Fast release dosage forms for antibiotics
A multiparticulate, pharmaceutical dosage form containing at least one antibiotic which is sparingly wettable with aqueous media or sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate and optionally sucrose ester. Also, an administration system having this dosage form arranged in a drinking straw with at least one barrier device for single administration, optionally together with a conveying liquid.
1. A multiparticulate, pharmaceutical dosage form comprising at least one antibiotic which is sparingly wettable with aqueous media or is sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate, wherein said dosage form contains 5 to 50 wt. % of carrageenan relative to the total weight of the dosage form and the weight ratio of tricalcium phosphate to carrageenan is from 1:1 to 1:10, and, at a pH value of 6-7, the antibiotic is released in a quantity of at least 88% within 30 min.
2. A dosage form according to claim 1 , further comprising at least one sucrose ester.
3. A dosage form according to claim 1 , wherein said dosage form is provided in the form of extruded pellets.
4. A dosage form according to claim 3 , where said extruded pellets have a spherical form.
5. A dosage form according to claim 2 , wherein the sucrose ester exhibits an HLB of 10-16.
6. A dosage form according to claim 2 , wherein the sucrose ester exhibits an HLB of 13-15.
7. A dosage form according to claim 1 , wherein said dosage form contains preferably 20-30 wt. % of carrageenan relative to the total weight of the dosage form.
8. A dosage form according to claim 1 , wherein said carrageenan is kappa-carrageenan.
9. A dosage form according to claim 1 , wherein the weight ratio of tricalcium phosphate to carrageenan is from 1:2 to 1:6.
10. A dosage form according to claim 1 , wherein the tricalcium phosphate is present as a finely divided powder with a particle size of <50 μm.
11. A dosage form according to claim 2 , wherein the sucrose ester is present in a quantity of from 1-10 wt. % relative to the total weight of the dosage form.
12. A dosage form according to claim 2 , wherein the sucrose ester is present in a quantity of from 4-6 wt. % relative to the total weight of the dosage form.
13. A dosage form according to claim 1 , further comprising at least one antibiotic selected from the group consisting of penicillins, cephalosporins and macrolides.
14. A dosage form according to claim 13 , wherein the at least one antibiotic is amoxicillin, clarithromycin, azithromycin (mono- or dihydrate) or cefixim, cefpodoxime or cefpodoxime proxetil.
15. A dosage form according to claim 1 , further comprising a gastric juice-resistant or saliva-resistant, flavor-neutral coating.
16. A dosage form according to claim 1 , wherein the particles have a size of <800 μm.
17. A dosage form according to claim 1 , wherein the dosage form comprises amoxicillin and a flavor-neutralizing coating.
18. A dosage form according to claim 1 , wherein the dosage form comprises clarithromycin and a flavor-neutralizing coating.
19. A method for producing a multiparticulate, pharmaceutical dosage form comprising at least one antibiotic which is sparingly wettable with aqueous media or is sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate, wherein said dosage form contains 5 to 50 wt. % of carrageenan relative to the total weight of the dosage form and the weight ratio of tricalcium phosphate to carrageenan is from 1:1 to 1:10, and, at a pH value of 6-7, the antibiotic is released in a quantity of at least 88% within 30 minutes, said method comprising the steps of:
mixing, granulating, extruding, subdividing and spheronizing the starting materials.
20. A method according to claim 19 , further comprising the step of classifying the starting materials by size.
21. A method according to claim 19 , further comprising the steps of providing at least one of a saliva-resistant, a gastric juice-resistant and a flavor-neutral coating.
22. A method according to claim 19 , further comprising the step of moist granulating the starting materials.
23. An administration system comprising a multiparticulate, pharmaceutical dosage form comprising at least one antibiotic which is sparingly wettable with aqueous media or is sparingly soluble in aqueous media and a combination of carrageenan and tricalcium phosphate, wherein said dosage form contains 5 to 50 wt. % of carrageenan relative to the total weight of the dosage form and the weight ratio of tricalcium phosphate to carrageenan is from 1:1 to 1:10, and, at a pH value of 6-7, the antibiotic is released in a quantity of at least 88% within 30 minutes, wherein said dosage form is arranged in a drinking straw with at least one preferably mobile barrier device for single administration.
24. An administration system according to claim 23 , wherein said dosage form is provided in the form of rounded extruded pellets.
25. A kit comprising an administration system according to claim 23 and a physiologically acceptable conveying liquid with a pH of ≦6.