JPS63243035A - Bitter drug-containing solid agent and production thereof - Google Patents
Bitter drug-containing solid agent and production thereofInfo
- Publication number
- JPS63243035A JPS63243035A JP62073981A JP7398187A JPS63243035A JP S63243035 A JPS63243035 A JP S63243035A JP 62073981 A JP62073981 A JP 62073981A JP 7398187 A JP7398187 A JP 7398187A JP S63243035 A JPS63243035 A JP S63243035A
- Authority
- JP
- Japan
- Prior art keywords
- bitter drug
- bitter
- calcium silicate
- drug
- containing solid
- 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
Links
- 229940079593 drug Drugs 0.000 title claims abstract description 31
- 239000003814 drug Substances 0.000 title claims abstract description 30
- 239000007787 solid Substances 0.000 title claims abstract description 18
- 238000004519 manufacturing process Methods 0.000 title claims description 6
- 239000003795 chemical substances by application Substances 0.000 title abstract 3
- 239000000378 calcium silicate Substances 0.000 claims abstract description 17
- 229910052918 calcium silicate Inorganic materials 0.000 claims abstract description 17
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims abstract description 17
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims abstract description 12
- 238000002156 mixing Methods 0.000 claims abstract description 7
- 235000005152 nicotinamide Nutrition 0.000 claims abstract description 6
- 239000011570 nicotinamide Substances 0.000 claims abstract description 6
- FAPWYRCQGJNNSJ-UBKPKTQASA-L calcium D-pantothenic acid Chemical compound [Ca+2].OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O.OCC(C)(C)[C@@H](O)C(=O)NCCC([O-])=O FAPWYRCQGJNNSJ-UBKPKTQASA-L 0.000 claims abstract description 4
- 229960002079 calcium pantothenate Drugs 0.000 claims abstract description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims abstract 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims abstract 3
- 238000002360 preparation method Methods 0.000 claims description 14
- 235000013343 vitamin Nutrition 0.000 claims description 6
- 239000011782 vitamin Substances 0.000 claims description 6
- 229940088594 vitamin Drugs 0.000 claims description 6
- 229930003231 vitamin Natural products 0.000 claims description 6
- 150000003722 vitamin derivatives Chemical class 0.000 claims description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 3
- 238000001035 drying Methods 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 abstract description 10
- 235000019658 bitter taste Nutrition 0.000 abstract description 7
- 239000008187 granular material Substances 0.000 abstract description 5
- 239000000126 substance Substances 0.000 abstract description 3
- 238000010521 absorption reaction Methods 0.000 abstract description 2
- 240000000982 Malva neglecta Species 0.000 abstract 1
- 235000000060 Malva neglecta Nutrition 0.000 abstract 1
- 229930003451 Vitamin B1 Natural products 0.000 abstract 1
- 239000004503 fine granule Substances 0.000 abstract 1
- 229960003495 thiamine Drugs 0.000 abstract 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 abstract 1
- 239000011691 vitamin B1 Substances 0.000 abstract 1
- 235000010374 vitamin B1 Nutrition 0.000 abstract 1
- 235000012241 calcium silicate Nutrition 0.000 description 11
- 238000000034 method Methods 0.000 description 5
- 230000001953 sensory effect Effects 0.000 description 5
- WUKWITHWXAAZEY-UHFFFAOYSA-L calcium difluoride Chemical compound [F-].[F-].[Ca+2] WUKWITHWXAAZEY-UHFFFAOYSA-L 0.000 description 4
- 239000010436 fluorite Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
- 235000013539 calcium stearate Nutrition 0.000 description 2
- 239000008116 calcium stearate Substances 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- AUNGANRZJHBGPY-UHFFFAOYSA-N D-Lyxoflavin Natural products OCC(O)C(O)C(O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-UHFFFAOYSA-N 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- AUNGANRZJHBGPY-SCRDCRAPSA-N Riboflavin Chemical compound OC[C@@H](O)[C@@H](O)[C@@H](O)CN1C=2C=C(C)C(C)=CC=2N=C2C1=NC(=O)NC2=O AUNGANRZJHBGPY-SCRDCRAPSA-N 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- 229930003471 Vitamin B2 Natural products 0.000 description 1
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- -1 amyl nicotinic acid Chemical compound 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 239000008406 cosmetic ingredient Substances 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 150000003840 hydrochlorides Chemical class 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 229960002477 riboflavin Drugs 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000011716 vitamin B2 Substances 0.000 description 1
- 235000019164 vitamin B2 Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】
発明の分野
本発明は苦味薬物にケイ酸カルシウムを配合して苦味薬
物の苦味をマスクした固形剤及びその製造方法に関する
。DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to a solid preparation in which the bitter taste of a bitter drug is masked by blending calcium silicate with a bitter drug, and a method for producing the same.
