JPH069381A - Soft capsule containing ibuprofen - Google Patents
Soft capsule containing ibuprofenInfo
- Publication number
- JPH069381A JPH069381A JP9204993A JP9204993A JPH069381A JP H069381 A JPH069381 A JP H069381A JP 9204993 A JP9204993 A JP 9204993A JP 9204993 A JP9204993 A JP 9204993A JP H069381 A JPH069381 A JP H069381A
- Authority
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- Japan
- Prior art keywords
- ibuprofen
- weight
- parts
- soft capsule
- fatty acid
- Prior art date
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- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、イブプロフェンを含有
する製剤に関し、更に詳しくは、イブプロフェンの吸収
の迅速化を達成した軟カプセル剤に関する。更に、本発
明は、イブプロフェンの吸収の迅速化を達成した、イブ
プロフェンを含有する感冒薬軟カプセル剤に関する。BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a preparation containing ibuprofen, and more particularly to a soft capsule preparation which achieves rapid absorption of ibuprofen. Furthermore, the present invention relates to a cold medicine soft capsule containing ibuprofen, which achieves rapid absorption of ibuprofen.
【０００２】[0002]
【従来の技術】イブプロフェンは、慢性関節リウマチ、
関節痛及び関節炎、神経痛、神経炎、頸腕症候群等の
他、カゼ症候群、術後の消炎、鎮痛剤としての効果を有
する。従来イブプロフェンは医療用医薬品としてこれら
の疾患に使用されてきたが、その有効性と安全性から、
近年、解熱、鎮痛のための一般用医薬品として販売され
始めている。BACKGROUND OF THE INVENTION Ibuprofen is used for rheumatoid arthritis,
In addition to joint pain and arthritis, neuralgia, neuritis, cervical arm syndrome, etc., it has an effect as a cold syndrome, postoperative inflammation, and an analgesic. Conventionally, ibuprofen has been used as a medical drug for these diseases, but due to its efficacy and safety,
In recent years, it has begun to be sold as an over-the-counter drug for antipyretic and analgesic drugs.
【０００３】しかしイブプロフェンの物性を反映して、
販売されているイブプロフェンの剤形は、顆粒剤、細粒
剤、錠剤が殆どであり、他に坐剤が僅かながら販売され
ているが、軟カプセル剤は販売されていない。However, reflecting the physical properties of ibuprofen,
Most of the dosage forms of ibuprofen that are sold are granules, fine granules, and tablets, while suppositories are sold slightly, but soft capsules are not.
【０００４】イブプロフェンは既述の通り解熱、鎮痛剤
として使用されるが、急性の痛みを迅速に鎮めることが
必要とされる場合があり、そのためには、薬効が素早く
発揮される必要がある。しかしながら、既存の一般用イ
ブプロフェン製剤は、かかる要求を充分に満たすもので
はなかった。また、イブプロフェンがカゼ症候群に対す
る効果を有するにも拘わらず、薬効の素早い発揮という
点でこのように不十分であり、イブプロフェンを含有し
その作用を速やかに発揮させるような優れた感冒薬はな
かった。[0004] Ibuprofen is used as an antipyretic and analgesic agent as described above, but it may be necessary to quickly suppress acute pain, and for that purpose, it is necessary to exert its drug effect quickly. However, the existing general-purpose ibuprofen formulation has not sufficiently satisfied such a requirement. In addition, although ibuprofen has an effect on the cold syndrome, it is thus insufficient in terms of rapid onset of drug effect, and there was no excellent cold medicine containing ibuprofen and capable of rapidly exerting its effect. .
【０００５】[0005]
【発明が解決しようとする課題】本発明は、内服後にイ
ブプロフェンの薬効が速やかに発揮されるよう、吸収を
一層迅速化した内服用イブプロフェン製剤の開発を目的
とする。本発明は更に、かかる吸収を迅速化したイブプ
ロフェンを含有することによる優れた感冒薬たる製剤を
提供することを目的とする。DISCLOSURE OF THE INVENTION An object of the present invention is to develop an ibuprofen preparation for internal use, in which absorption is further accelerated so that the medicinal effect of ibuprofen can be rapidly exhibited after oral administration. It is another object of the present invention to provide a preparation as an excellent cold medicine by containing ibuprofen whose absorption is accelerated.
