KR100904165B1 - Dispersible acetaminophen tablet and manufacturing process thereof - Google Patents

Abstract

The present invention relates to an acetaminophen suspension tablet for children and a method for preparing the same, which are easy to take and store, and improve the bitter taste using functional sugars of acetaminophen, which is used most often as an antipyretic and analgesic agent for children, to prepare it as a suspension tablet. This provides a formulation that is easier to take and easier to store than conventional acetaminophen children's tablets or syrups.

Acetaminophen, suspension tablets, powder coating, improvement of taste

Description

Acetaminophen suspension tablet and manufacturing method thereof

The present invention relates to an acetaminophen suspension tablet for children and a preparation method thereof, which is easy to take and store, and improves the bitter taste of acetaminophen, which is most used as an antipyretic and analgesic agent for children, by using functional sugars and appropriate disintegrating agent. By adding to prepare a suspension tablet, it is intended to provide a formulation that is easier to take and easier to store than conventional acetaminophen children's tablets or syrups.

Acetaminophen, also known as paracetamol, is the most widely used drug worldwide as an antipyretic analgesic for adults as well as children. Representative products include Janssen's TYRENOL series. Tablets include 80mg, 160mg, 325mg, 500mg and 650mg sustained-release formulations, depending on the acetaminophen-containing dosage, and also children's syrup. In particular, infants who do not have the ability to take tablets, acetaminophen tablets are pulverized and taken in the form of powder, and other than that, they are taken as syrup, and are widely used as home medicines as well as prescription drugs. However, acetaminophen has a very strong taste due to the nature of the taste, and in the case of tablets, it is manufactured using a raw material shielded with a bitter gourd. However, in the case of infants and pediatric patients, the tablets are crushed and taken, and the chyme shielding effect is lost through the grinding process, which is difficult for the infants and pediatric patients to take. In addition, in the case of syrup, sweeteners were used to reduce bitterness, but the storage and portability of the syrup are not easy.

SUMMARY OF THE INVENTION An object of the present invention is to provide an acetaminophen suspension tablet that is easily stored and portable at the same time, effectively improving the convenience of acetaminophen by enhancing the convenience of dosing.

Acetaminophen suspension tablet of the present invention has the advantage that the taste of acetaminophen can be effectively improved by using functional sugars, and at the same time, it can be suspended and taken quickly by adding an appropriate disintegrant. As a result, the medication compliance and storage of drugs in infants and pediatric patients has the advantage that it is significantly improved.

According to a preferred embodiment of the present invention, 46 to 58.5 weight percent of acetaminophen, 10.2 to 18 weight percent of functional sugars, 31 to 35 weight percent of disintegrant, and 0.3 to 1.0 weight percent of lubricant, based on the total weight of acetaminophen-containing suspension tablet An acetaminophen containing suspension tablet composition may be provided.

According to another suitable embodiment of the present invention, the functional saccharide is preferably sucralose.

According to another suitable embodiment of the invention, the disintegrant is preferably F-MELT.

According to another suitable embodiment of the present invention, the content of acetaminophen is 80 mg or 160 mg per tablet.

EMBODIMENT OF THE INVENTION Hereinafter, this invention is demonstrated in detail.

The acetaminophen suspension tablet formulations of the present invention are highly purified by mixing acetaminophen, sucralose as a functional saccharide for improving the taste of acetaminophen, F-MELT as a disintegrant to achieve a rapid suspension process, and glidants. Manufactured through a simple process.

The acetaminophen suspension tablet formulation of the present invention is composed of 46-58.5 wt% of acetaminophen, 10.2-18 wt% of sucralose, 31-35 wt% of F-MELT, and 0.3-1.0 wt% of a lubricant, based on the total weight of the preparation. .

Sucralose (Samyang Genex Co., Ltd., Korea) used as a bitter improver is a sweetener that is about 400 times sweeter than sugar and is completely harmless to the human body. Enable to provide The present invention may also use flavoring agents in conjunction with bitter improvers. The flavourant can be adjusted within the content range of the flavourant.

In addition, F-MELT (Fuji Chemical Co., Japan) used as a disintegrant can achieve rapid disintegration of tablets in water to prepare a rapid suspension, and at the same time, the tablet formulation is also very excellent in quality acetaminophen. Allow to provide suspension tablets. F-MELT is an excipient consisting of D-mannitol, xylitol, microcrystalline cellulose, crospovidone, dicalcium phosphate (Calcium Phosphate, Dibasic), and in the case of the present invention, F-MELT Type C Can be preferably used.

