JP3320802B2 - Capsule hard film composition - Google Patents
Capsule hard film compositionInfo
- Publication number
- JP3320802B2 JP3320802B2 JP31958292A JP31958292A JP3320802B2 JP 3320802 B2 JP3320802 B2 JP 3320802B2 JP 31958292 A JP31958292 A JP 31958292A JP 31958292 A JP31958292 A JP 31958292A JP 3320802 B2 JP3320802 B2 JP 3320802B2
- Authority
- JP
- Japan
- Prior art keywords
- capsule
- gelatin
- polyvinyl acetal
- polyethylene glycol
- film composition
- 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 - Fee Related
Links
Classifications
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/141—Feedstock
Landscapes
- Medicinal Preparation (AREA)
- Compositions Of Macromolecular Compounds (AREA)
Description
【０００１】[0001]
【産業上の利用分野】本発明は、硬ゼラチンカプセルや
そのバンドシールに用いるカプセル硬皮膜組成物に関す
る。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a hard gelatin capsule composition and a capsule hard film composition used for a band seal thereof.
【０００２】[0002]
【従来の技術】硬ゼラチンカプセルは、製剤化が容易で
あり、また服用がし易いことから、広く医薬品分野で用
いられている。しかしながら、従来の硬ゼラチンカプセ
ルは、粉末、顆粒等の吸湿性薬剤を充填すると、カプセ
ル皮膜に含有する水分が薬剤に吸収されてカプセル皮膜
の柔軟性が失われ、ヒビや割れが発生するという問題が
あった。特にカプセルに薬剤を充填した後の包装時や、
服用時にカプセルを包材から取り出すときに、カプセル
が破損し、内容薬剤がカプセルから漏出するという問題
があった。2. Description of the Related Art Hard gelatin capsules are widely used in the pharmaceutical field because they are easy to formulate and easy to take. However, when a conventional hard gelatin capsule is filled with a hygroscopic drug such as powder or granules, the moisture contained in the capsule film is absorbed by the drug, the flexibility of the capsule film is lost, and cracks and cracks occur. was there. Especially when packaging after filling the capsule with the drug,
When taking out the capsule from the packaging material at the time of ingestion, there is a problem that the capsule is broken and the contents drug leaks out of the capsule.
【０００３】また、ゼラチンに、グリセリン、ソルビト
ール、ポリエチレングリコール等の可塑剤を添加し、柔
軟性をもたせた硬ゼラチンカプセル硬皮膜組成物が知ら
れている。しかしながら、これらの硬ゼラチンカプセル
は、可塑剤の添加量によりカプセル皮膜が柔らかくなり
過ぎたり、乾燥速度が遅い等、カプセル製造時に問題が
あった。したがって、従来の硬ゼラチンカプセルは、水
分低下によるカプセル皮膜の脆弱化のため、充填する薬
剤が制限されているのが現実である。Further, a hard gelatin capsule hard film composition having flexibility by adding a plasticizer such as glycerin, sorbitol, or polyethylene glycol to gelatin has been known. However, these hard gelatin capsules have problems during capsule production, such as an excessively soft capsule film and a low drying rate depending on the amount of the plasticizer added. Therefore, in the conventional hard gelatin capsule, the filling agent is actually limited due to the weakening of the capsule film due to the decrease in water content.
【０００４】[0004]
【発明が解決しようとする課題】本発明の目的は、吸湿
性の薬剤を充填し、カプセル皮膜の水分量が低下したと
しても脆弱化せず、カプセルにヒビ、欠け等が生じるこ
とが極めて少なく、カプセルの破損による内容薬剤の漏
出を防止することができるカプセル硬皮膜組成物を提供
することにある。SUMMARY OF THE INVENTION It is an object of the present invention to fill a capsule with a hygroscopic agent so that it does not become brittle even if the water content of the capsule film is reduced, and the capsule is hardly cracked or chipped. It is another object of the present invention to provide a hard coating composition for a capsule capable of preventing leakage of contents of the capsule due to breakage of the capsule.
【０００５】[0005]
【課題を解決するための手段】本発明は、ゼラチンに対
し、ポリビニールアセタールジエチルアミノアセテート
１〜１０重量％及びポリエチレングリコール１〜１０重
量％を含有するカプセル硬皮膜組成物である。SUMMARY OF THE INVENTION The present invention is a capsule hard film composition containing 1 to 10% by weight of polyvinyl acetal diethylaminoacetate and 1 to 10% by weight of polyethylene glycol based on gelatin.