【０００６】[0006]
【課題を解決するための手段】本発明者らは、上記目的
の達成のため、従来の内服用製剤に比してイブプロフェ
ンの吸収速度を高めることのできる製剤を確立するた
め、種々の剤形について検討した。その結果、イブプロ
フェン原末を植物油中に単に懸濁させて含む軟カプセル
と市販のコーティング錠とが生物学的にほぼ同等な結果
を与えるとの知見を得、これを基に更に検討を重ねた結
果、イブプロフェンの吸収を特に迅速化する組成物を見
出し、前記目的に合致するイブプロフェンの吸収を迅速
化させた軟カプセル剤を完成した。また更に、該軟カプ
セル剤を基礎とすることにより、吸収を迅速化させたイ
ブプロフェンを含有する、薬効の発現の速やかな感冒薬
たる軟カプセル剤を完成した。[Means for Solving the Problems] In order to achieve the above-mentioned objects, the present inventors have established various preparations in order to establish a preparation capable of increasing the absorption rate of ibuprofen as compared with conventional preparations for oral administration. Was examined. As a result, it was found that soft capsules containing bulk ibuprofen powder simply suspended in vegetable oil and commercially available coated tablets give biologically similar results, and further studies were conducted based on this finding. As a result, a composition that particularly accelerates the absorption of ibuprofen has been found, and a soft capsule formulation that speeds up the absorption of ibuprofen, which meets the above object, has been completed. Furthermore, based on the soft capsule, a soft capsule, which is a common cold drug with rapid onset of drug effect, containing ibuprofen whose absorption was accelerated was completed.
【０００７】すなわち、本発明は、中鎖脂肪酸トリグリ
セリド及び／又は植物油にイブプロフェンを加えて５５
乃至６５℃の温度にて一旦溶解した後に室温まで冷却す
ることによって製造される懸濁液を封入してなることを
特徴とする軟カプセル剤である。該冷却は室温まででよ
く、更に冷却してもイブプロフェンの吸収の更なる促進
をもたらすことはない。冷却は、少量の場合には自然に
させればよいが、大量の場合には適宜な方法で強制的に
冷却するのが好ましい。That is, the present invention provides a medium-chain fatty acid triglyceride and / or vegetable oil to which ibuprofen is added.
A soft capsule which is characterized in that a suspension produced by dissolving once at a temperature of from to 65 ° C. and then cooling to room temperature is enclosed. The cooling may be up to room temperature and further cooling does not result in further enhancement of ibuprofen absorption. Cooling may be carried out naturally in the case of a small amount, but in the case of a large amount, it is preferable to forcibly cool it by an appropriate method.
【０００８】本発明において使用する植物油としては、
例えば、トウモロコシ油、大豆油、ゴマ油、サフラワー
油、綿実油、オリーブ油等が好ましいが、これらのうち
では大豆油が特に好ましい。また、「中鎖脂肪酸」は炭
素数６乃至１２のものをいい、この範囲内の脂肪酸のト
リグリセリドがイブプロフェンの特に迅速な吸収を与え
る。The vegetable oil used in the present invention includes:
For example, corn oil, soybean oil, sesame oil, safflower oil, cottonseed oil, olive oil and the like are preferable, but of these, soybean oil is particularly preferable. Further, "medium chain fatty acid" means one having 6 to 12 carbon atoms, and triglycerides of fatty acids within this range give particularly rapid absorption of ibuprofen.
