JPS601120A - Contraceptive soluble cotton preparation - Google Patents

Abstract

PURPOSE:To provide a soluble contraceptive agent having high contraceptive effect, long effective time, and excellent handleability and feeling to the applied part, by adding a spermicidal contraceptive to a water-soluble polymer, collecting the obtained water-soluble fibers in the form of cotton, and forming to a desired form. CONSTITUTION:A spermicidal contraceptive such as polyoxyethylene nonylphenyl ether is mixed and dispersed in a solution of a water-soluble polymer such as PVA, dextrin, etc. to obtain a spinning dope. The dope is spun to fibers of about 5-800mu diameter by falling stream spinning, centrifugal nozzle spinning of short fibers, etc., and the fibers are cut after the heat-treatment of the surface. The obtained short fibers are collected, pressed, and formed to a desired form such as film, sphere, tampon, etc. The rate of dissolution of the cotton can be controlled by controlling the diameter and the cross-sectional shape of the fiber and the saponification degree of PVA. Accordingly, a contraceptive having high initial contraceptive activity and keeping the activity nearly constantly for a long period, can be produced by this process.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a soluble contraceptive preparation, which is a novel and easy-to-use soluble contraceptive that dissolves in the cavity and exhibits an excellent contraceptive effect with spermicidal properties. The purpose is to provide the following.

Conventionally, spermicidal contraceptives that do not require post-treatment after use include jelly-like preparations, tablet-like preparations, and dissolvable film-like preparations, but jelly-like preparations require special tools and are easier to handle. Moreover, it has the disadvantage that its contraceptive effect lasts only a short time because it easily leaks out like tablet-like products. In addition, dissolvable film-like products are relatively easy to handle, but simple film-like products have the disadvantage of clumping together when melting, slowing down the dissolution rate, and conversely, the thickness may change due to fine uneven patterns. However, if the solubility is improved by making the drug more soluble, there is a contradiction that it may become unevenly distributed inside the body during use or leakage to the outside becomes large, making it impossible to achieve the desired contraceptive effect. In addition, dissolvable films have problems in how they are used because they are folded and inserted, and the "edges" of the folding may damage the mucous membranes of sensitive people, or at least cause psychological anxiety. Ta.

In order to solve such conventional drawbacks and problems, the present invention disperses or mixes a spermicidal contraceptive into water-soluble polymer fibers, and aggregates the contraceptive-containing soluble fibers into a single layer. By providing a dissolvable tablet for contraception, a novel dissolvable contraceptive agent with high contraceptive effect, long duration, excellent usability and handling, and shape flexibility and blendability is realized. This method opens up a new means for arbitrarily designing the temporal change in the concentration of eluted contraceptives.

In the simplest case of the present invention, that is, a soluble contraceptive preparation consisting only of homogeneous soluble fibers, distilled water mixed with a plasticizer such as glycerin to maintain the flexibility of the fibers is added to the human body. Safe and odorless, low vinegar water-soluble polymer material such as polyvinyl alcohol is gradually added to the solubility limit while stirring to prevent lumps from forming. After thorough stirring, the temperature is raised to about 80r~95C while stirring. A fluid and viscous solution is obtained. This solution is left to stand or heated to further remove water to thicken it and adjust the viscosity, and then polyoxyethylene 7 nonyl phenyl ether (7) nl zigocidal contraceptive is mixed in to prepare a dispersion.

The fiber stock solution thus produced is made into fibers with a thickness of approximately 5 to 800 microns by a dry spinning method such as a fluidized drop spinning method, a pressure nozzle dry spinning method, a centrifugal nozzle 21 fiber spinning method, or an elongation method. After further heat-treating the fiber surface, short fibers (for example, about 5 to 25 cm) are compressed and aggregated into an appropriate shape to obtain a soluble cotton preparation for contraception.

Here, to explain the flowing drop method, as shown in FIG. 1, the stock solution flows and falls from the stock solution reservoir 1 through the opening nozzle 2, and after being preheated by the heating device 3,
The heat from the drying heating device 5 and the air flow from the blower fan 4 remove moisture and harden the product. Next, the obtained fibers are pressure-molded into a predetermined cross-sectional shape by a forming roller 7 configured below the baffle plate 6, and the fiber surface is heated to a temperature of 80C to 120C by a heating device 8 to adjust the initial solubility. After being heat-treated with, it is cut into short fibers 13 by a cutter 9,
Cotton formulation 14 is obtained. In the figure, the number of flow drops is one in the principle diagram, but of course there may be more than one.

