Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Reexamination Certificate
2000-10-30
2002-09-17
Spear, James M. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
Reexamination Certificate
active
06451344
ABSTRACT:
This application is a 371 of PCT/JP 99/00285 filed Jan. 22, 1999.
1. Technical Field
The present invention relates to a sugar-coated tablet formed by coating a core tablet using a mixture of lactulose and raffinose having various physiological effects as the sugar coating base.
In this specification, the core tablet refers to a tablet that is produced by the tabletizing of a composition that exhibits pharmacological action, and the sugar coating base refers to a composition that is used to coat the core tablet.
2. Background Art
Currently, coatings for medicinal preparations are frequently used in order to mask the flavor or odor of a drug, ensure the safety of the druggist by preventing the generation of drug dust, improve the stability of the drug by protecting the drug from light, water and oxygen, and improve the efficacy or stability of the drug by imparting solubility in intestines or controlled release effects. In addition, known methods for coating medicinal preparations involve gelatin coating, dry coating, sugar coating, film coating and powder coating, but gelatin coating and dry coating are almost never used for the sole purpose of coating, whereas powder coating has been the subject of much investigation and is considered to be a future technology. Consequently, sugar coating and film coating are currently the main methods.
Conventional sugar coating bases have been aqueous solutions of sugar (syrups), and it is said that tablets with excellent hermetic properties and smooth surface are obtained by the formation of tight block-form structures of sugar crystal. Calcium lactate is also known, in addition to sugar, as a sugar coating base, and other known substances include talc used as a sugar coating dispersion agent, precipitated calcium carbonate used as a sugar coating suspension agent, gelatin, gum arabic and pullulan used as sugar coating binders, and carnauba wax used as a sugar coating glossing agent (Hisashi Ichibangase, Kaneto Uekama, and Yuki Odagiri, Eds.“Drug Product Development [Iyakuhin no Kaihatsu] Vol. 12, Preparation Materials [Seizai Sozail] I” Hirokawa Shoten, Heisei 2 Nen/1990).
In addition, the use of sugar alcohols as materials for coating foodstuffs has been disclosed (Japanese Laid-Open Patent Publication No. H9-313109, 1997), and the use of fine granulated sugar and corn starch as materials for coating compound-grain granules soluble in intestines has been disclosed (Japanese Laid-Open Patent Publication No. H5-186337, 1993).
On the other hand, lactulose is a type of disaccharide composed of galactose and fructose (4-O-&bgr;-D-galactopyranosyl-&agr;-D-fructose), and is manufactured by subjecting lactose to the Lobry de Bruyn transformation. Lactulose is known to be a Bifidobacteria stimulating factor (Diagnosis and New Drugs [Shindan to Shinyaku], Vol. 10(5), p.75 (1973)). The substance is used in prepared powdered milk and powdered milk for weaning. In addition, lactulose is known to have the action of mitigating diseases such as hepatic encephaly and hepatic coma, and the substance has previously been used for treating these patients (Psychiatric Medicine [Seishin Igaku], Vol. 15(10), 1101 (1973)). However, when lactulose is used by itself as a sugar coating base, its high viscosity makes it impossible to uniformly coat the core tablet.
Raffinose is a type of trisaccharide that is composed of D-glucose and D-fructose, and is manufactured from a beet syrup by isolating with chromatography. Raffinose has already received a general evaluation as a foodstuff material for special health needs by the Japan Health and Nutrition Foodstuff Society [Nihon Kenkou. Eiyou Shokuhin Kyoukail]. A method for manufacturing sugar coatings has also been disclosed in which a sucrose syrup containing raffinose at an extremely low concentration of 2% (wt %, likewise below when not otherwise specified) or less is used for coating (Japanese Patent Publication No. S58-50968(1983)).
However, as is clear from the prior art described above, sugar-coated tablets produced using a sugar coating base which contains, as its effective component, a mixture in which at least an equivalent amount of raffinose is mixed with lactulose having various physiological actions are unknown, and are absent from the literature.
SUMMARY OF THE INVENTION
The present invention provides a sugar-coated tablet that employs, as the sugar coating base, a mixture composed of raffinose and lactulose having various physiological effects, which does not employ any sucrose, and has anticariogenic properties.
The present invention relates to a sugar-coated tablet formed by coating a core tablet with a sugar coating base that contains, as its effective component, a mixture of lactulose and raffinose.
The present invention provides a sugar-coated tablet that does not stick to the oral cavity when taken, has no unpleasant texture when ingested, a good sensation (mouthfeel) and excellent taste.
DISCLOSURE OF THE INVENTION
With the foregoing in view, the inventors began with the use of lactulose having various physiological effects as a sugar coating base, attempting to manufacture a sugar-coated tablet using a sugar coating base composed of lactulose alone, and mixtures of lactulose and sucrose, oligosaccharides, sugar alcohols and other sugars. However, adequate product quality could not be obtained in the form of a sugar-coated tablet because it was not possible to uniformly coat the core tablet due to excessive viscosity.
The inventors thus carried out painstaking investigations towards a solution to these problems, and arrived at the present invention upon discovering that when at least one part (by weight) of raffinose is mixed with respect to 1 part (by weight) of lactulose for use as the sugar coating base, the viscosity of the mixed aqueous solution can be greatly reduced, making it possible to provide a sugar-coated tablet with a uniformly coated core tablet.
It is an object of the invention to provide a sugar-coated tablet formed using a sugar coating base that is a mixture of raffinose and lactulose having various physiological effects, containing no sucrose, which is primarily used in conventional sugar coating bases, which has anticariogenic properties result from the use of lactulose and raffinose.
A solution to the above problems provided by the present invention is a sugar-coated tablet formed by coating a core tablet with a sugar coating base that contains a mixture of lactulose and raffinose as its effective component.
The present invention, in a preferred aspect, contains a mixture containing a ratio of at least 1 part (by weight, likewise below when not otherwise specified) of raffinose with respect to 1 part (by weight) of lactulose.
In another preferred aspect, the core tablet contains, as its effective component, one or both of (a) and (b) below:
(a) cell powder of one or more selected from the group consisting of microorganisms of the genus Bifidobacterium, microorganisms of the genus Lactobacillus, microorganisms of the genus Streptococcus, microorganisms of the genus Pediococcus and microorganisms of the genus Leuconostoc (these microorganisms are all referred to below as “lactic acid bacteria”), and
(b) one or more selected from the group consisting of lactoferrin, peptide and lactulose.
The present invention is described below.
The lactulose and raffinose used in the sugar coating base of the present invention are commercially-available products, and can be manufactured by well-known methods. For example, lactulose can be manufactured as follows based on the methods disclosed in Japanese Laid-Open Patent Publication No. H3-169888 (1991) and Japanese Laid-Open Patent Publication No. H6-228179 (1994). Sodium hydroxide is added to a 10 wt % aqueous solution of commercial lactose, and said mixture is heated for 30 min at a temperature of 70° C., and cooled. Subsequently, the cooled solution is purified with an ion exchange resin, concentrated, and cooled to bring about crystallization. The unreacted lactose is then removed to obta
Asano Yuzo
Iiyama Yuriko
Mizota Teruhiko
Mori Tetsushi
Sotoyama Kazuyoshi
Morinaga Milk Industry Co. Ltd.
Oblon & Spivak, McClelland, Maier & Neustadt P.C.
Spear James M.
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