【０００９】イブプロフェンは室温においては中鎖脂肪
酸トリグリセリド又は植物油には難溶性である。しか
し、５５ないし６５℃の温度においてはこれらに溶解さ
せることができる。得られた溶液は、室温に戻すことに
より、イブプロフェンの微細な結晶を析出して懸濁物を
形成する。得られる懸濁物の外観性状は、含有されるイ
ブプロフェンの比率により変化するが、イブプロフェン
の比率が高まるにつれ半固形となる。該懸濁物を常法に
より軟カプセルに封入することにより本発明の軟カプセ
ル剤が製造される。Ibuprofen is sparingly soluble in medium chain fatty acid triglycerides or vegetable oils at room temperature. However, they can be dissolved in these at temperatures of 55 to 65 ° C. When the obtained solution is returned to room temperature, fine crystals of ibuprofen are precipitated to form a suspension. The appearance of the obtained suspension varies depending on the ratio of ibuprofen contained, but becomes semisolid as the ratio of ibuprofen increases. The soft capsule preparation of the present invention is produced by encapsulating the suspension in a soft capsule by a conventional method.
【００１０】本発明の製剤は、更に界面活性剤を含むこ
とができる。界面活性剤の添加は、５５乃至６５℃にお
けるイブプロフェンの溶解を容易にする効果を有する。The formulation of the present invention may further contain a surfactant. The addition of a surfactant has the effect of facilitating the dissolution of ibuprofen at 55 to 65 ° C.
【００１１】界面活性剤としては、ＨＬＢ（親水性親油
性バランス）値が１乃至２０のものを任意に選択して使
用し得る。本発明において通常使用される好ましい界面
活性剤としては、例えば、グリセリン脂肪酸エステル、
ソルビタン脂肪酸エステル、ショ糖脂肪酸エステル、ポ
リオキシエチレンソルビタン脂肪酸エステル等が挙げら
れる。As the surfactant, those having an HLB (hydrophilic / lipophilic balance) value of 1 to 20 can be arbitrarily selected and used. Preferred surfactants usually used in the present invention include, for example, glycerin fatty acid ester,
Examples thereof include sorbitan fatty acid ester, sucrose fatty acid ester, and polyoxyethylene sorbitan fatty acid ester.
【００１２】界面活性剤の配合量は、得られるイブプロ
フェンの最終的な懸濁物に対して通常３０重量％までと
するのが好ましく、２０重量％に相当する量までとする
のが一層好ましい。The amount of the surfactant compounded is usually preferably 30% by weight, more preferably 20% by weight, based on the final suspension of ibuprofen obtained.
【００１３】植物油又は中鎖脂肪酸トリグリセリドにイ
ブプロフェンを５５乃至６５℃にて完全に溶解し、室温
に戻したときに微細な結晶として析出させるためには、
該植物油等とのイブプロフェンの配合比は、イブプロフ
ェン１重量部に対して該植物油等が通常０．２乃至１０
重量部、好ましくは１乃至３重量部である。In order to completely dissolve ibuprofen in vegetable oil or medium-chain fatty acid triglyceride at 55 to 65 ° C. and precipitate as fine crystals when returning to room temperature,
The compounding ratio of ibuprofen with the vegetable oil or the like is usually 0.2 to 10 with respect to 1 part by weight of ibuprofen.
Parts by weight, preferably 1 to 3 parts by weight.
