JPS62242616A - Pharmaceutical preparation containing loxoprofen sodium - Google Patents

Abstract

PURPOSE:A pharmaceutical preparation containing loxoprofen sodium that contains additives so that the total water absorption reaches a specific value, thus preventing the adhesion of the drug to the vessel or between drug each other resulting in blocking whereby the prescription limitation can be kept wide and the preparation is kept good in the quality. CONSTITUTION:Additives are used so that the total water absorption reaches 1.7 or more, preferably 2.0 or more. The additives may be anything, as long as they keep the properties as the drug and are, e.g., dextrin, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, amicol, a variety of ion-exchange resins, etc. Although a better preparation is obtained, as the particle size of loxoprofen sodium becomes smaller in spite of low total water absorption, 1.7 or higher value is required at the lowest.

Description

[Detailed Description of the Invention] [Object of the Invention] Loxoprofen sodium (chemical name: 2-(4-(2-oxocyclopentan-1-ylmethyl)phenyl)furopionic acid sodium salt, which is an analgesic, anti-inflammatory, and antipyretic agent) ) has strong adhesion to equipment and containers.Therefore, it is difficult to formulate a drug unless special consideration is given to this fact, and even if it can be formed into a drug, it will not have the appropriate characteristics as a drug. It is not possible to create a formulation with

Conventionally, as remedies for this kind of adhesive drug, there have been prescriptions such as using a large amount of a lubricant such as magnesium stearate, or coating the drug particles with drug particles. However, when the former is applied to loxoprofe/sodium, the disintegration, dissolution, and bioavailability (bioavailability) of the preparation are
f; When it is made into a tablet, its hardness is significantly reduced. However, when applied to loxoglophene sodium, the latter results in the use of solvents, long and complicated processes, associated high formulation costs, and a decrease in bioavailability depending on the coating agent used. Of course, there are some drawbacks.

The present inventors conducted various studies on reducing the adhesion of loxoprofen sodium, and as a result, they decided to incorporate an additive into the loxoprofen sodium-containing formulation, which has a total water absorption capacity of more than a certain value. Is it possible to effectively prevent the difficulties that occur when manufacturing drugs, such as adhesion of drugs to machines during tabletting or capsule filling, adhesion of drugs to containers, and blocking caused by adhesion of drugs to each other? They discovered this and completed the present invention.

The formulation of the present invention is not only industrially advantageous compared to conventional formulations, but also has a wide range of formulations to choose from in terms of formulation quality, and therefore has the advantage of being able to be formulated without compromising quality. .

[Structure of the invention]

The present invention is an additive that has a total water absorption capacity of 1.7 or more, preferably 2.0 or more. Lokin Profue made by combining /
- Concerning sodium-containing preparations.

Here, the water absorption capacity of the n types of additives of the present invention is given by the following formula.

Total water absorption capacity = Σm, a1/m. (1) 1=1 m: Loxoprofen sodium (as anhydride)
Prescribed amount [111: Prescribed amount of additive 1 al: Weight of water that a unit weight of additive 1 can contain in an "appropriate kneading state" Here, "an appropriate kneading state" means "wet production" Funicular
The condition is below the plastic limit. Experimentally, the following situation is known. That is, generally, a powder sample is placed in a mortar, water is added to it, and the pestle is placed. If the amount of water added is small, the mixture will become dry, or as the amount of water added increases, it will become sticky.

In the present invention, the "appropriate kneading state" refers to a state before transitioning to a sticky state, which is a state where the kneading tool can hold its shape by itself when grasped with hands, and has a slightly firm texture. say.

The al values of examples of additives that can be used in the present invention are calculated as follows.

That is, microcrystalline cellulose: 1.0. Low substituted hydroxypropyl cellulose: 2. O, amorphous silicic anhydride: 1.
O, corn starch: 0.6, powdered lactose (particle size approximately 12 μ): 0.18, hydroxyglobil starch =
0.5, algin@: 1.5, calgeximethylcellulose: 2.0. Calgeximethyl cellulose calcium: 2.0. Magnesium stearate: almost negligible value.

The additives that can be used in the present invention are not particularly limited as long as they do not completely impair the properties of the drug; for example, in addition to the above, dextrin, hydroxypropyl cellulose,
Examples include hydroxyglobil methylcellulose, hydroxyethylcellulose, methylcellulose, amicol, flurane, mannitol, white sugar, starches, cyclodextrifs, polyvinylpyrrolidone, polyvinyl alcohol, and various ion exchange resins.

Note that as the particle size of loxoprofen sodium becomes smaller, a good preparation tends to be obtained even if the value of total water absorption capacity is small, but a total water absorption capacity of at least 1.7 is required.

The present invention is applicable to all solid preparations such as tablets, capsules, granules, and powders.

There are no particular limitations on the method for producing the preparation, and any known means such as dry mixing or wet mixing can be used.

〔Effect of the invention〕

Next, the present invention will be explained in more detail with reference to Example t, but the present invention is not limited thereto.

Example 1 (1) Preparation method The preparation of Example 1 was prepared as follows.

According to the recipe in Table 1 below, Loquindero 7ene sodium, microcrystalline cellulose, lactose, and low-substituted hydroxypropyl cellulose are mixed in a mortar, then an appropriate amount of water is added and kneaded, and the mixture is aerated. It was dried in a mold dryer at 60°C for 60 minutes. The dried product was sieved through a T-30 mesh sieve, and then magnesium stearate was added thereto and mixed for 10 minutes in a vffi mixer.

The resulting mixture was compressed into tablets using a flat scale with a diameter of 7.5 u.

Note that the formulation of Control Example 1 was also produced in the same manner.

Table 1 Parts: Parts by weight.

(2) Results The formulation of Example 1 could be compressed into tablets, but the formulation of Control Example 1 "sticked" to the punch and could not be compressed into tablets.

implementation? ! l 2 work 3 (1) Preparation method Example 2 The preparation 3 was manufactured as follows.

After mixing each component except magnesium stearate in a mortar according to the recipe in Table 2 below, the mixed rice was put into a dry grinder atomizer (Sample Mill manufactured by Fuji Denki ■) and φ
=1 Dragon screen gold was attached and pulverized and mixed. Magnesium stearate was added to the resulting pulverized product and mixed for 15 minutes using a ■ type mixer. The resulting mixture was filled into two capsules in a capsule filling machine (Hozliger, type GKF 700).

Note that the formulation of Control Example 2 was also produced in the same manner.

Table 2 Part=! Parts by weight are shown.

(2) Results The formulations of Examples 2 and 3 could be filled, but the formulation of Comparative Example 2 could not be filled because the powder stuck to the spindle of the rotating optical structure and there was a risk of damage to the filling machine. .

Claims (1)

[Claims] A preparation containing loxoprofen and sodium, characterized in that it contains additives so that the total water absorption capacity is 1.7 or more.