Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Reexamination Certificate
2001-08-30
2003-04-29
Fay, Zohreh (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
C514S912000
Reexamination Certificate
active
06555526
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to the treatment in an ophthalmologic field, more particularly, to ophthalmic pharmaceutical compositions for treating and/or preventing the ophthalmologic clinical symptoms and signs in Sjögren syndrome.
2. Description of the Prior Art
Sjögren syndrome is one of the frequently diagnosed diseases and is often found particularly in older ages. It is estimated that patients with such a syndrome will increase in number more and more as coming into the aging society. As characteristic features, Sjögren syndrome is accompanied by the invasion of lymphocytes into the lacrimal gland and the salivary gland, and the disruption of adenocytes, and is characterized mainly by dry eye and dry mouth. Sjögren syndrome is a cryptogenic disease or the like and is highly speculated as an autoimmune disease, and the criterion has been already established. The ophthalmologic clinical symptoms of Sjögren syndrome are, for example, foreign body sensation, burning, and itching. Treatments for Sjögren syndrome now used predominantly are symptomatic therapies such as the application of artificial tears and the wear of goggles and glasses for preventing dry eye. When the symptoms of patients with these treatments are not improved, they are then treated mainly with other symptomatic therapies such as surgeries and the administration of steroids and immunosuppressants in combination, which may restrict patient's normal social life because these therapies would require hospitalization, doctor's advice, or therapeutic devices. Conventional ophthalmic solutions used generally in the ophthalmologic field are easily portable and readily usable when in use, and therefore ophthalmic solutions, containing sodium hyaluronate for treating the ophthalmologic clinical symptoms and signs in Sjögren syndrome, have been commercialized recently, however, any satisfactory ophthalmic pharmaceutical composition for treating and/or preventing the syndrome has not been provided yet.
SUMMARY OF THE INVENTION
The object of the present invention is to provide an ophthalmic pharmaceutical composition with a satisfactory therapeutic and/or prophylactic effect on the ophthalmologic clinical symptoms and signs in Sjögren syndrome, as well as advantageous usefulness and safety; and more particularly to an ophthalmic solution, ointment, and eyewash.
In view of the foregoing, the present inventors screened substances which have a satisfactory therapeutic and/or prophylactic effect on the ophthalmologic clinical symptoms and signs in Sjögren syndrome and have safety even when used for a relatively-long period of time. As a result, the present inventors unexpectedly found that trehalose, which is widely used in food products and cosmetics, exerts an outstanding therapeutic and/or prophylactic effect on the clinical symptoms and signs in Sjögren syndrome without any side effect even after a relatively-long time administration; the present invention solves the above object by the ophthalmic pharmaceutical composition comprising trehalose as an effective ingredient.
Trehalose, a disaccharide composed of two glucose molecules linked together at their reducing residues, has 3-types of optical isomers of &agr;,&agr;-trehalose, &agr;,&bgr;-trehalose, and &bgr;,&bgr;-trehalose, which are hereinafter called “trehalose”, if specified otherwise. In the natural world, trehalose is widely distributed in bacterial, plant, and animal worlds. In the field of food products, trehalose has been being greatly increased in demand because of its remarkable characteristic features such as relatively-low sweetness, prevention of retrogradation of starches, and prevention of denaturation of proteins during freezing/drying. In the field of cosmetics, the use of trehalose has been wide-spreading because of its satisfactory moisture-retaining ability, and the safety of oral administration and dermatological application of trehalose has been already confirmed. However, as for the physiological functions of trehalose, there have only been known the improvement of osteoporosis and the regulation of metabolism of serum fatty acids, while in the field of ophthalmology, only reported is the action of trehalose to protect cells in the corneal endothelium and the corneal epithelium susceptible to damage induced by ophthalmic surgeries as disclosed in Japanese Patent Kokai No. 235,233/97.
As described above, trehalose per se is a well-known compound, however, it was firstly found in the present invention that trehalose exerts a satisfactory therapeutic and/or prophylactic effect on the ophthalmologic clinical symptoms and signs in Sjögren syndrome.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to an ophthalmic pharmaceutical composition for treating and/or preventing the ophthalmologic clinical symptoms and signs in Sjögren syndrome, which comprises trehalose as an effective ingredient. As described above, there exist three types of optical isomers of trehalose, i.e., &agr;,&agr;-trehalose, &agr;,&bgr;-trehalose, and &bgr;,&bgr;-trehalose, which all exert an effective therapeutic and/or prophylactic effect on the ophthalmologic clinical symptoms and signs in Sjögren syndrome, and therefore one or more of these optical isomers can be arbitrarily used in combination in the present invention. In the ophthalmic pharmaceutical compositions of the present invention, each of the optical isomers of trehalose can be used alone or two or more of them can be used in combination independently of their combination use and preparation methods, as long as they contain an effective amount of trehalose.
Any trehalose can be used in the present invention independently of its preparation methods and origin, as long as it does not spoil the present object. Examples of the methods for producing &agr;,&agr;-trehalose include the enzymatic methods as disclosed in Japanese Patent Kokai Nos. 143,876/95, 213,283/95, 322,883/95, 298,880/95, 66,187/96, 66,188/96, 336,388/96, and 84,586/96, where non-reducing saccharide-forming enzymes and trehalose-releasing enzymes are allowed to act on starch hydrolysates to form &agr;,&agr;-trehalose. The trehalose thus obtained can be advantageously used because of its economical merit and lesser possibility of the contamination of harmful impurities as compared with those prepared by synthetic methods. Examples of commercialized trehalose produced by the above enzymatic methods are “TREHA®”, a trehalose having a trehalose content of 98%, on a dry solid basis (d.s.b.), commercialized by Hayashibara Shoji, Inc., Okayama, Japan; and a reagent grade trehalose having a trehalose content of 99% or higher, d.s.b., commercialized by Hayashibara Biochemical Laboratories, Inc., Okayama, Japan. The trehalose usable in the present invention should not be restricted to the ones above, however, the above trehalose products can be advantageously used.
The &agr;,&bgr;-trehalose usable in the present invention can be produced, for example, by the method as disclosed in Japanese Patent Kokai No. 179,490/92 where an enzyme is allowed to act on a mixture of starch hydrolysate and lactose, while the &bgr;,&bgr;-trehalose usable in the present invention can be chemically synthesized easily. The trehalose used in the present invention should not necessarily be in an isolated form or may be in a mixture form of trehalose and other saccharides that are formed during the production of trehalose, as long as they do not spoil the therapeutic and/or prophylactic effect by trehalose on the ophthalmologic clinical symptoms and signs in Sjögren syndrome. Of course, impurities such as pyrogens should preferably be removed by using activated charcoal, ion-exchange chromatography, gel filtration chromatography, and membrane filtration because ophthalmic solutions are directly applied to the ocular-mucous membranes.
When administered to patients with the ophthalmologic clinical symptoms of Sjögren syndrome such as foreign body sensation, burning, and itching, the ophthalmic pharmaceu
Kurimoto Masashi
Matsuo Toshihiko
Yamauchi Hiroshi
Browdy and Neimark, P.LL.C.
Fay Zohreh
Kabushiki Kaisha Hayashibara Seibutsu Kagaku Kenkyujo
LandOfFree
Pharmaceutical composition for ophthalmic use does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pharmaceutical composition for ophthalmic use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pharmaceutical composition for ophthalmic use will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3078172