【００１４】更に、本発明は、上記イブプロフェン含有
軟カプセル剤に、抗ヒスタミン剤、中枢興奮剤、解熱鎮
痛剤、鎮咳・去痰剤、抗炎症剤、ビタミンよりなる群よ
り選ばれる１種以上の薬剤を更に含有させることにより
上記により達成されるイブプロフェンの迅速な吸収を利
用した、薬効の発現の速やかな感冒薬たる軟カプセル剤
である。かかる追加の薬剤としては、従来の感冒薬、鎮
咳去痰薬等に使用されている有効成分が適宜使用でき
る。例えば、抗ヒスタミン剤としてはｄ−又はｄｌ−マ
レイン酸クロルフェニラミン又は塩酸イソチペンジル
等、中枢興奮剤としてはカフェイン（抗ヒスタミン剤を
加えたときには加えることが好ましい。）等、解熱鎮痛
剤としてはラクチルフェネチジン又はアセトアミノフェ
ン等、鎮咳・去痰剤としてはｄｌ−塩酸メチルエフェド
リン、ヒベンズ酸チペピジン、リン酸ジヒドロコデイン
又はグアヤコールスルホン酸カリウム等、抗炎症剤とし
ては塩化リゾチーム等、生薬・漢方処方としてはマオウ
エキス、葛根湯エキス等、及び、ビタミンとしてはチア
ミン、リボフラビンその他各種のビタミン類をそれぞれ
使用することができる。これら各種の成分の添加は、治
療対象として特に重点をおいた症状の緩解を得るのに適
合するよう、適宜取捨選択して行うことができる。これ
らの追加の成分の添加は、軟カプセル剤の製造工程にお
ける適宜の段階において適宜の方法で行うことができる
が、例えば、上述の手順によりイブプロフェンの微細な
結晶を析出した懸濁物を形成した後、該懸濁物に上記の
所望の追加成分を添加し混合して均一に分散させ、これ
を常法により軟カプセルに封入することによるのが好ま
しい。以下、実施例により本発明を具体的に説明する
が、本発明はこれら実施例の個々の具体的特徴によって
限定されるものではない。Furthermore, the present invention further comprises one or more drugs selected from the group consisting of antihistamines, central stimulants, antipyretic analgesics, antitussives / expectorants, anti-inflammatory agents and vitamins, in addition to the above-mentioned soft capsule containing ibuprofen. It is a soft capsule that is a common cold drug with a rapid onset of drug effect, which utilizes the rapid absorption of ibuprofen achieved by the above inclusion. As such an additional drug, an active ingredient used in a conventional cold drug, antitussive expectorant, etc. can be appropriately used. For example, d- or dl-chlorpheniramine maleate or isothipendyl hydrochloride or the like as an antihistamine, caffeine (preferably added when an antihistamine is added) or the like as a central stimulant, and lactylphenetidine or an antipyretic analgesic or the like. Acetaminophen and the like, antitussive and expectorant dl-methylephedrine hydrochloride, tipepidine hibenzate, dihydrocodeine phosphate or potassium guaiacol sulfonate and the like, anti-inflammatory agents such as lysozyme chloride, and herbal medicine and kakkonto for herbal and Chinese medicine prescriptions. Extracts and the like, and as vitamins, thiamine, riboflavin and various other vitamins can be used. The addition of these various components can be appropriately selected and carried out so as to be suitable for obtaining relief of symptoms, which is particularly important as a treatment target. The addition of these additional components can be carried out by an appropriate method at an appropriate stage in the production process of the soft capsule, but for example, a suspension in which fine crystals of ibuprofen were precipitated was formed by the above-mentioned procedure. After that, it is preferable to add the above-mentioned desired additional component to the suspension, mix and uniformly disperse the mixture, and then encapsulate this in a soft capsule by a conventional method. Hereinafter, the present invention will be described in detail with reference to Examples, but the present invention is not limited to each specific feature of these Examples.
【００１５】[0015]
【実施例】 〔実施例１〕 イブプロフェン軟カプセル剤 油類としては中鎖脂肪酸トリグリセリドを用い、下記の
比率にイブプロフェンを添加し、加熱しつつ攪拌して溶
解させ、室温に戻して微細な結晶を生成させ半固形の組
成物とし、その２６５ｍｇを軟カプセルに充填する。Example 1 Ibuprofen Soft Capsule Medium-chain fatty acid triglyceride was used as the oil, ibuprofen was added in the following ratio, and the mixture was dissolved by stirring with heating, and the mixture was returned to room temperature to form fine crystals. A semi-solid composition is produced, 265 mg of which is filled into a soft capsule.
