JPH04235916A - Soft capsule agent of lopermide hydrochloride - Google Patents
Soft capsule agent of lopermide hydrochlorideInfo
- Publication number
- JPH04235916A JPH04235916A JP9113831A JP1383191A JPH04235916A JP H04235916 A JPH04235916 A JP H04235916A JP 9113831 A JP9113831 A JP 9113831A JP 1383191 A JP1383191 A JP 1383191A JP H04235916 A JPH04235916 A JP H04235916A
- Authority
- JP
- Japan
- Prior art keywords
- hydrochloride
- soft capsule
- loperamide hydrochloride
- capsule agent
- lopermide
- 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
- 239000007901 soft capsule Substances 0.000 title claims abstract description 19
- 239000003795 chemical substances by application Substances 0.000 title abstract 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 title 1
- 229960002983 loperamide hydrochloride Drugs 0.000 claims abstract description 20
- PGYPOBZJRVSMDS-UHFFFAOYSA-N loperamide hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 PGYPOBZJRVSMDS-UHFFFAOYSA-N 0.000 claims abstract description 20
- 239000002202 Polyethylene glycol Substances 0.000 claims abstract description 7
- 229920001223 polyethylene glycol Polymers 0.000 claims abstract description 7
- 238000003860 storage Methods 0.000 abstract description 3
- 230000007774 longterm Effects 0.000 abstract description 2
- 239000002775 capsule Substances 0.000 description 7
- 238000012360 testing method Methods 0.000 description 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000000843 powder Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000007902 hard capsule Substances 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 108010010803 Gelatin Proteins 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 239000012895 dilution Substances 0.000 description 2
- 238000010790 dilution Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 239000003793 antidiarrheal agent Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 229960001571 loperamide Drugs 0.000 description 1
- RDOIQAHITMMDAJ-UHFFFAOYSA-N loperamide Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(C(=O)N(C)C)CCN(CC1)CCC1(O)C1=CC=C(Cl)C=C1 RDOIQAHITMMDAJ-UHFFFAOYSA-N 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000001525 mentha piperita l. herb oil Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 235000019477 peppermint oil Nutrition 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 229940113115 polyethylene glycol 200 Drugs 0.000 description 1
- 229940068918 polyethylene glycol 400 Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【０００１】0001
【産業上の利用分野】本発明は塩酸ロペラミドを内容物
として含有する軟カプセル剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to soft capsules containing loperamide hydrochloride.
【０００２】0002
【従来の技術及び発明が解決しようとする課題】塩酸ロ
ペラミド〔化学名：４−［ ４−（パラ−クロロフェニ
ル）−４−ヒドロキシ−１−ピップ−エリジル ］−Ｎ
，Ｎ−ジメチル−２，２−ジフェニル−ブチラミド・塩
酸塩〕は下痢止めの治療薬として広く使用されている。
従来、この塩酸ロペラミドは硬カプセルとして市販され
ているが、塩酸ロペラミドの１カプセル中の含量は０．
２５ｍｇと極めて微量であるため、従来の硬カプセルは
１カプセル中の塩酸ロペラミドの含量を正確に均一に製
剤化するのが難しいという欠点があった。而して、従来
は、塩酸ロペラミドの原末を適当な粉体の賦形剤で希釈
混合して硬カプセル内容物としているが、より正確に作
ろうとすると、複数段階の粉末同士の希釈混合工程をと
らざるを得ないので、工程数が増え、経済的にもまた工
程ミスをできるだけ少なくするという製造管理上におい
ても極めて厄介であった。更にまた、近年は、患者がで
きるだけ服用し易くするために、より小型の製剤が求め
られているので、希釈に用いる粉体の賦形剤の添加量も
少なくせざるを得ないが、これが塩酸ロペラミドの含量
均一性を更に困難にしていた。[Prior art and problems to be solved by the invention] Loperamide hydrochloride [Chemical name: 4-[4-(para-chlorophenyl)-4-hydroxy-1-pip-erydyl]-N
, N-dimethyl-2,2-diphenyl-butyramide hydrochloride] is widely used as an antidiarrheal drug. Conventionally, this loperamide hydrochloride is commercially available as hard capsules, but the content of loperamide hydrochloride in one capsule is 0.
