JPH0352823A - Solid agent - Google Patents
Solid agentInfo
- Publication number
- JPH0352823A JPH0352823A JP18743189A JP18743189A JPH0352823A JP H0352823 A JPH0352823 A JP H0352823A JP 18743189 A JP18743189 A JP 18743189A JP 18743189 A JP18743189 A JP 18743189A JP H0352823 A JPH0352823 A JP H0352823A
- Authority
- JP
- Japan
- Prior art keywords
- calcium silicate
- crystalline cellulose
- starch
- amount
- drug
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 239000007787 solid Substances 0.000 title claims abstract description 19
- 239000000378 calcium silicate Substances 0.000 claims abstract description 21
- 229910052918 calcium silicate Inorganic materials 0.000 claims abstract description 21
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims abstract description 21
- 239000003814 drug Substances 0.000 claims abstract description 20
- 229940079593 drug Drugs 0.000 claims abstract description 20
- 239000001913 cellulose Substances 0.000 claims abstract description 19
- 229920002678 cellulose Polymers 0.000 claims abstract description 19
- 229920002472 Starch Polymers 0.000 claims abstract description 15
- 235000019698 starch Nutrition 0.000 claims abstract description 15
- 239000008107 starch Substances 0.000 claims abstract description 14
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 12
- 238000002360 preparation method Methods 0.000 claims description 10
- 238000000034 method Methods 0.000 abstract description 11
- 239000000843 powder Substances 0.000 abstract description 9
- 238000002156 mixing Methods 0.000 abstract description 3
- 239000002245 particle Substances 0.000 abstract description 3
- 239000013078 crystal Substances 0.000 abstract description 2
- 239000007909 solid dosage form Substances 0.000 description 7
- 239000008187 granular material Substances 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 230000000052 comparative effect Effects 0.000 description 3
- 238000007907 direct compression Methods 0.000 description 3
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 2
- 229920002261 Corn starch Polymers 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 239000008120 corn starch Substances 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- AMTPYFGPPVFBBI-UHFFFAOYSA-N acedapsone Chemical compound C1=CC(NC(=O)C)=CC=C1S(=O)(=O)C1=CC=C(NC(C)=O)C=C1 AMTPYFGPPVFBBI-UHFFFAOYSA-N 0.000 description 1
- 229950009438 acedapsone Drugs 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000002221 antipyretic Substances 0.000 description 1
- 229940125716 antipyretic agent Drugs 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 238000013329 compounding Methods 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000010436 fluorite Substances 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 238000000465 moulding Methods 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229960005489 paracetamol Drugs 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 238000009702 powder compression Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】 〔産業上の利用分野〕 本発明は薬物を含有する固形剤に関する。[Detailed description of the invention] [Industrial application field] The present invention relates to solid dosage forms containing drugs.
詳しくは、薬物にケイ酸カルシウム及び特定の化合物を
配合してたる固形剤に関する。Specifically, the present invention relates to a solid preparation containing a drug containing calcium silicate and a specific compound.
従来より、顆粒、錠剤等の固形剤を製造する際に、該固
形剤に適当た形を賦与してその特定の形状が，例えば運
搬時に破壊しないように、賦形剤と称される配合剤が使
用されてきた。代表的ｋ賦形剤としては結晶セルロース
が挙げられ、この結晶セルロースは粉末直接圧縮法によ
って製錠しうる良好ｋｗ．形剤として知られている。Conventionally, when manufacturing solid preparations such as granules and tablets, compounding agents called excipients have been used to give the solid preparation a suitable shape so that the specific shape does not break during transportation, for example. has been used. A typical k excipient is crystalline cellulose, which has a good kw. Known as excipient.
ところで、固形剤によっては、その固形剤中の薬物量を
出来るだけ多くしたい場合があり、少量の配合で賦形性
の優れた賦形剤が望まれていた。又、薬物の種類によっ
ては、それ自身の成形性に乏しいために固形剤中に多量
に配合すること力１極めて麹かしい場合があった。例え
ば、解熱剤として知られているアセトアミノ７エン７０
重量部に前記代表的賦形剤である結晶セルロース３０重
量部を配合して２ ０ ０ （ｌの打錠圧で直接製錠な
試みても、キャツビング現象が生じ成形不能である。Incidentally, depending on the solid dosage form, there are cases where it is desired to increase the amount of drug in the solid dosage form as much as possible, and there has been a desire for an excipient that has excellent excipient properties even when mixed in a small amount. Furthermore, depending on the type of drug, it may be extremely moldy when incorporated in a large amount into a solid preparation due to its poor moldability. For example, acetamin 7ene 70, which is known as an antipyretic agent,
Even if 30 parts by weight of crystalline cellulose, which is the typical excipient, was blended with 30 parts by weight and the tablet was directly made at a tableting pressure of 200 liters, a caving phenomenon occurred and it was impossible to form the tablet.
