JPH0526770B2 - - Google Patents
Info
- Publication number
- JPH0526770B2 JPH0526770B2 JP58053015A JP5301583A JPH0526770B2 JP H0526770 B2 JPH0526770 B2 JP H0526770B2 JP 58053015 A JP58053015 A JP 58053015A JP 5301583 A JP5301583 A JP 5301583A JP H0526770 B2 JPH0526770 B2 JP H0526770B2
- Authority
- JP
- Japan
- Prior art keywords
- disintegrant
- tablet
- specific gravity
- tablets
- bulk specific
- 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.)
- Expired - Lifetime
Links
- 239000007884 disintegrant Substances 0.000 claims description 16
- 239000001913 cellulose Substances 0.000 claims description 14
- 229920002678 cellulose Polymers 0.000 claims description 14
- 230000005484 gravity Effects 0.000 claims description 14
- 239000000843 powder Substances 0.000 claims description 13
- 239000000203 mixture Substances 0.000 claims description 12
- 229940079593 drug Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 239000004615 ingredient Substances 0.000 claims description 9
- 239000007787 solid Substances 0.000 claims description 6
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical group [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 3
- 239000002253 acid Substances 0.000 claims description 3
- 239000011575 calcium Substances 0.000 claims description 3
- 229910052791 calcium Inorganic materials 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- CHRHZFQUDFAQEQ-UHFFFAOYSA-L calcium;2-hydroxyacetate Chemical compound [Ca+2].OCC([O-])=O.OCC([O-])=O CHRHZFQUDFAQEQ-UHFFFAOYSA-L 0.000 description 14
- 235000010980 cellulose Nutrition 0.000 description 13
- 230000000052 comparative effect Effects 0.000 description 13
- 239000007916 tablet composition Substances 0.000 description 8
- 230000000704 physical effect Effects 0.000 description 7
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 6
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 6
- 239000008101 lactose Substances 0.000 description 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
- 238000000034 method Methods 0.000 description 6
- 239000007788 liquid Substances 0.000 description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- 238000007906 compression Methods 0.000 description 4
- 230000006835 compression Effects 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 239000000454 talc Substances 0.000 description 4
- 229910052623 talc Inorganic materials 0.000 description 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 3
- 238000005299 abrasion Methods 0.000 description 3
- 239000011668 ascorbic acid Substances 0.000 description 3
- 235000010323 ascorbic acid Nutrition 0.000 description 3
- 229960005070 ascorbic acid Drugs 0.000 description 3
- 239000006185 dispersion Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 235000019359 magnesium stearate Nutrition 0.000 description 3
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 3
- 239000008108 microcrystalline cellulose Substances 0.000 description 3
- 229940016286 microcrystalline cellulose Drugs 0.000 description 3
- 238000000465 moulding Methods 0.000 description 3
- 238000006386 neutralization reaction Methods 0.000 description 3
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 description 2
- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 description 2
- 238000007907 direct compression Methods 0.000 description 2
- 210000000936 intestine Anatomy 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 238000006467 substitution reaction Methods 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- ABBQHOQBGMUPJH-UHFFFAOYSA-M Sodium salicylate Chemical compound [Na+].OC1=CC=CC=C1C([O-])=O ABBQHOQBGMUPJH-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 229930003451 Vitamin B1 Natural products 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 229920013820 alkyl cellulose Polymers 0.000 description 1
- FQPFAHBPWDRTLU-UHFFFAOYSA-N aminophylline Chemical compound NCCN.O=C1N(C)C(=O)N(C)C2=C1NC=N2.O=C1N(C)C(=O)N(C)C2=C1NC=N2 FQPFAHBPWDRTLU-UHFFFAOYSA-N 0.000 description 1
- 229960003556 aminophylline Drugs 0.000 description 1
- 150000008064 anhydrides Chemical group 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 125000002057 carboxymethyl group Chemical class [H]OC(=O)C([H])([H])[*] 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 239000012153 distilled water Substances 0.000 description 1
- BXKDSDJJOVIHMX-UHFFFAOYSA-N edrophonium chloride Chemical compound [Cl-].CC[N+](C)(C)C1=CC=CC(O)=C1 BXKDSDJJOVIHMX-UHFFFAOYSA-N 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000007542 hardness measurement Methods 0.000 description 1
- 229920013821 hydroxy alkyl cellulose Polymers 0.000 description 1
- 229910052742 iron Inorganic materials 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000000691 measurement method Methods 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 239000000449 pharmaceutical disintegrant Substances 0.000 description 1
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 229960004025 sodium salicylate Drugs 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000009967 tasteless effect Effects 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 229960003495 thiamine Drugs 0.000 description 1
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 description 1
- 235000010374 vitamin B1 Nutrition 0.000 description 1
- 239000011691 vitamin B1 Substances 0.000 description 1
- 235000019158 vitamin B6 Nutrition 0.000 description 1
- 239000011726 vitamin B6 Substances 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Description
本発明は直接打錠成型することにより、硬度な
らびに崩壊性に優れた固形薬剤を得ることのでき
る粉粒体組成物に関するものであり、詳しくは、
特定範囲の嵩比重を有する繊維素グリコール酸カ
ルシウムを崩壊剤として配合してなる粉粒体組成
物に関するものである。
固形薬剤は経口摂取後、胃や腸の消化液中で崩
壊し、薬効成分を放出し、胃や腸の壁面から人体
に薬効成分を吸収させるものであるが、取扱い時
は形状が安定して保持されながら、消火液中での
崩壊を充分に行わせるため、多くの場合崩壊剤が
配合使用される。繊維素グリコール酸カルシウム
は医薬用崩壊剤として最も多用されているが、無
味、無臭、白色であつて崩壊性、膨潤倍率、圧縮
成形性などが良好であるなどの利点を有するため
であり、カルボキシメチルセルロースカルシウム
として日本薬局方に収載され、ECG−505の商品
名（ニチリン化学工業株式会社製造）で市販され
ている。
しかしながら薬効成分の種類によつてはカルシ
ウムと反応性のあるものには使用できないこと
や、崩壊剤を多量に用いると固形薬剤の強度が不
足するなどの問題点が指摘されている。従つてそ
の他の崩壊剤として、澱粉、ホルマール化ゼラチ
ン、アルギン酸、繊維素グリコール酸（遊離酸
型）、低置換度ヒドロキシアルキルセルロース、
低置換度アルキルセルロースなどが提案されてお
り、一部使用されているが、着色性のあるもの、
味のわるいもの、多量に使用しないと崩壊が充分
でないものなどそれぞれ問題点を有しており、総
合的にみて繊維素グリコール酸カルシウムに勝る
ものは見出されていない。因みに繊維素グリコー
ル酸カルシウムはECG−505の単一グレード商品
のみが市販されており、一般的な性質は水中１重
量％分散液の媒体のPHは５〜5.5で、粘度は200メ
ツシユ通過、無水グルコース単位当りのカルボキ
シメチル基の置換度は0.55〜0.6である。この水
中１％分散液の媒体PHを以下中和度と呼称する。
発明者等は種々検討の結果、崩壊剤に使用する
繊維素グリコール酸カルシウムとして、比較的嵩
比重の小さいものを使用することにより、同じ重
量の崩壊剤を使用した場合従来のものより硬度の
大きい錠剤が得られることを見出した。その効果
は、成型前の粉粒体組成物中の共有する他の成分
の物性や打錠条件によつて多少異なるが、同程度
の崩壊性であれば硬度の改良された錠剤が、同程
度の硬度であれば崩壊性にすぐれた錠剤をうるも
のである。
本発明に使用するのに適当な繊維素グリコール
酸カルシウムの嵩比重は250g／以上、550g／
以下である。嵩比重550g／以上であれば、
従来の市販品と同様であり250g／以下である
と、粉粒体の流動性が悪くなり打錠の際の充填性
が悪くなる。ここでいう粉体嵩比重とは次の方法
で測定した値である。
嵩比重測定方法
200mlメスシリンダーを用意し、粉体試料を200
ml目盛まで徐々に投入し、層積する。メスシリン
ダーの底部と床面の距離が５cmになる様持ち上げ
て手を離し、シリンダーを落下させる。この操作
を10回繰り返した後の容積（ml）を読み取つた
後、粉体試料の重量を量る。
嵩比重（ｇ／）＝〔重量（ｇ）／容積（ml）〕×
1000
本発明はまた、薬効成分が水溶性薬剤であると
き特に有効である。一般にサルチル酸ナトリウ
ム、ビタミンB1、ビタミンB6、アスコルビン
酸、塩酸エフエドリン、アミノフイリンなどの水
溶性薬剤を薬効成分とする固形薬剤は、崩壊性の
よいものは得やすいが、打錠時にキヤツピングを
起こしやすく、硬度にすぐれたものが得られ難い
傾向があるので、本発明の組成物はその問題点を
解決するものである。
尚、本発明に使用する嵩比重の小さい繊維素グ
リコール酸カルシウムも、その製造方法は特公昭
43−7960に示された方法に準じており、繊維素グ
リコール酸の遊離酸型のものに湿潤状態で炭酸カ
ルシウムを作用させることによつて得られるが、
原料繊維素のグリコール酸の無水グリコース残基
あたりの置換度が比較的低く、且つ中和度も低PH
域に止めることにより嵩比重の小さい繊維素グリ
コール酸カルシウムを得ることができる。
以下に実施例及び参考例をあげて本発明を具体
的に説明する。
実施例１及び比較例１
嵩比重の異なる繊維素グリコール酸カルシウム
を崩壊剤として使用し、薬効成分としてアスコル
ビン酸、賦形剤として乳糖を配合した粉粒体組成
物から直打法によつて錠剤を製造した。
錠剤組成及び製剤条件は次の通りである。
錠剤組成
アスコルビン酸 50.0
乳糖 43.5
崩壊剤 5.0
タルク 1.0
ステアリン酸マグネシウム 0.5
100.0重量％
打錠条件
打錠機：畑鉄工所、HT−pl8A
成型条件：錠径８mmφ、錠剤厚み４mm
重量210mg、打錠圧1.1ton
錠剤物性は次の方法で測定した。
崩壊性 日本薬局方準拠崩壊度試験機
（富山産業株式会社）
測定温度：37±２℃
試験液：水及び局方第１液（人工胃液）
ｎ＝10：崩壊に要する時間の平均値で示
す。
硬度 モンサント硬度計使用
磨損度 萓垣式摩損度試験機
25回転 ３分間処理
100個の錠剤を処理し粉末化したもの
の重量を百分率で示す。
第１表に錠剤の物性と崩壊剤として使用した繊
維グリコール酸カルシウムの性状を示す。
（*但し、中和度は試料を100倍の蒸留水に分散
させたときの媒体のPHで表わす。）
The present invention relates to a powder composition that can be directly compressed into a tablet to obtain a solid drug with excellent hardness and disintegrability.
The present invention relates to a powder composition containing cellulose calcium glycolate having a bulk specific gravity within a specific range as a disintegrant. After solid drugs are orally ingested, they disintegrate in the digestive juices of the stomach and intestines, releasing their medicinal ingredients and allowing them to be absorbed into the human body through the walls of the stomach and intestines, but their shape remains stable during handling. A disintegrating agent is often used in combination to ensure sufficient disintegration in the extinguishing liquid while being retained. Calcium glycolate is most commonly used as a pharmaceutical disintegrant because it has advantages such as being tasteless, odorless, white, and having good disintegration properties, swelling ratio, compression moldability, etc. It is listed in the Japanese Pharmacopoeia as methylcellulose calcium and is commercially available under the trade name ECG-505 (manufactured by Nichirin Chemical Industry Co., Ltd.). However, problems have been pointed out, such as the inability to use certain medicinal ingredients that are reactive with calcium, and the use of a large amount of disintegrant, resulting in insufficient strength of the solid drug. Therefore, other disintegrants include starch, formalized gelatin, alginic acid, cellulose glycolic acid (free acid type), low-substituted hydroxyalkylcellulose,
Low-substituted alkylcelluloses have been proposed and are used in some cases, but those with coloring properties,
Each of them has its own problems, such as those that taste bad and those that do not disintegrate sufficiently unless used in large quantities, and overall, no one has been found that is superior to cellulose calcium glycolate. Incidentally, only a single grade product of ECG-505 is commercially available for cellulose calcium glycolate, and the general properties are that the pH of the medium of a 1% by weight dispersion in water is 5 to 5.5, the viscosity is 200 mesh passing, and it is anhydrous. The degree of substitution of carboxymethyl groups per glucose unit is 0.55-0.6. The medium pH of this 1% dispersion in water is hereinafter referred to as the degree of neutralization. As a result of various studies, the inventors found that by using a cellulose calcium glycolate that has a relatively low bulk specific gravity as a disintegrant, the hardness is greater than that of conventional ones when the same weight of disintegrant is used. It has been found that tablets can be obtained. The effect varies somewhat depending on the physical properties of other components in the powder composition before molding and the tableting conditions, but if the disintegration property is the same, the tablet with improved hardness will be the same. If the hardness is , it is possible to obtain tablets with excellent disintegration properties. The bulk specific gravity of cellulose calcium glycolate suitable for use in the present invention is 250 g/or more, 550 g/
It is as follows. If the bulk specific gravity is 550g/or more,
This is the same as conventional commercially available products, and if it is 250 g/or less, the fluidity of the powder and granules will be poor and the filling properties during tableting will be poor. The powder bulk specific gravity referred to here is a value measured by the following method. Bulk specific gravity measurement method Prepare a 200ml graduated cylinder and add 200ml of powder sample.
Gradually add to the ml mark and layer. Lift the graduated cylinder so that the distance between the bottom and the floor is 5 cm, release your hand, and let the cylinder fall. After repeating this operation 10 times and reading the volume (ml), weigh the powder sample. Bulk specific gravity (g/) = [weight (g)/volume (ml)] x
1000 The present invention is also particularly effective when the medicinal ingredient is a water-soluble drug. In general, solid drugs containing water-soluble drugs such as sodium salicylate, vitamin B1, vitamin B6, ascorbic acid, efuedrine hydrochloride, and aminophylline as medicinal ingredients have good disintegration properties, but are susceptible to capping during tablet compression. However, since it tends to be difficult to obtain a material with excellent hardness, the composition of the present invention solves this problem. In addition, the production method of the cellulose calcium glycolate, which has a small bulk specific gravity and is used in the present invention, is
43-7960, and is obtained by treating the free acid form of cellulose glycolic acid with calcium carbonate in a wet state.
The degree of substitution per glycose anhydride residue of glycolic acid in raw material cellulose is relatively low, and the degree of neutralization is also low PH.
By keeping the amount within the range, it is possible to obtain cellulose calcium glycolate having a small bulk specific gravity. The present invention will be specifically explained below with reference to Examples and Reference Examples. Example 1 and Comparative Example 1 Tablets were made by direct compression from a powder composition containing cellulose calcium glycolate having different bulk specific gravity as a disintegrant, ascorbic acid as a medicinal ingredient, and lactose as an excipient. was manufactured. The tablet composition and formulation conditions are as follows. Tablet composition Ascorbic acid 50.0 Lactose 43.5 Disintegrant 5.0 Talc 1.0 Magnesium stearate 0.5 100.0% by weight Tableting conditions Tablet machine: Hata Iron Works, HT-pl8A Molding conditions: Tablet diameter 8 mmφ, tablet thickness 4 mm Weight 210 mg, tablet pressure 1.1 The physical properties of the tablets were measured using the following method. Disintegration Disintegration tester according to the Japanese Pharmacopoeia (Toyama Sangyo Co., Ltd.) Measurement temperature: 37±2℃ Test liquid: Water and Pharmacopoeia No. 1 liquid (artificial gastric fluid) n=10: Shown as the average value of the time required for disintegration . Hardness: Uses Monsanto hardness tester. Abrasion level: Hagaki type abrasion tester. 25 rotations, 3 minutes treatment. The weight of the powdered product obtained by processing 100 tablets is shown as a percentage. Table 1 shows the physical properties of the tablet and the properties of the fiber calcium glycolate used as a disintegrant. ( * However, the degree of neutralization is expressed as the pH of the medium when the sample is dispersed in 100 times the volume of distilled water.)
【表】
打錠時のキヤツピング発生は比較例１（使用繊
維素グリコール酸カルシウムはECG−505規格相
当品）の場合22個／100個であつたが、、実施例１
はキヤツピングは全く発生せずスムースに成型が
できた。また、実施例１は比較例１に比し崩壊性
が殆んど同じで硬度摩損度の向上した錠剤が得ら
れた。
実施例２及び比較例２
実施例１及び比較例１に用いたのと同じ崩壊剤
を用い、賦形剤として乳糖のほかに微結晶セルロ
ース（アビセルPH101旭化成製）を添加し、硬
度の高い錠剤の得られる組成を用いて同様に製剤
した。
錠剤組成及び製剤条件は次の通りである。
錠剤組成
アスコルビン 50.0
微結晶セルロース 28.0
乳糖 14.0
崩壊剤 5.0
タルク 2.5
ステアリン酸マグネシウム 0.5
100.0重量％
打錠条件
打錠機：菊水製作所製、クリーンプレスコレク
ト 24
成型条件：錠径８mmφ、錠剤厚み４mm、
重量200mg、打錠圧1ton
錠剤物性は次の方法で測定した。
硬度 試験機：テンシロンUTM−１
（東洋精機）
圧縮ロードセル：100Kg／cm2
圧壊荷重棒直径：2.0mm
圧縮速度 ：0.4mm／min
摩損度、崩壊性、実施例１に同じ。
測定結果を第２表に示す。[Table] The occurrence of capping during tableting was 22/100 in Comparative Example 1 (the cellulose calcium glycolate used was equivalent to the ECG-505 standard), but in Example 1.
