JPH04318001A - Processed starch excellent in bindability and disintegrability - Google Patents

Abstract

PURPOSE:To provide a specified processed starch and a pharmaceutical preparation composition prepared therefrom. CONSTITUTION:The objective processed starch excellent in both bindability and disintegrability can be obtained by heating treatment of raw starch in the presence of moisture. The present starch is 8-15wt.% in water content, <10wt.% in cold water solubles and 5-15ml/g in swollen volume. The objective pharmaceutical preparation composition can be obtained by formulation of the present processed starch followed by direct tableting or dry granulation. In contrast to the conventional processed starch, the present starch has a combined function of bindability and disintegrability; therefore, the pharmaceutical preparation of the present invention is high in hardness with promoted disintegration, leading to facilitating its quality design.

Description

[Detailed description of the invention]

0001

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a processed starch with excellent binding and disintegrating properties used in pharmaceuticals, and a pharmaceutical composition containing the processed starch.

0002

[Prior Art] Starches have been widely used as pharmaceutical excipients with binding, disintegrating, and bulking effects due to their ease of availability and the sense of security that comes from the fact that they are natural products and have been used for a long time. Ta. Starches are divided into three types: raw starch, physically modified starch, and chemically modified modified starch. Among these, modified starch has various physicochemical properties that can be expressed by changing the degree of gelatinization, is low in price, and is chemically the same as raw starch, so it has a high reactivity with drugs. It is widely used because there are almost no Suspending raw starch in water and heating it until it boils to make starch paste, which is used as a binder for wet granulation, is the oldest use of modified starch, but there are many other uses as well. Modified starches have been proposed.

[0003] The processed starch described in Japanese Patent Publication No. 46-21471 is obtained by compacting and drying raw starch with a moisture content of about 20 to 50% by weight using a differential roll mill or the like at a temperature of 20 to 50°C. , obtained by crushing
It is soluble in cold water in the range of about 4-40% by weight, its dry substance swelling power is based on about 2.5-12, the free density is about 0.5-0.7 g/ml, and the water is about 9-16% based on the total weight.

[0004] The processed starch described in Japanese Patent Publication No. 59-47600 is made by turning raw starch into a slurry and heating it at a temperature of 50°C or higher and about 10°C higher than the gelatinization initiation temperature. It is obtained by swelling the outer thin film structure of starch without destroying it and then drying it, and the bulk density is 0.25 g/cc or more, the cold water soluble content is less than 10% by weight, and the swelling volume is Approximately 3-15ml/g,
Water retention capacity is about 2 or more.

[0005] The processed starch described in JP-A-58-32828 is obtained by gelatinizing raw starch, cooling it, and then drying it, and has a degree of swelling of 3.0 to 6.0. . The modified starch described in JP-A-60-233019 is derived from cold water-soluble granular starch obtained by treating starch with acid, alkali, and/or α-amylase enzyme at a temperature below the gelatinization temperature. It is something.

[0006] Also, commercially available products include Starch 1500 (manufactured by Nippon Colorcon Co., Ltd.) and PCS (manufactured by Asahi Kasei Industries, Ltd.).
There are partially pregelatinized starches such as

[0007]

[Problem to be solved by the invention] However,
The modified starch described in Japanese Patent No. 21471 has excellent binding properties when formed into tablets by direct compression, but lacks the ability to disintegrate tablets in water. In addition, special public service 59-4
The modified starches described in JP-A No. 7600 and JP-A No. 58-32828 have excellent disintegration properties when incorporated into tablets, granules, and capsules, but have poor binding properties when used in direct tabletting methods. Due to its poor properties, it cannot be added in large quantities.
In addition, it was necessary to use other binders in combination. In addition, the modified starch described in JP-A No. 60-233019 is effective as a binder for tablets used in direct compression method or dry granule compression method, but the disintegration properties of tablets are affected, especially when manufactured under high compression pressure. This had the disadvantage of impairing the disintegration of tablets when they were made into tablets. Regarding commercially available products, Starch 1500 exhibits binding properties when used in the direct compression method, but has the drawback of slowing down the tablet disintegration time. Furthermore, when PCS is incorporated into tablets and granules, it exhibits the best disintegration properties among processed starches, but it has almost no function as a binder for direct tablet compression.