In addition to polyvinyl alcohol, the water-soluble polymer material is preferably amylose such as dextrin, or a mixture thereof. Especially polymerization degree 200-80
0. Low acetic acid pharmaceutical polyvinyl alcohol with a degree of saponification of 70 to 95 is suitable, and dextrin may be added to this. In addition to glycerin, plasticizers include trimethylolpropane, diethylene glycol, and dipropylene glycol, but glycerin is preferred. Spermicidal contraceptives include polyoxyethylene nonylphenyl ether,
Menphegol, other spermicidal substances can be used alone or in combination.

Moreover, the dissolution rate or dissolution duration can be adjusted by the diameter and cross-sectional shape of the fibers, and the degree of saponification of polyvinyl alcohol (or the respective solubility factors for other water-soluble polymers).

That is, as will be described later, the dissolution rate of a unit weight of a cotton formulation is approximately inversely proportional to the diameter of the fiber, or proportional to the cross-sectional perimeter per unit cross-sectional area. The higher the degree of oxidation, the slower the dissolution rate. In addition, the dissolution rate and the duration of dissolution are inversely proportional to the same weight of drug, so the higher the dissolution rate, the higher the concentration of dissolved contraceptives and the instant contraceptive effect, but the shorter the duration. increases, but
This is associated with a decrease in the concentration of eluted contraceptives and the instantaneous contraceptive effect. Therefore, in order to create a soluble contraceptive drug consisting only of homogeneous soluble fibers, it is necessary to adjust the cross-sectional circumference of the fibers in order to maintain a sufficient contraceptive effect and to achieve a dissolution rate that lasts as long as possible. The degree of saponification of polyvinyl alcohol must be determined.

Due to its fibrous properties, the dissolvable contraceptive tablets constructed in this way are soft and have a significantly large dissolution surface area, unlike dissolvable films, and dissolve in a state in which the fibers gradually become thinner, so they are less likely to be unevenly distributed. It has a high contraceptive effect as there is no risk of leakage to the outside, and it has the advantages of having no psychological resistance for women due to its sticky shape and flexibility in shape, and also has the property of absorbing moisture internally and spreading. Therefore, the contraceptive effect is further increased.

Next, we developed a soluble cotton contraceptive preparation with excellent contraceptive effects and an extremely long duration, which is made by mixing and blending soluble fibers with different saponification degrees, different cross-sectional areas and cross-sectional shapes, and containing multiple types of spermicidal contraceptives. I will explain about it.

The above-mentioned soluble contraceptive preparation consisting only of homogeneous soluble fibers has excellent contraceptive effects and ease of handling, but, like the soluble contraceptive film, it has poor dissolution rate and duration. Since they are in an inversely proportional relationship, there is a contradiction and drawback that increasing the initial contraceptive effect shortens the duration, and increasing the duration reduces the initial contraceptive effect. Therefore, in order to obtain a sufficient contraceptive effect, it is necessary to increase the initial concentration of the contraceptive dissolved and to design the subsequent concentration so that it remains constant over time at a predetermined level. In the present invention, this is accomplished by blending contraceptive-containing dissolving fibers with different dissolution rates. For example, if you blend a fiber with a short duration but a very high dissolution rate and a fiber with a slow dissolution rate but a long duration, the initial contraceptive concentration will increase at once because the former dissolves in a short time. The latter then dissolves slowly, resulting in a long-lasting contraceptive effect. Furthermore, by blending fibers with several types of dissolution rates at a constant ratio, it is possible to increase the initial concentration of the contraceptive and to keep the subsequent 0 degree of dissolution constant over time.

Here, the dissolution rate can be adjusted by the degree of saponification, the radius or peripheral length of the fibers, the cross-sectional shape, etc.

The dissolution rate of polyvinyl alcohol can be adjusted by the degree of saponification. In the range of saponification degree of 88 to 95, the lower the saponification degree, the higher the solubility, so it is possible to blend them in combinations such as saponification degrees of 87 and 90°93, for example.