【０００６】以下、本発明を詳細に説明する。本発明に
用いるポリビニールアセタールジエチルアミノアセテー
トは、次式：Hereinafter, the present invention will be described in detail. The polyvinyl acetal diethylaminoacetate used in the present invention has the following formula:
【０００７】[0007]
【化１】 Embedded image
【０００８】で示される構成単位を有する高分子化合物
である。中でも、アセタール化度５８〜６８％、粘度
（１０％メタノール溶液を、２５±０．１℃で測定）が
９．０〜１６．０センチポアズのものが好ましい。市販
品としては、胃溶性錠剤コーティング剤として知られる
ＡＥＡ三共［三共（株）製］を用いることができる。ポ
リビニールアセタールジエチルアミノアセテートの配合
量は、ゼラチンに対し１〜１０重量％である。A polymer compound having a structural unit represented by the following formula: Among them, those having a degree of acetalization of 58 to 68% and a viscosity (measured at 25 ± 0.1 ° C. of a 10% methanol solution) of 9.0 to 16.0 centipoise are preferred. As a commercially available product, AEA Sankyo [manufactured by Sankyo Co., Ltd.] known as a gastric-soluble tablet coating agent can be used. The amount of polyvinyl acetal diethylaminoacetate is 1 to 10% by weight based on gelatin.
【０００９】本発明に用いるポリエチレングリコールと
しては、日本薬局方又は日本薬局方外医薬品成分規格に
収載されているものであれば特に制限はないが、中でも
好ましいのは、ポリエチレングリコール４０００であ
る。ポリエチレングリコールの配合量は、ゼラチンに対
し１〜１０重量％である。また、ポリビニールアセター
ルジエチルアミノアセテートとポリエチレングリコール
との配合量の組合せは、ゼラチンに対しそれぞれ５重量
％含有するのが最も好ましい。[0009] The polyethylene glycol used in the present invention is not particularly limited as long as it is listed in the Japanese Pharmacopoeia or the Pharmaceutical Ingredients outside the Japanese Pharmacopoeia, but polyethylene glycol 4000 is particularly preferred. The blending amount of polyethylene glycol is 1 to 10% by weight based on gelatin. Most preferably, the combination of the amounts of polyvinyl acetal diethylaminoacetate and polyethylene glycol is 5% by weight based on gelatin.
【００１０】本発明のカプセル硬皮膜組成物の製造方法
としては、ゼラチンとポリビニールアセタールジエチル
アミノアセテートとポリエチレングリコールとを上記所
定量含有する水溶液を調製した後、これに酸化チタン、
食用色素等の着色剤を添加し、粘度を調整し、カプセル
製造機で成形する方法を挙げることができる。また、ゼ
ラチンとポリビニールアセタールジエチルアミノアセテ
ートとポリエチレングリコールとを含有する水溶液を調
製するに際しては、次の方法によるのが好ましい。The method for producing the capsule hard film composition of the present invention includes preparing an aqueous solution containing the above-mentioned predetermined amounts of gelatin, polyvinyl acetal diethylaminoacetate and polyethylene glycol, and then adding titanium oxide,
A method in which a coloring agent such as an edible dye is added, the viscosity is adjusted, and the mixture is molded using a capsule manufacturing machine. In preparing an aqueous solution containing gelatin, polyvinyl acetal diethylaminoacetate and polyethylene glycol, the following method is preferably used.
【００１１】まず、ポリビニールアセタールジエチルア
ミノアセテートを酸性水溶液に溶解する。ポリビニール
アセタールジエチルアミノアセテートの濃度は、２０〜
３０重量％が好ましい。次に、ポリビニールアセタール
ジエチルアミノアセテート水溶液のｐＨをゼラチンと同
じ弱酸性（ｐＨ５〜６）に調整する。次にゼラチン水溶
液と混合する。この際、ポリビニールアセタールジエチ
ルアミノアセテート水溶液は高温でゲル化する性質があ
るため注意を要する。First, polyvinyl acetal diethylaminoacetate is dissolved in an acidic aqueous solution. The concentration of polyvinyl acetal diethylaminoacetate is 20 to
30% by weight is preferred. Next, the pH of the polyvinyl acetal diethylaminoacetate aqueous solution is adjusted to the same weak acidity (pH 5 to 6) as gelatin. Next, it is mixed with an aqueous gelatin solution. At this time, care must be taken because the polyvinyl acetal diethylaminoacetate aqueous solution has a property of gelling at high temperatures.
