Tablet quickly disintegrating in oral cavity
The present invention provides rapid disintegrating tablets in oral cavity having a shortened disintegration time in oral cavity as well as a sufficient hardness compared to rapid disintegrating tablets of the prior art. The above objective is solved by a composition in which the inorganic excipient and the disintegrating agent are dispersed in the complex particles consisting of mannitol and other saccharide(s) in a specific ratio, and rapid disintegrating tablets in oral cavity obtained by direct compression of the composition.
1. A tablet composition which comprises:
(a) saccharides comprised of a combination of mannitol and one or more of other saccharide(s) selected from sorbitol, erythritol, maltitol, lactose, and trehalose in an amount of 40 to 90 parts by weight;
(b) an inorganic excipient in an amount of 1 to 30 part(s) by weight; and
(c) a disintegrating agent in an amount of 5 to 40 parts by weight,
wherein a total amount of components (a), (b) and (c) is 100 parts by weight,
wherein a weight ratio of mannitol to other saccharide(s) is (98 to 75): (2 to 25),
wherein the tablet composition exhibits an oral disintegration time of within 40 seconds, and
wherein mannitol and other saccharide(s) form complex particles, which exhibit a melting point depression, and the inorganic excipient and the disintegrating agent are dispersed in the complex particles.
2. The composition according to claim 1 , wherein:
(a) saccharides are 50 to 80 parts by weight;
(b) the inorganic excipient is 2 to 15 parts by weight; and
(c) the disintegrating agent is 10 to 35 parts by weight.
3. The composition according to claim 1 , wherein:
(a) saccharides are 65 to 80 parts by weight;
(b) the inorganic excipient is 3 to 10 parts by weight; and
(c) the disintegrating agent is 17 to 34 parts by weight.
4. The composition according to claim 1 , wherein the complex particles form a solid dispersion.
5. The composition according to claim 1 , wherein an endothermic peak of the saccharides is shifted to a low temperature side by 0.5 to 10° C. compared to an endothermic peak measured from mannitol only.
6. The composition according to claim 1 , wherein the ratio by weight of mannitol to other saccharide(s) is (97 to 75): (3 to 25).
7. The composition according to claim 1 , wherein the ratio by weight of mannitol to other saccharide(s) is (96 to 81): (4 to 19).
8. The composition according to claim 1 , wherein the inorganic excipient has an average pore diameter of 100 nm or less and is a pharmaceutically acceptable inorganic compound containing any of aluminum, magnesium and calcium.
9. The composition according to claim 1 , wherein the inorganic excipient is selected from magnesium aluminometasilicate, magnesium aluminosilicate, synthetic hydrotalcite, calcium silicate, calcium hydrogen phosphate, calcium carbonate, talc and dry aluminum oxide gel.
10. The composition according to claim 1 , wherein the disintegrating agent has an average particle diameter of 60 μm or less, and is selected from crospovidone, low-substituted hydroxypropyl cellulose, crystalline cellulose and croscarmellose sodium.
11. The composition according to claim 10 , wherein the disintegrating agent has an average particle diameter of 20 μm or less.
12. The composition according to claim 1 ; wherein the disintegrating agent is crospovidone having an average particle diameter of 20 μm or less and crystalline cellulose having an average particle diameter of 40 μm or less.
13. The composition according to claim 1 , which contains 5 to 13 parts by weight of crospovidone and 12 to 21 parts by weight of crystalline cellulose as the disintegrating agent.
14. The composition according to claim 1 , which is obtained by spray-drying an aqueous solution or an aqueous dispersion comprising the saccharides, the disintegrating agent and the inorganic excipient.
15. The composition according to claim 14 , which is obtained by spray-drying the dispersion obtained by dissolving or dispersing, in advance, mannitol and other saccharide(s) in an aqueous medium and then homogeneously dispersing the disintegrating agent and the inorganic excipient.
16. The composition according to claim 1 , which further contains 0.01 to 100 parts by weight of a pharmacologically active ingredient and/or 0.01 to 1000 parts by weight of a component which does not deteriorate a disintegrating property based on 100 parts by weight of a total amount of the saccharides, the inorganic excipient and the disintegrating agent.
17. The tablet composition according to claim 1 , wherein the tablet composition exhibits an oral disintegration time of within 30 seconds.
18. The tablet composition according to claim 1 , wherein the tablet composition exhibits an oral disintegration time of within 20 seconds.