JPS63243034A - Solid agent containing low-melting substance - Google Patents

Solid agent containing low-melting substance

Info

Publication number
JPS63243034A
JPS63243034A JP7398087A JP7398087A JPS63243034A JP S63243034 A JPS63243034 A JP S63243034A JP 7398087 A JP7398087 A JP 7398087A JP 7398087 A JP7398087 A JP 7398087A JP S63243034 A JPS63243034 A JP S63243034A
Authority
JP
Japan
Prior art keywords
calcium silicate
substance
vitamin
melting point
low
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.)
Granted
Application number
JP7398087A
Other languages
Japanese (ja)
Other versions
JP2626975B2 (en
Inventor
Kimio Tateishi
立石 公男
Norio Shimogaki
紀夫 下垣
Satoru Yamagiwa
山際 哲
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Eisai Co Ltd
Original Assignee
Eisai Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Eisai Co Ltd filed Critical Eisai Co Ltd
Priority to JP62073980A priority Critical patent/JP2626975B2/en
Publication of JPS63243034A publication Critical patent/JPS63243034A/en
Application granted granted Critical
Publication of JP2626975B2 publication Critical patent/JP2626975B2/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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  • Medicinal Preparation (AREA)

Abstract

PURPOSE:To obtain a solid agent having sufficient hardness causing neither sticking nor capping, by blending a low-melting substance with a specific amount of calcium silicate. CONSTITUTION:A low-melting substance having <=60 deg.C melting point is blended with >=30wt.% calcium silicate as an absorbent and, if necessary, a drug, silicic anhydride or other additives and pharmaceutically manufactured by a conventional procedure to give the aimed substance. A vitamin E-related substance is used as the low-melting substance and d-alpha-tocopherol and vitamin A palmitate may be cited. The calcium silicate has 0.08-0.12 apparent specific gravity and large bulk and liquid absorption amount and specific calcium silicate of jairolite type (trade name furolite R) is preferable.

Description

【発明の詳細な説明】 産業上の利用分野 本発明は低融点物質を含有する固形剤に関する。[Detailed description of the invention] Industrial applications The present invention relates to solid formulations containing low melting point substances.

詳しくは本発明は低融点物質にケイ酸カルシウムを配合
して成る高含量の低融点物質を含有する固形剤に関する
More specifically, the present invention relates to a solid formulation containing a high content of a low melting point substance, which is formed by blending the low melting point substance with calcium silicate.

発明の背景 従来ビタミンEやビタミンE二/コチン酸エステルのよ
うな油性薬物及びメンフェゴールや生薬エキスなどの低
融点薬物を含有する固形剤の製造に当たっては、軽質無
水ケイ酸などに該薬物を吸着させていた。
Background of the Invention Conventionally, in the production of solid preparations containing oil-based drugs such as vitamin E and vitamin E di/cotinic acid esters, and low-melting point drugs such as memphegol and herbal medicine extracts, the drugs have been adsorbed onto light silicic anhydride or the like. was.

このような方法の欠点は例えば錠剤の場合に打錠時にス
ティッキング(sticking)や、キャッピング(
capping)を生ずることがあり、また硬度不足の
ため実際の生産上において欠けや割れの発生することが
ある。品質上にも問題があった。そのため固形剤におい
て大量の吸着剤を使用しなければならず、したがって薬
物の含量は極めて少量に制限せざるを得なかった。
Disadvantages of such methods include, for example, sticking and capping during tablet compression.
capping), and chipping or cracking may occur during actual production due to insufficient hardness. There were also quality issues. Therefore, a large amount of adsorbent must be used in solid preparations, and the drug content must therefore be limited to an extremely small amount.

発明の駐 本発明者らは今回、吸着剤としてケイ酸カルシウムを使
用することにより上記のすべての問題が解決できること
を見出した。すなわち低融点薬物に対して30重量%以
上のケイ酸カルシウムを配合した場合にスティッキング
やキャッピングを起さず、十分な硬度を有する固形剤が
得られるのである。換言すれば、ケイ酸カルシウムを使
用した場合にケイ酸カルシウムに対して、その約3.3
倍までの薬物を含有させることができるのである。
The present inventors have now discovered that all of the above problems can be solved by using calcium silicate as an adsorbent. In other words, when 30% by weight or more of calcium silicate is blended with the low melting point drug, a solid agent that does not cause sticking or capping and has sufficient hardness can be obtained. In other words, when calcium silicate is used, about 3.3
It is possible to contain up to twice as much drug.