【００１６】 イブプロフェン ２８重量部中鎖脂肪酸トリグリセリド ７２重量部 全量 １００重量部Ibuprofen 28 parts by weight Medium chain fatty acid triglyceride 72 parts by weight Total 100 parts by weight
【００１７】〔実施例２〕 イブプロフェン軟カプセル
剤 油類としては中鎖脂肪酸トリグリセリドを用い、下記の
範囲の比率で界面活性剤を加えた混合物にイブプロフェ
ンを添加し、加熱しつつ攪拌して溶解させ、室温に戻し
て微細な結晶を生成させて半固形の組成物とし、その２
６５ｍｇを軟カプセルに充填する。但し、下記組成中、
サラシミツロウの量とグリセリン脂肪酸エステルの量の
和は２０重量部以下とし、ポリソルベート８０の量とセ
スキオレイン酸ソルビタンの量の和は１０重量部以下と
する。Example 2 Ibuprofen Soft Capsule Medium-chain fatty acid triglyceride was used as oils, and ibuprofen was added to a mixture containing a surfactant in a ratio within the following range, and the mixture was dissolved by stirring while heating. , Return to room temperature to generate fine crystals to give a semi-solid composition, part 2
Fill soft capsules with 65 mg. However, in the following composition,
The sum of the amount of salix beeswax and the amount of glycerin fatty acid ester is 20 parts by weight or less, and the sum of the amount of polysorbate 80 and the amount of sorbitan sesquioleate is 10 parts by weight or less.
【００１８】 イブプロフェン ２８重量部 中鎖脂肪酸トリグリセリド ４７乃至７１重量部 サラシミツロウ ０．５乃至２０重量部 グリセリン脂肪酸エステル ０．５乃至２０重量部 ポリソルベート８０ ０乃至１０重量部セスキオレイン酸ソルビタン ０乃至１０重量部 全量 １００重量部Ibuprofen 28 parts by weight Medium chain fatty acid triglyceride 47 to 71 parts by weight Sarashi beeswax 0.5 to 20 parts by weight Glycerin fatty acid ester 0.5 to 20 parts by weight Polysorbate 800 to 10 parts by weight Sorbitan sesquioleate 0 to 10 parts by weight part 100 parts by weight of the total amount
【００１９】〔試験例〕以下の処方に従って製造した本
発明のカプセル剤と市販のコーティング錠とを用いて、
イブプロフェンの生物学的利用性を健常被検者を対象と
して比較試験した。（１カプセル中） 被験者それぞれにイブプロフェン７５ｍｇを含有するカ
プセル剤又は錠剤を投与し、一定時間の経過後、被検者
から血液サンプルを採取して、血中のイブプロフェン含
量を測定した。結果を図１に示す。Test Example Using the capsule of the present invention produced according to the following formulation and a commercially available coated tablet,
The bioavailability of ibuprofen was comparatively tested in healthy subjects. (1 capsule) A capsule or tablet containing 75 mg of ibuprofen was administered to each subject, and after a certain period of time, a blood sample was collected from the subject to measure the ibuprofen content in blood. The results are shown in Fig. 1.
【００２０】製剤における薬物の生物学的利用性とは、
当該製剤の投与後に薬物が循環血液中に移行する速度、
及び移行量を表すものと理解されている。また、血中濃
度と時間軸とによって囲まれる面積（ＡＵＣ）は生体内
の薬物量に対応しており、最高血中濃度（Ｃｍａｘ）及
びその時間（Ｔｍａｘ）は、ＡＵＣ同様、薬物体内動態
パラメーターとして重要な意味を有している。The bioavailability of a drug in a formulation is
The rate of transfer of the drug into the circulating blood after administration of the formulation,
And is understood to represent the amount transferred. Further, the area surrounded by the blood concentration and the time axis (AUC) corresponds to the amount of the drug in the living body, and the maximum blood concentration (Cmax) and its time (Tmax) are the pharmacokinetic parameters of the drug, similar to AUC. Has an important meaning as
【００２１】図１に示した血中濃度の変化を示す曲線か
ら、ＡＵＣ，Ｃｍａｘ，Ｔｍａｘを算出し、得られた値
に基づいてイブプロフェンの相対的な生物学的利用率を
求め、表１に示した。AUC, Cmax and Tmax were calculated from the curve showing the change in blood concentration shown in FIG. 1, and the relative bioavailability of ibuprofen was calculated based on the obtained values. Indicated.