Since the amount of loperamide hydrochloride is extremely small at 25 mg, conventional hard capsules have the disadvantage that it is difficult to formulate a formulation with an accurate and uniform content of loperamide hydrochloride in one capsule. Conventionally, the bulk powder of loperamide hydrochloride is diluted and mixed with an appropriate powder excipient to form the contents of hard capsules, but in order to make it more accurately, a multi-step dilution and mixing process of powders is required. As a result, the number of steps increases, which is extremely troublesome both economically and in terms of manufacturing control, which is to minimize process errors. Furthermore, in recent years, there has been a demand for smaller preparations to make them as easy for patients to take, so the amount of excipients added to the powder used for dilution has to be reduced. This made the content uniformity of loperamide even more difficult.
【０００３】ところで、軟カプセル剤は油状物質を包含
させる最適の剤形として開発されたものであり、通常は
薬効成分を植物油等に溶解した内容物を軟カプセル皮膜
で被包して軟カプセル剤としている。また薬効成分が溶
解し得ない場合は、懸濁液状の内容物を被包して軟カプ
セル剤とすることもあるが、塩酸ロペラミドの様に１カ
プセル中の含量が極微量であり、正確な含量均一性が要
求される製剤の場合には、この方法は不適当である。ま
た懸濁状態の液を内容物とした軟カプセル剤は不透明と
なるので、外観的に商品価値を高めるために、カプセル
皮膜中にタール色素、酸化チタン等の不要物を配合しな
ければならない。By the way, soft capsules were developed as an optimal dosage form for containing oily substances, and are usually made by encapsulating the contents of medicinal ingredients dissolved in vegetable oil or the like in a soft capsule film. It is said that In addition, if the medicinal ingredient cannot be dissolved, the suspension may be encapsulated to form a soft capsule, but the amount contained in one capsule is extremely small, such as with loperamide hydrochloride, and the exact amount cannot be determined. This method is unsuitable for formulations requiring content uniformity. In addition, since soft capsules containing suspended liquid become opaque, unnecessary materials such as tar pigments and titanium oxide must be added to the capsule film in order to increase the commercial value in terms of appearance.
【０００４】0004
【課題を解決するための手段】かかる実状において、本
発明者は鋭意研究を行った結果、塩酸ロペラミドをポリ
エチレングリコールに溶解して軟カプセル皮膜中に内包
せしめれば、良好な含量均一性が保証でき、長期間安定
な軟カプセル剤が得られることを見出し、本発明を完成
した。[Means for Solving the Problems] Under these circumstances, the present inventor has conducted intensive research and found that if loperamide hydrochloride is dissolved in polyethylene glycol and encapsulated in a soft capsule film, good content uniformity can be guaranteed. The present invention was completed based on the discovery that soft capsules can be obtained that are stable for a long period of time.
【０００５】すなわち、本発明は塩酸ロペラミドのポリ
エチレングリコール溶液を内容物として含有する軟カプ
セル剤を提供するものである。Specifically, the present invention provides a soft capsule containing a polyethylene glycol solution of loperamide hydrochloride.
【０００６】本発明の軟カプセル剤を調製するには、ま
ず塩酸ロペラミドをポリエチレングリコールに溶解させ
る。ポリエチレングリコールとしては、分子量２００
〜６００ の常温で液状のものが好ましい。ポリエチレ
ングリコールの量は塩酸ロペラミド１重量部に対して８
０重量部以上、特に３００〜８００ 重量部が好ましい
。この内容物には、少量の水、グリセリン、ハッカ油、
甘味料等を適宜配合することができる。この内容物を被
膜するカプセル皮膜としては通常のものを使用すること
ができる。またカプセルの製造は、シーラー、ライナー
、アクコゲル、シームレス等の何れの方法でもよく、製
造機も種々のものを使用することができる。To prepare the soft capsules of the present invention, loperamide hydrochloride is first dissolved in polyethylene glycol. Polyethylene glycol has a molecular weight of 200
Preferably, it is liquid at room temperature of ~600°C. The amount of polyethylene glycol is 8 parts by weight of loperamide hydrochloride.
It is preferably 0 parts by weight or more, particularly 300 to 800 parts by weight. The contents include a small amount of water, glycerin, peppermint oil,
Sweeteners and the like can be added as appropriate. A conventional capsule film can be used to cover the contents. Capsules may be manufactured by any method such as sealer, liner, Accogel, seamless, etc., and various manufacturing machines can be used.