発明の背景
従来、苦味薬物の苦味路を軽減させるために種々の手段
が採用されている。例えば苦味薬物にカルボキシメチル
セルロース（ＣＭ（ｌやアラビアゴムなどを配合する方
法があるけ扛ど、この方法は単に苦味が雪面上に分散す
るのを抑制するのみであって効果は十分でない。ｆ、た
甘味剤などと混合する方法も効果不十分である。薬物表
面をコーティングすることも行われているが、この方法
にニジ製造された固形剤は服用の際に口中がザラつ〈感
じがあり、また歯の間に挾まれたりして不快感が生ずる
。BACKGROUND OF THE INVENTION In the past, various means have been employed to alleviate the bitter taste tract of bitter drugs. For example, there is a method of adding carboxymethylcellulose (CM) or gum arabic to bitter drugs, but this method only suppresses the dispersion of bitterness on the snow surface and is not sufficiently effective.f However, methods of mixing the drug with sweeteners, etc., are also insufficiently effective.Coating the drug surface is also used, but solid preparations manufactured using this method have a rough texture in the mouth when taken. It also causes discomfort when it gets caught between the teeth.
今回本発明者らは、苦味薬物にケイ酸カルシウムを配合
することにより、苦味が大いに減少さｎ。This time, the present inventors have found that by incorporating calcium silicate into a bitter drug, the bitterness is greatly reduced.
しかも口中における感じがまろやかな固形剤が得られる
ことを見出した。Moreover, it has been found that a solid preparation with a mellow feel in the mouth can be obtained.
発明の開示
本発明は、ケイ酸カルシウムと苦味薬物とを配合して成
る苦味薬物含有固形剤を提供するものである。更に本発
明はケイ酸カルシウムと苦味薬物溶液とを混和し、乾燥
することを包含する苦味薬物含有固形剤の製造方法をも
提供するものである。DISCLOSURE OF THE INVENTION The present invention provides a bitter drug-containing solid preparation comprising calcium silicate and a bitter drug. Furthermore, the present invention also provides a method for producing a solid preparation containing a bitter drug, which includes mixing calcium silicate and a bitter drug solution and drying the mixture.
本発明に使用さｎる苦味薬物は苦味を有する任意の薬物
であシ、例えばビタミンＢＩ、Ｂ２、Ｂ６、パントテン
酸カルシウム、ニコチン酸アミドなど、ならびに種々の
塩酸塩及び硫酸塩などがある。The bitter drug used in the present invention is any drug that has a bitter taste, such as vitamins BI, B2, B6, calcium pantothenate, nicotinamide, and various hydrochlorides and sulfates.
本発明において使用するのに適したケイ酸カルシウムは
多孔性の粉体である。本発明に特に好適なケイ酸カルシ
ウムは徳山１達株式会社からフローライトの商品名で市
販されているものである。Calcium silicates suitable for use in the present invention are porous powders. A particularly suitable calcium silicate for the present invention is that commercially available from Tokuyama Ittatsu Co., Ltd. under the trade name Fluorite.
このフローライトは化学式：
％式％
（式中、］、 ＜ ｍ ＜ ２、かつ２ ＜ ｎ ＜
３ ）を有するケイ酸カルシウムであり、粉体グレード
、粒剤り゛レード及び打錠グレードがあるが、本発明に
使用するのに適するものは粉体グレードのフローライ）
Ｒ，ＲＮ及びＳである。This fluorite has the chemical formula: %formula%, where ], < m < 2, and 2 < n <
3), and there are powder grade, granule grade, and tablet grade, but the one suitable for use in the present invention is powder grade Fluorite).
R, RN and S.
これらのフローライトは嵩が極めて太きく、約１０１０
０Ｏ／１００１であり、吸油量も４００〜６００ｒｎｌ
／／１００ｆと太きい。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１〜５
０に収載されており、更にまた米国薬局方（ＮＦ−Ｘ■
）のケイ酸カルシウムの規格値にも適合する。These fluorites are extremely bulky, approximately 1010
0O/1001 and oil absorption amount is 400~600rnl
//100f and thick. Regarding safety, the Japanese Non-Pharmaceutical Drug Code 4600 and General Purpose Cosmetic Ingredients 1 to 5
It is listed in the United States Pharmacopoeia (NF-X■
) also meets the standard values for calcium silicate.
苦味薬物にケイ酸カルシウムを配合するに当っては、両
者を単に混合すｎばＬい。両者の配合割合は臨界的では
なく、実験的に定めることができる。しかしながら、苦
味薬物に対しケイ酸カルシウムは１重量比以上を配合す
ることが好捷しい。When adding calcium silicate to a bitter drug, it is sufficient to simply mix the two. The blending ratio of both is not critical and can be determined experimentally. However, it is preferable to mix calcium silicate in a weight ratio of 1 or more to the bitter drug.
