JPH02188524A - Hard capsule filled with sodium picosulfate solution - Google Patents
Hard capsule filled with sodium picosulfate solutionInfo
- Publication number
- JPH02188524A JPH02188524A JP490089A JP490089A JPH02188524A JP H02188524 A JPH02188524 A JP H02188524A JP 490089 A JP490089 A JP 490089A JP 490089 A JP490089 A JP 490089A JP H02188524 A JPH02188524 A JP H02188524A
- Authority
- JP
- Japan
- Prior art keywords
- sodium picosulfate
- macrogol
- solution
- hard capsule
- concentration
- 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
- GOZDTZWAMGHLDY-UHFFFAOYSA-L sodium picosulfate Chemical compound [Na+].[Na+].C1=CC(OS(=O)(=O)[O-])=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS([O-])(=O)=O)C=C1 GOZDTZWAMGHLDY-UHFFFAOYSA-L 0.000 title claims abstract description 26
- 229960005077 sodium picosulfate Drugs 0.000 title claims abstract description 26
- 239000007902 hard capsule Substances 0.000 title claims abstract description 19
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims abstract description 21
- 229960003511 macrogol Drugs 0.000 claims abstract description 16
- URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 claims abstract description 14
- 239000002904 solvent Substances 0.000 claims abstract description 10
- 235000013773 glyceryl triacetate Nutrition 0.000 claims abstract description 7
- 239000001087 glyceryl triacetate Substances 0.000 claims abstract description 7
- 229960002622 triacetin Drugs 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims abstract description 4
- 239000007788 liquid Substances 0.000 claims description 13
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 abstract description 15
- 239000003814 drug Substances 0.000 abstract description 4
- 230000002475 laxative effect Effects 0.000 abstract description 4
- 238000002156 mixing Methods 0.000 abstract description 3
- 239000000126 substance Substances 0.000 abstract description 3
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 230000001105 regulatory effect Effects 0.000 abstract 2
- 239000006172 buffering agent Substances 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 10
- 239000002775 capsule Substances 0.000 description 8
- 230000000052 comparative effect Effects 0.000 description 5
- 239000007901 soft capsule Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 1
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 description 1
- SIIZPVYVXNXXQG-UQTMIEBXSA-N [(2r,3r,4r,5r)-5-(6-aminopurin-9-yl)-4-[[(2r,3s,4r,5r)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl]oxy-3-hydroxyoxolan-2-yl]methyl [(2r,3r,4r,5r)-2-(6-aminopurin-9-yl)-4-hydroxy-5-(phosphonooxymethyl)oxolan-3-yl] hydrogen phos Chemical compound C1=NC2=C(N)N=CN=C2N1[C@@H]1O[C@H](COP(O)(=O)O[C@H]2[C@@H](O[C@H](COP(O)(O)=O)[C@H]2O)N2C3=NC=NC(N)=C3N=C2)[C@@H](O)[C@H]1OP(O)(=O)OC[C@H]([C@@H](O)[C@H]1O)O[C@H]1N1C(N=CN=C2N)=C2N=C1 SIIZPVYVXNXXQG-UQTMIEBXSA-N 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000000694 effects Effects 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
- 239000008141 laxative Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 239000012669 liquid formulation Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000011259 mixed solution Substances 0.000 description 1
- 210000000214 mouth Anatomy 0.000 description 1
- 239000001632 sodium acetate Substances 0.000 description 1
- 235000017281 sodium acetate Nutrition 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 229910000406 trisodium phosphate Inorganic materials 0.000 description 1
- 235000019801 trisodium phosphate Nutrition 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野］
本発明は医薬品として有用な、緩下作用を有するピコス
ルファートナトリウムを有効成分として含有する液体を
充填してなる硬カプセル剤に関するものである。[Detailed Description of the Invention] [Industrial Application Field] The present invention relates to hard capsules filled with a liquid containing as an active ingredient sodium picosulfate, which is useful as a pharmaceutical and has a laxative effect. .
［背景技術］
ピコスルファートナトリウムは、少量で強力な緩下作用
を示し、しかも副作用が少ないので、有用な緩下薬とし
て使用されている物質である。[Background Art] Sodium picosulfate is a substance used as a useful laxative because it exhibits a strong laxative effect in small amounts and has few side effects.