更に、従来の製錠方法は、一般にまず顆粒を製造し、次
いで該顆粒を打錠し錠剤とするものであり、工程的、コ
スト的に手間がかかる上に、各工程でりコンタミネーシ
ョンの問題もあった。従って、上記顆粒圧縮法の諸欠点
を克服するために、粉末直接圧縮法による錠剤の麹法が
望まれていた。Furthermore, conventional tabletting methods generally first produce granules and then compress the granules into tablets, which is time-consuming in terms of process and cost, and also poses the problem of contamination at each step. There was also. Therefore, in order to overcome the drawbacks of the above-mentioned granule compression method, there has been a desire for a koji method for making tablets using a powder direct compression method.
本発明者らは、薬物を出来るだけ多く配合し，且つ粉末
直接圧縮法で製剤出来る固形剤について鋭意研究した結
果、本発明に到った。The present inventors have arrived at the present invention as a result of extensive research into solid preparations that can be formulated using a powder direct compression method and containing as much drug as possible.
即ち、本発明は、薬物、ケイ酸カルシウム、並びにデン
プン及び／または結晶セルロースからなる固形剤におい
て，ケイ酸カルシウムを薬物に対して１０〜４５重量％
配合させ、且つデンプン及び／または結晶セルロースを
ケイ酸カルシウムに対して４０〜２００重量％配合させ
てなることを特徴とする固形剤である。That is, the present invention provides a solid preparation consisting of a drug, calcium silicate, and starch and/or crystalline cellulose, in which the calcium silicate is contained in an amount of 10 to 45% by weight based on the drug.
It is a solid agent characterized by containing 40 to 200% by weight of starch and/or crystalline cellulose based on calcium silicate.
本発明において使用される薬物は一般に粉末状である。The drug used in the present invention is generally in powder form.
特にそれ自身が極めて成形性に乏しい粉末状薬物におい
て最適である。It is particularly suitable for powdered drugs which themselves have very poor moldability.
本発明において使用されるケイ酸カルシウムは伺ら制限
されないが、製剤を目的とするので粉末状であることが
望ましい。該粉末状ケイ酸カルシウムとしては、特に、
花弁状結晶構造を有するジャイロ型特殊ケイ酸カルシウ
ムであるフローライト（商品名、徳山曹達株式会社製）
が好適に用いられる。Although the calcium silicate used in the present invention is not particularly limited, it is preferably in powder form since it is intended for use in pharmaceutical preparations. As the powdered calcium silicate, in particular,
Fluorite, a gyro-type special calcium silicate with a petal-like crystal structure (trade name, manufactured by Tokuyama Soda Co., Ltd.)
is preferably used.
上記ケイ酸カルシウムは薬物に対してｌＯ〜４５重社％
配合させることが必須である。The above calcium silicate is lO~45% based on the drug.
It is essential to blend them.
ｌＯ重量噂より少ない場合は、後述りデンプン及び／ま
たは結晶セルロースを添加配合しても成形不能である。If the weight is less than the rumored 1O weight, it will not be possible to mold it even if starch and/or crystalline cellulose, which will be described later, is added and blended.
４５重量％より大きい場合は、威形は可能であり強度も
発現するが、固形剤として重要な要素のひとつである崩
壊性が悪くなり実用的でｔｘい。又、ケイ酸カルシウム
の量が多くたると、固形剤中に出来るだけ多くの薬物を
含有させるという本発明の目的に沿わなくなる。If it is larger than 45% by weight, it is possible to form a strong shape and exhibit strength, but the disintegration property, which is one of the important factors for a solid agent, deteriorates and is not practical. Moreover, if the amount of calcium silicate is too large, the purpose of the present invention, which is to contain as much drug as possible in the solid preparation, will not be met.
本発明において、ケイ酸カルシウムと伴にデンプン及び
／１たは結晶セルロースを用いることが必須である。該
化合物はケイ酸カルシウムと組合わせることにより成形
を可能にするとともに固形剤の破壊強度を向上させる。In the present invention, it is essential to use starch and/or crystalline cellulose together with calcium silicate. When combined with calcium silicate, this compound enables molding and improves the breaking strength of the solid agent.
とりわけ、デンプンは破壊強度を向上させるだけでなく
、崩壊性り向上にも寄与するので特に好ましい。デンプ
ンとしては、トウモロコシデンプン、バレイショデンプ
ン等の粉末状デンプンが何ら制限ｔｘ ＜使用される。In particular, starch is particularly preferred since it not only improves the breaking strength but also contributes to improving the disintegration property. As the starch, powdered starches such as corn starch and potato starch are used without any restrictions.
結晶セルロースとしては、パルプなどのセルロース原料
から化学的、機械的手段により得られる粉末状結晶セル
ロースが使用される。好ましくは、旭化成工業一から「
アピセル」の商品名で市販されている平均粒径４０μ〜
１２０μの白色粉末状結晶セルロースが採用される。As the crystalline cellulose, powdery crystalline cellulose obtained from cellulose raw materials such as pulp by chemical and mechanical means is used. Preferably, from Asahi Kasei Kogyo 1, “
Commercially available under the trade name “Apicel” with an average particle size of 40μ~
120μ white powder crystalline cellulose is employed.
上記デンプン及び／または結晶セルロースは、ケイ酸カ
ルシウムに対して４０〜２５０ｘｍ％配合させることが
必要である。４０重Ｍ％より少ない場合は破壊強度が小
さい。The above-mentioned starch and/or crystalline cellulose must be blended in an amount of 40 to 250 xm% based on calcium silicate. When the amount is less than 40% by weight, the breaking strength is low.
２５０ｍ量％より大きい場合も破壊強度が減少する。即
ち４０〜２５０重ｔｉ１％の範囲でケイ酸カルシウムと
共存させた時に破壊強度Ｏ向上現象がみられる。本発明
の固形剤中のケイ酸カルシウムの量が少ｋい時は、該デ
ンプン及び／または結晶セルロースの量は上記数値範囲
の１１かで出来るだけ大きい値をとることが好ましい。The fracture strength also decreases when the amount is greater than 250 m%. That is, when it coexists with calcium silicate in the range of 40 to 250 wt 1%, an improvement in fracture strength O is observed. When the amount of calcium silicate in the solid agent of the present invention is small, the amount of starch and/or crystalline cellulose is preferably as large as possible within the above numerical range.
本発明の固形剤は、錠剤、顆粒剤、カプセル剤、細粒剤
、散剤ｔｘどの種々の形態をとりつる。又、本発明り固
形剤、崩壊剤、滑沢剤結合剤及びその他の添加剤を本発
明の目的を損わない限り含有させることができる。The solid preparation of the present invention can take various forms such as tablets, granules, capsules, fine granules, and powders. In addition, the solid agent, disintegrant, lubricant binder, and other additives of the present invention can be included as long as they do not impair the object of the present invention.
本発明の固形剤は、薬物を多量に含有するにもかかわら
ず固形剤としてのｆ分ｋ破壊強度を有する。又、錠剤と
する場合は、顆粒を経る工程を必要とせず粉末直接圧縮
法によって成形が可能である。特に必須成分のひとつと
してデンプンを用いる場合は、破壊強度とともに十分た
崩壊性も有し好ましい。更に、本発明の固形剤を構成す
る原料粉末混合物は流動性に富み、粉末直接圧縮法によ
る直接製錠に好適である。The solid dosage form of the present invention has the f-minute k breaking strength as a solid dosage form, even though it contains a large amount of drug. In addition, in the case of making a tablet, it can be molded by a powder direct compression method without requiring a granulation process. In particular, when starch is used as one of the essential components, it is preferable because it has sufficient breaking strength and disintegration properties. Furthermore, the raw material powder mixture constituting the solid dosage form of the present invention has high fluidity and is suitable for direct tablet production by direct powder compression method.
又、本発明の固形剤はその組成によっては、低圧条件で
の打錠が可能であるので、例えば、マイクロカプセル化
された薬物を配合させる場合のように薬物粒子を破壊せ
ずに製剤する必要がある時に有利である。Furthermore, depending on the composition, the solid preparation of the present invention can be compressed into tablets under low pressure conditions, so it is not necessary to formulate the drug particles without destroying them, as is the case, for example, when blending microencapsulated drugs. It is advantageous when there is
実施例ｌ
粉砕して１００号ふるいで分取した薬物としてり７エナ
セチン（以下、ＰＣ剤とも略記する）、トウモロコシデ
ンプン、フローライ｝Ｒ（徳山曹達■製）をそれぞれ６
０℃で、８時間乾燥した。これらを表１に示す割合の各
成分、及び滑沢剤として１重＆１％りステアリン酸マグ
不シウムを混合したσつち、日栄精工■ＫＳ−２型打錠
機を用いて２ｏｏｍｙ／錠の錠剤を得た。Example 1 As drugs, which were crushed and separated using a No. 100 sieve, 7 Enacetin (hereinafter also abbreviated as PC agent), corn starch, and Florai}R (manufactured by Tokuyama Soda ■) were mixed into 6 pieces each.
It was dried at 0°C for 8 hours. These were mixed with each component in the proportions shown in Table 1 and 1% & 1% magnonium stearate as a lubricant. Got the tablets.
該錠剤の引張破壊強度を■木屋製作所ＫＨＴ−２０型デ
ジタル硬度計を用いて測定し、固形剤の機械的強度σ）
指標とした。結果は、あわせて表１に示す。The tensile breaking strength of the tablet was measured using a Kiya Seisakusho KHT-20 digital hardness meter, and the mechanical strength of the solid dosage form σ)
It was used as an indicator. The results are also shown in Table 1.
実施例２〜５、比較例１〜５
表１に示す各成分を所定社用いた以外は、実施例１と同
様に行って製錠し、ついで引張破壊強度を測定した。Examples 2 to 5, Comparative Examples 1 to 5 Tablets were made in the same manner as in Example 1, except that each component shown in Table 1 was used by a specified company, and then the tensile breaking strength was measured.
但し、薬物としてアセトアミノフエン（以下、ＡＣ剤と
も略記する）、バレインヨデンプン、結晶セルロースと
してアゼセルＰｌ｛一１０１ （旭化成工業＠製）を使
用した。However, as the drug, acetaminophen (hereinafter also abbreviated as AC agent), valaineyostarch, and crystalline cellulose used Azecel Pl{-101 (manufactured by Asahi Kasei Kogyo@).
実施例６〜９、比較例３〜５
表２に示す各成分を所定量用いて、１５００ｔで打錠し
た以外は実施例ｌと同様に行った。Examples 6 to 9, Comparative Examples 3 to 5 The same procedure as in Example 1 was conducted except that each component shown in Table 2 was used in a predetermined amount and the tablets were compressed at 1500 tons.
結果はあわせて表２に示す。The results are also shown in Table 2.
実施例１０．比較例６Example 10. Comparative example 6
Claims (1)
結晶セルロースからなる固形剤において、ケイ酸カルシ
ウムを薬物に対して１０〜４５重量％配合させ、且つデ
ンプン及び／または結晶セルロースをケイ酸カルシウム
に対して４０〜２５０重量％配合させてなることを特徴
とする固形剤。In a solid preparation consisting of a drug, calcium silicate, and starch and/or crystalline cellulose, calcium silicate is blended in an amount of 10 to 45% by weight based on the drug, and starch and/or crystalline cellulose is blended in an amount of 40% by weight based on the amount of calcium silicate. A solid agent characterized by containing ~250% by weight.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18743189A JPH0352823A (en) | 1989-07-21 | 1989-07-21 | Solid agent |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP18743189A JPH0352823A (en) | 1989-07-21 | 1989-07-21 | Solid agent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH0352823A true JPH0352823A (en) | 1991-03-07 |
Family
ID=16205941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP18743189A Pending JPH0352823A (en) | 1989-07-21 | 1989-07-21 | Solid agent |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0352823A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006131575A (en) * | 2004-11-08 | 2006-05-25 | Tokuyama Corp | Low-melting drug-containing granule and tablet produced by using the same |
| WO2007097333A1 (en) * | 2006-02-20 | 2007-08-30 | Asahi Breweries, Ltd. | Granules, tablets and method of producing the same |
| WO2012002253A1 (en) | 2010-06-29 | 2012-01-05 | 旭化成ケミカルズ株式会社 | Composite particles which contain both cellulose and inorganic compound |
-
1989
- 1989-07-21 JP JP18743189A patent/JPH0352823A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2006131575A (en) * | 2004-11-08 | 2006-05-25 | Tokuyama Corp | Low-melting drug-containing granule and tablet produced by using the same |
| WO2007097333A1 (en) * | 2006-02-20 | 2007-08-30 | Asahi Breweries, Ltd. | Granules, tablets and method of producing the same |
| WO2012002253A1 (en) | 2010-06-29 | 2012-01-05 | 旭化成ケミカルズ株式会社 | Composite particles which contain both cellulose and inorganic compound |
| US8951636B2 (en) | 2010-06-29 | 2015-02-10 | Asahi Kasei Chemicals Corporation | Composite particles which contain both cellulose and inorganic compound |
| US9446137B2 (en) | 2010-06-29 | 2016-09-20 | Asahi Kasei Chemicals Corporation | Composite particles which contain both cellulose and inorganic compound |
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