JPH0465809B2 - - Google Patents
Info
- Publication number
- JPH0465809B2 JPH0465809B2 JP58200427A JP20042783A JPH0465809B2 JP H0465809 B2 JPH0465809 B2 JP H0465809B2 JP 58200427 A JP58200427 A JP 58200427A JP 20042783 A JP20042783 A JP 20042783A JP H0465809 B2 JPH0465809 B2 JP H0465809B2
- Authority
- JP
- Japan
- Prior art keywords
- acetaminophen
- composition
- soft capsules
- macrogol
- propylene glycol
- 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 - Lifetime
Links
Landscapes
- Medicinal Preparation (AREA)
Description
本発明は軟カプセル充填用組成物、更に詳細に
は、アセトアミノフエン又はアセトアミノフエン
配合薬剤の軟カプセル充填用組成物に関する。
アセトアミノフエンは発熱を伴う感冒、炎症性
疾患の解熱剤として、また頭痛、生理痛、筋肉痛
等の鎮痛剤として、単独あるいは他の医薬品と併
用して使用されている。
しかしながら、アセトアミノフエンは斯かる目
的で使用する場合、通常１回の服用量が150〜300
mgと多く、しかも一般に使用されている軟カプセ
ル用基剤に溶解し難いため、これを従来一般に使
用されている油脂又は液状脂肪酸類等の基剤に分
散させて流動性のある軟カプセル用充填剤を得よ
うとすると、アセトアミノフエン１重量部に対し
基剤を1.5〜2.5重量部使用しなければならない
が、斯くするとカプセルが大型となるかあるいは
１回に服用するカプセル数が多くなり、服用に困
難をきたすことを免れなかつた。
一方、総合感冒剤、解熱剤及び鎮痛剤に使用さ
れる他の成分は、その配合量が少ないかあるいは
当該基剤に溶解するため、アセトアミノフエンを
配合しない場合は軟カプセル化が容易である。し
かし、アセトアミノフエンは解熱鎮痛剤として極
めて優れているため、上記薬剤に好んで配合され
るが、一方ではこれが当該薬剤を軟カプセル化す
る際の隘路となつており、その結果、アセトアミ
ノフエン配合薬剤の軟カプセル製剤は提供されて
いない。
本発明者は、斯かる難点を解決すべく鋭意研究
の結果、充填用基剤として特定の水溶性基剤を用
いれば、少量でもアセトアミノフエンを均一に分
散でき、充填に適した流動性を有する軟カプセル
充填用組成物が得られることを見出し本発明を完
成した。
すなわち、本発明はアセトアミノフエン又はア
セトアミノフエン配合薬剤をマクロゴール又は
（及び）プロピレングリコールに分散せしめた軟
カプセル充填用組成物を提供するものである。
本発明において、アセトアミノフエンに配合さ
れる他の医薬品としては、通常総合感冒剤、鎮痛
剤、解熱剤等に使用されるものは何れも使用する
ことができ、例えば臭化水素酸デキストロメトル
フアン、塩酸メチルエフエドリン、ヒベンズ酸チ
ペピジン、リン酸ジヒドロコデイン等の鎮咳去痰
剤、マレイン酸クロルフエニラミン等の抗ヒスタ
ミン剤、ビタミンＣ、塩酸チアミン、リボフラビ
ン等のビタミン剤、その他無水カフエイン、アリ
ルイソプロピルアセチル尿素等を挙げることがで
きる。
アセトアミノフエン又はその配合薬剤は、マク
ロゴール又は（及び）プロピレングリコール１重
量部に対して1.5重量部未満まで分散することが
できるが、特に0.7〜1.4重量部となるように分散
させるのが好ましい。
本発明の軟カプセル充填用組成物は、予め微粉
としたアセトアミノフエン又はその配合薬剤をマ
クロゴール又は（及び）プロピレングリコールに
分散させるか、又はアセトアミノフエン又はその
配合薬剤をマクロゴール又は（及び）プロピレン
グリコールに加え、その中で微細化して分散させ
ることにより製造される。斯くして製造されたア
セトアミノフエンの微粉末を含む懸濁液は軟カプ
セルに充填するのに適した流動性を有する。
次に実施例を挙げて本発明を説明する。
実施例 １
予め微粉としたアセトアミノフエンを下記第１
表に示す各種基剤中に分散させて懸濁液を調製
し、その流動性を調べた。その結果を第１表に示
す。なお、流動性は、流動性良好（○）、一応流
動性有り（△）、流動性無し（×）の３段階に評
価した。
The present invention relates to a composition for filling soft capsules, and more particularly to a composition for filling soft capsules of acetaminophen or acetaminophen-containing drugs. Acetaminophen is used alone or in combination with other medicines as an antipyretic for colds and inflammatory diseases accompanied by fever, and as an analgesic for headaches, menstrual pain, muscle pain, and the like. However, when acetaminophen is used for this purpose, the usual dose is 150 to 300.