これまで、ピコスルファートナトリウムは、液剤として
、あるいは軟カプセル剤として市場に提供されているが
、液体充填硬カプセル剤としては、従来、ピコスルファ
ートナトリウムが溶解し得る溶媒で、しかも、その溶液
が経時的に安定であり、かつ、硬カプセルのゼラチン被
膜に影響を与えないという溶媒が見出し得ないなめ、市
場には提供されていなかった。Until now, sodium picosulfate has been provided on the market as a liquid or as a soft capsule, but liquid-filled hard capsules have conventionally been prepared using a solvent that can dissolve sodium picosulfate, It has not been possible to find a solvent that is stable over time and does not affect the gelatin coating of hard capsules, so it has not been available on the market.
本発明者らは、ピコスルファートナトリウムを溶解せし
めた液体を充填した硬カプセル剤を得るため、種々研究
を重ねた結果、本発明により、医薬品として、極めて優
れたピコスルファートナトリウム含有の硬カプセル剤を
提供することに成功した。The present inventors have conducted various studies in order to obtain hard capsules filled with a liquid in which sodium picosulfate is dissolved, and as a result of the present invention, the hard capsules containing sodium picosulfate are extremely excellent as pharmaceuticals. successfully provided the drug.
すなわち、本発明は、ピコスルファートナトリウムを６
、１ ｗ／ｗ％〜２０．０ｗ／ｗ％の濃度になるよう
にマクロゴール２００、マクロゴール３００、マクロゴ
ール４００、マクロゴール６００、マクロゴール１００
０、マクロゴール１５００およびマクロゴール１５４０
より選ばれた溶媒もしくは、選ばれた溶媒の混合物に溶
解して得られた溶液に、７０Ｗｚ’Ｗ％〜３０ｗ１′ｗ
％になるようにトリアセチンを混和し、それに緩衝剤を
加えて、ｐＨを４〜１０に調製した液を硬カプセルに充
填してなることを特徴とするピコスルファートナトリウ
ム液充填硬カプセル剤を提供するものである。That is, in the present invention, sodium picosulfate is
, 1 w/w% to 20.0 w/w% macrogol 200, macrogol 300, macrogol 400, macrogol 600, macrogol 100.
0, macrogol 1500 and macrogol 1540
70Wz'W% to 30w1'w to the solution obtained by dissolving in a selected solvent or a mixture of selected solvents.
To provide a sodium picosulfate liquid-filled hard capsule, which is obtained by filling hard capsules with a liquid in which triacetin is mixed with the liquid so as to have a pH of 4 to 10 by adding a buffer thereto. It is something to do.
本発明の硬カプセル剤に使用される各マクロゴール溶媒
は、通常軟カプセル刑に用いる場合にはその適用が可能
とされているものであるが、硬カプセル剤に用いると保
存中にカプセルが変形したり、液漏れを生じたりするた
め使用できないものであった。しかしながら、本発明に
おいては、ピコスルファートナトリウムのマクロゴール
溶液に７（ｈｖ／ｗ％〜３０ｗ／ｗ％になるようにトリ
アセチン（Ｃｓ Ｈｓ ａＯａ）を混和することにより
上記の如き問題点を解決したものである。The macrogol solvents used in the hard capsules of the present invention are usually applicable when used in soft capsules, but when used in hard capsules, the capsules may deform during storage. It could not be used because it would leak or leak. However, in the present invention, the above problems were solved by mixing triacetin (Cs Hs aOa) into the macrogol solution of sodium picosulfate at a concentration of 7 (hv/w% to 30w/w%). It is something.
なお、前記の各種マクロゴールは、使用にあたって、選
択した各溶媒を適宜混合して、その分子量を調整して使
用することができる。In addition, when using the above-mentioned various macrogol, the molecular weight can be adjusted by appropriately mixing each selected solvent.
Ｌ記の緩衝剤としては、マクロゴールに溶解し得、また
、その溶液のｐＨを調整し得て、しかも、生理学的にそ
の使用を許容される物質が用いられる０例えば水酸化ナ
トリウム、酢酸ナトリウム、リン酸三ナトリウム等はそ
の適切な例である。As the buffer agent listed in L, a substance that can be dissolved in macrogol, can adjust the pH of the solution, and is physiologically acceptable for use is used. For example, sodium hydroxide, sodium acetate, etc. , trisodium phosphate, etc. are suitable examples.