[0008] As mentioned above, conventionally processed starch
When used in the direct compression method or dry granulation method, there is no starch that satisfies the functions of binding and disintegrating properties at the same time, and a modified starch that has both functions has been desired.

[0009]

[Means and effects for solving the problem] As a result of intensive studies, the present inventor has discovered that raw starch is obtained by heating raw starch in the presence of water, has a water content of 8 to 15%, and has a cold water soluble content. It has been found that a modified starch with a swelling volume of less than 10% and a swelling volume of 5 to 15 ml/g has both binding and disintegrating functions when used in a direct compression method or a dry granule compression method,
This led to the present invention.

[0010] That is, the present invention provides raw starch in the presence of water.
A modified starch obtained by heat treatment, which has a water content of 8 to 15%, a cold water soluble content of less than 10%, and a swelling volume of 5 to 15 ml/g, which has excellent binding properties and disintegration properties. and a pharmaceutical composition containing the processed starch. The processed starch of the present invention has a specified water content, cold water soluble content, swelling volume, and excellent binding properties, so the powder or granules can be compressed into tablets using a direct compression method or a dry granule compression method. In some cases, tablets with high hardness can be obtained. In addition, when granules are made using a dry granulation method, granules with high strength and less pulverization can be produced. At the same time, it also has excellent disintegration properties, so when a preparation containing the processed starch is administered into the body, the processed starch absorbs water and swells, resulting in rapid disintegration and drug elution. do. In addition, compared to other binders such as crystalline cellulose and lactose, it has good disintegration properties, has high stability against drugs, and has both binding and disintegration functions, making formulations simple. This has the advantage of making it easier.

The present invention will be explained in detail below. The processed starch referred to in the present invention is obtained by heat-treating raw starch in the presence of moisture, and has a moisture content of 8 to 1.
5%, preferably 10-15%, cold water soluble content less than 10%, preferably less than 5%, swelling volume 5-15 ml/g
, preferably 5 to 11 ml/g. Also preferably, the bulk density is 0.35 to 0.65 g
/ml, particularly preferably 0.4-0.6g/ml, 10
The 0 mesh (opening 150 μm) fraction is 50% or less, particularly preferably 30% or less.

[0012] The term "modified starch" as used herein refers to starch obtained by heat treatment in the presence of moisture and drying, and does not include starch that has been chemically modified. Further, when the processed starch of the present invention is placed in water and observed under a microscope, most of the particles, although swollen, maintain their starch particle morphology, and individual particles can be identified. Non-birefringent starch in which the individual particles are destroyed to the extent that they cannot be identified increases the cold water soluble content, which is undesirable as described below. Furthermore, when observed with a polarizing microscope, there are more particles exhibiting non-birefringence than particles exhibiting birefringence.

[0013] When the water content of the processed starch is 8% or less, the plasticity of the starch decreases and, at the same time, the elastic recovery after compression increases, resulting in a decrease in binding properties. Moisture content is 15
% or more, the plasticity of the starch increases, but it is not preferable because the moisture contained in the particles oozes out onto the particle surface due to compression, and conversely the binding property decreases. Preferably it is 10-15%. Modified starch with a cold water soluble content of 10% or more has many components that absorb water and dissolve, so when used in tablets, it dissolves in the disintegration liquid and becomes sticky, slowing down the penetration of liquid into the inside of the tablet. Therefore, the disintegration is delayed, which is undesirable. Preferably it is less than 7%. Swelling volume is 5ml
If the amount is less than /g, swelling due to water absorption is small, and therefore sufficient force cannot be applied to disintegrate the tablet. Swelling volume is 15m
In order to produce processed starch of 1/g or more, it is necessary to increase the degree of gelatinization, and at the same time, the cold water soluble content also increases, so the upper limit is 15 ml/g. Preferably 5-11
ml/g.

