Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
1999-04-07
2001-01-09
Harrison, Robert H. (Department: 1619)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
C424S464000, C424S499000, C514S961000
Reexamination Certificate
active
06171616
ABSTRACT:
RELATED APPLICATION
This application claims the priority of Japanese Patent application No. 10-117780 filed on Apr. 13, 1998, which is incorporated herein by reference.
BACKGROUND OF THE INVENTION
1. Field of the Invention
This invention relates in general to a solid preparation for medicinal tablets, granules, and such, as well as a method of manufacturing it, and more particularly to a solid preparation which contains for a binder or a disintegrant methyl cellulose whose MeO content and aqueous solution viscosity are in specified ranges, as well as a method of manufacturing it.
2. The Prior Art
Solid preparations such as medicinal granules and tablets have advantages in that they are convenient for administering and easy to take.
However, a solid preparation may be worn away during transportation unless it has an adequate hardness; on the other hand if it is too hard then it may not disintegrate and be absorbed after it is inside the body.
In order to improve the hardness and the disintegration properties required of such a solid preparation, it is desirable to improve additives such as binders and disintegrants to be blended in the solid preparation.
Conventionally known substances for the binder of a solid preparation include methyl cellulose, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, and polyvinylpyrolidone (hereafter abbreviated as MC, HPMC, HPC, and PVP).
Of these binders, MC is used as an additive for medicinal drugs which is a stable binder over a wide range of pH.
For example, Japanese unexamined patent publication Tokkai Hei 4-164025 reports to the effect that MC whose 2 wt % aqueous solution is 80 cP or higher at 20° C. can be used for the matrix base agent for controlled release tablets.
Solid preparations are mainly manufactured by the wet granulation method. Depending on the drug, an adequate hardness cannot be obtained by a normal amount of binder. If the amount to be added is increased to solve this problem, then although an increase in the hardness is achieved there is a problem in that the disintegration time in the body becomes longer.
Therefore, the development of a solid preparation containing a binder which quickly disintegrates even if the amount to be added is increased has been desired.
As for the MC, the commercially available low viscosity product has a viscosity of 15 cP, which is high. If this is used to prepare an aqueous solution of the binder such that an adequate hardness can be achieved, then the viscosity will be higher than 600 cP. In general, the viscosity of an aqueous solution used in the wet granulation method is 600 cP or less. Therefore, there is a problem in that this low viscosity product pushes the viscosity of the binder aqueous solution too high and hence denies the option of increasing the amount to be added to the solid preparation.
Furthermore, in the case where the MC is used in a powder form to granulate a solid preparation using water, there is also a problem in that dissolution of the MC powder takes time because of its high viscosity.
Based on the aforementioned problems, the inventors conducted earnest research to obtain a solid preparation which has an adequate hardness and at the same time disintegrates quickly, and discovered that the aforementioned problems can be solved by adding, for a binder or disintegrant, a MC whose MeO content and aqueous solution viscosity are in specific ranges to the solid preparation, thus completing the present invention.
The object of the present invention is to provide a solid preparation which has an adequate hardness and at the same time disintegrates quickly for easy absorption, as well as a method of manufacturing it.
BRIEF SUMMARY OF THE INVENTION
That is, the present invention provides a solid preparation characteristically containing for a binder methyl cellulose whose MeO content is 27.5-31.5 wt % and whose 2 wt % aqueous solution has a viscosity of 2-12 cP at 20° C.
Also, the present invention provides said solid preparation wherein said methyl cellulose content is 0.5-10 wt % of the solid preparation.
Furthermore, the present invention provides a method of manufacturing a solid preparation for granulating active ingredients which is a method of manufacturing said solid preparation wherein methyl cellulose which has a MeO content of 27.5-31.5 wt % and whose 2 wt % aqueous solution has a viscosity of 2-12 cP at 20° C. is added as a binder for granulation.
DETAILED DESCRIPTION OF THE INVENTION
The configuration of the present invention is described below.
The characteristics of the present invention are a solid preparation prepared by adding, for a binder, methyl cellulose whose MeO content is 27.5-31.5 wt % and whose 2 wt % aqueous solution has a viscosity of 2-12 cP, preferably 2-5 cP, at 20° C. during the granulation process of the solid preparation, as well as the fact that the binder contained in the solid preparation acts as a disintegrant at the same time.
Conventionally, there have been examples of MC with a MeO content of 27.5-31.5 wt % used as the film agent on the surface of a solid preparation (Tokkai Sho 60-84215 and Tokkai Sho 60-13719) wherein the viscosity of its 2 wt % aqueous solution was 3-15 cP. However, the present invention is the first case where MC whose MeO content is 27.5-31.5 wt % and whose 2 wt % aqueous solution has a viscosity of 2-12 cP at 20° C. is added during the granulation process and used as a binder which is contained inside.
The MC used in the present invention has an advantage in that, in the wet granulation method where it is used in the form of an aqueous solution, it can evenly spread all over the granulation powder and it can be used in a high concentration.
Also in the wet granulation method where the binder MC is added in the form of powder and granulation is carried out using water, a solid preparation with superior binding properties and also satisfactory disintegrating properties can be obtained even if a large amount is added, due to its high solubility in water.
In the present invention, it is not suitable to use MC with a 2 wt % aqueous solution viscosity higher than 12 cP because then the controlled release effect becomes too strong.
A commercial product manufactured and distributed by the applicant of the present invention can be used for the MC which has the aforementioned specific MeO content and viscosity range. The viscosity grade of the MC to be added can be selected from within the aforementioned viscosity range according to the solubility of the active ingredient in water.
The blend ratio of the aforementioned MC in the solid preparation is preferably 0.5-10 wt %, more preferably 1-5 wt %, of the total solid preparation. Acceptable blend ratios include those which allow granulation when manufacturing the solid preparation and give adequate disintegration properties to the solid preparation. More than 10 wt % MC is not preferable because then release of the active ingredient in the solid preparation slows down and the viscosity of the granulation material during the granulation process significantly increases, making it impossible to achieve even granulation.
In addition to the aforementioned MC and the active ingredient, the solid preparation of the present invention can contain other additives which are normally added during the manufacturing process of a solid preparation. Examples of these excipients such as lactose, starch and its derivatives, powder cellulose, crystalline cellulose, and calcium hydrogen phosphate, as well as lubricants such as magnesium stearate, calcium stearate, and talc. Furthermore, other binders, disintegrants, surfactants, coloring agents, sweetening agents, perfumes, etc. can be added as necessary.
The solid preparation of the present invention can be manufactured using conventional manufacturing methods such as the stirring-granulation method and the fluidized bed granulation method. The granulated solid preparation can be mixed with a lubricant and tablets can be formed by using a tablet machine in a conventional manner.
In the method of manufacturing the solid preparation o
Kokubo Hiroyasu
Tanno Fumie
Harrison Robert H.
Shin-Etsu Chemical Co. , Ltd.
Townsend & Banta
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