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JP-2026075088-A - Composition, method for manufacturing the composition, molded article, and method for manufacturing the molded article.

JP2026075088AJP 2026075088 AJP2026075088 AJP 2026075088AJP-2026075088-A

Abstract

[Problem] To provide a method for obtaining a granular composition by wet granulation of a raw material powder composition containing a drug and crystalline cellulose, the method for producing the composition having good productivity and excellent uniformity, the composition produced by the method, and a method for producing a molded article from the composition. [Solution] The present invention relates to a method for producing a composition comprising a drug (A) and crystalline cellulose (B), comprising a granulation step of wet granulating a raw material powder composition comprising the drug (A) and the crystalline cellulose (B), wherein the crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less, and the wet granulation is performed by fluidized bed granulation under granulation conditions in which the ratio of the amount of material added to the airflow (amount of material added/airflow) is 4.0 g/( m³ /h) or more and 65.0 g/( m³ /h) or less. [Selection Diagram] None

Inventors

  • 吉田 歩美
  • 玉利 楓
  • 山本 佳穂
  • 樋口 雅治

Assignees

  • 旭化成株式会社

Dates

Publication Date
20260507
Application Date
20251021
Priority Date
20241021

Claims (14)

  1. A method for producing a composition containing a drug (A) and crystalline cellulose (B), The process includes a granulation step of wet granulating a raw material powder composition containing the drug (A) and the crystalline cellulose (B), The crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less. The aforementioned wet granulation is performed by fluidized bed granulation under granulation conditions where the ratio of the amount of material added to the airflow (amount of material added/airflow) is 4.0 g/( m³ /h) or more and 65.0 g/( m³ /h) or less. A method for producing a composition.
  2. The method for producing the composition according to claim 1, wherein the wet granulation is performed under granulation conditions where the ratio of the amount charged to the liquid velocity per spray gun (amount charged / (liquid velocity / number of spray guns)) is 3 min·granules or more and 800 min·granules or less.
  3. The method for producing the composition according to claim 1, wherein the wet granulation is carried out under granulation conditions where the spray pressure is 0.15 MPa or more and 0.60 MPa or less.
  4. The method for producing the composition according to claim 1, wherein the wet granulation is carried out under granulation conditions where the inlet temperature is 50°C or higher and 90°C or lower.
  5. The method for producing the composition according to claim 1, wherein the wet granulation is performed by fluidized bed granulation using a column having a tapered cylindrical shape.
  6. A method for producing the composition according to claim 1, wherein the content ratio of drug (A) to the total amount of the raw material powder composition is 40% by mass or more.
  7. A method for producing the composition according to claim 1, wherein the content ratio of the crystalline cellulose (B) relative to the total amount of the raw material powder composition is 5% by mass or more.
  8. The method for producing the composition according to claim 1, wherein the wet granulation is performed under granulation conditions in which the amount of material added relative to the maximum processing capacity in a single granulation operation in a fluidized bed granulator (amount of material added / maximum processing capacity) is 0.20 or more and 1.00 or less.
  9. A method for producing the composition according to claim 1, wherein the wet granulation is carried out under granulation conditions where the input amount is 300 g or more and 1500 g or less.
  10. A method for producing a molded article, comprising: producing a composition containing the drug (A) and the crystalline cellulose (B) by the method for producing the composition described in any one of claims 1 to 9; and molding the obtained composition to produce a molded article.
  11. The manufacturing method according to claim 10, wherein the molded body is a tablet.
  12. The product contains drug (A) and crystalline cellulose (B), The crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less. The percentage of particles (+2 mm) remaining on a sieve with a mesh size of 2 mm is 0.3% or less. composition.
  13. The product contains drug (A) and crystalline cellulose (B), The crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less. The proportion of drug (A) in the total amount of the composition is 40% by mass or more. A composition that is a wet-process granulated material.
  14. A molded article comprising a wet-process granule containing a drug (A) and crystalline cellulose (B), The crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less. The mass CV is 1% or less, and the number of molded bodies containing white material out of 100 is 5 or less. Molded body.

