Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Reexamination Certificate
2001-08-28
2002-12-24
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...
C424S443000, C424S444000, C424S448000, C604S307000, C604S304000, C602S057000, C602S058000
Reexamination Certificate
active
06497897
ABSTRACT:
TECHNICAL FIELD
The present invention relates to a sustained released pharmaceutical plaster agent for percutaneous administration, and a method of preparing same. More specifically, the present invention relates to a plaster agent comprising a knitted fabric comprising specific hollow fibers and a tackifier (or adhesive) layer containing a medicine or drug and a film, and having a high safety factor, excellent sustained releasability and easy handleability, and to a process for efficiently preparing the same.
The present invention relates to a plaster agent containing nitric acid esters useful for the prophylaxis and amelioration of circulatory diseases, particularly cardiac diseases such as stenocardia and arrhythmia.
The present invention further relates to an estradiol-containing plaster agent useful for the prophylaxis and amelioration of disorders frequently observed in women after menopause, such as menopausal disorders, oestroporosis, and Alzheimer dementia.
The present invention further relates to a buprenorphin-containing plaster agent useful for the relief of pain after surgery, from various cancers, and from myocardial infarctions, and further, from lumbago, chronic articular rheumatism, trauma, and exodontia, in particular the pain accompanying various cancers, and as an anesthesia aid.
BACKGROUND ART
In the development of pharmaceuticals, simultaneously with the development of novel compounds having excellent pharmacological effects, various investigations have been made into changes of the dosage forms and an optimization of the administration forms, to to further enhance the effects of these novel compounds or compounds already used as pharmaceuticals.
For example, to prolong the persistency time of a pharmaceutical with a short half-life period, which is also a parameter of the effective persistency time of a pharmaceutical in the body, the development of slow release preparations has been made, which will enable the pharmacologically effective ingredient to be absorbed by the human body at the minimum effective level or higher and the maximum safe level or lower, i.e., in the effective level region in the blood, over a long time.
As examples of slow release preparations, there are known preparations for a percutaneous absorption such as ointments, sprays and coatings. These preparations are coated by hand onto the skin, and therefore, the dose is not constant, and further, a problem arises in that the ointment may adhere to and contaminate the clothing of the patient.
As measures for alleviating these drawbacks, there are known tape agents and plaster agents which incorporate a predetermined amount of a medicine and are molded to a predetermined size (e.g., see Japanese Unexamined Patent Publications (Kokai) Nos. 57-116011, 58-134020), and the use of the method using the tape agent and plaster agent can solve many problems due to the use of an ointment or spray coating.
Also, when a medicine is percutaneously administered, it is known that the ratio of the liver metabolism, which is the phenomenon whereby the pharmacological effect disappears upon receiving the metabolism of the drug in the liver, can be markedly alleviated compared with the case when the medicine is orally administered, and therefore, a tape agent and plaster agent (hereinafter referred to as plaster agent) is an excellent medicine administration form when the medicine can be percutaneously absorbed.
Nevertheless, frequent use of such a plaster agent has shown that some problems arise with the plaster agent of the prior art.
Among such problems, the most frequent is a skin rash generated at the site at which the plaster agent is plastered to a patient. Generally speaking, a sustained release preparation is frequently administered to a patient with chronic diseases, and therefore, the plaster agent is frequently used over a long term, and thus a skin rash is often generated. Further, a problem arises in that, once a skin rash is generated, the afflicted site is susceptible to a growth of the rash. According to statistics, the generation of a skin rash by a plaster agent occurs in 20 to 50% of all patients.
Another problem of the plaster agent is a change of the medicine level in the blood. The factors causing a change of this level in the blood are complicated, and include the plaster agent, the skin, and the human metabolism functions, and therefore, it is not easy to hold the medicine level in the blood at a constant value.
Still another problem concerns the handleability. More specifically, a skin rash could be more or less alleviated by making the support of the plaster agent as thin as possible, enhancing the flexibility, and making the plaster agent smaller to alleviate a skin rash caused by the plaster, but another problem arises in that it is very difficult to plaster the plaster agent correctly at a predetermined position on the patient. For example, recently, plaster agents containing as an effective component nitric acid esters are widely used as therapeutic agents for circulatory diseases such as stenocardia, but the above-mentioned various problems, particularly the skin rash problems, still remain and, therefore, plaster agents capable of stably maintaining the concentration of medicines in the blood and not having the above-mentioned problems are needed in this field.
On the other hand, as the cause of menopausal disorders, oestoroporosis, and Alzheimer dementia, frequently observed in women after menopause, a reduction of estrogen accompanying the menopause is regarded as important, and estradiol, estradiol and derivatives thereof have been clinically applied primarily as oral agents and injections.
When estrogen is frequently used, however, side effects such as an increase in an uterus body cancer are observed, and therefore, it is necessary to enhance the biological availability (hereinafter abbreviated as BA) during use, as much as possible, at a minimum necessary dose, while maintaining a stable medicine level in the blood.
Among various estrogens clinically applied, estradiol is one of the natural estrogens which are inherently synthesized and utilized in the living body, has a pharmacologically high activity, and although considered to be the most suitable estrogen for use as a pharmaceutical from the aspect of safety, it has been little used. This is because estradiol, when administered orally, is rapidly metabolized in digestive organs and the liver and the BA is lowered. To maintain the necessary drug level in the blood, a large amount of estradiol must be administered, but this means that an undesirable large amount of harmful metabolites by products will be produced in the blood.
The loss of the BA in estradiol can be markedly ameliorated by a percutaneous administration, and a stable drug level in blood can be still maintained.
Estradiol and derivatives thereof such as esters are known to be percutaneously absorbed, as disclosed in Japanese Patent Publication (Kokoku) No. 46-5427, Japanese Unexamined Patent Publication (Kokai) No. 57-154122, etc. Particularly, the plaster agent disclosed in Japanese Unexamined Patent Publication (Kokai) No. 57-154122 provides an excellent improvement of the BA and stabilization of the drug level in the blood. Nevertheless, although the estradiol-containing plaster agent compensates for a reduction of estrogen accompanying the menopause, the therapeutical period can last for several months to several years, and therefore, a steadfast compliance by the patient is an essential requirement. Particularly, in the presence of a plaster agent, although an uncomfortable feeling during plastering often exists, a generation of a skin rash is a serious problem, an insufficient consideration of this point has been made in the prior art.
In the prior art as described above, in the case of an oral agent, which requires a relatively lower compliance by the patient, the BA is lower and a generation of side effects is a serious problem, but in the case of a percutaneous absorption type plaster agent with a high BA and a stable medicine level in the
Hidaka Osafumi
Kato Toshiyuki
Magoshi Osam
Ohe Michisuke
Sakai Tomoki
Ghali Isis
Page Thurman K.
Sughrue & Mion, PLLC
Teijin Limited
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