Preparations for oral administration
The present invention provides a preparation for oral administration containing a medicinal substance having cGMP-specific phosphodiesterase inhibitory activity and showing decrease of solubility in the neutral and alkaline regions, wherein an acidic substance is compounded promote the dissolution of the medicinal substance in digestive tract and thus the efficacy can be expressed at the early stage after administration, and which preparation is useful in treatment of erectile dysfunction.
1. A preparation for oral administration comprising
(A) as an active ingredient a compound (S)-2-(2-hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(2-pyrimidinylmethyl)carbamoyl]pyrimidine in the free form; and
(B) an organic acidic substance,
wherein said compound is compounded with said organic acidic substance.
2. The preparation according to claim 1 , wherein the organic acidic substance is selected from the group consisting of fumaric acid, tartaric acid, succinic acid, malic acid, ascorbic acid and aspartic acid.
3. The preparation according to claim 1 , wherein the organic acidic substance is fumaric acid.
4. The preparation according to claim 1 , wherein the compounding ratio of the compound and the organic acidic substance is in the range of 1:0.05 to 1:30.
5. The preparation according to claim 1 , which further contains a carbonate.
6. The preparation according to claim 5 , wherein the carbonate is one or more substances selected from the group consisting of alkali metal carbonates, alkali metal hydrogen carbonates and alkali earth metal carbonates.
7. The preparation according to claim 5 , wherein the carbonate is calcium carbonate.
8. The preparation according to claim 5 , wherein the content of a carbonate is 10 weight % or less of the total amount of the preparation.
9. The preparation according to claim 1 , which is in the form of tablet.
10. A tablet which comprises
(A) (S)-2-(2-hydroxymethyl-1-pyrrolidinyl)-4-(3-chloro-4-methoxybenzylamino)-5-[N-(2-pyrimidinylmethyl)carbamoyl]pyrimidine,
(B) fumaric acid and
(C) calcium carbonate.