【００１２】混合方法としては、例えば、予め比較的低
温でゼラチンとポリビニールアセタールジエチルアミノ
アセテートとの１：１混合液を調製しておき、この混合
液をゼラチン溶液に添加する方法を挙げることができ
る。この混合液は温度を上げてもゲル化しないので、操
作性が向上する。次に、ゼラチンとポリビニールアセタ
ールジエチルアミノアセテートとを混合した溶液に、上
記所定量のポリエチレングリコールを混合し、その他の
所望の添加剤を混合し、粘度を調整してカプセル製造機
に供給する組成物を得る。As a mixing method, for example, a method of preparing a 1: 1 mixed solution of gelatin and polyvinyl acetal diethylaminoacetate at a relatively low temperature in advance and adding this mixed solution to a gelatin solution can be mentioned. . Since the mixed solution does not gel even when the temperature is increased, the operability is improved. Next, the above-mentioned predetermined amount of polyethylene glycol is mixed with a solution in which gelatin and polyvinyl acetal diethylaminoacetate are mixed, other desired additives are mixed, the viscosity is adjusted, and the composition is supplied to a capsule manufacturing machine. Get.
【００１３】[0013]
実施例１ ポリビニールアセタールジエチルアミノアセテート［Ａ
ＥＡ三共、三共（株）製］６００g を酸性溶液に溶解
し、２５重量％ＡＥＡ水溶液を調製した。この溶液に水
酸化ナトリウムを添加して、ｐＨを５．７に調整した
後、冷却して放置し、脱泡した。Example 1 Polyvinyl acetal diethylaminoacetate [A
EA Sankyo, Sankyo Co., Ltd.] was dissolved in an acidic solution to prepare a 25 wt% AEA aqueous solution. Sodium hydroxide was added to this solution to adjust the pH to 5.7, and then cooled and left to degas.
【００１４】このＡＥＡ水溶液と同量の３４％重量ゼラ
チン水溶液を混合し、１：１ＡＥＡ−ゼラチン混合液を
調製した。次に、別途調製した３４％重量ゼラチン水溶
液に、上記の１：１ＡＥＡ−ゼラチン混合液を、ゼラチ
ンの総量に対しＡＥＡが５重量％になるように混合し
た。これに、６０℃に加温した６０重量％ポリエチレン
グリコール４０００水溶液を、ゼラチンの総量に対し５
重量％になるように混合した後、酸化チタン及び食用色
素を添加して粘度を調整し、カプセル製造機に供給する
組成物を得た。A 34% by weight aqueous gelatin solution was mixed with the same amount of the AEA aqueous solution to prepare a 1: 1 AEA-gelatin mixed solution. Next, the above 1: 1 AEA-gelatin mixed solution was mixed with a separately prepared 34% by weight aqueous gelatin solution so that AEA was 5% by weight based on the total amount of gelatin. Then, a 60% by weight aqueous solution of polyethylene glycol 4000 heated to 60 ° C. was added to the total amount of gelatin by 5%.
After mixing to give a weight%, titanium oxide and an edible dye were added to adjust the viscosity to obtain a composition to be supplied to a capsule manufacturing machine.
【００１５】この組成物を、カプセル製造機に供給し、
カプセルを製造した。得られたカプセルについて、下記
の空カプセル衝撃試験の結果を表１に、充填カプセル加
圧試験を表２に、崩壊試験を表３に示す。The composition is supplied to a capsule making machine,
Capsules were manufactured. Table 1 shows the results of the following empty capsule impact test, Table 2 shows the filled capsule pressurization test, and Table 3 shows the disintegration test of the obtained capsules.
【００１６】空カプセル衝撃試験 得られたカプセルについて、インパクト・テスター（カ
プスゲル社製）を使用し、カプセルの胴部を突破るとき
の、カプセルの厚さ当たりの仕事量（mJ/mm ）を測定
し、耐衝撃性について評価した。 Empty Capsule Impact Test Using the impact tester (manufactured by Capsugel), the work volume per capsule thickness (mJ / mm) when breaking through the body of the capsule was measured for the obtained capsule. Then, the impact resistance was evaluated.
【００１７】充填カプセル加圧試験 得られたカプセルにコーンスターチを充填し、カプセル
に５kgの荷重をかけたときに、カプセル５０個中破損し
たカプセルの割合（％）で評価した。 Filled Capsule Pressure Test The obtained capsules were filled with corn starch, and when a load of 5 kg was applied to the capsules, the percentage (%) of the broken capsules out of 50 capsules was evaluated.
【００１８】崩壊試験 第十二改正日本薬局方に準拠し、乳糖を充填したカプセ
ルを、３７±２℃の蒸留水に浸漬し、カプセルの開口時
間、内容物の放出完了時間及びカプセルの溶解完了時間
で評価した。また、上記試験については、ゼラチンに対
し５重量％のポリエチレングリコールを含む組成物から
なるカプセル、及び従来品の試験結果を併記した。 Disintegration test Lactose-filled capsules are immersed in distilled water at 37 ± 2 ° C. in accordance with the 12th revised Japanese Pharmacopoeia, and the capsule opening time, content release completion time, and capsule dissolution completion Evaluated by time. In the above test, the results of a capsule made of a composition containing 5% by weight of polyethylene glycol based on gelatin and the test results of a conventional product are also shown.
