JPS5965010A - Capsule for oily of fatty suppository - Google Patents

Abstract

PURPOSE:A capsule for oily of fatty suppositories, consisting of a hollow shell, molded from an oily or fatty base material for the suppositories, and capable of filling the hollow part with a drug, and having reduced undesirable change in the base material caused by the mixing with the drug, etc. CONSTITUTION:A capsule for suppositories consisting of a hollow shell, molded from an oily or fatty base material, e.g. cacao butter, and capable of filling the hollow part with a drug 4. Preferably, the above-mentioned hollow shell 1 is constituted of a spindle-, torpedo- or cannonball-shaped body 2 having one opened end and a plug 3 for sealing up the above-mentioned opening. The use of the above-mentioned capsule will not cause the undesirable change in the physical properties of the base material due to the mixing with the drug, and the base material can be easily selected. Furthermore, the capsule has many advantages as follows: The previously mass produced capsules provide the preparation of aimed suppositories only by filling the hollow part with various drugs if necessary, and the drug is not deteriorated by warming, etc.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to a hollow oleaginous planing barrel whose interior can be filled with pharmaceuticals to prepare planing.

Planing has long been used as a method of administering pharmaceuticals, and recently, from the standpoint of post-administration absorption and zero drug metabolism, it has been used not only for local treatment such as the anus, but also for systemic treatment such as analgesics and antibiotics. Throwing the desired medicine! It is also attracting attention as a law.

Currently, the most common types of planing are divided into the following three types, with oil-based planing being the most widely used.

In addition to this, there is water-soluble planing, which is made by adding IXW4 to a water-soluble substance that is solid at room temperature, such as macrogol, similar to oil-based planing, but it has drawbacks such as irritation. 1. As a third type of planing, there is a product called cardiac cabrel made in the same manner as oral soft capsules in which the internal pharmaceutical oil-based solution or oil-based suspension is wrapped in gelatin encapsulation. However, since the capsule of this product is water-soluble L-latin, the chemicals that can be put inside are limited to oil-based ones, oil-based solutions, or oil-14fiiTi fluids, and the rectal insertion site has to resist the force of the anal sphincter muscle. The main reason for this is that the inside is completely filled with no space, that it is difficult due to the manufacturing process to maintain the correct shape when inserted, and that if the L-latin membrane is thickly covered to increase strength, it will not disintegrate in the rectum. There are many restrictions on actual formulation due to the fact that it makes people want to eat it. Furthermore, the surface of the gelatin encapsulation is not slippery and if it absorbs moisture, it is extremely difficult to use.

The oil-based planing currently used is oil-based planing 1j1.
7S! Drug'? ! A mixture of 1 and 1 souvenirs is mixed uniformly, usually ¥8-121, quality 30-40
Il1g11 detective 3...3. ;Eye 11. +1, car 1n
3-iPi! It is shaped like a spindle, a torpedo, or a cannonball.

As the oil-based base material, cacao butter and lauric oil-based natural oils and fats that melt at temperature are generally used, but in recent years, hydrogenated oils and fats that have been hydrogenated to various oils and fats have also been used. It is used. In addition, from the viewpoint of hardness, moldability, etc., appropriate fat acid diglyceride, monoglyceride, etc. are added to these fats and oils f1.

Usually, these oily base materials are heated and melted, and then tZ
*V product at 211W? After uniformly dispersing it as a powder, pour it into a mold, take it out from the cold after cooling, and plan it using the J method! ! 7a has been completed.

The obtained planed material needs to have an appropriate hardness to be inserted into the anus at room temperature, and at the same time it needs to melt at the body temperature inside the anus. The interaction between the base material and the base material is important, and even if the base material alone exhibits appropriate strength and desirable body temperature melting when solidified by cooling, it may not be possible to solidify when combined with a drug. Circumstances change, especially the thawing state of hard melons during production (and subsequent storage).
There may be significant changes during the J process, and the effectiveness of planing cannot be expected.

In order to prevent this, various base materials f1 are blended, (
It becomes necessary to add additives such as other melting agents.

Additionally, when mixing pharmaceuticals with oil-based base materials, if the pharmaceuticals are insoluble, the mixed pharmaceuticals may settle and collect at the tip after being injected into the mold and before solidifying. . In addition, for pharmaceuticals that are dissolved and mixed with the base material over a uniform heating time, crystals of the pharmaceutical may precipitate and grow during planing during storage after manufacture, resulting in embrittlement of the drug product. This may occur.

Furthermore, pharmaceuticals that are decomposed and deactivated by heat cannot be manufactured by the above-mentioned melting method, and another method is also used in which a mixture of an oily base material and a pharmaceutical is compression molded while cold. However, except for certain pharmaceutical products, C is uniformly mixed with an oil-based base material (i). 1
5 Due to the interaction between the drug and the base material (
As a result of 111 studies aimed at providing a planing method that can eliminate the various drawbacks of planing, it was possible to form a hollow shell in advance using only an oil-based base material for planing, and the hollow part of this shell was The present invention has been completed by discovering that the above objects can be achieved by filling the container with pharmaceuticals.

The invention will be explained in detail below with reference to preferred embodiments shown in the drawings.

FIG. 1 is a cross-sectional view of a hollow shell 1 used in the oil-based planing coupler C of the present invention, with one end extending from 1-11. It consists of a bullet-shaped main body 2 and a plug 3 for sealing the opening. The shell main body 2 and the plug 3 may be made of materials conventionally used as oil-based base materials for planing, such as natural oils and fats such as cacao butter and lauric butter, various hydrogenated oils and fats, and (J) These fats and oils can be used with addition of fatty acid diglyceride, 7-glyceride, etc.

