Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2001-04-05
2004-06-01
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S435000, C424S441000, C424S464000, C424S474000
Reexamination Certificate
active
06743443
ABSTRACT:
TECHNICAL FIELD
The present invention relates to an intraoral quickly disintegrating tablet containing a phosphodiesterase inhibitor having an effect of improving the erectile dysfunction and to a method for manufacturing the tablet.
The present invention also relates to an intraoral quickly disintegrating tablet containing a slightly soluble pharmaceutical agent such as a phosphodiesterase inhibitor having an improved solubility and to a method for manufacturing the tablet.
PRIOR ART
It is reported in JP-B9-503996 that pyrazonopyrimidinone compounds having an inhibitory action to a cyclic GMP phosphodiesterase type V are useful for the therapy of erectile dysfunction by means of oral administration. Further, 5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)-phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one (general name: sildenafil) belonging to the same classification and being represented by the formula (I) surely shows duration of its pharmaceutical effect at least for two hours when it is orally administered (
British J. Urology,
78, 257-261, 1996.) and, therefore, there is a high possibility that they are used for a highly practical drug therapy for erectile dysfunction as a substitute for an injection therapy of papaverine hydrochloride or prostaglandin E
1
into corpus cavernosum penis which has been carried out in an urological field. In addition, with regard to a compound having an inhibitory action to a cyclic GMP phosphodiesterase type V, there is disclosed a pyrazolopyrimidinone derivative represented by the formula (II) {1,3-dimethyl-6-(2-propoxy -5-methanesulfonamidophenyl)-1,5-dihydropyrazolo[3,4-d]-pyrimidin-4-one} in JP-A 7-70128 while, in WO 97/03675, there are mentioned a compound represented by the formula (IV) {(6R,12aR)-2,3,6,7,12,12a-hexahydro-2-methyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2′, 1′:6,1]pyrido[3,4-b]-indol-1,4-dione)} and a compound represented by the formula (V) {(3S,6R,12aR)-2,3,6,7,12,12a-hexahydro-2,3-dimethyl-6-(3,4-methylenedioxyphenyl)-pyrazino[2′, 1′:6,1]pyrido[3,4-b]indol-1,4-dione}.
Further, in WO 93/07124, there is mentioned a compound represented by the formula (III) {2-(4-carboxypiperidino)-4-(3,4-methylenedioxybenzyl)amino-6-chloroquinazoline}. Furthermore, the compounds of a fused pyridazine type represented by the formula (VI) mentioned in JP-A 10-114657 have an inhibitory action to a cyclic GMP phosphodiesterase type V and are useful as therapeutic agents for erectile dysfunction.
It has been said that the number of the latent patients of erectile dysfunction are about 3,000,000 in Japan and are about 20,000,000 in U. S. A. It has been also reported that, while the number of the patients of erectile dysfunction in U. S. A. are only 2-7% of the male population of younger than 50 years age, the rate increases together with aging and 15% of males of fifties and a little over 30% of males of sixties are suffering from this disease. Most of them are derived from organic disorder and, taking the advent of an aging society in near future into consideration, it may be concluded that oral preparations of cyclic GMP phosphodiesterase inhibitors will play a very big role in improving the quality of life (QOL) of the patients suffering from erectile dysfunction.
However, when the conventional oral preparations containing a cyclic GMP phosphodiesterase inhibitor are administered, there is a possibility that, for example, administration of tablets is difficult or that powdery or granular agent adheres in the mouth or comes into artificial teeth whereby a part of the preparation is dropped out since aged people have a low swallowing ability.
When a consideration is made on the standpoint of the aged people as such, there is a very high demand for “therapeutic preparations for erectile dysfunction which can be easily taken, easily swollen and easily handled” which is able to be “one of the means whereby control of the carnal desire which is the fundamental desire of human being can be embodied”. Even in ordinary and healthy adults, therapeutic preparations for erectile dysfunction which can be taken at any place without water greatly contribute to their QOL.
On the other hand, intraoral quickly disintegrating tablets have been known as the tablets which are quickly disintegrated in the mouth and, since they can be easily taken without water, they are recently receiving public attention as a dosage form which is suitable for the people having insufficient swallowing functions such as aged people and small children.
It has been known that the intraoral quickly disintegrating tablets can be prepared, for example, by the use of wet powder. With regard to a method where wet powder is dried without a tableting step whereupon the intraoral quickly disintegrating tablets are prepared, there is disclosed for example in JP-A 5-511543 for “a solid preparation which is quickly disintegrated in the mouth comprising an active ingredient, a saccharide selected from lactose and/or mannitol and agar”.
On the other hand, with regard to an intraoral quickly disintegrating tablet prepared by a compression-molding of wet powder filled in a molding machine, there are disclosed, for example, “a method for the manufacture of an intraoral quickly disintegrating tablet where a mixture containing a pharmaceutical ingredient, a saccharide and water which is in an amount of moisturizing the particle surface of the saccharide is made into a tablet” in JP-A 5-271054; “an intraoral quickly disintegrating tablet comprising a pharmaceutical agent, a saccharide, a sugar alcohol and a water-soluble polymer and being prepared by moisturizing and molding” in JP-A 9-48726; and “a wet-process tablet where a pharmaceutical agent is mixed with a saccharide, a filler, etc., kneaded after addition of water and/or organic solvent, filled in a mold and subjected to a compression-molding and a method for manufacturing the same” in JP-A 6-218028. Further, with regard to a method for the molding of an intraoral quickly disintegrating tablet, there is disclosed in JP-A 8-19589 for an invention concerning “a method for the manufacture of a tablet where wet powder is filled in a hole for molding the tablet and at least one side of the wet powder in the hole is made into a shape of a tablet by means of a metal mold for molding with a film for prevention of adhesion and an apparatus for manufacturing the tablet”.
However, there has been no report yet for a preparation containing a cyclic GMP phosphodiesterase inhibitor and being able to greatly contribute in such a QOL improvement and for a method of manufacturing such a preparation.
Incidentally, in the case of a slightly soluble pharmaceutical agent, it is not preferred to directly apply the intraoral quickly disintegrating tablet using the above-mentioned known means and the method for manufacturing the tablet. That is because the low solubility of the slightly soluble pharmaceutical agent delays the time for reaching the effective blood level by oral administration and long time is required for achieving the pharmaceutical effect and also because there is a risk that a sufficient pharmaceutical effect is not achieved due to a low bioavailability.
In general, one of the most important factors among various factors affecting the absorption of a pharmaceutical agent via digestive tracts is its solubility and, especially in the case of a slightly soluble pharmaceutical agent, it is quite often that its dissolving rate determines the rate of absorption. Various methods have been known for promoting the solubility of a pharmaceutical agent and they may be roughly classified into the following three. Thus, (1) to increase the surface area of the pharmaceutical particles; (2) to use amorphous or metastable crystals; and (3) to utilize various types of salt or to add a solubilizer. As to the specific means therefor, making the pharmaceutical agent into fine powder, formation of a solvate and
Furitsu Hisao
Kato Akira
Ohwaki Takayuki
Yasui Masanobu
Birch & Stewart Kolasch & Birch, LLP
Eisai Co. Ltd.
Spear James M.
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