【表１】 [Table 1]
【００２２】表１から明らかな通り、本発明の軟カプセ
ル剤では、イブプロフェンの生物学的利用性について市
販コーティング錠との比較において向上が見られる。特
に、図１の血中濃度曲線が示す通り、本発明のカプセル
剤を投与した場合のイブプロフェンの吸収は、市販コー
ティング錠の場合と比して迅速である。この差は、薬効
のより迅速な発現を必要とする急性の痛みに対して使用
する場合に重要な意義を有する。従って、本発明のイブ
プロフェン含有軟カプセル剤は、かかる痛みに対処する
上で従来の製剤より一層有用である。As is clear from Table 1, the soft capsules of the present invention show an improvement in the bioavailability of ibuprofen in comparison with the commercially available coated tablets. In particular, as shown by the blood concentration curve in FIG. 1, the absorption of ibuprofen when the capsule of the present invention is administered is faster than that of the commercially available coated tablet. This difference has important implications when used for acute pain that requires a more rapid onset of efficacy. Therefore, the ibuprofen-containing soft capsule of the present invention is more useful than conventional formulations in treating such pain.
【００２３】〔実施例３〕 感冒薬軟カプセル剤 下記処方に従い、油類及び界面活性剤の混合物にイブプ
ロフェンを添加し、加熱しつつ攪拌して溶解させ、室温
に戻して微細な結晶を生成させて半固形の組成物とし、
これに、予め混合しておいた他の成分を添加して均一に
混合し、その適当量を軟カプセルに充填する。 イブプロフェン ４５０．０重量部 ｄ−マレイン酸クロルフェニラミン ３．５重量部 ｄｌ−塩酸メチルエフェドリン ６０．０重量部 塩化リゾチーム ６０．０重量部 中鎖脂肪酸トリグリセリド ２１１４．５重量部 サラシミツロウ ９０．０重量部 グリセリン脂肪酸エステル ９０．０重量部 ポリソルベート８０ ６６．０重量部セスキオレイン酸ソルビタン ６６．０重量部 ３０００．０重量部[Example 3] Soft drug for cold medicine According to the following formulation, ibuprofen was added to a mixture of oils and a surfactant, and dissolved by stirring with heating, followed by returning to room temperature to form fine crystals. A semi-solid composition,
To this, other components that have been mixed in advance are added and uniformly mixed, and an appropriate amount thereof is filled in a soft capsule. Ibuprofen 450.0 parts by weight d-chlorpheniramine maleate 3.5 parts by weight dl-methylephedrine hydrochloride 60.0 parts by weight lysozyme chloride 60.0 parts by weight medium chain triglyceride 2114.5 parts by weight salami beeswax 90.0 parts by weight Parts glycerin fatty acid ester 90.0 parts by weight polysorbate 80 66.0 parts by weight sorbitan sesquioleate 66.0 parts by weight 3000.0 parts by weight
【００２４】〔実施例４〕 感冒薬軟カプセル剤 下記処方に従い実施例３と同様にして軟カプセル剤を製
造する。 イブプロフェン ４５０．０重量部 ｄ−マレイン酸クロルフェニラミン ３．５重量部 ヒベンズ酸チペピジン ７５．０重量部 ｄｌ−塩酸メチルエフェドリン ６０．０重量部 グアヤコールスルホン酸カリウム ２５０．０重量部 カフェイン ７５．０重量部 硝酸チアミン ２５．０重量部 リボフラビン １２．０重量部 中鎖脂肪酸トリグリセリド １７３７．５重量部 サラシミツロウ ９０．０重量部 グリセリン脂肪酸エステル ９０．０重量部 ポリソルベート８０ ６６．０重量部セスキオレイン酸ソルビタン ６６．０重量部 ３０００．０重量部[Example 4] Cold drug soft capsule A soft capsule is produced in the same manner as in Example 3 according to the following formulation. Ibuprofen 450.0 parts by weight d-Chlorpheniramine maleate 3.5 parts by weight Tipepidine hibenzate 75.0 parts by weight dl-Methylephedrine hydrochloride 60.0 parts by weight Potassium guaiacol sulfonate 250.0 parts by weight Caffeine 75.0 Parts by weight thiamine nitrate 25.0 parts by weight riboflavin 12.0 parts by weight medium chain fatty acid triglyceride 1737.5 parts by weight salix beeswax 90.0 parts by weight glycerin fatty acid ester 90.0 parts by weight polysorbate 80 66.0 parts by weight sorbitan sesquioleate 66.0 parts by weight 3000.0 parts by weight