[0014] Also, the bulk density of the processed starch is 0.35ml/
If it is less than g, the powder becomes light and has poor fluidity as a powder. Another drawback is that the tablets become thicker after compression. If the bulk density is 0.65 g/ml or more, the deformability during compression will be low, resulting in low bonding properties, which is not preferable. Particularly preferably, it is 0.40 to 0.60 g/ml. When the particle size of the processed starch is large, with a 100 mesh fraction of 50% or more, the content of processed starch varies widely between formulations, resulting in large variations in tablet hardness and disintegration time. In addition, since the tablet shows block-like disintegration, the dissolution of the drug is delayed, which is undesirable. Particularly preferably 30%
It is as follows.

The method for producing processed starch of the present invention will be described. This production method consists of heating raw starch in the presence of moisture to swell the starch particles without destroying the particle morphology, followed by drying and, if necessary, pulverization. The moisture content of raw starch during heating should be about 50% or more based on the dry weight of raw starch. The lower the temperature, the higher the temperature. Therefore, it is preferable to perform the heat treatment in a paste-like or slurry-like state with a water content of 100% or more, since this is advantageous in terms of energy cost. Further, heating in this state is preferable because uniform heating can be applied to all particles. Regarding the heating temperature, it is difficult to specify because the gelatinization start temperature varies depending on the starch type, particle size, production area, refining conditions, water content of raw starch, etc., but in paste or slurry form, the starch type The gelatinization start temperature specific to
It is preferable to process at a temperature higher than 0°C but lower than that. By the way, "Starch Science Handbook" (supervised by Jiro Nikoku, published by Asakura Shoten)
1977, p. 36), the gelatinization initiation temperature of the main starches by the photopaste method is 66.8°C for corn;
, potato; 61.0℃, tapioca; 65.4℃, sweet potato;
The temperature is 65.8°C.

Next, regarding the heating method, starch is added to 5 to 50%.
After making an aqueous suspension containing starch, the temperature is increased by passing hot water through the jacket in a jacketed stirring tank, or by directly adding hot water to the starch suspension while stirring, or instead of hot water. Methods include blowing steam or heating the starch suspension through a plate heat exchanger. You can also increase the starch content and heat it in a sealed state at a high temperature. The heating time can be freely selected from several tens of seconds to about an hour, but if the paste or slurry is heated for a long time at a temperature nearly 10°C above the gelatinization start temperature, gelatinization will progress too much and the starch particle morphology will change. is destroyed and the amount of cold water soluble content increases, which is undesirable. After the predetermined heating is completed, it is preferable to add a step of cooling to a temperature below the gelatinization start temperature because the quality becomes constant. Before, during, or after heating, soluble starch, dextrin, and pregelatinized starch may be added so that the cold water soluble content of the starch does not exceed 10%. Also,
During or after heating, the cold water soluble content of starch is 10%.
It is also possible to add stirring, grinding, etc. to an extent that does not exceed . Next, regarding the drying method, spray dryers, flash dryers, etc., which can instantly dry paste or slurry materials, are most suitable. If the solid content concentration is high, water may be added and then dried using the above method, but
It is also possible to directly dry it at a temperature lower than the gelatinization start temperature.

[0017] The raw starch that is the raw material for the processed starch of the present invention will be described. Examples of raw starches include terrestrial starches such as corn, wheat, and rice, and rhizome starches such as potato, tapioca, and sweet potato, and any of these may be used. Also, a mixture of two or more raw starches may be used. Since the degree of gelatinization of rhizome starch varies greatly depending on the temperature, it can be used if the conditions are strictly controlled, for example, by cooling immediately after reaching a predetermined temperature. In addition, manufacturing is easy if, for example, a method using a plate heat exchanger is used.