本発明において使用されるケイ酸カルシウムは、見掛比
重0.08〜0,12を有し、嵩及び吸液量の大きいも
のであり、特に好ましいケイ酸カルシウムは化学式: %式% (式中、I<m<2.2<n<3である。)で示される
ジャイロライト型特殊ケイ酸カルシウムであり、徳山曹
達株式会社から「フローライトR」の商品名で市販され
ているものである。このフローライトRは粉体であり、
嵩が大きく成形性が良好である。また安全性については
日本薬局方外医薬品コード4600及び汎用化粧品原料
1−50に収載されており、米国薬局方(NF−XVI
)のケイ酸カルシウムの規格値にも適合する。
The calcium silicate used in the present invention has an apparent specific gravity of 0.08 to 0.12, and has a large volume and liquid absorption. Particularly preferable calcium silicate has the chemical formula: % formula % (in the formula , I<m<2.2<n<3.), and is commercially available from Tokuyama Soda Co., Ltd. under the trade name "Fluorite R". . This Fluorite R is a powder,
It has a large bulk and good moldability. Regarding safety, it is listed in the Japanese Non-Pharmaceutical Drug Code 4600 and General Purpose Cosmetic Ingredients 1-50, and is listed in the United States Pharmacopoeia (NF-XVI
) also meets the standard values for calcium silicate.

本発明の低融点物質上しては、例えばd−α−トコフェ
ロール、dσ−α−トコフェロール、d−α−酢酸トコ
フェロール、dρ−α−酢酸トコフエa−fiv、d(
1−α−ニコチン酸トコフェロール、ビタミンAパルミ
テート、フィトナジオン、メナテトレノン、ユビデカレ
ノン、メンフェゴール、テブレノンならびにカッコソー
軟エキス、トウキ軟エキス及びセンキュー軟エキスのよ
うな生薬軟エキスなどがある。
Examples of the low melting point substances of the present invention include d-α-tocopherol, dσ-α-tocopherol, d-α-tocopherol acetate, dρ-α-tocopherol acetate a-fiv, d(
Examples include tocopherol 1-α-nicotinate, vitamin A palmitate, phytonadione, menatetrenone, ubidecarenone, memphegol, tebrenone, and soft extracts of herbal medicines such as kakkoso soft extract, touki soft extract, and senkyu soft extract.

本発明の固形剤は錠剤、顆粒、カプセル剤、フィルム錠
、糖衣錠、細粒、又は散剤などのような形態であること
ができる。
The solid dosage form of the present invention can be in the form of tablets, granules, capsules, film tablets, sugar-coated tablets, fine granules, or powders.

本発明の固形剤(j、他の薬物、無水ケイ酸又はその他
の添加剤を配合することができる。
The solid agent of the present invention (j) may contain other drugs, silicic anhydride, or other additives.

次に、実施例を掲げて本発明を更に具体的lこ説明する
Next, the present invention will be explained in more detail with reference to Examples.

3一 実施例 1 ヘンシェルミキサーFM−25[(株)三井三池製作断
裂コ?こフローライトR3609を入れ、混合しながら
酢酸dC−α−トコフェロール36ogを添加し、フロ
ーライトRに吸着させた。その後メチルセルロース36
gを添加し、常法にしたがい造粒、乾燥、整粒を行い酢
酸 dσ−α−トコフェロールの吸着顆粒を得た。
31 Example 1 Henschel Mixer FM-25 [Made by Mitsui Miike Co., Ltd.] This Fluorite R3609 was added, and while mixing, 36 og of dC-α-tocopherol acetate was added and adsorbed onto Fluorite R. Then methyl cellulose 36
g was added thereto, followed by granulation, drying, and granulation according to a conventional method to obtain adsorbed granules of dσ-α-tocopherol acetate.