本発明の硬カプセル剤を製造する際の溶液の調製ならび
に硬カプセル剤への充填は、いずれも、慣用の薬剤溶液
の調製法あるいは硬カプセル剤への充填法を用いて行わ
れるものである。Preparation of the solution and filling of the hard capsules in producing the hard capsules of the present invention are both carried out using conventional drug solution preparation methods or hard capsule filling methods.
以下に本発明を実施例、比較例ならびに実験例により、
更に具体的に説明する。The present invention will be explained below using Examples, Comparative Examples, and Experimental Examples.
This will be explained more specifically.
実施例１
マクロゴール４００とトリアセチンの同等量の混液に、
２．５Ｗｚ’Ｗ％になるようにピコスルファートナトリ
ウムを溶解し、次に、その溶液のＤＨを水酸化ナトリウ
ムを加えることにより７．５に調整し、得られた液１０
０■を５号カプセルに充填した。Example 1 A mixture of macrogol 400 and triacetin in equal amounts,
Sodium picosulfate was dissolved to a concentration of 2.5 Wz'W%, and then the DH of the solution was adjusted to 7.5 by adding sodium hydroxide.
0■ was filled into a No. 5 capsule.
実施例２および３
下記に表示した処方に従い、ピコスルファートナトリウ
ム溶液を調製し、得られた各液１００■をとり、５号カ
プセルに充填した。Examples 2 and 3 Sodium picosulfate solutions were prepared according to the recipe shown below, and 100 ml of each solution was taken and filled into No. 5 capsules.
実施例２ 実施例３
ピコスルファートナトリウム ２．５■
２．５■マクロゴール４００
２９．０ｍマクロゴー
ル１５００ ６３．８ｍｇ
３４．８９トリアセチン ６３．
８Ｎ ６３．８■ＤＨ調節剤
適量 適量水酸化ナトリウム （ＤＨ７，５
とする） （ｐＨ７，５とする）なお、実施ＰＡ３にお
いては、マクロゴール４００とマクロゴール１５００と
を混合し、その平均分子量が約１０００となるようにし
て調製した。Example 2 Example 3 Sodium picosulfate 2.5■
2.5 ■Macro goal 400
29.0m macro goal 1500 63.8mg
34.89 Triacetin 63.
8N 63.8■DH regulator
Appropriate amount Appropriate amount Sodium hydroxide (DH7.5
In Example PA3, Macrogol 400 and Macrogol 1500 were mixed to have an average molecular weight of about 1000.
比較例１
マクロゴール４００とトリアセチンの同等量の混液に、
２．５ｗ／ｗ％になるようにピコスルファートナトリウ
ムを溶解し、得られた溶液１００■を５号カプセルに充
填した。Comparative Example 1 A mixed solution of equivalent amounts of macrogol 400 and triacetin was added,
Sodium picosulfate was dissolved to a concentration of 2.5 w/w%, and 100 ml of the resulting solution was filled into No. 5 capsules.
比較例２
マクロゴール４００に２．５ｗ／ｗ％になるようにピコ
スルファートナトリウムを溶解し、得られた溶液にさら
に、水酸化ナトリウムを加えてそのｐＨを７．５に調整
した。調整後、その液１００■を５号カプセルに充填し
た。Comparative Example 2 Sodium picosulfate was dissolved in Macrogol 400 to a concentration of 2.5 w/w%, and sodium hydroxide was further added to the resulting solution to adjust the pH to 7.5. After adjustment, 100 ml of the liquid was filled into a No. 5 capsule.
実験例１
比較例１および実施例１で得られた各カプセル剤につき
、それらを温度６０℃の条件下に１４日間放置し、７日
後および１４日後のピコスルファートナトリウムの残存
率、充填液のｐＨ及び液の性状を、それぞれ、測定した
。Experimental Example 1 Each of the capsules obtained in Comparative Example 1 and Example 1 was left at a temperature of 60°C for 14 days, and the residual rate of sodium picosulfate and the filling liquid were evaluated after 7 and 14 days. The pH and properties of the liquid were measured.
ピコスルファートナトリウムの測定は液体クロマトグラ
フィーで行い、最初の値を１００として残存率を求めた
。その結果を表１に示す。Sodium picosulfate was measured by liquid chromatography, and the residual rate was determined with the initial value as 100. The results are shown in Table 1.
