CN1204257A - Surface-stabilised pharmaceutical preparation for application on skin - Google Patents
Surface-stabilised pharmaceutical preparation for application on skin Download PDFInfo
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- CN1204257A CN1204257A CN 96198914 CN96198914A CN1204257A CN 1204257 A CN1204257 A CN 1204257A CN 96198914 CN96198914 CN 96198914 CN 96198914 A CN96198914 A CN 96198914A CN 1204257 A CN1204257 A CN 1204257A
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- active substance
- layer
- skin
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- described pharmaceutical
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Abstract
A transdermal pharmaceutical preparation containing an active substance and of predetermined contact area comprises a non-adhesive back layer which is permeable to the active substance and an adhesive layer which sticks to the skin. The preparation is characterised in that the back layer contains at least one third of the total quantity of active substance contained in the preparation.
Description
The present invention relates to a kind of through the pharmaceutical preparation of skin to the human body release of active agent.
Just know that pharmaceutically active substance can move by human body skin from Middle Ages, and on skin, use or apply enough pharmaceutically active substances and can therefore produce therapeutic effect.These effects have more than and are limited to skin and subcutaneous tissue, and when using suitable material, these effects also can arrive organ far away, and reason is that these active substances are to absorb the back to distribute by blood circulation.That has for example sold in the market contains hormone ointment and emulsifiable paste.And can buy wind resistance damp disease semi-solid preparation; After being coated on it on skin, they just play therapeutical effect by part or systemic effect.In this relation, the degree that active substance absorbs is not only the concentration by active substance, and the unmanageable size by the skin surface for the treatment of is determined in other material.And user also is difficult to the accurately layer thickness of the used preparation of control, and this thickness helps medical outcome.For this reason, adopt the treatment measure of these forms just to relate to unacceptable defective.
Except that active material concentration, the Transcutaneous Therapeutic System (TTS) that yet definitely defines application surface does not then have this shortcoming.Present known TTS has several common base substances:
1. a non-sticky bottom that does not see through the TTS component is used to prevent not expect the release to environment of the volatility TTS component that occurs, also can be used for preventing contacting the unfavorable effect that causes with other surface, and has also guaranteed the mechanical stability of TTS.
2. because TTS directly is bonded on the skin, being autohension so face the layer of skin, is the part autohension at least.
3. because these autohension provides removing of antiseized effect protective layer used storage purpose before using.
Usually, this bottom is made of suitable material, for example plastic foil; But paper, non-textile or textile also are suitable.
Do not consider acquired progress, above-mentioned TTS also has some shortcomings.For example, do not see through active substance and its surface and carried out the comfort of pasting that the bottom of stabilizing treatment has damaged patient.The hardness of used film can produce the area constraints of not expecting.Because some pharmaceutically active substances have the relevant relatively low skin rate travel of wearing with its surface, expects that bigger system surfaces so that enough effective TTS to be provided, also is applicable to these active substances.
Adopt elastomeric material to do the trial that bottom pasting comfort with improvement and carried out many times (for example U.S.5,246,705); Yet, clearly the material that does not see through medicament has been made restriction.Another shortcoming of prior art TTS is that its thickness sometimes makes patient feel under the weather.In traditional design, substrate is only arranged, adhesion layer or optional bin-storing layer are mainly used in storage and discharge this active substance, and for this reason, according to definition, the bottom that does not see through active substance is not have this respect function.
The objective of the invention is just to provide a kind of pharmaceutical preparation on the skin of sticking to given contact surface size, it comprises a non-sticky bottom and the storage storehouse that contains active substance that the viscous layer by the ixoderm skin forms, and does not have the shortcoming of prior art.
According to the present invention, this purpose reaches by contain the active substance that accounts for said preparation active substance total amount 1/3rd at least in this bottom.In diffusion process, comprised this bottom, its favourable result be according to the present invention in this system, it has two functions: on the one hand, its forms part active substance storage storehouse, on the other hand, it is that a bottom prevents that this plaster from adhering on textile or other article.Be the most astoundingly to find that its inevitable active substance permeability no longer is disadvantageous usually, produce significant loss owing to have only volatile active matter and/or adjuvant to discharge to environment by bottom.
The example of such pharmaceutically active substance comprises nicotine and nitroglycerine.Other terpenes of ethanol, propylene glycol and other low-molecular-weight alcohol, menthol, cineole, limonene and some, the low-molecular-weight fatty acid, as capric acid, dimethyl sulfoxide all is a conventional additives in such preparation, and what can be emerged from said preparation by bottom for it.Beyond thought is that (for example, EP 0.366,240, P, 3,1.24 for restriction widely about the bottom that can see through active substance; Perhaps EP 0,402,407, P.5,1.4) result proves without basis basically, is much higher than amount to external diffusion because pass the amount of the active substance that viscous layer divides a word with a hyphen at the end of a line to skin from this bottom.
Because its thickness is little and make the probability of bottom host material with highly elastic material, except they different functional, the TTS of preparation of the present invention and other standard design has obvious difference in appearance.Because the said preparation careful wrinkle of skin of having fitted, so be to feel only to be affixed on one deck very thin on the skin with respect to its effect of stiff adhesive film.In this respect, theme of the present invention is that it is between TTS and is applied to intermediate products between the ointment of skin surface.
The production method of in process of production most of active substance being introduced this bottom has avoided forming because of expansion the moving process of fold.
Many materials all are applicable to such bottom, and the part example is as polyvinyl alcohol, styrene-dienes block copolymer, polyurethane, polrvinyl chloride, polymethyl acyl ester, and many other suitable substantially materials.