was able to be molded smoothly without any capping. In addition, in Example 1, tablets with almost the same disintegration properties and improved hardness and friability compared to Comparative Example 1 were obtained. Example 2 and Comparative Example 2 The same disintegrant as used in Example 1 and Comparative Example 1 was used, and microcrystalline cellulose (Avicel PH101 manufactured by Asahi Kasei) was added as an excipient in addition to lactose to form tablets with high hardness. A similar formulation was made using the resulting composition. The tablet composition and formulation conditions are as follows. Tablet composition Ascorbine 50.0 Microcrystalline cellulose 28.0 Lactose 14.0 Disintegrant 5.0 Talc 2.5 Magnesium stearate 0.5 100.0% by weight Tableting conditions Tableting machine: Kikusui Seisakusho, Clean Press Collect 24 Molding conditions: Tablet diameter 8 mmφ, tablet thickness 4 mm, Weight 200 mg , tableting pressure 1 ton Tablet physical properties were measured by the following method. Hardness Testing machine: Tensilon UTM-1 (Toyo Seiki) Compression load cell: 100Kg/cm 2 Crushing load rod diameter: 2.0mm Compression speed: 0.4mm/min Friability, collapsibility, same as Example 1. The measurement results are shown in Table 2.
【表】
打錠時のキヤツピング発生は、比較例２（ECG
−505規格相当品使用）の場合７個／100個であつ
たが、実施例２では全く発生しなかつた。実施例
は比較例に比し、硬度は略同程度であるが、崩壊
性、磨損度においてすぐれていた。
実施例３及び比較例３
薬効成分としてアスピリンを用いた粉粒体組成
物から直打法によつて錠剤を製造し、錠剤物性を
測定した。
錠剤組成
アスピリン 55.0
微結晶セルロース 21.5
乳糖 10.5
崩壊剤 10.0
タルク 2.5
ラブリーワツクス 0.5 （フロイント産業製滑沢剤）
100.0重量％
打錠条件及び錠剤物性測定方法は実施例２と同
様の方法を用いた。
測定結果を第３表に示す。[Table] The occurrence of capping during tableting was compared with Comparative Example 2 (ECG
-505 (using a product equivalent to the standard), the number was 7/100, but in Example 2, no such occurrence occurred. The Examples had approximately the same hardness as the Comparative Examples, but were superior in collapsibility and abrasion. Example 3 and Comparative Example 3 Tablets were manufactured from powder compositions using aspirin as a medicinal ingredient by a direct compression method, and the physical properties of the tablets were measured. Tablet composition Aspirin 55.0 Microcrystalline cellulose 21.5 Lactose 10.5 Disintegrant 10.0 Talc 2.5 Lovely Wax 0.5 (Lubricant manufactured by Freund Industries) 100.0% by weight The same methods as in Example 2 were used for the tableting conditions and the method for measuring the physical properties of the tablets. The measurement results are shown in Table 3.
【表】
比較例３は特に嵩比重の大きな崩壊剤を使用し
た例である。実施例は比較例に比し、崩壊性が略
同等であるが硬度にすぐれた錠剤を得た。
参考例
嵩比重の異なる繊維素グリコール酸カルシウム
を崩壊剤として使用し、薬効成分を含まない模擬
錠剤を作製し、同様に錠剤物性を測定した。
錠剤組成
乳糖 93.5
崩壊剤 5.0
タルク 1.0
ステアリン酸マグネシウム 0.5
100.0重量％
打錠条件
粉粒体組成物0.75gを15mmφの杵を用い厚さ４
mmの錠剤に成型。
崩壊性
25mmφ×2mの管中に局方第１液（人工胃液）
を満し、水面から錠剤を落して液中に落下させ、
完全に分散するのに要する時間を測定した。
測定結果を第４表に示す。[Table] Comparative Example 3 is an example in which a disintegrant having a particularly large bulk specific gravity was used. Tablets were obtained in the Examples, which had substantially the same disintegrability as the Comparative Examples, but were superior in hardness. Reference Example Using cellulose calcium glycolate with different bulk specific gravity as a disintegrant, simulated tablets containing no medicinal ingredients were prepared, and the physical properties of the tablets were measured in the same manner. Tablet composition: Lactose 93.5 Disintegrant: 5.0 Talc: 1.0 Magnesium stearate: 0.5 100.0% by weight Tableting conditions: 0.75 g of the powder composition was rolled using a 15 mmφ punch to a thickness of 4
Molded into mm tablets. Disintegratability Pharmacopoeia No. 1 liquid (artificial gastric juice) in a 25mmφ x 2m tube
, drop the tablet from the water surface into the liquid,
The time required for complete dispersion was measured. The measurement results are shown in Table 4.