Next, a pharmaceutical composition using the processed starch of the present invention will be described. The pharmaceutical composition of the present invention is a tablet, granule, or capsule filled with granules. This results in tablets, granules, and capsules that are superior in tablet (granule) hardness and disintegration time (as a result, drug dissolution rate) compared to cases where conventional processed starch is used. In addition, in the case of a drug that would be unstable if crystalline cellulose or lactose were added, a drug with good stability can be obtained by using modified starch. Furthermore, the term "preparation" as used herein should also be considered to include food products in the form of tablets, granules, and capsules, such as tablet confections and functional foods, which are made by the method described below. The amount of processed starch added is influenced by the amount of drug compounded and the size of the preparation, but is approximately 2 to 70% to satisfy both binding and disintegrating functions. Preferably it is about 5 to 50%. In addition, other additives include
Commonly used additives such as crystalline cellulose, lactose, and cornstarch can be added.

Next, the method for producing the pharmaceutical composition will be described. First, regarding tablets, a powder consisting of one or more drugs, modified starch, and other additives if necessary is mixed,
Examples include the so-called direct compression method, in which the powder is compressed as it is, and the dry granule compression method, in which the powder is compressed into a plate or tablet shape, then crushed to form granules, and the granules are further compressed. Granules are made by making granules by the above method and sieving if necessary. Capsules are made by filling capsules with the above granules. Furthermore, tablets and granules may be coated with a film or coated with sugar.

[0020]

[Examples] The present invention will be explained below with reference to Examples. The method for evaluating the physical properties of processed starch and tablets is as follows. Modified starch/moisture content (%) The weight loss when drying 10g of sample at 105℃ for 6 hours is 10
Divide by and find.

- Cold water soluble content (%) Add 3 g (in terms of dry matter) of the sample to 297 ml of pure water at 25°C, and stir for 2 minutes at 1500 rpm using an Ace homogenizer (manufactured by Nippon Seiki Co., Ltd.). The resulting suspension is then filtered using filter paper. Take 30ml of filtrate and
Dry at 5°C until constant weight. dry weight to 1000
Multiply the amount and divide by the weight of the sample used to determine the cold water soluble content.

- Swelling volume (ml/g) Add 5 g of sample to approximately 80 g of pure water at 25°C and disperse. Pour the dispersion into a 100 ml graduated cylinder with a stopper, and add pure water to make 100 ml. After sealing the container and leaving it for 24 hours, divide the swollen sample volume by 5 to obtain the swollen volume. - Bulk density (g/ml) Measure the volume of the sample when 30 g of the sample is poured little by little into a 100 ml measuring cylinder. Divide 30g by the sample volume to obtain the bulk density.

・100 mesh fraction (%) Yanagimoto Seisakusho (
A 100 mesh sieve (
This is the residue on the sieve after 30 g of sample was sieved for 30 minutes using a sieve (opening 150 μm). Tablet/Hardness (kg) It is expressed as the force when the tablet is broken by applying force in the radial direction using a Schroinger hardness tester manufactured by Freund Sangyo Co., Ltd. The number of repetitions is 20, and the average value is taken.

- Disintegration time (minutes) The disintegration test was carried out using a disintegration tester NT-2HS manufactured by Toyama Sangyo Co., Ltd. using pure water as a disintegration liquid. The number of repetitions is 6, and the average value is taken. Note that the disc is not used.

[0025]

[Example 1] Cornstarch (manufactured by Nippon Deka Chemical Co., Ltd.) 1k
g was dispersed in 7 kg of warm water at 60°C, and while stirring this slurry, the temperature was raised at a rate of 1°C/min until it reached 68°C, then 2 kg of water at about 20°C was added, and heat treatment was carried out. stopped. Next, the slurry was sprayed using a small spray dryer (manufactured by Okawara Kakoki Co., Ltd.) at an inlet temperature of about 160°C and a slurry supply rate of 7 kg/hr to obtain modified starch (A). . Table 1 shows the physical properties of processed starch (A).