表
５５〜９０％ＲＨ）に３０日間、■温度４０’（＋１°
）、湿度７５％（±５％） ＲＨ条件下に１４日間、い
ずれも、開放状態で放置して観察し、カプセルの液漏れ
を認めるまでの日数を測定した。その結果を表２に示す
。Table 55-90% RH) for 30 days, ■ Temperature 40' (+1°
), humidity 75% (±5%) RH conditions for 14 days, all were left open and observed, and the number of days until leakage of the capsule was observed was measured. The results are shown in Table 2.
表 ２
実験例２
実施例１および比較例２で得られた各カプセル剤につき
■室内条件下（温度２２〜２８℃、湿度実験例１および
実験例２の各結果に示されているように、本発明のピコ
スルファートナトリウム液充填硬カプセル剤は、経時点
に安定であり、長期間の保管が可能であることが明らか
である。Table 2 Experimental Example 2 For each capsule obtained in Example 1 and Comparative Example 2, ■ Indoor conditions (temperature 22 to 28°C, humidity, as shown in the results of Experimental Example 1 and Experimental Example 2, It is clear that the sodium picosulfate liquid-filled hard capsules of the present invention are stable over time and can be stored for a long period of time.
本発明により、現在市場に提供されているピコスルファ
ートナトリウムの軟カプセル剤に比べて口腔内に付着し
にくいという利点を有し、また、ピコスルファートナト
リウムの液剤に比べて、携帯に便利で飲みやすいという
点で、極めて有用なピコスルファートナトリウムの硬カ
プセル剤が提供されるのであり、したがって、本発明の
有用性は著しく大きい。The present invention has the advantage that it is less likely to adhere to the oral cavity compared to the soft capsules of sodium picosulfate currently available on the market, and is more convenient to carry than the liquid formulations of sodium picosulfate. A very useful hard capsule of sodium picosulfate is provided in that it is easy to swallow, and therefore, the usefulness of the present invention is extremely large.
Claims (1)
０．０ｗ／ｗ％の濃度になるようにマクロゴール２００
、マクロゴール３００、マクロゴール４００、マクロゴ
ール６００、マクロゴール１０００、マクロゴール１５
００およびマクロゴール１５４０より選ばれた溶媒もし
くは、選ばれた溶媒の混合物に溶解して得られた溶液に
、７０ｗ／ｗ％〜３０ｗ／ｗ％になるようにトリアセチ
ンを混和し、それに緩衝剤を加えて、ｐＨを４〜１０に
調製した液を硬カプセルに充填してなることを特徴とす
るピコスルフアートナトリウム液充填硬カプセル剤。1) Sodium picosulfate from 0.1 w/w% to 2
Macrogol 200 to a concentration of 0.0w/w%
, Macrogoal 300, Macrogoal 400, Macrogoal 600, Macrogoal 1000, Macrogoal 15
00 and Macrogol 1540, or a mixture of the selected solvents, triacetin is mixed at a concentration of 70 w/w% to 30 w/w%, and a buffer is added thereto. In addition, a sodium picosulfate liquid-filled hard capsule is obtained by filling hard capsules with a liquid adjusted to have a pH of 4 to 10.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP490089A JPH0830010B2 (en) | 1989-01-13 | 1989-01-13 | Picosulfate sodium liquid filled hard capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP490089A JPH0830010B2 (en) | 1989-01-13 | 1989-01-13 | Picosulfate sodium liquid filled hard capsule |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH02188524A true JPH02188524A (en) | 1990-07-24 |
| JPH0830010B2 JPH0830010B2 (en) | 1996-03-27 |
Family
ID=11596541
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP490089A Expired - Fee Related JPH0830010B2 (en) | 1989-01-13 | 1989-01-13 | Picosulfate sodium liquid filled hard capsule |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0830010B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995011024A1 (en) * | 1993-10-19 | 1995-04-27 | The Procter & Gamble Company | Picosulphate dosage form |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2019507121A (en) * | 2016-01-28 | 2019-03-14 | シーティーシー バイオ，インコーポレイテッド | Laxative composition |
-
1989
- 1989-01-13 JP JP490089A patent/JPH0830010B2/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995011024A1 (en) * | 1993-10-19 | 1995-04-27 | The Procter & Gamble Company | Picosulphate dosage form |
| US5631022A (en) * | 1993-10-19 | 1997-05-20 | The Procter & Gamble Company | Picosulfate dosage form |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH0830010B2 (en) | 1996-03-27 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
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