JPS5832816A - Contraceptive film pharmaceutical - Google Patents

Abstract

PURPOSE:A contraceptive film pahrmaceutical, consisting of a polyvinyl alcohol film, cntaining a contraceptive agent, and having improved solubility and handleability by fine uneven patterns on one or both sides thereof, easily handleable, and having great contraceptive effects. CONSTITUTION:A contraceptive film pharmaceutical, obtained by forming fine uneven patterns having 200-1,200 individual protrusions per cm<2> on one or both sides of a polyvinyl alcohol film, containing a contraceptive agent, particularly a surfactant and/or contraceptive agent having antispermatocidal action and an average polymerization degree of preferably 300-500 and a saponification degree of 85-95mol%, and preferably further heat-teating the resultant film. The recesses of the film pharmaceutical is rapidly dissolved by the body fluid in the vagina, and the protrusions form fine gelatinous particles. The contraceptive agent contained on both of them enhances the contraceptive effects and will not easily flow out of the vagina.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a contraceptive film preparation, and particularly aims to provide a contraceptive film preparation with improved dissolution time and handling properties.

Attempts have already been made to provide a film-like contraceptive (contraceptive membrane) that is easy to handle and has a high contraceptive effect, as an alternative to the conventionally known jelly or tablet-like contraceptives. It is difficult to use the product itself, or a product with sufficient performance in terms of dissolution performance and long-lasting effect has not been obtained.

Film-shaped contraceptives, that is, contraceptive film preparations, contain a commonly used spermicide such as polyoxyethylene nonylphenyl ether, along with a small amount of an emollient if necessary, in a film made of a water-soluble polymeric substance. However, from a performance standpoint, this device must be sufficiently flexible and strong so that it can be easily rolled up or folded and inserted into the vagina. In this case, it is desirable that the film has enough dissolvability to prevent it from sticking or tearing even when it comes into contact with wet fingers, etc., and at the same time, after being inserted into the vagina, it rapidly dissolves in body fluids and immediately has a contraceptive effect. There must be.

Another important performance is that the drug stays in the vagina for 1 to 2 hours, but conventional contraceptives have the disadvantage that they tend to leak out of the vagina in a short period of time. The present invention aims to provide a contraceptive film i11 that solves the above conventional disadvantages, and is made of a contraceptive-containing polyvinyl film with a fine uneven pattern on one or both sides. It is characterized by being made of an alcohol film.

The present invention provides the following advantages.

(1) Sufficiently pliable and durable, with a soft feel,
Easy to insert into the vagina and has excellent handling.

(2) Even if held with wet fingers, it will not stick, stick, or tear (resistant to initial wetness).

(3) After a short period of time in the vagina (2 to 3 minutes after insertion), it rapidly disintegrates or dissolves into fine particles, forming fine gel particles that can easily flow out of the vagina. It provides reliable contraceptive effect for a long time.

(4) The effect of 13) above can be obtained by inserting it into the vagina once at the beginning, so there is no need to insert it additionally in the middle.

To explain this, it is necessary for the polyvinyl alcohol film used in the present invention to have a fine uneven pattern on at least one side, and this specifically requires 200 to 1.200 individual protrusions per 1aI. (Especially 300~
1,200 pieces) is desirable. Due to this uneven structure, this film quickly breaks up (disintegrates) into small pieces in the vagina and dissolves to form small gel particles, ensuring a sufficiently long residence time in the vagina. Contraceptive effect can be obtained.

In order for this film to disintegrate and dissolve well in the vagina, it is desirable that the film has a thickness of 50 to 150 microns.For example, as shown in the example below, the thickness of the convex part is 120 microns, and the thickness of the concave part is 120 microns. This is done by increasing the thickness, and the convex portions form fine gel particles. Since both the dissolved part and the gel particles contain the contraceptive agent, spermicidal activity is very reliable.

The embossing process on ordinary polyvinyl alcohol film has a so-called fine-grained structure, which improves the appearance, flexibility, and solubility of the film to some extent, but in the case of such an embossed film, water (body fluids) and When they come into contact with each other, they do not become a single gel-like liquid or a lumpy mass as in the case of the general pillar preventive agent of Tablet I, but do not become a dispersed state of fine gel particles as in the present invention. Generally speaking, the same is true for polyvinyl alcohol, but when a water-soluble resin forms a gel, it has the effect of hindering the penetration of water, and in this case, the essential effect of the spermicide is not sufficiently effective. However, with the structure of the present invention, fine gel particles are formed by mixing with the partially dissolved portion, and these particles do not easily flow out of the vagina, so that the contraceptive effect is reliably achieved. .