[Table 1] Composition of F-MELT Type C

Furtherance range Pharmacopoeia D-mannitol 50-66% USP-NF / EP / JP Xylitol 2-10% USP-NF / EP / JP Microcrystalline cellulose 10-20% USP-NF / EP / JP Crospovidone 5-9% USP-NF / EP / JP Calcium Phosphate, Dibasic 2-9% USP-NF / EP / JP

In the following the invention is illustrated by the following examples. However, the present invention is not limited to these examples.

Example

Example 1

Preparation of Acetaminophen 80mg Suspension Tablet

To 800 g of acetaminophen, 200 g of sucralose, 590 g of F-MELT, 100 g of strawberry micron and 10 g of magnesium stearate were added and mixed uniformly, followed by tableting at a mass of 170 mg per tablet to prepare a suspension tablet containing acetaminophen 80 mg.

Raw material name Usage per tablet (mg) weight% Acetaminophen 80.0 47.06 Sucralose 20.0 11.76 F-MELT 59.0 34.71 Strawberry Micron 10.0 5.88 Magnesium stearate 1.0 0.59 system 170.0 100.00

Example 2

Preparation of Acetaminophen 160mg Suspension Tablet

Sucrose 300g, F-MELT 890g, and magnesium stearate 10g were uniformly mixed with 1600g of acetaminophen, and then, tableted at a mass of 280mg per tablet to prepare 160mg of acetaminophen.

Raw material name Usage per tablet (mg) weight% Acetaminophen 160.0 57.14 Sucralose 30.0 10.71 F-MELT 89.0 31.79 Magnesium stearate 1.0 0.36 system 280.0 100.00

Comparative Example 1

Acetaminophen 80mg Regular Tablet

500 g of acetaminophen was uniformly mixed with 500 g of straight sugar lactose, 3400 g of microcrystalline cellulose, 50 g of sodium starch glycolate, and 10 g of magnesium stearate, followed by compression to a mass of 170 mg per tablet to prepare 80 mg of acetaminophen.

Raw material name Usage per tablet (mg) weight% Acetaminophen 80.0 47.06 Direct lactose 50.0 29.41 Microcrystalline cellulose 34.0 20.00 Sodium starch glycolate 5.0 2.94 Magnesium stearate 1.00 0.59 system 170.0 100.00

Comparative Example 2

Tylenol Tablets for Children 80mg (Jansen Co., Ltd.)

Comparative Example 3

Tylenol tablets 160mg (Korea Janssen Co., Ltd.)

Taste improvement and disintegration performance of acetaminophen suspension tablets prepared according to the present invention were evaluated as follows. The results are shown in Table 1 and Table 2.

Experimental Example 1

In order to measure the degree of rapidity of suspension of acetaminophen suspension tablets, suspension tests were performed in 5 ml of purified water, the capacity of about a tablespoon for children.

Test formulation Suspension time (complete disintegration time in 5ml purified water) Example 1 Suspension Tablet 20 seconds Example 2 Suspension Tablet 23 seconds

Acetaminophen formulations according to embodiments of the invention disintegrate and suspend very quickly.

Experimental Example 2

Examples 1 and 2 were suspended in 5 ml of purified water, which is a one-time dose of a children's spoon, to confirm the improvement of acetic aminophene suspension tablets. Compared.

Test Example Bitterness Very write write Write a little Rarely used Write Example 1 Suspension O Example 2 Suspension O Comparative Example 1 Grind Suspension O Comparative Example 2 Grind Suspension O Comparative Example 3 Grind Suspension O

As a result, the taste improvement effect of the acetaminophen suspension tablet of this invention was very excellent.

According to the present invention, by improving the bitter taste of acetaminophen, which is most often used as an antipyretic and analgesic for children by using functional sugars, and preparing it as a suspension tablet by adding a suitable disintegrant, the existing acetaminophen children's tablet or syrup It is possible to provide formulations which are more convenient to take and which are easier to store.

Claims (4)

46 to 58.5 weight percent of acetaminophen, 10.2 to 12 weight percent of sucralose, 31 to 35 weight percent of disintegrant, and 0.3 to 0.6 weight percent of lubricant, based on the total weight of acetaminophen-containing suspension tablet, The disintegrant is 50 to 66% by weight of D-mannitol, 2 to 10% by weight of xylitol, 10 to 20% by weight of microcrystalline cellulose, 5 to 9% by weight of crospovidone and 2 to 9% by weight of dicalcium phosphate Acetaminophen-containing suspension tablet composition, characterized in that the composition comprising a delete delete The acetaminophen-containing suspension tablet composition according to claim 1, wherein the content of acetaminophen is 80 mg or 160 mg per tablet.