【００２５】〔実施例５〕 感冒薬カプセル剤 下記処方に従い実施例３と同様にして軟カプセル剤を製
造する。 イブプロフェン ３００．０重量部 ラクチルフェネチジン ２００．０重量部 ｄｌ−マレイン酸クロルフェニラミン ７．５重量部 リン酸ジヒドロコデイン ２４．０重量部 ｄｌ−塩酸メチルエフェドリン ６０．０重量部 無水カフェイン １５０．０重量部 塩酸チアミン ２５．０重量部 酪酸リボフラビン １２．０重量部 中鎖脂肪酸トリグリセリド １９０９．５重量部 サラシミツロウ ９０．０重量部 グリセリン脂肪酸エステル ９０．０重量部 ポリソルベート８０ ６６．０重量部セスキオレイン酸ソルビタン ６６．０重量部 ３０００．０重量部[Example 5] Cold drug capsule A soft capsule is produced in the same manner as in Example 3 according to the following formulation. Ibuprofen 300.0 parts by weight Lactylphenetidine 200.0 parts by weight dl-Chlorpheniramine maleate 7.5 parts by weight Dihydrocodeine phosphate 24.0 parts by weight dl-Methylephedrine hydrochloride 60.0 parts by weight Anhydrous caffeine 150.0 Parts by weight thiamine hydrochloride 25.0 parts by weight riboflavin butyrate 12.0 parts by weight medium chain fatty acid triglyceride 1909.5 parts by weight beeswax 90.0 parts by weight glycerin fatty acid ester 90.0 parts by weight polysorbate 80 66.0 parts by weight sesquioleic acid Sorbitan 66.0 parts by weight 3000.0 parts by weight
【００２６】〔実施例６〕 感冒薬軟カプセル剤 下記処方に従い実施例３と同様にして軟カプセル剤を製
造する。 イブプロフェン ４５０．０重量部 ｄ−マレイン酸クロルフェニラミン ３．５重量部 ｄｌ−塩酸メチルエフェドリン ６０．０重量部 マオウエキス ６０．０重量部 中鎖脂肪酸トリグリセリド ２１１４．５重量部 サラシミツロウ ９０．０重量部 グリセリン脂肪酸エステル ９０．０重量部 ポリソルベート８０ ６６．０重量部セスキオレイン酸ソルビタン ６６．０重量部 ３０００．０重量部[Example 6] Soft drug for cold medicine A soft capsule was prepared in the same manner as in Example 3 according to the following formulation. Ibuprofen 450.0 parts by weight d-Chlorpheniramine maleate 3.5 parts by weight dl-Methylephedrine hydrochloride 60.0 parts by weight Ephedra extract 60.0 parts by weight Medium chain fatty acid triglyceride 2114.5 parts by weight Salami beeswax 90.0 parts by weight Glycerin fatty acid ester 90.0 parts by weight Polysorbate 80 66.0 parts by weight Sorbitan sesquioleate 66.0 parts by weight 3000.0 parts by weight
【００２７】〔実施例７〕 感冒薬軟カプセル剤 下記処方に従い実施例３と同様にして軟カプセル剤を製
造する。 イブプロフェン ４５０．０重量部 ｄ−マレイン酸クロルフェニラミン ３．５重量部 ｄｌ−塩酸メチルエフェドリン ６０．０重量部 渇根湯エキス ６０．０重量部 中鎖脂肪酸トリグリセリド ２１１４．５重量部 サラシミツロウ ９０．０重量部 グリセリン脂肪酸エステル ９０．０重量部 ポリソルベート８０ ６６．０重量部セスキオレイン酸ソルビタン ６６．０重量部 ３０００．０重量部Example 7 Cold Agent Soft Capsule A soft capsule was prepared in the same manner as in Example 3 according to the following formulation. Ibuprofen 450.0 parts by weight d-Chlorpheniramine maleate 3.5 parts by weight dl-Methylephedrine hydrochloride 60.0 parts by weight Dr. Root extract 60.0 parts Medium chain fatty acid triglyceride 2114.5 parts by weight Salami beeswax 90. 0 parts by weight Glycerin fatty acid ester 90.0 parts by weight Polysorbate 80 66.0 parts by weight Sorbitan sesquioleate 66.0 parts by weight 3000.0 parts by weight
【図１】 各イブプロフェン製剤投与後のイブプロフェ
ンの血中濃度の推移を示す。FIG. 1 shows the change in blood ibuprofen concentration after administration of each ibuprofen preparation.