[0026]

Example 2 Processed starch (B) was obtained in the same manner as in Example 1 except that the inlet temperature of the spray dryer was about 130°C. Table 1 shows the physical properties of the processed starch (B).

[0027]

[Comparative Example 1] The method was carried out in accordance with Japanese Patent Publication No. 59-47600. Cornstarch (manufactured by Nippon Star Chemical Co., Ltd.) 1k
g was dispersed in 7 kg of 60°C warm water, and while stirring this slurry, the temperature was raised at a rate of 1°C/min to 65°C, and then heated for 20 minutes. Then, the inlet temperature is set to about 180
Processed starch (C) was prepared in the same manner as in Example except that the temperature was
I got it. Table 1 shows the physical properties of processed starch (C).

[0028]

[Comparative Example 2] Processed starch (D) was obtained in the same manner as in Example 1 except that the inlet temperature of the spray dryer was about 115°C. Table 1 shows the physical properties of modified starch (D).

[0029]

[Example 3] Processed starch (C) was left in an atmosphere of 25°C and 75% RH for 12 hours and 24 hours, respectively, to obtain processed starches (E) and (F). Table 1 shows the physical properties of processed starches (E) and (F).

[0030]

[Comparative Example 3] Processed starch (C) was left to stand under the conditions of Example 3 for 72 hours to obtain processed starch (G). Table 1 shows the physical properties of modified starch (G).

[0031]

[Example 4] Processed starch (H) was obtained in the same manner as in Example 1, except that the temperature was heated to 65°C and the inlet temperature of the spray dryer was set to about 150°C. Processed starch (H)
The physical properties of are shown in Table 1.

[0032]

[Example 5] Processed starch (I) was obtained in the same manner as in Example 4 except that the mixture was heated to 72°C. Table 1 shows the physical properties of modified starch (I).

[0033]

[Comparative Example 4] Processed starch (J) was obtained in the same manner as in Example 4 except for heating to 63°C. Table 1 shows the physical properties of modified starch (J).

[0034]

[Comparative Example 5] Processed starch (K) was obtained in the same manner as in Example 4 except that it was heated to 80°C and kept warm for 1 hour. Table 1 shows the physical properties of processed starch (K).

[0035]

[Example 6] Phenacetin (manufactured by Yamamoto Chemical Co., Ltd., fine powder)
200 parts, crystalline cellulose (manufactured by Asahi Kasei Corporation, Avicel PH-101), 400 parts, lactose (manufactured by DMV, 10
0 mesh), 5 parts of magnesium stearate (manufactured by Taihei Kagaku Co., Ltd.) and 100 parts of modified starch (A) were mixed in a conventional manner. ), using Collect 12), tablet diameter 8 mm
Tablets with an average tablet weight of 200 mg were obtained. Tablet physical properties are shown in Table 2.

[0036]

[Example 7] The same procedure as in Example 6 was carried out except that modified starch (B) was used. Tablet physical properties are shown in Table 2.

[0037]

[Example 8] The procedure of Example 6 was repeated except that modified starch (E) was used. Tablet physical properties are shown in Table 2.

[0038]

[Example 9] The same procedure as in Example 6 was carried out except that modified starch (F) was used. Tablet physical properties are shown in Table 2.

[0039]

[Example 10] Example 6 except for using modified starch (H)
operated in the same way. Tablet physical properties are shown in Table 2.

[0040]

[Example 11] Example 6 except for using modified starch (I)
operated in the same way. Tablet physical properties are shown in Table 2.

[0041]

[Comparative Example 6] The same procedure as in Example 6 was carried out except that modified starch (C) was used. Tablet physical properties are shown in Table 2.

[0042]

[Comparative Example 7] The same procedure as in Example 6 was carried out except that modified starch (D) was used. Tablet physical properties are shown in Table 2.

[0043]

[Comparative Example 8] The same procedure as in Example 6 was carried out except that modified starch (G) was used. Tablet physical properties are shown in Table 2.