本発明の固形剤は錠剤、顆粒剤、細粒、散剤、その他任
意の形態であることができる。The solid preparation of the present invention can be in the form of tablets, granules, fine particles, powders, or any other form.
本発明の固形剤は無水ケイ酸又はその他の賦形剤及び甘
味剤などを配合することができる。The solid preparation of the present invention may contain silicic anhydride or other excipients and sweeteners.
次に実施例を掲げて本発明を更に具体的に説明する。Next, the present invention will be described in more detail with reference to Examples.
実施例１
水溶性ビタミンＢｚ ７．５部、ビタミンＢｓ１２部
及びニコチン酸アミド１ｏ部を水２００部に溶解し、フ
ローライトＳの６３．９部と混合した。これを乾燥して
粉末とした。官能試験の結果を表１に示す。Example 1 7.5 parts of water-soluble vitamin Bz, 12 parts of vitamin Bs, and 10 parts of nicotinic acid amide were dissolved in 200 parts of water, and mixed with 63.9 parts of Fluorite S. This was dried to form a powder. The results of the sensory test are shown in Table 1.
対照例Ａ
水溶性ビタミンＢ２ ７゜５部、ビタミン８６１２部、
ニコチン酸アミｌ−９１０部、マンニット６００部及び
ポリビニルピロリドンに−３０の５０部を常法の湿式円
筒造粒法で顆粒とし、乾燥した。官能試験の結果を表Ｉ
に示す。Control example A Water-soluble vitamin B2 7°5 parts, vitamin 8612 parts,
910 parts of amyl nicotinic acid, 600 parts of mannitol, and 50 parts of polyvinylpyrrolidone-30 were made into granules by a conventional wet cylindrical granulation method and dried. Table I shows the results of the sensory test.
Shown below.
実施例２
実施例１で得た粉末１００部をマンニット６００部及び
ポリビニルピロリドンに−３０の５０部と共にアルコー
ルを造粒媒として常法にニジ顆粒剤とした。官能試験の
結果を表１に示す。Example 2 100 parts of the powder obtained in Example 1 was made into Niji granules in a conventional manner using 600 parts of mannitol, 50 parts of -30 in polyvinylpyrrolidone, and alcohol as a granulation medium. The results of the sensory test are shown in Table 1.
実施例３
ニコチン酸アミド１０部を水に溶解し、フローライ）Ｒ
Ｎ５０部と混合した。これを乾燥して粉末とし、更にス
テアリン酸カルシウム１０部を混合した。官能試験の結
果を表ＩＫ示す。Example 3 10 parts of nicotinic acid amide was dissolved in water and
Mixed with 50 parts of N. This was dried to form a powder, and 10 parts of calcium stearate was further mixed therein. The results of the sensory test are shown in Table IK.
官能試験
上記実施例１〜３及び対照例において得られた各固形剤
を３０名のパネルに各々０．５７づつ服用させ、苦味に
ついての評価をした。評価は０（殆ど苦くない）から、
３（極めて苦い）までの４等級において行った。結果を
下記表ＩＫ総括して示す。Sensory Test Each of the solid preparations obtained in Examples 1 to 3 and the control example above was administered in doses of 0.57 to a panel of 30 people, and the bitterness was evaluated. Ratings range from 0 (almost not bitter).
Performed in 4 grades up to 3 (extremely bitter). The results are summarized in Table IK below.
表 １
上表かられかるようにケイ酸カルシウムを配合しない対
照例Ａの試料については全部のパネラーが極めて苦いと
感じた。これに対し、ケイ酸カルシウムを配合した実施
例１〜３における本発明の固形剤の場合には大多数のパ
ネラ−が殆ど苦くないと感じた。Table 1 As can be seen from the above table, all panelists felt that the sample of Control A, which did not contain calcium silicate, was extremely bitter. On the other hand, in the case of the solid preparations of the present invention in Examples 1 to 3 containing calcium silicate, the majority of panelists felt that they were hardly bitter.
実施例４
ニコチン酸アミド１０部を水に溶解し、フローライ）Ｆ
ＬＮ４０部及び無水ケイ酸１０部と混合した。こｆＬを
乾燥して粉末とし、更にステアリン酸カルシウム１０部
を混合した。Example 4 10 parts of nicotinic acid amide was dissolved in water and
It was mixed with 40 parts of LN and 10 parts of silicic anhydride. This fL was dried to form a powder, and 10 parts of calcium stearate was further mixed therein.