Description

This invention relates to a composition containing a drug and crystalline cellulose, a method for producing a composition containing a drug and crystalline cellulose by wet granulation, and a method for producing a molded article from the composition. Traditionally, tablets are manufactured by uniformly mixing a raw material powder composition containing the drug, excipients, and other additives, and then compressing the mixture using a tablet press. Furthermore, to improve the physical properties of tablets, or to improve the handling characteristics of difficult-to-handle powders, tablets may be manufactured by pre-granulating the drug together with excipients and other additives, compressing the resulting granules, or by further mixing these granules with other components to obtain a mixture, and then compressing the resulting mixture. Dry granulation and wet granulation methods are used for granulating the raw material powder composition. Tablets require various properties, including uniformity of drug content, drug dissolution, disintegration, and hardness. To improve these properties, various modifications, such as improvements to excipients and other additives, are widely employed. For example, Patent Document 1 describes how using cellulose powder with a specific average particle size and bulk density as an excipient can yield tablets with excellent hardness, abrasion resistance, and disintegration properties. Patent Document 2 describes how using cellulose powder with a high proportion of mannose and xylose in its sugar composition as an excipient can yield tablets with good disintegration properties while maintaining excellent active pharmaceutical ingredient recovery. Japanese Patent Publication No. 2020-180083International Publication No. 2020/202598 The following describes in detail embodiments for carrying out the present invention (hereinafter simply referred to as "this embodiment"). This embodiment is illustrative for explaining the present invention and is not intended to limit the present invention to the following content. The present invention can be appropriately modified and implemented within the scope of its gist. <Method for manufacturing the composition> The method for producing a composition according to this embodiment is a method for producing a composition comprising a drug (A) and crystalline cellulose (B), and includes a granulation step of wet granulating a raw material powder composition comprising the drug (A) and the crystalline cellulose (B). In the method for producing a composition according to this embodiment, the crystalline cellulose (B) has a bulk density of 0.30 g/mL or less and a compressibility of 45.0% or less, and the wet granulation is performed by fluidized bed granulation under granulation conditions in which the ratio of the amount charged to the airflow (amount charged/airflow) is 4.0 g/( m³ /h) or more and 65.0 g/( m³ /h) or less. In the method for producing a composition according to this embodiment, by using crystalline cellulose (B) with a bulk density and compressibility within a specific range as an excipient, even when fluidized bed granulation is performed under granulation conditions with a relatively large amount charged/airflow, the fluidity (intra-bed fluidity) of the raw material powder composition in the fluidized bed granulator is good, and uniform granulation can be achieved. The various components of the method for manufacturing the composition according to this embodiment will be described in detail below. [Drug (A)] In this specification, "drug" refers to a substance added to a mixed powder, molded product, processed product, etc., to exert a desired function or effect in the fields of pharmaceuticals, health foods, food products, industrial applications, etc. For example, in the pharmaceutical field, this refers to the active pharmaceutical ingredient. The following are examples of suitable drugs (A) used in the method for producing the composition according to this embodiment. The active ingredient in the drug is preferably the active ingredient of an orally administered drug. Examples of orally administered drugs include antipyretics, analgesics, and anti-inflammatory drugs, hypnotics and sedatives, anti-drowsiness drugs, anti-vertigo drugs, pediatric analgesics, stomachic drugs, antacids, digestive drugs, cardiac drugs, antiarrhythmic drugs, antihypertensive drugs, vasodilators, diuretics, anti-ulcer drugs, intestinal regulators, osteoporosis treatment drugs, antitussives and expectorants, anti-asthmatic drugs, antibacterial agents, frequent urination improvers, tonics, vitamins, etc. The active ingredient may be used alone or in combination of two or more. Specifically, for example, aspirin, aluminum aspirin, acetaminophen, ethenzamide, sazapyrine, salicylamide, lactylphenetidine, isotibenzyl hydrochloride, diphenylpyraline hydrochloride, diphenhydramine hydrochloride, difeterol hydrochloride, triprolidine hydrochloride, triperena