Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form
Reexamination Certificate
2000-05-24
2002-09-24
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
C424S464000, C424S465000, C424S484000, C424S488000
Reexamination Certificate
active
06455053
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a rapidly dissolving solid preparation. More particularly, it relates to a rapidly dissolving solid preparation which rapidly disintegrates and dissolves at the ingestion site where there occurs a limited amount of moisture such as the interior of the oral cavity.
BACKGROUND ART
There has been conventionally pursued a development of a solid preparation which will rapidly disintegrate and dissolve in the oral cavity as a preparation which is easy for the patients having a difficulty in swallowing, the elderly persons, or children to ingest. For example, in each of Japanese Laid-Open Patent Publication Nos. Sho 53-44619, Sho 58-113124, Hei 3-56412 and Hei 3-86837, and Japanese National Phase PCT Laid-Open Publication No. Hei 9-502622, there is proposed a solid preparation using a lyophilization technology. Further, in Japanese Laid-Open Patent Publication No. Hei 2-32014 or Hei 5-271054, there is proposed a solid preparation based on a triturated tablet obtained by pressure-molding a wetted preparation powder under a low pressure, and subsequently drying it.
Still further, in each of Japanese Laid-Open Patent Publication No. Sho 58-194808, Japanese National Phase PCT Laid-Open Publication No. Hei 6-502194, Japanese Laid-Open Patent Publication Nos. Hei 5-310558, Hei 8-99904, Hei 8-208520, Hei 8-208521, Hei 8-333243, and Hei 9-71523, there is disclosed a solid preparation resulting from compression-molding which dissolves and disintegrates in the oral cavity. Also, in WO93/12769, there is proposed a solid preparation obtained by dispersing a mixed powder of a drug, and lactose and/or mannitol in an agar aqueous solution, filling it in a mold, and subsequently drying it.
However, each of the conventional preparations proposed above is not pharmaceutically sufficient, and includes various problems. For example, with the pressure molding method, it is possible to enhance the hardness not only by the manufacturing method based on ordinary compression molding, but also by the method based on the triturated tablet. However, the preparation obtained by this method often exhibits a longer dissolution and disintegration time in the oral cavity. Further, it sometimes requires addition of a water-insoluble disintegrator, often resulting in an unpleasant ingestion feeling when the preparation is dissolved in the oral cavity. Also, because gelatin and agar are natural substances, the solid preparation using them is susceptible to discoloration with time, may sometimes impair the stability of the drug to be combined with, and further miscellaneous germs tend to proliferate therein.
In contrast, the preparation prepared by the use of the lyophilization technique has a large void, and hence the dissolution rate in the oral cavity is very high. However, the preparation itself is bulky, and it is generally difficult to increase the drug content. Further, since it is often difficult to store and handle the preparation on a daily basis, the preparation is brittle and easy to collapse due to a low hardness, and it also has a high hygroscopicity. Especially, under the climatic conditions of high temperature and high humidity, the preparation may change its shape very easily due to moisture absorption, and only picking it up for ingestion may cause it to adhere to the finger, and these may interfere with the handling of the preparation.
DISCLOSURE OF THE INVENTION
It is an object of the present invention to provide a rapidly dissolving solid preparation which disintegrates and dissolves rapidly in the oral cavity and the like, and has a practical hardness, whereby solving foregoing problems, and a manufacturing method thereof.
In order to attain such an object, a first embodiment of the present invention provides a rapidly dissolving solid preparation obtained by mixing a drug, and a saccharide having a solubility of 30 g or less in 100 g of water at room temperature and a saccharide having a solubility of 30 g or more in 100 g of water at room temperature in water in such an amount as not to completely dissolve the saccharide having a solubility of 30 g or less in 100 g of water at room temperature, and then removing the moisture therefrom.
Further, a second embodiment of the present invention provides a rapidly dissolving solid preparation obtained by dissolving and dispersing a drug, a saccharide, and polyvinylpyrrolidone in an organic solvent, and then removing the organic solvent therefrom.
Still further, a third embodiment provides a rapidly dissolving solid preparation obtained by dissolving and/or dispersing a drug in an aqueous solution of a saccharide, and lyophilizing it.
BEST MODE FOR CARRYING OUT THE INVENTION
A rapidly dissolving solid preparation in a first embodiment to a third embodiment of the present invention is characterized by the procedure in which, a drug as well as a saccharide are dissolved and dispersed in an aqueous solution, an organic solvent, or the like, resulting in a suspension composition, and the resultant is dried to obtain the rapidly dissolving solid preparation.
Below, a detailed description will be given individually to the rapidly dissolving solid preparation in the first embodiment to the third embodiment.
The first embodiment of the rapidly dissolving solid preparation provided by the present invention is the rapidly dissolving solid preparation obtained by mixing a drug, and a saccharide having a solubility of 30 g or less in 100 g of water at room temperature and a saccharide having a solubility of 30 g or more in 100 g of water at room temperature in water in such an amount as not to completely dissolve the saccharide having a solubility of 30 g or less in 100 g of water at room temperature, and then removing the moisture therefrom.
The rapidly dissolving solid preparation of the present invention is specifically manufactured in the following manner. A drug, and a saccharide having a solubility of 30 g or less in 100 g of water at room temperature and a saccharide having a solubility of 30 g or more in 100 g of water at room temperature are mixed in water in such an amount as not to completely dissolve the saccharide having a solubility of 30 g or less in 100 g of water at room temperature to obtain a creamy suspension. Subsequently, the suspension is charged in a mold for a preparation, and then the moisture is removed therefrom.
Namely, the first rapidly dissolving solid preparation prepared by the present invention is characterized that a saccharide having both a low solubility and a high solubility in water is used in combination with a drug to produce a creamy composition which is an aqueous suspension, and the moisture is subsequently removed therefrom.
According to the study by the present inventors, if a drug and a saccharide having a low solubility in water alone are combined, the resulting suspension is not a desired creamy composition, and the separation of the drug and the saccharide from the moisture occurs during charge, making it impossible to achieve uniform charging. Further, in the solid preparation after drying the composition, irregularities will occur on the surface thereof, and hence the utility as a practical preparation is poor.
On the other hand, the composition obtained by combining a drug and a saccharide having a high solubility in water alone becomes a composition in the aqueous solution state. Therefore, drying for achieving a solid preparation cannot be carried out sufficiently with room temperature blast or suction drying, or even if drying can be performed, much time is required, resulting in poor productivity.
However, surprisingly, they have found that the solid preparation obtained by using a drug and both of the saccharide having a low solubility in water and the saccharide having a high solubility in water in combination to prepare a creamy composition which is an aqueous suspension, and subjecting the composition to air-drying or suction drying at ordinary temperature to remove the moisture therefrom is as follows. That is, the solid preparation has a practically accep
Ikeda Yasuo
Imamori Katsumi
Kasai Syuichi
Kurazumi Toshiaki
Okada Minoru
Crowell & Moring LLP
Fubara Blessing
Page Thurman K.
SSP Co. Ltd.
LandOfFree
Quickly soluble solid preparations does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Quickly soluble solid preparations, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Quickly soluble solid preparations will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2838784