Saponification degrees of 70 to 88 are still useful, although their properties are not simple. For other water-soluble polymers, a different solubility ratio 7.
Adjust with the lid.

In addition, when the soluble fiber has a circular cross section, the relationship between the radius r of the fiber and the dissolution rate V is as follows: where L is the average length of the fiber, n is the number of fibers, and P is the density of the fiber, ■ is the diameter of the fiber. As the total volume, the total weight W of the fiber is W-ρv=nπρrL If S is the total surface area of the fiber, k (K, T) is the degree of saponification, and the surface heat treatment temperature T is the dissolution rate constant, then Therefore, the dissolution rate per unit weight is inversely proportional to r.

Furthermore, if the cross-sectional shape of the soluble fiber is not circular, where S is the cross-sectional area of the fiber and l is the cross-sectional perimeter of the fiber, 1 v = k (K, T) - · - S, and the per unit weight is The dissolution rate is proportional to the cross-sectional perimeter per unit cross-sectional area. Therefore, in the case of a circular cross-section, it depends on the radius of the fiber, and in the case of a non-circular cross-section,
The perimeter per unit area allows for a high resolution rate for the membrane.

In addition, the dissolution curve and duration of the circular cross-section soluble fiber in a state where the solubility is maintained constant are calculated from the above-mentioned formula for the circular cross-section and the dissolution rate definition formula W ``'''dt. With weight and τ as duration, w=w −a=t+ ' t2 0 0 4 f = −JW ex = 2k(K,T)7:α 0
ρ, and it becomes a positive parabola with a minimum at the duration point.

Since all of the eluted components do not flow out, the actual dissolution curve becomes a gentle curve except for the initial dissolution, and the duration is much longer than τ.

This makes it convenient for membrane applications in which fibers with different dissolution rates are blended to increase the initial contraceptive concentration while keeping the subsequent dissolution concentration essentially constant. This indicates that the preparation has superior properties.

An example of a blend is a cotton formulation made by blending soluble fibers containing spermicidal contraceptives with a saponification degree of 88 and fiber diameters of 10 microns, 50 microns, and 80 microns, and a saponification degree of 93 and a fiber diameter of 120 microns. If it is possible, it is also possible to standardize the diameter of the fibers to about 60 microns, and have a saponification degree of 88 and a cross-sectional perimeter of 9 per unit cross-sectional area that is 5 times that of a circular cross-section, and a saponification degree of 90 and a unit cross-sectional area. A cotton formulation can also be prepared by blending products whose cross-sectional circumference is 1, 2, or 4 times that of a circular cross-section. Here, the cross-sectional peripheral length can be adjusted by configuring the cross-sectional shape to be oval as shown in FIG.

Alternatively, instead of increasing the surface area by increasing the cross-sectional circumference, the cross-sectional shape of the fibers, such as a scaly shape, can be varied in the axial direction as shown in (C) in Figure 2 to increase the surface area and increase the dissolution rate. It is also good to raise it. Even if the fibers are waved like curly hair, the soft feel will be increased.

Furthermore, as shown in Figure 2(d), if soluble fibers containing spermicidal contraceptives are coated with water-soluble polymeric materials containing spermicidal contraceptives with different dissolution rates, the result will be equivalent to a blend. You can expect good results. The coating may also be multi-layered.

Next, if a soluble contraceptive agent is made by blending multiple types of soluble fibers containing spermicidal contraceptives with different spermicidal action sites or other substances with spermicidal contraceptive effects, Since the sperm is attacked from multiple directions, the contraceptive effect is even more reliable. The point of action may change over time, and one fiber may still contain multiple contraceptives.

Furthermore, to prevent bacterial infection and mask body odor,
If necessary, it is also possible to add additional functions according to each purpose, such as by blending fibers containing disinfectants or fragrances.

It has a lot of properties and can be made into any shape.

If the Kotton formulation is compressed into a film as shown in Figure 3(e), it will have the same properties as a film formulation, but at the same time, it will have a large dissolution surface area, which is a characteristic of textile agents, and will have less uneven distribution and leakage to the outside. , a film-like cotton formulation with properties that allows for blending and design over time can be created.