この顆粒100部に噴霧乳糖90部、タルク1o部を添
加して混合し、打錠用粉末を得た。これをロータリー型
打錠機で1錠200mgとなるように製錠した。
90 parts of atomized lactose and 10 parts of talc were added to 100 parts of the granules and mixed to obtain a powder for tabletting. This was tableted using a rotary tablet machine so that each tablet weighed 200 mg.

実施例 2 フローライトRを540gにした点を除いて、実施例1
の手順をくり返した。
Example 2 Example 1 except that Fluorite R was 540 g.
The procedure was repeated.

実施例 3 フローライトRが2409であった点を除いて実施例1
の手順をくり返した。
Example 3 Example 1 except that Fluorite R was 2409
The procedure was repeated.

実施例 4 フローライトRが144gであった点を除いて実施例1
の手順をくり返した。
Example 4 Example 1 except that Fluorite R was 144 g.
The procedure was repeated.

=4一 対照例 A フローライトRの代りに無水ケイ酸、沈降製、サイロー
ド244(商品名) 360gを使用した点を除いて実
施例1の手順をくり返した。
=4 - Control Example A The procedure of Example 1 was repeated except that 360 g of Silicic Anhydride, Cylord 244 (trade name) manufactured by Seikan Co., Ltd., was used instead of Fluorite R.

対照例 B フローライトRの代わりに無水ケイ酸水加物〔カープレ
ックス(商品名))36hを使用した点を除いて実施例
1の手順をくり返した。
Control Example B The procedure of Example 1 was repeated except that Fluorite R was replaced by silicic anhydride hydrate (Carplex (trade name)) 36h.

上記のようにして製造した錠剤について、打錠障害発生
の有無を下表に総括して示す。
The table below summarizes the presence or absence of tableting failure for the tablets produced as described above.

実施例1並びに対照例A及びBにおいて得られた錠剤の
硬度(本屋式硬度計による)と打錠圧との関係を図面に
示す。ケイ酸カルシウムの使用によりすぐれた硬度が得
られることがわかる。
The relationship between the hardness of the tablets obtained in Example 1 and Control Examples A and B (according to a Honya type hardness tester) and tableting pressure is shown in the drawing. It can be seen that excellent hardness can be obtained by using calcium silicate.

実施例 5 dり一α−M’lトコフェロール500gとフローライ
トR150gとをヘンシェルミキサーFM25((株)
三井三池製作所製〕で10分間混合し、更に適量の水を
加えて細粒状になるまで混合した。
Example 5 500 g of d Riichi α-M'l tocopherol and 150 g of Fluorite R were mixed in a Henschel mixer FM25 (Co., Ltd.).
(manufactured by Mitsui Miike Seisakusho) for 10 minutes, and then an appropriate amount of water was added and mixed until the mixture became fine granules.

このものを常法にしたがって乾燥後篩分して32メツシ
ユから150メツシユまでの間の乾燥物を得た。
This material was dried in a conventional manner and then sieved to obtain a dry product having a size of 32 to 150 meshes.

このものは日本薬局方の細粒剤規格に適合する粒度分布
であった。
This product had a particle size distribution that met the Japanese Pharmacopoeia's fine granule standards.

実施例 6 実施例1で得た錠剤1000gを常法のパン・コーティ
ング法により下記糖衣液を用いて1錠360mgになる
まで糖衣を行い、カルナウバロウにより艶出しを行って
糖衣錠1800gを得た。
Example 6 1,000 g of the tablets obtained in Example 1 were sugar-coated using the following sugar-coating solution by a conventional pan coating method until each tablet weighed 360 mg, and then glazed with carnauba wax to obtain 1,800 g of sugar-coated tablets.

糖衣液処方 白 糖      600部 タルク        80部 アラビアゴム末    20部 実施例 7 実施例1で得た錠剤300gを71イコーター・ミニ〔
(株)フロイント製〕を用いて、下記フィルム液により
フィルムコーティング操作を1錠210mgになるまで
行い、フィルム錠を得た。
Sugar Coating Solution White Sugar 600 parts Talc 80 parts Gum Arabic powder 20 parts Example 7 300 g of the tablets obtained in Example 1 were added to 71 Ecoater Mini [
(manufactured by Freund Co., Ltd.), film coating was performed using the following film solution until each tablet weighed 210 mg to obtain film tablets.

