Orally rapidly disintegrating tablet, and process for producing same

Abstract

Disclosed is an orally rapidly disintegrating tablet characterized in that the tablet can be produced in a conventional tablet production facility and has a satisfactory level of hardness for practical applications, and the change in properties of the tablet (i.e., decreased in hardness of the tablet, and delay of the time required for disintegration of the tablet in the oral cavity) are rarely caused by factors such as humidity. The orally rapidly disintegrating tablet has hardness of 40 N or more, can be disintegrated in the oral cavity within 60 seconds, and is produced by compression molding of a mixture of (a) an active ingredient, (b) an excipient having good water wettability, (c) a water-insoluble polymer that has good moldability and does not substantially cause the decrease in the water wettability of the excipient and (d) a disintegrating agent.

Description

technical field

[0001] The present invention can be prepared by conventional tablet production equipment, and the present invention relates to a novel orally rapidly disintegrating tablet having practical formulation strength in various steps of preparation, dispensing, and formulation, and having rapid disintegration properties in the oral cavity, and the A preparation method of a novel orally rapidly disintegrating tablet. Background technique

[0002] Generally, orally rapidly disintegrating tablets are highly required during medical procedures in patients suffering from Parkinson's disease, Alzheimer's disease, or dysphagia, and in patients who have difficulty getting up after surgery. At present, a variety of oral rapidly disintegrating tablets including preparations prepared by freeze-drying have been developed and marketed. The research and development of rapidly disintegrating tablets has become the mainstream at present.

[0003] Orally rapidly disintegrating tabl...

Examples

experiment example 1

[0083]Excipients (97 parts by weight (or 90 parts by weight)) and water-insoluble A mixture (300 mg) of polymer (hydroxypropylmethylcellulose acetate succinate, HPMC-AS, grade: HF) (3 parts by weight (or 10 parts by weight)) was compression-molded to obtain tablets. The water wettability (wetting time) and hardness of each tablet were measured according to the following evaluation procedure, and based on the measurement results (see Table 1 below), the excipients were divided into the following 2 groups.

[0084] Group A: Excipients with good water wettability and compressibility when the tablet contains water-insoluble polymers, which exhibit tablet wetting times within 300 seconds, and tablet hardness exceeding that of excipients alone. 3 times that of the formulation.

[0085] Group B: Excipients with poor water wettability or compressible formability when the tablet contains a water insoluble polymer, which exhibit a tablet wetting time greater than 300 seconds, and a tab...

experiment example 2

[0094] To a mixture of D-mannitol (97 parts by weight) and various water-insoluble polymers (3 parts by weight) was added 80% (W / W) aqueous ethanol (5 parts by weight). The mixture was kneaded in a stainless steel container, then granulated with a No. 22 mesh sieve described in the Japanese Pharmacopoeia, and the resulting granules were dried in a ventilated box type drier at 50° C. for 2 hours to obtain granulated granules. The granulated granules (300 mg) were compression-molded (flat punch: 10 mm in diameter, tableting pressure: 1000 kg / punch) using a tableting analyzer (manufactured by Kikusui Seisakusho Co., Ltd.) to obtain tablets. The water wettability (wetting time) and hardness of each tablet were measured in accordance with the evaluation procedure in Experimental Example 1. Based on the measurement results (Table 2 below), the water-insoluble polymers are divided into the following 3 groups:

[0095] Group 1: Water-insoluble polymers that do not cause a decrease in...

experiment example 3

[0101] According to Examples 1 to 3 and Comparative Examples 1 to 2, tablets were prepared using various excipients in Experimental Example 1 and a water-insoluble polymer (HPMC-AS / HF). Tablet hardness was measured according to the evaluation procedure in Experimental Example 1. The disintegration time of the tablet in the oral cavity was measured by the following method.

[0102] Disintegration time of the tablet in the mouth:

[0103] Put one tablet in each mouth of three healthy adult males, and measure the time when the tablet is completely disintegrated with saliva when gently put in the mouth (ie, do not chew or vigorously move the tongue, etc.) to calculate the average value.