Claims (5)
油にイブプロフェンを加えて５５乃至６５℃の温度にて
溶解した後、該混合物を室温まで冷却することによって
生ずるイブプロフェンの懸濁物を封入してなることを特
徴とする軟カプセル剤。1. A suspension of ibuprofen formed by adding ibuprofen to medium-chain fatty acid triglyceride and / or vegetable oil, dissolving the mixture at a temperature of 55 to 65 ° C., and cooling the mixture to room temperature. A soft capsule characterized by the following.
油の量がイブプロフェン１重量部に対して０．２乃至１
０重量部であることを特徴とする、請求項１に記載の軟
カプセル剤。2. The amount of medium-chain fatty acid triglyceride and / or vegetable oil is 0.2 to 1 with respect to 1 part by weight of ibuprofen.
The soft capsule of claim 1, wherein the soft capsule is 0 part by weight.
油が少なくとも１種類の界面活性剤を含有することを特
徴とする、請求項１又は２に記載の軟カプセル剤。3. The soft capsule according to claim 1, wherein the medium-chain fatty acid triglyceride and / or the vegetable oil contains at least one kind of surfactant.
ェン懸濁物全量の１乃至３０重量％に相当する量である
ことを特徴とする、請求項３に記載の軟カプセル剤。4. The soft capsule according to claim 3, wherein the content of the surfactant is an amount corresponding to 1 to 30% by weight of the total amount of the obtained ibuprofen suspension.
ミン剤、中枢興奮剤、解熱鎮痛薬、鎮咳・去痰剤、抗炎
症剤、生薬、漢方処方、ビタミンよりなる群より選ばれ
る１種以上の薬剤を更に含有させてなることを特徴とす
る、請求項１乃至４のいずれかに記載の軟カプセル剤。5. A suspension of ibuprofen containing at least one drug selected from the group consisting of antihistamines, central stimulants, antipyretic analgesics, antitussives / expectorants, anti-inflammatory drugs, herbal medicines, Chinese herbs, and vitamins. The soft capsule preparation according to any one of claims 1 to 4, further comprising:
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP9204993A JPH069381A (en) | 1992-03-26 | 1993-03-25 | Soft capsule containing ibuprofen |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP10062992 | 1992-03-26 | ||
| JP4-100629 | 1992-03-26 | ||
| JP9204993A JPH069381A (en) | 1992-03-26 | 1993-03-25 | Soft capsule containing ibuprofen |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH069381A true JPH069381A (en) | 1994-01-18 |
Family
ID=26433539
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP9204993A Pending JPH069381A (en) | 1992-03-26 | 1993-03-25 | Soft capsule containing ibuprofen |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH069381A (en) |
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| KR20020076439A (en) * | 2001-03-28 | 2002-10-11 | 한국유나이티드제약 주식회사 | Formulation of transparent soft capsule for cough and cold remedies and its process |
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