【０００７】[0007]
【発明の効果】本発明の塩酸ロペラミド軟カプセル剤は
長期間の保存においても安定であると共に、携帯に便利
であり、正確な量を服用できるという利点を有する。Effects of the Invention The loperamide hydrochloride soft capsules of the present invention are stable even during long-term storage, are convenient to carry, and have the advantage of being able to be taken in precise doses.
【０００８】[0008]
【実施例】次に実施例及び試験例を挙げて、本発明を更
に詳細に説明する。EXAMPLES Next, the present invention will be explained in more detail with reference to Examples and Test Examples.
【０００９】実施例１
（イ）ゼラチン１０ｋｇ、グリセリン３ｋｇ及び精製水
７ｋｇを８０℃で３時間加熱攪拌してゼラチンのゾル溶
液として、真空脱気したのち５０℃の恒温槽に貯留して
、軟カプセル皮膜用剤とした。
（ロ）ポリエチレングリコール２００ １ｋｇ中に、塩
酸ロペラミド３．１２５ｇを入れ、８０℃で１時間加熱
攪拌して澄明溶液とする。この液及び（イ）の軟カプセ
ル皮膜用剤を用いて常法により、ライナー社製ロータリ
ー充填機により内容量８０ｍｇの軟カプセルを製した。Example 1 (a) 10 kg of gelatin, 3 kg of glycerin, and 7 kg of purified water were heated and stirred at 80°C for 3 hours to form a gelatin sol solution, vacuum degassed, and stored in a constant temperature bath at 50°C to soften it. It was used as a capsule coating agent. (b) Add 3.125 g of loperamide hydrochloride to 1 kg of polyethylene glycol 200, and heat and stir at 80° C. for 1 hour to obtain a clear solution. Using this liquid and the soft capsule coating agent of (a), soft capsules having a content of 80 mg were prepared using a rotary filling machine manufactured by Reiner Co., Ltd. in a conventional manner.
【００１０】実施例２
ポリエチレングリコール４００ １ｋｇ中に塩酸ロペラ
ミド２．５ｇを入れ、８０℃で１時間加熱攪拌して澄明
溶液とする。
この液を用いて実施例１と同様の製造工程により内容量
１００ｍｇ の軟カプセルを製した。Example 2 2.5 g of loperamide hydrochloride was added to 1 kg of polyethylene glycol 400, and heated and stirred at 80° C. for 1 hour to obtain a clear solution. Using this liquid, soft capsules with an internal capacity of 100 mg were manufactured by the same manufacturing process as in Example 1.
【００１１】試験例１
実施例１で得た塩酸ロペラミド軟カプセルの保存安定性
を試験した結果は表１のとおりである。Test Example 1 Table 1 shows the results of testing the storage stability of the loperamide hydrochloride soft capsules obtained in Example 1.
【表１】[Table 1]
【００１２】試験例２
実施例２で得た塩酸ロペラミド軟カプセルの含量の均一
性試験の結果は表２のとおりである。Test Example 2 Table 2 shows the results of the content uniformity test of the loperamide hydrochloride soft capsules obtained in Example 2.
【表２】[Table 2]
Claims (1)
ール溶液を内容物として含有することを特徴とする軟カ
プセル剤。1. A soft capsule containing a polyethylene glycol solution of loperamide hydrochloride.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9113831A JPH04235916A (en) | 1991-01-11 | 1991-01-11 | Soft capsule agent of lopermide hydrochloride |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9113831A JPH04235916A (en) | 1991-01-11 | 1991-01-11 | Soft capsule agent of lopermide hydrochloride |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH04235916A true JPH04235916A (en) | 1992-08-25 |
Family
ID=11844221
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP9113831A Pending JPH04235916A (en) | 1991-01-11 | 1991-01-11 | Soft capsule agent of lopermide hydrochloride |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH04235916A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0815854A1 (en) * | 1996-06-28 | 1998-01-07 | McNEIL-PPC, INC. | Artificial hip joint acetabular cup having two shells and its manufacture |
-
1991
- 1991-01-11 JP JP9113831A patent/JPH04235916A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0815854A1 (en) * | 1996-06-28 | 1998-01-07 | McNEIL-PPC, INC. | Artificial hip joint acetabular cup having two shells and its manufacture |
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