[0104] result)

[0105] The hardness of each tablet and the disintegration time of each tablet in the oral cavity are shown in Table 3 below. As can be seen from Table 3, the hardness of each tablet (i.e. the tablets of Examples 1 to 3) made by using the excipients of Group A is greater than 4...

technical field

[0001] The present invention can be prepared by conventional tablet production equipment, and the present invention relates to a novel orally rapidly disintegrating tablet having practical formulation strength in various steps of preparation, dispensing, and formulation, and having rapid disintegration properties in the oral cavity, and the A preparation method of a novel orally rapidly disintegrating tablet. Background technique

[0002] Generally, orally rapidly disintegrating tablets are highly required during medical procedures in patients suffering from Parkinson's disease, Alzheimer's disease, or dysphagia, and in patients who have difficulty getting up after surgery. At present, a variety of oral rapidly disintegrating tablets including preparations prepared by freeze-drying have been developed and marketed. The research and development of rapidly disintegrating tablets has become the mainstream at present.

[0003] Orally rapidly disintegrating tabl...

Examples

experiment example 1

[0083]Excipients (97 parts by weight (or 90 parts by weight)) and water-insoluble A mixture (300 mg) of polymer (hydroxypropylmethylcellulose acetate succinate, HPMC-AS, grade: HF) (3 parts by weight (or 10 parts by weight)) was compression-molded to obtain tablets. The water wettability (wetting time) and hardness of each tablet were measured according to the following evaluation procedure, and based on the measurement results (see Table 1 below), the excipients were divided into the following 2 groups.

[0084] Group A: Excipients with good water wettability and compressibility when the tablet contains water-insoluble polymers, which exhibit tablet wetting times within 300 seconds, and tablet hardness exceeding that of excipients alone. 3 times that of the formulation.

[0085] Group B: Excipients with poor water wettability or compressible formability when the tablet contains a water insoluble polymer, which exhibit a tablet wetting time greater than 300 seconds, and a tab...

experiment example 2

[0094] To a mixture of D-mannitol (97 parts by weight) and various water-insoluble polymers (3 parts by weight) was added 80% (W / W) aqueous ethanol (5 parts by weight). The mixture was kneaded in a stainless steel container, then granulated with a No. 22 mesh sieve described in the Japanese Pharmacopoeia, and the resulting granules were dried in a ventilated box type drier at 50° C. for 2 hours to obtain granulated granules. The granulated granules (300 mg) were compression-molded (flat punch: 10 mm in diameter, tableting pressure: 1000 kg / punch) using a tableting analyzer (manufactured by Kikusui Seisakusho Co., Ltd.) to obtain tablets. The water wettability (wetting time) and hardness of each tablet were measured in accordance with the evaluation procedure in Experimental Example 1. Based on the measurement results (Table 2 below), the water-insoluble polymers are divided into the following 3 groups:

[0095] Group 1: Water-insoluble polymers that do not cause a decrease in...

experiment example 3

[0101] According to Examples 1 to 3 and Comparative Examples 1 to 2, tablets were prepared using various excipients in Experimental Example 1 and a water-insoluble polymer (HPMC-AS / HF). Tablet hardness was measured according to the evaluation procedure in Experimental Example 1. The disintegration time of the tablet in the oral cavity was measured by the following method.

[0102] Disintegration time of the tablet in the mouth:

[0103] Put one tablet in each mouth of three healthy adult males, and measure the time when the tablet is completely disintegrated with saliva when gently put in the mouth (ie, do not chew or vigorously move the tongue, etc.) to calculate the average value.

[0104] result)

[0105] The hardness of each tablet and the disintegration time of each tablet in the oral cavity are shown in Table 3 below. As can be seen from Table 3, the hardness of each tablet (i.e. the tablets of Examples 1 to 3) made by using the excipients of Group A is greater than 4...

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