フィルム液処方 ヒドロキシプロピルメチルセルロース 75部(信越化
学制、商品名TC−5R) ポリエチレングリコール6000     25部エチ
ルアルコール        500部実施例 8 da−α−ニコチン酸トコフェロール(融点45℃ニア
− 常温では固体)を約80℃で過温して液状化し、その5
00gとフローライトR300mgとをヘンシェルミキ
サーFM−25C(株)三井三池製作所製〕でIO分間
混合し、後は実施例5と同様に操作して日本薬局方の細
粒剤規格に適合する細粒剤を得た。
Film liquid formulation Hydroxypropyl methylcellulose 75 parts (Shin-Etsu Chemical, trade name TC-5R) Polyethylene glycol 6000 25 parts Ethyl alcohol 500 parts Example 8 Tocopherol da-α-nicotinate (melting point 45°C near- solid at room temperature) was added to approx. Liquefied by overheating at 80℃, Part 5
00g and 300mg of Fluorite R were mixed for 10 minutes using a Henschel mixer FM-25C (manufactured by Mitsui Miike Seisakusho Co., Ltd.), and then the same procedure as in Example 5 was performed to obtain fine granules that meet the Japanese Pharmacopoeia's fine granule standards. obtained the drug.

【図面の簡単な説明】[Brief explanation of drawings]

図面は実施例1ならびに対照例A及びBにおいて得られ
た錠剤の硬度と打錠圧力との関係を示すグラフ図である
The drawing is a graph showing the relationship between the hardness and tableting pressure of the tablets obtained in Example 1 and Control Examples A and B.

Claims (1)

【特許請求の範囲】 1、ケイ酸カルシウムを、低融点物質に対して30重量
%以上配合して成る固形剤。 2、低融点物質が融点60℃以下を有するものである特
許請求の範囲第1項記載の固形剤。 3、低融点物質が油性薬物である特許請求の範囲第1項
記載の固形剤。 4、油性薬物がビタミンE関連薬物である特許請求の範
囲第3項記載の固形剤。 5、ビタミンE関連物質がビタミンE、ビタミンE酢酸
エステル又はビタミンEニコチン酸エステルである特許
請求の範囲第4項記載の固形剤。 6、錠剤、顆粒、カプセル剤、フィルム錠、細粒又は散
剤の形態にある特許請求の範囲第1項記載の固形剤。
[Claims] 1. A solid agent containing 30% by weight or more of calcium silicate based on a low melting point substance. 2. The solid preparation according to claim 1, wherein the low melting point substance has a melting point of 60°C or less. 3. The solid preparation according to claim 1, wherein the low melting point substance is an oily drug. 4. The solid preparation according to claim 3, wherein the oil-based drug is a vitamin E-related drug. 5. The solid preparation according to claim 4, wherein the vitamin E-related substance is vitamin E, vitamin E acetate or vitamin E nicotinate. 6. The solid preparation according to claim 1, which is in the form of a tablet, granule, capsule, film tablet, fine granule or powder.
JP62073980A 1987-03-30 1987-03-30 Tablets containing low-melting oily substances Expired - Lifetime JP2626975B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP62073980A JP2626975B2 (en) 1987-03-30 1987-03-30 Tablets containing low-melting oily substances

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP62073980A JP2626975B2 (en) 1987-03-30 1987-03-30 Tablets containing low-melting oily substances

Publications (2)

Publication Number Publication Date
JPS63243034A true JPS63243034A (en) 1988-10-07
JP2626975B2 JP2626975B2 (en) 1997-07-02

Family

ID=13533757

Family Applications (1)

Application Number Title Priority Date Filing Date
JP62073980A Expired - Lifetime JP2626975B2 (en) 1987-03-30 1987-03-30 Tablets containing low-melting oily substances

Country Status (1)

