed., Williams and Wilkin's, Los Angeles, 1982, p. 421.
Moore, et al., International Journal of Pharmaceutics, 34 (1986) pp. 35-43, "Absorption Enhancement of Growth Hormone from the Gastrointestinal Tract of Rats".
Palin, et al., J. Pharm. Pharmacol, 1982, vol. 34, pp. 707-710, "The Effect of Oils on the Lymphatic Absorption of DDT".
Palin, et al., J. Pharm. Pharmacol, 1984, vol. 36, pp. 641-643, "The Effect of Different Oils on the Absorption of Probucol in the Rat".
Omran, et al., Pharm. Acta Helv., vol. 58, No. 8 (1983), pp. 237-140, "Bioavailability Studies on an Orally Administered, Oily Suspension of a Water Soluble Drug".

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