In the case of conventional jelly-like and tablet-like contraceptives, attempts have been made to produce as low a viscosity or thin liquid as possible in the vagina in order to increase the contraceptive effect; This could also cause it to leak out of the body.

On the other hand, the raw material polyvinyl alcohol used for producing this film has a low polymerization degree, especially 300 to 50.
Partially saponified polyvinyl alcohol of about 0 is desirable. If the degree of polymerization is too low, the film will be weak and its strength against initial wetting will be weakened, and if the degree of polymerization is too high, the rate of dissolution in the vagina will be slow, resulting in insufficient contraceptive effect. I won't be able to do it. Furthermore, another reason why the above polymerization degree range is desirable is that polyoxyethylene nonylphenyl ether, which is often used as a spermicide, is stably and uniformly contained in a polyvinyl alcohol film having a polymerization degree within this range. It has been observed that during storage, the spermicide and optionally used plasticizer may ooze out onto the film surface or become non-uniform within the film. In addition, since this polyvinyl alcohol is assumed to be easily dissolved by intravaginal body fluids, it is desirable that it be a partially saponified product, and the desired degree of saponification is approximately 85 to 95 mol%. be.

The contraceptive film preparation of the present invention is usually produced as follows. That is, the raw material polyvinyl alcohol described above, a plasticizer if necessary, and a surfactant having a spermicidal effect and/or a contraceptive are dissolved in water, and this is cast and molded using a plate having a fine uneven pattern. Alternatively, it can be manufactured by forming a film using a conventional method and then pressure-molding the film into a fine uneven pattern.

The film having a fine uneven pattern obtained as described above is cut into a suitable size, for example, 5 x 5, to make a contraceptive film preparation.This film is then heat-treated for a short time. By doing so, even better effects can be obtained. That is, when the film is heat-treated at a temperature of 80-95°C for 30 seconds to several minutes, the strength against initial wetting is sufficient, and therefore the handling property is significantly improved, whereas in the vagina, after 2-3 minutes. The ability to quickly and finely disintegrate into fine gel particles afterwards is more reliably imparted.

Next, a specific example will be given.

Example polyokine ethylene nonylphenyl ether 17! ,
Partially saponified polyvinyl alcohol 59N with a degree of polymerization of 400
y, 5 parts glycerin and 130 parts water? [Dissolved in p. By this solution casting method, the height part is 120 microns and the bottom part is 70 microns.
A film having a fine illumination pattern (pitch 500 microns) with each micron being independent was produced, and this was heat-treated at 90° C. for 1 minute.

The contraceptive-containing polyvinyl alcohol film thus obtained was cut to produce a contraceptive film preparation of 5×5 cm.

Even if this film preparation gets wet with water, it does not immediately adhere to fingers, etc., is flexible and can be bent and inserted into the vagina easily, and can be immediately divided in body fluids at 37°C. It became fine gel particles and became dissolved after 2 to 5 minutes.

This product has also been shown to have a much longer vaginal residence time and sufficient contraceptive efficacy compared to other contraceptives in numerous clinical trials.

Claims (1)

[Scope of Claims] 1. A contraceptive film preparation comprising a contraceptive-containing polyvinyl alcohol film having a finely textured pattern on one or both sides of the film. 2. The finely textured pattern has 200 individually independent protrusions per cIl. -1,200 contraceptive film preparation 3 according to claim 1, wherein the polyvinyl alcohol film has an average density of 300 to 50
Special J which is made from polyvinyl alcohol of 0.
Contraceptive film preparation 4 according to FFji desired scope FINt1gxq4; Contraceptive film preparation according to claim 1, wherein the polyvinyl alcohol film is made from polyvinyl alcohol with a Jt conversion degree of 85 to 95 mol%. 5. The contraceptive agent is a surfactant having a spermicidal effect and/or a contraceptive. 6. The contraceptive film preparation according to claim 1 is a heat-treated film preparation. Contraceptive film preparation according to item 1