Claims (1)
苦味薬物含有固形剤。 ２、多孔性無水ケイ酸を配合して成る特許請求の範囲第
１項に記載の苦味薬物含有固形剤。 ３、苦味薬物がビタミンＢ＿１、Ｂ＿２、Ｂ＿６、パン
トテン酸カルシウム、ニコチン酸アミド、その他塩酸塩
及び硫酸塩である特許請求の範囲第１項又は第２項に記
載の苦味薬物含有固形剤。 ４、ケイ酸カルシウムと苦味薬物溶液とを混和し、乾燥
することを特徴とする苦味薬物含有固形剤の製造方法。 ５、多孔性無水ケイ酸を配合する特許請求の範囲第４項
に記載の苦味薬物含有固形剤の製造方法。 ６、苦味薬物がビタミンＢ＿１、Ｂ＿２、Ｂ＿６、パン
トテン酸カルシウム、ニコチン酸アミド、その他塩酸塩
及び硫酸塩である特許請求の範囲第４項または第５項に
記載の苦味薬物含有固形剤の製造方法。[Claims] 1. A bitter drug-containing solid preparation containing calcium silicate as an essential ingredient. 2. The bitter drug-containing solid preparation according to claim 1, which contains porous silicic anhydride. 3. The bitter drug-containing solid preparation according to claim 1 or 2, wherein the bitter drug is vitamin B_1, B_2, B_6, calcium pantothenate, nicotinic acid amide, or other hydrochloride or sulfate. 4. A method for producing a solid drug containing a bitter drug, which comprises mixing calcium silicate and a bitter drug solution and drying the mixture. 5. The method for producing a bitter drug-containing solid preparation according to claim 4, which comprises blending porous silicic anhydride. 6. The method for producing a solid preparation containing a bitter drug according to claim 4 or 5, wherein the bitter drug is vitamin B_1, B_2, B_6, calcium pantothenate, nicotinic acid amide, or other hydrochloride or sulfate. .
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP62073981A JP2626976B2 (en) | 1987-03-30 | 1987-03-30 | Solid agent with reduced bitterness and method for producing the same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP62073981A JP2626976B2 (en) | 1987-03-30 | 1987-03-30 | Solid agent with reduced bitterness and method for producing the same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS63243035A true JPS63243035A (en) | 1988-10-07 |
| JP2626976B2 JP2626976B2 (en) | 1997-07-02 |
Family
ID=13533787
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP62073981A Expired - Lifetime JP2626976B2 (en) | 1987-03-30 | 1987-03-30 | Solid agent with reduced bitterness and method for producing the same |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2626976B2 (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100472590B1 (en) * | 2001-05-17 | 2005-03-08 | 가부시키가이샤니혼트림 | Oral Intake Solution |
| JP2008007496A (en) * | 2005-12-28 | 2008-01-17 | Zenyaku Kogyo Kk | Method for producing preparation using stirring type granulator |
| EP2617293A4 (en) * | 2010-09-16 | 2014-04-02 | Yasuyuki Yamada | Bitterness-masking ingredient and bitterness-masking method |
| CN112674348A (en) * | 2020-12-23 | 2021-04-20 | 石药集团中诺药业（泰州）有限公司 | Preparation method of B-vitamin buccal tablet and chewable tablet |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS55105566U (en) * | 1978-05-26 | 1980-07-23 | ||
| JPS59162553U (en) * | 1983-04-18 | 1984-10-31 | 株式会社フジクラ | Long body feeding device |
| JPS61168066U (en) * | 1985-04-09 | 1986-10-18 |
Family Cites Families (2)
| 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 |
| US3247064A (en) | 1962-03-30 | 1966-04-19 | Shionogi & Co | Multivitamin tablet stabilized with porous silica |
-
1987
- 1987-03-30 JP JP62073981A patent/JP2626976B2/en not_active Expired - Lifetime
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS55105566U (en) * | 1978-05-26 | 1980-07-23 | ||
| JPS59162553U (en) * | 1983-04-18 | 1984-10-31 | 株式会社フジクラ | Long body feeding device |
| JPS61168066U (en) * | 1985-04-09 | 1986-10-18 |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100472590B1 (en) * | 2001-05-17 | 2005-03-08 | 가부시키가이샤니혼트림 | Oral Intake Solution |
| JP2008007496A (en) * | 2005-12-28 | 2008-01-17 | Zenyaku Kogyo Kk | Method for producing preparation using stirring type granulator |
| EP2617293A4 (en) * | 2010-09-16 | 2014-04-02 | Yasuyuki Yamada | Bitterness-masking ingredient and bitterness-masking method |
| CN112674348A (en) * | 2020-12-23 | 2021-04-20 | 石药集团中诺药业（泰州）有限公司 | Preparation method of B-vitamin buccal tablet and chewable tablet |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2626976B2 (en) | 1997-07-02 |
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