mg, and it is difficult to dissolve in commonly used soft capsule bases, so it is dispersed in commonly used bases such as oils and fats or liquid fatty acids to fill fluid soft capsules. In order to obtain a drug, it is necessary to use 1.5 to 2.5 parts by weight of the base for 1 part by weight of acetaminophen, but this results in larger capsules or a larger number of capsules to be taken at one time. I had no choice but to have difficulty taking the drug. On the other hand, other ingredients used in general cold remedies, antipyretics, and analgesics are easily encapsulated in soft capsules when acetaminophen is not blended, because their blending amounts are small or they dissolve in the base. However, since acetaminophen is extremely excellent as an antipyretic analgesic, it is preferred to be added to the above drugs, but on the other hand, this has become a bottleneck in encapsulating the drug in soft capsules, and as a result, acetaminophen Soft capsule formulations of combination drugs are not provided. As a result of intensive research to solve these difficulties, the present inventor found that by using a specific water-soluble base as a filling base, acetaminophene can be uniformly dispersed even in a small amount, and fluidity suitable for filling can be achieved. The present invention was completed by discovering that a composition for filling soft capsules having the following properties can be obtained. That is, the present invention provides a composition for filling soft capsules in which acetaminophen or an acetaminophen-containing drug is dispersed in macrogol or/and propylene glycol. In the present invention, as other pharmaceuticals to be mixed with acetaminophen, any of those normally used as general cold medicines, analgesics, antipyretics, etc. can be used, such as dextromethorphan hydrobromide. , antitussive expectorants such as methylephedrin hydrochloride, tipepidine hibenzoate, dihydrocodeine phosphate, antihistamines such as chlorpheniramine maleate, vitamins such as vitamin C, thiamine hydrochloride, riboflavin, and other anhydrous caffein, allylisopropylacetylurea, etc. can be mentioned. Acetaminophene or its compounded drug can be dispersed in an amount of less than 1.5 parts by weight per 1 part by weight of macrogol or (and) propylene glycol, but it is particularly preferable to disperse it in an amount of 0.7 to 1.4 parts by weight. . The composition for filling soft capsules of the present invention can be prepared by dispersing acetaminophen or a compounded drug thereof into a fine powder in advance in macrogol or (and) propylene glycol, or by dispersing acetaminophen or a compounded drug thereof in macrogol or (and) acetaminophen or a compounded drug thereof. ) It is manufactured by adding it to propylene glycol and finely dispersing it therein. The thus produced suspension containing fine powder of acetaminophene has fluidity suitable for filling into soft capsules. Next, the present invention will be explained with reference to Examples. Example 1 Acetaminophen, which had been made into a fine powder in advance, was prepared in the following manner.
A suspension was prepared by dispersing it in the various bases shown in the table, and its fluidity was examined. The results are shown in Table 1. The fluidity was evaluated in three stages: good fluidity (◯), some fluidity (△), and no fluidity (×).