In advantageous embodiment, bottom is covered by a supporting layer, and this supporting layer is removed after use; It adheres to its whole surface, and antiseized effect is provided.Spendable favourable pharmaceutically active substance comprises steroid hormone, to the central nervous system or to the effective active substance of Alzheimer.Rheumatism or aspirin.
Embodiment:
Embodiment 1:
A) with 10g styrene-isoprene-styrene copolymer-(Cariflex
RT 1107) thoroughly be dissolved in the 20g Petroleum of boiling range between 80-100 ℃.
Add the 100mg 17-that is dissolved in the 5g ethyl acetate; With this material mix homogeneously, by the gap (gap) of using width to be about 150 μ m it is coated on one deck release polyester film, obtaining weight per unit area after 4 hours 35 ℃ of dryings then is 30g/m
2Conforming layer.
B) in separate operation, prepare 20g hydrogenated rosin glyceride resin (Staybelite Ester in the Petroleum between 80 ℃-100 ℃ in 10g ethyl acetate and 10g boiling range
5E) with 8g styrene-isoprene-styrene copolymer-(Cariflex
TR 1107) solution; Add the at room temperature thorough dissolved 17-of 0.12g.Use width to be about the gap of 100 μ m, this material is coated on the release polyester film.35 ℃ of dryings 30 minutes, 60 ℃ of dryings obtain weight per unit area after 15 minutes be 23g/m
2Conforming layer.
The A that so makes is layer (bottom) and B layer (storage storehouse) mutual lamination on each layer mutually mutually, obtain artificial inseparable synthetic simultaneously, the release polyester film of B phase and viscous layer and bottom are stamped in the profile of a corresponding said preparation geometry with the known method of those of ordinary skill, remove outside residue then.
Each form of administration is packed in the independent sealing bag.
User takes out medicine from packing, remove protective layer (discharge pad) from viscous layer, and this administration type is adhered to correct position at skin, and final removing from this back side provides antiseized and as the polyester film of supporting layer.
Below, according to Fig. 1-3, illustrated the structure of preparation of the present invention in more detail with reference to embodiment.
What Fig. 1 showed is the profile of the basic structure of percutaneous plaster, and this percutaneous plaster comprises and contains active substance and can see through the bottom (2) of active substance and the storage storehouse that contains active substance that forms with viscous layer (3).
Fig. 2 shows is plaster according to Fig. 1, but has the supporting layer 1 that adheres to bottom (2) fully.
Fig. 3 shows is plaster according to Fig. 1 and Fig. 2, but this viscous layer (3) also is used to the non-sticky of this viscous layer fully, removable supporting layer (4) covers.
Claims (10)
1. contact area that has to sizing, the transdermal drug preparation that contains active substance, comprise non-sticky bottom that can see through active substance and the viscous layer that adheres to skin, it is characterized in that this bottom contains the active substance that accounts for the contained active substance total amount 1/3rd of said preparation at least.
2. pharmaceutical preparation according to claim 1 is characterized in that this bottom is adhered to the supporting layer covering on its whole surface, and this supporting layer provides antitack agent and removes after use.
3. pharmaceutical preparation according to claim 1 and 2 is characterized in that this viscous layer is adhered to the non-sticky protective layer covering on its whole surface, and this protective layer is removed before being applied to skin.
4. according to one or several the described pharmaceutical preparatioies of aforementioned claim, it is characterized in that thickness that viscous layer and bottom have altogether is less than 80 μ m, preferably less than 40 μ m.
5. according to one or the described pharmaceutical preparation of the aforementioned claim in a few top, it is characterized in that it contains a kind of steroid hormone as pharmaceutically active substance.
6. according to one or several described pharmaceutical preparatioies of claim 1-4, it is characterized in that it has maincenter is looked the effective pharmaceutically active substance through system.
7. according to one or several described pharmaceutical preparatioies of claim 1-4, it is characterized in that it has the effective pharmaceutically active substance of Alzheimer.
8. according to one or several described pharmaceutical preparatioies of claim 1-4, it is characterized in that it comprises a kind of rheumatism as pharmaceutically active substance.
9. according to one or several described pharmaceutical preparatioies of claim 1-4, it is characterized in that it comprises aspirin as pharmaceutically active substance.
10. produce method according to the transdermal drug preparation of aforementioned claim; it is characterized in that; the first step with a kind of polymer that uses as host material by adding that solvent is made solution or by being heated into melt; at least add 1/3rd of predetermined active substance; mix homogeneously; apply this antiseized support membrane with this mixture; form an exsiccant conforming layer; and in division step; but the diffusion viscosity material that contains residue being quality is also by also dry on coated this antiseized protecting film; the layer of so making is mutual lamination on each layer, forms paster by punching press.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 96198914 CN1204257A (en) | 1995-12-09 | 1996-12-04 | Surface-stabilised pharmaceutical preparation for application on skin |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19546024.3 | 1995-12-09 | ||
| CN 96198914 CN1204257A (en) | 1995-12-09 | 1996-12-04 | Surface-stabilised pharmaceutical preparation for application on skin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1204257A true CN1204257A (en) | 1999-01-06 |
Family
ID=5129214
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 96198914 Pending CN1204257A (en) | 1995-12-09 | 1996-12-04 | Surface-stabilised pharmaceutical preparation for application on skin |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1204257A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101068589B (en) * | 2003-11-17 | 2010-05-12 | Lts罗曼治疗方法有限公司 | Device for the transdermal administration of active ingredients |
-
1996
- 1996-12-04 CN CN 96198914 patent/CN1204257A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101068589B (en) * | 2003-11-17 | 2010-05-12 | Lts罗曼治疗方法有限公司 | Device for the transdermal administration of active ingredients |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |