Oral antimicrobial pharmaceutical compositions
View Patent ↗The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.
1. A controlled release oral pharmaceutical composition comprising:
(1) a tablet core comprising:
a) rifamycin SV in an amount effective for the treatment of an infection of the colon;
b) a lipophilic substance having a melting point less than about 90° C.;
c) lecithin; and
d) a hydrophilic substance comprising a carboxyvinyl polymer or carboxyvinyl copolymer; and
(2) a coating on said tablet core, said coating comprising a gastro-resistant substance.
2. The composition of claim 1 , wherein said rifamycin SV comprises from about 20% to about 60% by weight of the total weight of said composition.
3. The composition of claim 1 , wherein said lipophilic substance comprises from about 1% to about 3.4% by weight of the total weight of the composition.
4. The composition of claim 1 , wherein said hydrophilic substance comprises from about 8.4% to about 23% by weight of the total weight of the composition.
5. The composition of claim 1 , wherein said gastro-resistant substance comprises at least one methacrylic acid polymer.
6. The composition of claim 1 , wherein
a) said rifamycin SV comprises from about 20% to about 60% by weight of the total weight of said composition;
b) said lipophilic substance comprises from about 1% to about 3.4% by weight of the total weight of the composition;
c) said hydrophilic substance comprises from about 8.4% to about 23% by weight of the total weight of the composition; and
d) said gastro-resistant substance comprises at least one methacrylic acid polymer.
7. The composition of claim 1 , wherein said composition is resistant to dissolution for 2 hours in an environment at pH 1.
8. The composition of claim 1 , wherein said composition is resistant to dissolution for 1 hour in an environment at pH 6.4.
9. The composition of claim 1 , wherein said composition is resistant to dissolution for 2 hours in an environment at pH1 and is resistant to dissolution for 1 hour in an environment at pH 6.4.
10. The composition of claim 1 , further comprising mannitol, magnesium stearate, titanium dioxide, talc, and triethylcitrate.
11. The composition of claim 1 , wherein said infection of the colon is travellers' diarrhea.