アセトアミノフエン 900（mg）
マレイン酸クロルフエニラミン 7.5
臭化水素酸デキストロメトルフアン 45
塩酸メチルエフエドリン 30
無水カフエイン 75
ビタミンＣ 100プロピレングリコール 942.5
2100
実施例 ３
下記組成の軟カプセル充填用組成物を調製し
た。
〔組成〕
アセトアミノフエン 900（mg）
マレイン酸クロルフエニラミン 7.5
ヒベンズ酸チペピジン 75
dl−塩酸メチルエフエドリン 60
無水カフエイン 75マクロゴール−400 1042.5
2160
実施例 ４
下記組成の軟カプセル充填用組成物を調製し
た。
〔組成〕
アセトアミノフエン 900（mg）
マレイン酸クロルフエニラミン 7.5
リン酸ジヒドロコデイン 15
dl−塩酸メチルエフエドリン 30
無水カフエイン 75
塩酸チアミン 24
リボフラビン 12マクロゴール−300 1096.5
2160
Acetaminophen 900 (mg) Chlorpheniramine maleate 7.5 Dextromethorphan hydrobromide 45 Methylefedrin hydrochloride 30 Anhydrous caffein 75 Vitamin C 100 Propylene glycol 942.5 2100 Example 3 Composition for filling soft capsules with the following composition was prepared. [Composition] Acetaminophen 900 (mg) Chlorpheniramine maleate 7.5 Tipepidine hibenzate 75 dl-methylefedrin hydrochloride 60 Anhydrous caffein 75 Macrogol-400 1042.5 2160 Example 4 A composition for filling soft capsules having the following composition was prepared. Prepared. [Composition] Acetaminophene 900 (mg) Chlorpheniramine maleate 7.5 Dihydrocodeine phosphate 15 dl-methylefedrin hydrochloride 30 Caffeine anhydrous 75 Thiamine hydrochloride 24 Riboflavin 12 Macrogol-300 1096.5 2160
Claims (1)
配合薬剤をマクロゴール又は（及び）プロピレン
グリコールに分散せしめたことを特徴とする軟カ
プセル充填用組成物。 ２ アセトアミノフエン配合薬剤が総合感冒剤、
鎮痛剤又は解熱剤である特許請求の範囲第１項記
載の組成物。 ３ マクロゴール又は（及び）プロピレングリコ
ール１重量部にアセトアミノフエン又はアセトア
ミノフエン配合薬剤0.7〜1.4重量部を分散させた
ものである特許請求の範囲第１項又は第２項記載
の組成物。[Scope of Claims] 1. A composition for filling soft capsules, characterized in that acetaminophen or an acetaminophen-containing drug is dispersed in macrogol or/and propylene glycol. 2 Drugs containing acetaminophen are general cold medicines,
The composition according to claim 1, which is an analgesic or an antipyretic. 3. The composition according to claim 1 or 2, wherein 0.7 to 1.4 parts by weight of acetaminophen or an acetaminophen-containing drug is dispersed in 1 part by weight of macrogol or (and) propylene glycol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP20042783A JPS6092214A (en) | 1983-10-26 | 1983-10-26 | Composition for filling soft capsules |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP20042783A JPS6092214A (en) | 1983-10-26 | 1983-10-26 | Composition for filling soft capsules |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS6092214A JPS6092214A (en) | 1985-05-23 |
| JPH0465809B2 true JPH0465809B2 (en) | 1992-10-21 |
Family
ID=16424115
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP20042783A Granted JPS6092214A (en) | 1983-10-26 | 1983-10-26 | Composition for filling soft capsules |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS6092214A (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5484606A (en) * | 1994-01-24 | 1996-01-16 | The Procter & Gamble Company | Process for reducing the precipitation of difficulty soluble pharmaceutical actives |
| JP5852816B2 (en) * | 2010-09-10 | 2016-02-03 | ロート製薬株式会社 | Liquid pharmaceutical composition and soft capsule containing the same |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US10172797B2 (en) | 2013-12-17 | 2019-01-08 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| CA2955229C (en) | 2014-07-17 | 2020-03-10 | Pharmaceutical Manufacturing Research Services, Inc. | Immediate release abuse deterrent liquid fill dosage form |
| AU2015336065A1 (en) | 2014-10-20 | 2017-05-04 | Pharmaceutical Manufacturing Research Services, Inc. | Extended release abuse deterrent liquid fill dosage form |
-
1983
- 1983-10-26 JP JP20042783A patent/JPS6092214A/en active Granted
Non-Patent Citations (5)
| Title |
|---|
| JOURNAL OF PHARMACEUTICAL SCIENCES=1974 * |
| PHARMACEUTICAL TECHNOLOGY=1977 * |
| THE JOURNAL OF CLINICAL PHARMACOLOGY=1974 * |
| THE MERCK INDEX=1976 * |
| THE THEORY AND PRACTICE OF INDUSTRIAL PHARMACY=1970 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6092214A (en) | 1985-05-23 |
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