[0044]

[Comparative Example 9] The same procedure as in Example 6 was carried out except that modified starch (J) was used. Tablet physical properties are shown in Table 2.

[0045]

[Comparative Example 10] Example 6 except for using modified starch (K)
operated in the same way. Tablet physical properties are shown in Table 2.

[0046]

[Comparative Example 11] Corn starch (C
S, manufactured by Nippon Deka Chemical Co., Ltd.) in the same manner as in Example 6. Table 1 shows the physical properties of CS, and Table 2 shows the tableting results.

[0047]

[Example 12] 1.5 kg of cornstarch is dispersed in 4 kg of 60°C hot water, and then the temperature is raised to 67°C. Next, transfer this to a tray and use a hot air dryer at 40℃ to reduce the moisture content to about 12%.
After drying until dry, the starch was ground with a bantam mill (manufactured by Hosokawa Micron) to obtain processed starch (L). Table 3 shows the physical properties of the processed starch (L).

[0048]

[Comparative Example 12] Except for drying until the moisture content is about 7%,
The same procedure as in Example 12 was carried out to obtain processed starch (M). Table 3 shows the physical properties of the modified starch (M).

[0049]

[Example 13] Same as Example 4, except that before spray drying, treatment was performed at 500 rpm for 5 minutes using a batch type attritor 10S (Mitsui Miike Kakoki Co., Ltd., using alumina balls of 3 mm diameter). Processed starch (N) was obtained. Table 3 shows the physical properties of processed starch (N).

[0050]

[Example 14] Processed starch (O) was obtained in the same manner as in Example 13, except that it was processed for 20 minutes using a batch type attritor 10S. Table 3 shows the physical properties of modified starch (O).

[0051]

Comparative Example 13 Processed starch (P) was obtained in the same manner as in Example 13, except that it was treated for 40 minutes using a batch type attritor 10S. Table 3 shows the physical properties of processed starch (P).

[0052]

[Comparative Example 14] Processed starch (Q ) was obtained. Table 3 shows the physical properties of modified starch (Q).

[0053]

[Example 15] Processed starch (R) was obtained in the same manner as in Example 2 except that potato starch (manufactured by Nippon Star Chemical Co., Ltd.) was used and the temperature reached was 62°C. Table 3 shows the physical properties of modified starch (R).

[0054]

[Example 16] The same procedure as in Example 2 was carried out, except that dextrin (manufactured by Matsutani Chemical Co., Ltd., Pine Index-100) was added in an amount of 3% based on the solid content of corn starch before spray drying. Processed starch (S) was obtained. Table 3 shows the physical properties of processed starch (S).

[0055]

[Comparative Example 15] Technology 3 of Japanese Patent Publication No. 46-21472
It was carried out in accordance with the method. That is, after adding water to cornstarch to make the water content 25%, it was ground three times using a roll mill (NR-42A, manufactured by Noritake Company), and dried at 60° C. in a hot air dryer until the water content was 8%. Next, after pulverizing with a bantam mill, the starch was humidified to a moisture content of 12% to obtain processed starch (T). Table 3 shows the physical properties of processed starch (T).

[0056]

[Comparative Example 16] Example 2 of JP-A-60-233019
It was carried out in accordance with the method. That is, 1 kg of corn starch is dispersed in 1.5 kg of water, and 2.5 g of calcium chloride is added. Adjust the pH to 6.0-6.5 by adding dilute sodium hydroxide solution. After adding 250 ml of 4% α-amylase (manufactured by Kanto Kagaku Co., Ltd.) solution, the temperature was raised to 55° C. and reacted for 4 hours. Then adjust the pH to 2-3 with dilute hydrochloric acid.
After holding for 15 minutes, dilute sodium hydroxide is added again to bring the pH to about 6. After filtering and washing the residue, it is dried with a hot air dryer and ground with a bantam mill to obtain processed starch (U).
I got it. Table 3 shows the physical properties of the processed starch (U).

