JPS6314716A - Sustained release suppository - Google Patents

Abstract

PURPOSE:A sustained release suppository gradually releasing a drug to digestive tubes and keeping medicinal effects for a long period, obtained by blending a high-melting suppository base with hydrogenated lecithin. CONSTITUTION:100pts.wt. high-melting suppository base having 40-45 deg.C melting point is blended with >=5pts.wt. hydrogenated lecithin. Prolongation can be regulated by properly selecting the amount of the hydrogenated lecithin blended, can suppress rapid rise in drug concentration in blood after suppository administration and prevent side effects caused by drug. An anti-inflammatory analgesic is especially preferable as the suppository used.

Description

[Detailed Description of the Invention] [Field of Industrial Application] The present invention relates to a long-lasting suppository, and more specifically, to a long-lasting suppository characterized by containing hydrogenated lecithin. By compounding, the release of the drug from the suppository is controlled.

[Conventional technology]

There is a growing demand for the development of long-acting preparations, especially long-acting anti-inflammatory and analgesic preparations, as the population ages. In an aging society, there is an increasing need for drugs to treat rheumatism, as well as drugs to treat circulatory system disorders and mental disorders. Treatment for rheumatism generally takes a long time, and insomnia caused by pain often causes mental stress, leading to anxiety in social life. Many anti-inflammatory analgesics have been developed for this purpose, but most of them have excellent absorption in the gastrointestinal tract, are rapidly eluted after administration, and are quickly transferred into the body.

[Problem that the invention seeks to solve]

Although many drug preparations have excellent gastrointestinal absorption, they have the following drawbacks.

■ Occurrence of side effects due to markedly high blood drug concentration in the early period after administration.

■ Drugs that disappear quickly from the blood have a short effective time.

Therefore, there is a strong desire for a formulation that can control the release of the drug from the formulation, prevent the initial high blood concentration, and exhibit sustained drug release.

In other words, there is a need for a preparation that is useful in preventing the complication of repeated administration of the preparation and at the same time providing a sound sleep without requiring nighttime administration.

[Means for solving problems]

The present inventors have completed the present invention as a result of intensive research to improve the drawbacks of conventional suppositories as described above.

That is, the present invention involves hydrogenation of a high melting point suppository base.

The present invention provides a long-lasting suppository characterized by containing lecithin.

The hydrogenated lecithin used in the present invention is a phospholipid derived from egg yolk or plants.

The purpose of the long-acting suppository of the present invention is to delay the disintegration or dispersion of the preparation and slow down the release of the drug.
It is necessary to use a base with a high melting point (a base with a low melting point will cause rapid disintegration of the preparation).

The composition of the suppository base is not particularly limited, but it is necessary to use one with a high melting point of 40°C to 45°C.

Depending on the amount of hydrogenated lecithin added, it can be used even if the temperature is 45°C or higher.

The long-acting suppository of the present invention uses a base with a high melting point, and the base alone does not melt in the gastrointestinal tract and prevents drug release.
By incorporating hydrogenated lecithin, water channels are formed within the formulation matrix by utilizing the water-swelling properties of hydrogenated lecithin, thereby controlling the elution of the drug.

Therefore, the amount of hydrogenated lecithin to be blended needs to be adjusted appropriately depending on the ingredients of the suppository base and the drug to be blended, but it is preferably blended in an amount of 5 parts by weight or more per 100 weight parts of the suppository.

The drug used in the long-acting suppository of the present invention may be any antibiotic, anticancer drug, antipyretic, etc., but in particular, indomethacin, diclofenac sodium, ibuprofen, aspirin, quinolidine hydrochloride, thiaramide hydrochloride, ketoprofen, sodium salicylate, Anti-inflammatory analgesics such as sulpirin, phenylbutacin, flufenamic acid, aminopyrine, and mevirizole are effective.

〔Effect of the invention〕

Since the suppository composition of the present invention can gradually release the drug into the gastrointestinal tract, it can maintain its drug efficacy for a long time. Further, by appropriately selecting the blending amount of hydrogenated lecithin, the sustainability can be adjusted.

Therefore, by suppressing the rapid increase in blood drug concentration after suppository administration,
It is possible to prevent the occurrence of side effects caused by drugs. Furthermore, because the effect lasts, the drug's efficacy does not wear off during sleep, ensuring a sound sleep and eliminating anxiety and pain for patients.

〔Example〕

EXAMPLES Hereinafter, the present invention will be explained in more detail with reference to Examples, but the present invention is not limited to these Examples.

Example 1 Suppository base (Witepsol E-85 (
Guina □Mitsuto Nobel product name), mp40
℃ or higher) and hydrogenated lecithin (iodine value 10).
After dissolving diclofenac sodium (Iliclo
fenacNa) was dispersed in a suspended state and then molded to prepare a long-lasting suppository of the present invention having the composition shown in Table 1. For comparison, suppositories containing no hydrogenated lecithin were also prepared.

Table 1 Example 2 In the same manner as in Example 1, suppositories having the composition shown in Table 2 were prepared.

Table 2 1] Example 3 In the same manner as in Example 1, suppositories having the composition shown in Table 3 were prepared.

Table 3 Example 4 In the same manner as in Example 1, suppositories having the compositions shown in Table 4 were prepared.

Table 4 Note) *1: Product name manufactured by Dynamite Nobel Co., Ltd. Example 5 Suppositories having the composition shown in Table 5 were prepared in the same manner as in Example 1.

Table 5 Experimental Example 1 The suppository release tester (
A dissolution test was conducted using Toyama Sangyo Co., Ltd.).

The results are shown in Figures 1-5.

As shown in Figures 1 to 5, the product of the present invention had a sustained effect. And the higher the hydrogenated lecithin content, the faster the elution.
The elution rate can be controlled by selecting the lecithin content depending on the purpose. In this case, it is necessary to select the lecithin content depending on the solubility of the main drug. For drugs with low solubility, the amount of lecithin is increased, and for drugs with high solubility, the amount of lecithin is decreased.

[Brief explanation of drawings]

FIGS. 1 to 5 are graphs showing the dissolution test results of the suppositories obtained in Examples 1 to 5, respectively.

Claims (1)

[Claims] 1. A long-lasting suppository characterized by blending hydrogenated lecithin with a high melting point suppository base.