Glue the Kotton preparation into an oval shape as shown in Figure 3(f),
If the product is molded in the fall, it will yield a solid formulation that has a much softer and gentler image than a film-type product and is less psychologically resistant to women.

The cotton formulation can also be formed into a spherical shape as shown in FIG. 3(g). This has excellent insertability and has little psychological resistance.

If the tampon preparation is formed into a tampon shape as shown in FIG. 3(h), it will be easier to insert and will be handled more naturally.

In addition, if the cotton preparation is made into a hollow tampon shape as shown in Figure 3 (i), the sperm will tend to gather in the center, so the B I
An increase in the T effect can be expected.

In this way, dissolvable contraceptive tablets/preparations have the property of spreading internally due to their fibrous or tablet-like nature, are less unevenly distributed and leak to the outside, and have various dissolution rates,
Since the shape and the fiber containing the spermicidal contraceptive can be blended, the initial contraceptive effect is increased, and the subsequent pregnancy effect can be sustained for a long time, so it has excellent contraceptive effect and is rich in shape flexibility. In addition, it is a soluble contraceptive with excellent functional properties because it is soft and has little psychological resistance when used, and can be blended with fibers containing fragrances and bactericides.

[Brief explanation of the drawing]

FIG. 1 is an explanatory diagram of the principle of the fluidized fall method. Figures 2 (,) to (d) are examples of the shape of dissolved fibers, Figure 3 (,)
) to (i) are examples of shapes of cotton formulations. 1. Stock solution reservoir, 2. Opening nozzle. 3. Heating device for increasing temperature, 4. Blower fan. 5. Heating device for drying, 6. Wind plate. 7. Forming roller, 8. Heating device for heat treatment. 9... Cutter, 10... Receiving box, 11... undiluted solution flow. 12... Molded fiber, 13... Short fiber. 14...Cotton formulation.

Claims (1)

[Scope of Claims] 1.) A soluble cotton preparation for contraception, which is formed into a desired shape by assembling soluble fibers made of a water-soluble polymeric substance containing a spermicidal contraceptive into a cotton shape. 2.) The soluble fiber is formed by flowing and dropping a water-soluble polymer liquid material containing a spermicidal contraceptive from an open nozzle, and drying and hardening it with a heating device midway through the process. Dissolved contraceptive preparation as described. 3.) Patent claim R11j Encircle--, in which the soluble fibers containing a plurality of spermicidal contraceptives having different dissolution rates are produced from the water-soluble polymeric substances having different solubility, and the fibers are aggregated in a cluster shape. A soluble contraceptive preparation as described in Section 1. 4) The soluble cotton preparation for contraception according to claim 1, wherein the soluble fibers containing a plurality of types of spermicidal contraceptives having different cross-sectional areas are aggregated in a cotton shape. 5.) The soluble cotton preparation for contraception according to claim 1, wherein the soluble fibers containing a spermicidal contraceptive agent having a plurality of types of different unit cross-sectional areas and circumferential lengths are assembled in a cotton shape. 6.) The soluble cotton preparation for contraception according to claim 1, wherein the cross-sectional shape of the soluble fibers is varied in the axial direction. 7) The soluble cotton preparation for contraception according to claim 1, wherein the soluble fiber is coated with a water-soluble polymeric material containing a spermicidal contraceptive and having different dissolution rates. 8.) The soluble cotton preparation for contraception according to claim 1, which is formed by collecting the soluble fibers containing a plurality of different spermicidal contraceptives in a cotton shape. 9) The soluble cotton preparation for contraception according to claim 1, which comprises a soluble fiber containing a bactericide mixed with the fiber. 10.) The soluble cotton preparation for contraception according to claim 1, which comprises a fragrance-containing soluble fiber mixed with the fiber. 11.) The soluble cotton preparation for contraception according to claim 1, wherein the cotton preparation is compressed into a film. 12.) The soluble cotton preparation for contraception according to claim 1, characterized in that the cotton preparation is shaped into a shoe-like shape. 13) The soluble cotton preparation for contraception according to claim 1, characterized in that the curved cotton preparation is formed into a spherical shape. 14) The soluble cotton preparation for contraception according to claim 1, wherein the cotton preparation is shaped like a tampon. 15.) The soluble cotton preparation for contraception according to claim 1, characterized in that the cotton preparation is shaped like a hollow tampon.