【表】
比較例４に使用した繊維素グリコール酸カルシ
ウムはECG−505規格相当品であるが比較例１〜
３に使用したものとは製造ロツトが異なる。
上記の結果からみてこの発明に用いられる嵩比
重の小さい繊維素グリコール酸カルシウムを用い
た参考例の模擬錠剤の方が比較例４のそれよりも
崩壊性と硬度ともに優れていた。[Table] The cellulose calcium glycolate used in Comparative Example 4 is equivalent to the ECG-505 standard, but Comparative Examples 1~
The production lot is different from that used in 3. In view of the above results, the simulated tablet of the reference example using cellulose calcium glycolate with a small bulk specific gravity used in the present invention was superior to that of comparative example 4 in both disintegration and hardness.
Claims (1)
加えられる添加剤からなる粉粒体組成物におい
て、崩壊剤が嵩比重250g／以上、550g／以
下の繊維素グリコール酸カルシウムであることを
特徴とする固形薬剤用粉粒体組成物。 ２ 薬効成分が水溶性薬剤である特許請求の範囲
第１項記載の固形薬剤用粉粒体組成物。[Scope of Claims] 1. A powder composition comprising a medicinal ingredient, an excipient, a disintegrant, and additives added as necessary, in which the disintegrant is cellulose glycol with a bulk specific gravity of 250 g/ to 550 g/ A powder composition for a solid drug, characterized in that it is calcium acid. 2. The powder composition for a solid drug according to claim 1, wherein the medicinal ingredient is a water-soluble drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5301583A JPS59176217A (en) | 1983-03-28 | 1983-03-28 | Powder composition for solid pharmaceutical preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP5301583A JPS59176217A (en) | 1983-03-28 | 1983-03-28 | Powder composition for solid pharmaceutical preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS59176217A JPS59176217A (en) | 1984-10-05 |
| JPH0526770B2 true JPH0526770B2 (en) | 1993-04-19 |
Family
ID=12931073
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP5301583A Granted JPS59176217A (en) | 1983-03-28 | 1983-03-28 | Powder composition for solid pharmaceutical preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS59176217A (en) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS59193815A (en) * | 1983-04-15 | 1984-11-02 | Daicel Chem Ind Ltd | Preparation of tablet |
| JPS6048934A (en) * | 1983-08-29 | 1985-03-16 | Daicel Chem Ind Ltd | Powdery composition for tablet |
| JP4698000B2 (en) * | 2000-06-27 | 2011-06-08 | 旭化成ケミカルズ株式会社 | Easily water-soluble drug-containing tablets |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5247914A (en) * | 1975-10-11 | 1977-04-16 | Lilly Industries Ltd | Tablet and its prepation |
| JPS5827984A (en) * | 1981-08-10 | 1983-02-18 | Kurisutaru Eng Kk | Regenerating method for alkali etching solution of aluminum and alloy thereof |
| JPS5842722A (en) * | 1981-09-08 | 1983-03-12 | Kawasaki Steel Corp | Manufacture of steel with not less than 55kgf/mm2 yield strength or offset yield stress strength at 0.2% permanent set and superior resistance to sulfide stress corrosion cracking |
-
1983
- 1983-03-28 JP JP5301583A patent/JPS59176217A/en active Granted
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5247914A (en) * | 1975-10-11 | 1977-04-16 | Lilly Industries Ltd | Tablet and its prepation |
| JPS5827984A (en) * | 1981-08-10 | 1983-02-18 | Kurisutaru Eng Kk | Regenerating method for alkali etching solution of aluminum and alloy thereof |
| JPS5842722A (en) * | 1981-09-08 | 1983-03-12 | Kawasaki Steel Corp | Manufacture of steel with not less than 55kgf/mm2 yield strength or offset yield stress strength at 0.2% permanent set and superior resistance to sulfide stress corrosion cracking |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS59176217A (en) | 1984-10-05 |
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