[0057]

[Comparative Example 17] Commercially available starch 1500 (manufactured by Nippon Colorcon Co., Ltd.) was used as modified starch (V). Table 3 shows the physical properties of modified starch (V).

[0058]

[Comparative Example 18] Commercial product PCS (manufactured by Asahi Kasei Industries, Ltd.) was used as modified starch (W). Table 3 shows the physical properties of processed starch (W).

[0059]

[Example 17] 495 g of L-ascorbic acid (manufactured by Takeda Pharmaceutical Co., Ltd.) and 500 parts of modified starch (L) were mixed, and then 5 parts of magnesium stearate were mixed.
The mixture was compressed in the same manner as above to obtain tablets. Tablet physical properties are shown in Table 4.

[0060]

[Example 18] Example 1 except for using modified starch (N)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0061]

[Example 19] Example 1 except for using modified starch (O)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0062]

[Example 20] Example 1 except for using modified starch (R)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0063]

[Example 21] Example 1 except for using modified starch (S)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0064]

[Comparative Example 19] Example 1 except for using modified starch (M)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0065]

[Comparative Example 20] Example 1 except for using modified starch (P)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0066]

[Comparative Example 21] Example 1 except for using modified starch (Q)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0067]

[Comparative Example 22] Example 1 except for using modified starch (T)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0068]

[Comparative Example 23] Example 1 except for using modified starch (U)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0069]

[Comparative Example 24] Example 1 except for using modified starch (V)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0070]

[Comparative Example 25] Example 1 except for using modified starch (W)
It was operated in the same manner as in 7. Tablet physical properties are shown in Table 4.

[0071]

[Example 22] 400g of modified starch (B), aspirin (
Hoei Yakuko Co., Ltd.) 400g, 200 mesh lactose (D
(manufactured by MV) were mixed, and 10 g of magnesium stearate was further added and mixed. Next, the mixed powder was processed using a roller compactor mini (Freund Sangyo Co., Ltd.).
After compressing it onto a plate under a pressure of 2 tons, it was crushed. Next, the crushed material was sieved to pass through a 12 mesh (opening 1410 μm), and then through an 80 mesh (opening 18
The remaining granules (0 μm) were compressed using a rotary tablet machine in the same manner as in Example 6 to obtain tablets. Table 5 Tablet physical properties
Shown below.

[0072]

[Example 23] Example 2 except for using modified starch (N)
The procedure was the same as in 2. Table 5 shows the physical properties of the tablet.

[0073]

[Comparative Example 26] Example 2 except for using modified starch (C)
The procedure was the same as in 2. Table 5 shows the physical properties of the tablet.

[0074]

[Comparative Example 27] Example 2 except using modified starch (T)
The procedure was the same as in 2. Table 5 shows the physical properties of the tablet.

[0075]

[Comparative Example 28] Example 2 except using modified starch (U)
The procedure was the same as in 2. Table 5 shows the physical properties of the tablet.

[0076]

[Table 1]

[0077]

[Table 2]

[0078]

[Table 3]

[0079]

[Table 4]

[0080]

[Table 5]

[0081]

[Effect of the invention] When a processed starch with specified physical properties that has both binding and disintegrating functions is used to formulate tablets by direct compression or dry granulation, it has excellent binding properties, resulting in tablet hardness. Alternatively, preparations with high granule strength can be made. Furthermore, since it has excellent disintegration properties, the preparation disintegrates quickly after administration, resulting in a rapid dissolution rate of the drug. As mentioned above, since modified starch has both binding and disintegrating functions, it can be formulated simply and has high stability against drugs, which facilitates quality design.

Claims (2)

[Claims] Claim 1: Processed starch obtained by heat-treating raw starch in the presence of moisture, with a moisture content of 8 to 15%.
, cold water soluble content is less than 10%, swelling volume is 5-15ml/
A processed starch with excellent binding and disintegrating properties. 2. A pharmaceutical composition comprising the modified starch according to claim 1.