【００１９】[0019]
【表１】 [Table 1]
【００２０】[0020]
【表２】 [Table 2]
【００２１】[0021]
【表３】 [Table 3]
【００２２】表１及び表２から明らかなように、カプセ
ル強度が、特に低水分領域において、従来品及びポリエ
チレングリコール添加品にくらべ優れており、表３から
明らかなように、崩壊性については、従来品と同等であ
り、日本薬局方に適合する。As is clear from Tables 1 and 2, the capsule strength is superior to the conventional product and the polyethylene glycol-added product especially in the low moisture region. It is equivalent to the conventional product and conforms to the Japanese Pharmacopoeia.
【００２３】[0023]
【発明の効果】本発明のカプセル硬皮膜組成物は、吸湿
性の薬剤を充填し、カプセル皮膜の水分量が低下したと
しても脆弱化せず、カプセルにヒビ、欠け等が生じるこ
とが極めて少なく、カプセルの破損による内容薬剤の漏
出を防止することができる。The capsule hard film composition of the present invention is filled with a hygroscopic agent, does not become brittle even when the moisture content of the capsule film is reduced, and the capsule is hardly cracked or chipped. In addition, leakage of the contents medicine due to breakage of the capsule can be prevented.
フロントページの続き (72)発明者 清水 豊一 神奈川県相模原市南橋本４−３−36 ワ ーナー・ランバート株式会社 カプスゲ ル事業本部内 (56)参考文献 特開 平５−176974（ＪＰ，Ａ) 特開 平３−80930（ＪＰ，Ａ) 特開 昭49−81526（ＪＰ，Ａ) 特開 昭63−22014（ＪＰ，Ａ) 特開 昭61−28440（ＪＰ，Ａ) 特開 平６−192035（ＪＰ，Ａ) 特開 平５−255073（ＪＰ，Ａ) 特開 平１−308223（ＪＰ，Ａ) 特公 昭44−25900（ＪＰ，Ｂ１) 特表 平４−502027（ＪＰ，Ａ) (58)調査した分野(Int.Cl.7，ＤＢ名) C08L 89/00 - 89/06 C08L 29/00 - 29/14 C08L 71/00 - 71/14 A61K 9/48 ＣＡ（ＳＴＮ)Continued on the front page (72) Inventor Toyoichi Shimizu 4-3-36 Minamihashimoto, Sagamihara-shi, Kanagawa Pref. Warner Lambert Co., Ltd. Capsugel Business Unit (56) References JP-A-5-176974 (JP, A) JP-A-3-80930 (JP, A) JP-A-49-81526 (JP, A) JP-A-62-22014 (JP, A) JP-A-61-28440 (JP, A) JP-A-6-192035 (JP, A) JP, A) JP-A-5-255073 (JP, A) JP-A-1-308223 (JP, A) JP-B-44-25900 (JP, B1) JP-A-4-502027 (JP, A) (58) ) Field surveyed (Int. Cl. 7 , DB name) C08L 89/00-89/06 C08L 29/00-29/14 C08L 71/00-71/14 A61K 9/48 CA (STN)
Claims (1)
ルジエチルアミノアセテート１〜１０重量％及びポリエ
チレングリコール１〜１０重量％を含有するカプセル硬
皮膜組成物。1. A capsule hard coat composition containing 1 to 10% by weight of polyvinyl acetal diethylaminoacetate and 1 to 10% by weight of polyethylene glycol based on gelatin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP31958292A JP3320802B2 (en) | 1992-11-30 | 1992-11-30 | Capsule hard film composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP31958292A JP3320802B2 (en) | 1992-11-30 | 1992-11-30 | Capsule hard film composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH06157915A JPH06157915A (en) | 1994-06-07 |
| JP3320802B2 true JP3320802B2 (en) | 2002-09-03 |
Family
ID=18111879
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP31958292A Expired - Fee Related JP3320802B2 (en) | 1992-11-30 | 1992-11-30 | Capsule hard film composition |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP3320802B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1721604A4 (en) * | 2004-03-04 | 2008-04-30 | Takeda Pharmaceutical | PREPARATION OF STABLE CAPSULE |
| ITMI20070762A1 (en) * | 2007-04-13 | 2008-10-14 | Sicit Chemitec Spa | BIODEGRADABLE BLENDS BASED ON HYDROLYSED PROTEINS AND FUNCTIONAL ETHYLENE COPOLYMERS |
-
1992
- 1992-11-30 JP JP31958292A patent/JP3320802B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| JPH06157915A (en) | 1994-06-07 |
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