Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
2000-10-24
2002-10-29
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
C424S447000, C424S448000, C424S449000, C424S401000
Reexamination Certificate
active
06471984
ABSTRACT:
TECHNICAL FIELD
This invention relates to a plasticizer and a patch containing the plasticizer.
In particular, this invention relates to such a plasticizer that is excellent in plasticizing effect on a base for a patch, high in safety, stability and compatibility with the base, odorless and exhibits a refreshing effect, and also relates to a cataplasm (poultice) and a tape-aid (plaster) each containing the plasticizer.
BACKGROUND ART
Antiphlogistic and analgesic patches are generally used for lumbago, sprain, muscular pain, stiff shoulders, etc. from old times. However, those conventional patches still leave room for improvement in their overall feelings at the time of use, which include adhesion, stickiness and fitness (fit feeling) to the skin, pain caused on peeling, and odor. Further, in the case of a so-called systemic transdermal preparation which has often been used recently and make a medicine therein percutaneously absorbed to produce an intended therapeutic effect, it is indispensable to keep the preparation in contact with the skin for a long time. When a patch preparation is used for this purpose, the adhesion thereof to the skin is necessitated much more than usual because the therapeutic effect is greatly influenced by the area of the patched skin.
The feelings realized by the application of a patch to the skin, such as adhesion or fitness to the skin and pain caused by peeling off the patch, depend on the properties of the base of the patch. Generally, as the base becomes softer, it is improved in the adhesion and fitness and causes less pain upon peeling. Therefore, incorporating into a base an additive which plasticizes and softens the base is supposedly the simplest and surest method in order to easily improve the properties of the base without significantly changing the formulation to obtain the intended pharmaceutical characteristics.
However, at present, there is absolutely no such excellent plasticizer as to exhibit high compatibility with the base of the patch, plasticizing effect, high safety and excellent feelings of use such as smell.
Plasticizers now used for medicines include glycols such as propylene glycol and polyethylene glycol, some surfactants, fatty oils such as castor oil, and fatty acid esters typified by isopropyl myristate.
However, when these plasticizers are used for patches, fully satisfactory results cannot always be obtained for the following reasons: their plasticizing effects are insufficient for obtaining the intended pharmaceutical characteristics; these plasticizers have only low compatibility with the base to cause bleeding with time; the use thereof is limited because of their odor; decomposition or coloring is caused with time because of instability of the plasticizers; and unfavorable side effects are caused because the plasticizers irritate the skin.
An object of the present invention is to solve the above-described problems by providing a plasticizer capable of showing an excellent effect of plasticizing a base for a patch, and having high safety, stability and compatibility with the base. Another object of the present invention is to provide a patch, particularly, a cataplasm and a tape-aid, containing the plasticizer and having excellent overall feelings when in use such as adhesion and fitness to the skin and pain caused by peeling off the patch.
DISCLOSURE OF THE INVENTION
The above objects of this invention can be attained by using 3-L-menthoxypropane-1,2-diol as a plasticizer for the base of a patch.
The crux of this invention resides in a plasticizer composed of 3-L-menthoxypropane-1,2-diol, and in a patch, particularly a cataplasm and a tape-aid, containing the plasticizer in its base.
3-L-menthoxypropane-1,2-diol (which is also called 3-{(1R, 2S, 5R)-[5-methyl-2-(1-methylethyl) cyclohexyl]oxy}-1,2-propanediol) which is the plasticizer of this invention, is a known substance described in, e.g., Japanese Pat. Appln. Laid-Open Gazette No. Sho 58-88334 (88334/83) as a substance having a cooling or refreshing activity. Further, Japanese Pat. Appln. Laid-Open Gazette No. Sho 60-25908 (25908/85) discloses that this compound is useful as a cosmetic material, has an excellent cooling effect and is extremely safe for the skin. However, there has not been found any example of using said known substance as a plasticizer, to say nothing of an attempt to plasticize or soften the base for a patch by the use of this substance to obtain the desired pharmaceutical characteristics. Such an attempt has been made for the first time by the inventors of the present invention and the invention is based on this entirely new finding.
3-L-Menthoxypropane-1,2-diol is present in the forms of R- and S-optical isomers because it has an asymmetric carbon atom at the 2-position to which a hydroxyl group is attached. In the present invention, this compound may be used as a plasticizer in the form of racemic modification or singly in the R- or S-form obtained by resolution.
The base for the patch of this invention contains 3-L-menthoxypropane-1,2-diol in an amount of preferably 0.1 to 20% by weight, more preferably 0.5 to 10% by weight, of the total amount of the base. When the amount is less than 0.1% by weight, no sufficient effects as the plasticizer will be exhibited, while when it exceeds 20% by weight, no stable preparation will be prepared.
The drug to be used in the patch of this invention is not particularly limited but may be arbitrarily selected from among known conventional drugs. Such drugs include steroidal anti-inflammatory agents such as prednisolone, dexamethasone, hydrocortisone, fluocinolone acetonide, betamethasone valerate, betamethasone dipropionate, clobetasone butyrate and prednisolone succinate; nonsteroidal anti-inflammatory agents such as methyl salicylate, glycol salicylate, indomethacin, diclofenac, ibuprofen, ketoprofen, flufenamic acid, ketorolac, flurbiprofen, felbinac, suprofen, prarioprofen, tiaprofen, loxoprofen, tenidap, aspirin, actarit, mizoribine, oxaprozin, auranofin, indomethacin farnesyl, oxaprozin, mofezolac and etodolac, and their ester derivatives; antiallergic agents such as tranilast, azelastine, ketotifen, ibudilast, oxatomide, emedastine and epinastine; antihistamic agents such as diphenhydramine, chlorpheniramine, promethazine and tripelennamine; central nervous system stimulants such as chlorpromazine, nitrazepam, diazepam, phenobarbital and reserpine; hormones such as insulin, testosterone, norethisterone, methyltestosterone, progesterone and estradiol; antihypertensive agents such as clonidine, reserpine, guanethidine sulfate and efonidipine; cardiotonics such as digitoxin and digoxin; antiarrhythmic agents such as propranolol hydrochloride, procainamide hydrochloride, ajimalin, pindolol and tulobuterol hydrochloride; coronary vasodilators such as nitroglycerin, isosorbide dinitrate, papaverine hydrochloride and nifedipine; local anesthetics such as lidocaine, benzocaine, procaine hydrochloride and tetracaine; analgetic agents such as morphine, aspirin, codeine, acetanilide and aminopyrine; skeletal muscle relaxants such as eperisone, tizanidine, tolperisone and inaperisone; antifungal agents such as acetophenylamine, nitrofurazone, pentamycin, naphthiomate, miconazole, omoconazole, clotrimazole and butenafine hydrochloride; antineoplastic agents such as 5-fluorouracil, busulfan, actinomycin, bleomycin and mitomycin; investigational agents for urinary incontinence such as terodiline hydrochloride and oxybutynin hydrochloride; antiepileptics such as nitrazepam and meprobamate; antiparkinson agents such as chlorzoxazone and levodopa; assistants to the prohibition of smoking such as nicotine; vitamins and prostaglandins, though the drug usable in the patch is of course not limited to them. Further, those drugs may be used in the form of organic salt or inorganic salt.
The content of the drug is preferably 0.1 to 20% by weight, more preferably 0.5 to 10% by weight, of the total amount of the base for the patch, though it is not particularly limited.
The patch according to this in
Hirashima Nobuchika
Miyata Daisuke
Oda Hideshi
Ghali Isis
Hisamitsu Pharmaceutical Co. Inc.
Kubovcik & Kubovcik
Page Thurman K.
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