Country Link
JP (1) JP2626975B2 (en)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11178895A (en) * 1997-12-22 1999-07-06 Nippon Kayaku Co Ltd Prevention of tabletting failure during tablet manufacture and manufacture of tablet
JPH11302157A (en) * 1998-04-17 1999-11-02 Eisai Co Ltd Tablet quickly disintegrating in oral cavity
JP2001294533A (en) * 2000-04-14 2001-10-23 Asahi Beer Yakuhin Kk Method for producing granulated material and tablet
WO2007097333A1 (en) * 2006-02-20 2007-08-30 Asahi Breweries, Ltd. Granules, tablets and method of producing the same
JP2009518321A (en) * 2005-12-07 2009-05-07 ニコメド ファーマ エイエス Pre-compressed calcium-containing compound
JP2009137892A (en) * 2007-12-06 2009-06-25 Asahi Kasei Chemicals Corp Powder for molding, compression molding composition using the same, and method for producing the powder for molding
WO2012091039A1 (en) * 2010-12-27 2012-07-05 富田製薬株式会社 Particulate formulation
WO2015099139A1 (en) 2013-12-27 2015-07-02 中外製薬株式会社 Solid preparation comprising tofogliflozin and method for producing same
CN112584710A (en) * 2019-06-06 2021-03-30 美国华纳国际生物科技股份有限公司 Self-emulsifying solid dispersion composition for medicine or health care product

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2858215A (en) * 1956-07-02 1958-10-28 Barnett Lab Inc Process of preparing vitamin oils in particle form
JPS5711911A (en) * 1980-06-25 1982-01-21 Tsumura Juntendo Inc Preparation of herb medicine tablet
JPS58213073A (en) * 1982-06-07 1983-12-10 Masatoshi Yamada Solidification of oily substance

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2858215A (en) * 1956-07-02 1958-10-28 Barnett Lab Inc Process of preparing vitamin oils in particle form
JPS5711911A (en) * 1980-06-25 1982-01-21 Tsumura Juntendo Inc Preparation of herb medicine tablet
JPS58213073A (en) * 1982-06-07 1983-12-10 Masatoshi Yamada Solidification of oily substance

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH11178895A (en) * 1997-12-22 1999-07-06 Nippon Kayaku Co Ltd Prevention of tabletting failure during tablet manufacture and manufacture of tablet
JPH11302157A (en) * 1998-04-17 1999-11-02 Eisai Co Ltd Tablet quickly disintegrating in oral cavity
JP2001294533A (en) * 2000-04-14 2001-10-23 Asahi Beer Yakuhin Kk Method for producing granulated material and tablet
JP2009518321A (en) * 2005-12-07 2009-05-07 ニコメド ファーマ エイエス Pre-compressed calcium-containing compound
WO2007097333A1 (en) * 2006-02-20 2007-08-30 Asahi Breweries, Ltd. Granules, tablets and method of producing the same
JP2009137892A (en) * 2007-12-06 2009-06-25 Asahi Kasei Chemicals Corp Powder for molding, compression molding composition using the same, and method for producing the powder for molding
WO2012091039A1 (en) * 2010-12-27 2012-07-05 富田製薬株式会社 Particulate formulation
JP5585920B2 (en) * 2010-12-27 2014-09-10 富田製薬株式会社 Particulate preparation
WO2015099139A1 (en) 2013-12-27 2015-07-02 中外製薬株式会社 Solid preparation comprising tofogliflozin and method for producing same
KR20160101719A (en) 2013-12-27 2016-08-25 추가이 세이야쿠 가부시키가이샤 Solid preparation comprising tofogliflozin and method for producing same
EP3482748A1 (en) 2013-12-27 2019-05-15 Chugai Seiyaku Kabushiki Kaisha Solid preparations containing tofogliflozin and method for producing the same
KR20210082557A (en) 2013-12-27 2021-07-05 추가이 세이야쿠 가부시키가이샤 Solid preparations containing tofogliflozin and process of producing the same
CN112584710A (en) * 2019-06-06 2021-03-30 美国华纳国际生物科技股份有限公司 Self-emulsifying solid dispersion composition for medicine or health care product

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