In addition, the thickness of the hollow shell should be appropriately selected to have a sufficient hollow volume to fill 1 monme of the drug, and a thickness sufficient to ensure handling and strength of 1 mm for planing. In general, the top of the head should be about 5 mm thick, the sides should be about 1.5 to 2 mm thick, and the hollow part should preferably be filled with about 500 g of powdered medicine of Vi degree. .

In the illustrated example, the shape of the hollow shell is a cannonball shape, but it can also be planed into a spindle shape, torpedo shape, etc. If the shape is frightening, then the shape is! l! It is not limited to 1.

The main body 263 J of the hollow shell body and the σ stopper 3 are made by [Using a mold corresponding to the shape of each bottle, heated and melted oleaginous base material is poured into the mold, and this is cooled and solidified. It can be easily manufactured by removing it from the mold afterwards.

FIG. 2 is a planing cross-sectional view of a lζ sitting capsule manufactured using the oil-based planing capsule of the present invention. , 1-1 parts with stopper 3
It is sealed. Filled medicines can be in any form such as powder, solution or suspension. When sealing, if the surface of the stopper 3 is moistened and melted and then crimped onto the white part of the main body 2, the two will surely come into close contact after cooling.
A3 There is no possibility that the contents will leak out.

By using the oleaginous planing capsule of the present invention as described above, planing can be produced without mixing the base material and the drug, so that undesirable changes in physical properties of the base material due to mixing the drug can be avoided. It never brings. Therefore, regardless of the type of drug, the most suitable oleaginous base material may be selected by considering the melting state of only the oleaginous base material in the rectum. In addition, with regard to changes in strength and melting state during storage, consideration should be given to the product 7゛1 containing only fats and oils as the base material.

Furthermore, if the oil-based planed capsules of the present invention are mass-produced in advance, it is possible to fill them with various pharmaceuticals as needed and make the planed capsules. Since there is no need to apply fJ heating and cooling before filling medicines, it is a great product for heating medicines! 1゛j There is no risk of causing deterioration.

In addition, the oleaginous planing capsule of the present invention is different from the conventional rectal capsule using gelatin, and since it uses an oleaginous base material, it is similar to the oleaginous planing in J:. It can be easily inserted, and the medicines filled inside can be powdered or FB.
Either 'd' or 'd'a may be used, and the drug is filled with the drug as a dilute aqueous solution that dissolves the shell of the base material at room temperature.
It's all about ability. Furthermore, when adding adjuvants to promote absorption from the cardiobiliary mucosa,
Since the auxiliary agent can be incorporated into the drug without being dispersed in the base material, it is more effective than the conventional case in which the auxiliary agent is dispersed in the base material. Also, duration 1
If the powder is filled with a blended pharmaceutical powder that has been added with J and T, it is possible to make the planing process more sustainable.

Hereinafter, examples rFj and reference examples of the present invention will be listed (further explanation will be provided).

Example 1 ゜F) Cocoa butter melted completely at OT was poured into a mold and taken out from a 20" Ct cold 141 sheet mold 15. Shell (main body external height 35 a + m, outer diameter 101 nn +; hollow part height 301 nIn, inner i' (Ir, 5 III
nl: Top thickness 5mm, side thickness 1,75m
m H plug thickness 5 mm) was manufactured.

Reference 1<411.

I-i'i+! 100 m of indomezacin powder was filled into the hollow part of the main body of the hollow shell body subjected to ir:I in Example 1, and 1 part was sealed with a stopper to prepare 1 drug of indomezacin. :a Example 2 Base material obtained by adding fatty acid monoglyrelide to hydrogenated vegetable oil [Litepsol H15J (CI+a+n1Sc)
l+c Werke Witten (product name made in West Germany) was melted at 50°C, poured into a mold, and heated at 20°C.
After cooling to zero, it was removed from the mold to produce a hollow shell having the same shape and dimensions as in Example 1.

Reference Example 2゜Above Example 2'C・1 in the hollow part of the main body of the hollow shell obtained
Squirrel [J Mycin Powder 1! i 0 Hl fill up jshin 1
), then open [1 part with stopper J, and seal (], Ellis IJ
Ishin suppositories were prepared.

Reference Example 3゜In the hollow part of the main body of the 19 hollow shell body obtained in Example 2 above, one drop of the Jili 1fJ solution diluted with 5 times the amount of water was poured into the hollow part of the hollow shell body at 0.5 m, Q filled 1i 1. Later, l1tl l
', '1 part/,,, 1', x for J,, ') is dense 14
Extract suppositories were prepared.

[Brief explanation of the drawing]

FIG. 1 is a cross-sectional view showing a preferred embodiment of the oil-and-fat bamboo planing microphone 1-1 according to the present invention. Fill the pot with medicine and show the planing made by A 'J' l1J
This is a diagram. 1...Hollow shell, 2...Main body, 3...Bung, 4...
・Medical products. Figure 1 Figure 2

Claims (1)

[Scope of Claims] 1. An oil-based planing capler having a hollow shell formed from a planing oil-based base material and having a diameter of 1 hole so that the hollow portion can be filled with pharmaceuticals. 2. The hollow shell has a spindle shape with a frontage at one end, and a torpedo shape J
The oil flit M planing capsule according to claim 1, comprising a shell-shaped main body and a plug for sealing the opening.