JPH0774153B2 - Loxoprofen / sodium-containing preparation - Google Patents
Loxoprofen / sodium-containing preparationInfo
- Publication number
- JPH0774153B2 JPH0774153B2 JP61085257A JP8525786A JPH0774153B2 JP H0774153 B2 JPH0774153 B2 JP H0774153B2 JP 61085257 A JP61085257 A JP 61085257A JP 8525786 A JP8525786 A JP 8525786A JP H0774153 B2 JPH0774153 B2 JP H0774153B2
- Authority
- JP
- Japan
- Prior art keywords
- sodium
- loxoprofen
- formulation
- preparation
- containing preparation
- 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
Description
【発明の詳細な説明】 〔発明の目的〕 鎮痛・消炎・解熱剤であるロキソプロフエン・ナトリウ
ム（化学名:2−〔４−（２−オキソシクロペンタン−１
−イルメチル）フエニル〕プロピオン酸ナトリウム塩）
は薬物同志または機器、容器に対する付着性が強い。従
つて、この事実に対しては特別に配慮した処方でなけれ
ば製剤化困難であり、例え製剤化出来たとしても薬物と
して適当な特性を有する製剤を作製することはできな
い。DETAILED DESCRIPTION OF THE INVENTION [Object of the Invention] Loxoprofen sodium (chemical name: 2- [4- (2-oxocyclopentane-1) which is an analgesic / anti-inflammatory / antipyretic agent]
-Ylmethyl) phenyl] propionic acid sodium salt)
Has strong adhesion to drugs, equipment, and containers. Therefore, it is difficult to formulate this fact unless a formulation that gives special consideration to this fact, and even if it can be formulated, it is not possible to produce a formulation having suitable properties as a drug.
従来、このような付着性薬物に対する改善処方として
は、例えばステアリン酸マグネシウムの様な滑沢剤を多
量に使用するか、あるいは薬物粒子または薬物を含む粒
子をコーテイングする等の処方がある。しかし、前者を
ロキソプロフエン・ナトリウムに適用すると、該製剤の
崩壊性、溶出性さらには生物学的利用能（bioavailabil
ity）を損い、錠剤とした場合には、その硬度が著しく
低下するという欠点を有する。また、後者をロキソプロ
フエン・ナトリウムに適用すると、溶媒の使用や長く複
雑な工程のため、それに付随して製剤費用が高くなるこ
と、使用されるコーテイング剤によつては生物学的利用
能の低下が生ずること等の欠点を有する。Conventionally, as an improved formulation for such an adhesive drug, there is a formulation in which a lubricant such as magnesium stearate is used in a large amount, or drug particles or particles containing a drug are coated. However, when the former is applied to loxoprofen sodium, the disintegration property, dissolution property and bioavailability
in the form of tablets, the hardness of the tablets is significantly reduced. In addition, when the latter is applied to loxoprofen sodium, the formulation cost will increase due to the use of a solvent and a long and complicated process, and depending on the coating agent used, bioavailability will increase. It has drawbacks such as deterioration.
本発明者らは、ロキソプロフエン・ナトリウムの付着性
低減について種々検討した結果、ある値以上の総吸水能
を有するように添加物を配合することによりロキソプロ
フエン・ナトリウム含有製剤を製造する際に生じる困
難、即ち、薬物の打錠時やカプセル充填時の機械に対す
る付着、薬物の容器に対する付着および薬物同志の付着
によるブロツク化を有効に防止し得ることを見出して本
発明を完成した。As a result of various studies on the reduction of the adhesion of loxoprofen / sodium, the present inventors have prepared a loxoprofen / sodium-containing preparation by adding additives so as to have a total water absorption capacity of a certain value or more. The present invention has been completed by finding that the difficulty caused by the above, that is, the adhesion of the drug to the machine at the time of tableting or capsule filling, the adhesion of the drug to the container, and the blocking due to the adhesion of the drugs can be effectively prevented.
本発明の処方は従来の処方と比較して、工業的に有利で
あるばかりでなく、製剤品質の観点からも選択する処方
の範囲が広く、従つて品質を損うことなく製剤化できる
利点を有する。The formulation of the present invention is not only industrially advantageous as compared with the conventional formulation, but also has a wide range of formulations to be selected from the viewpoint of formulation quality, and therefore has the advantage that it can be formulated without impairing the quality. Have.
本発明は総吸水能が1.7以上、好ましくは2.0以上、にな
るように添加物を配合してなるロキソプロフエン・ナト
リウム含有製剤に関する。The present invention relates to a loxoprofen / sodium-containing preparation obtained by blending additives so that the total water absorption capacity is 1.7 or more, preferably 2.0 or more.
ここに、本発明のｎ種類の添加物の総吸水能は次式によ
つて与えられる。Here, the total water absorption capacity of the n kinds of additives of the present invention is given by the following equation.
mo:ロキソプロフエン・ナトリウム（無水物として）の
処方量 mi:添加物ｉの処方量 ai:単位重量の添加物ｉが「適度の練合状態」において
含水して得る水の重量 ここに、「適度の練合状態」とは「湿式造粒時の造粒に
適した含水練合状態」を意味し、Funicular領域にあつ
て塑性限界以下の状態である。実験的には次の様な状態
をいう。即ち、一般に粉末試料を乳鉢に入れ、これに水
を加えて乳棒を用いて練合する場合において、添加水量
が少量のときはパサパサの状態であるが、添加水量の増
加と共にネバネバの状態へ移行する。本発明の「適度の
練合状態」とはネバネバの状態に移行前の状態であつ
て、練合物を手で握つたときに自らその形を保持するこ
とができ、かつやや腰のある状態をいう。 m o : Formulation amount of loxoprofen sodium (as an anhydride) m i : Formulation amount of additive i a i : Weight of water obtained by containing unit weight of additive i in a “moderate kneading state” Here, the "moderate kneading state" means "a water-containing kneading state suitable for granulation during wet granulation", and is a state below the plastic limit in the Funicular region. Experimentally, it means the following states. That is, in general, when a powder sample is placed in a mortar, and water is added to this and kneading is performed using a pestle, when the amount of added water is small, it is in a dry state, but as the amount of added water increases, it shifts to a sticky state. To do. The "moderate kneading state" of the present invention is a state before shifting to a sticky state, in which the shape can be retained by itself when the kneaded product is grasped by a hand, and a state having a slight waist. Say.
本発明に使用し得る添加物例のaiの値は次の通りであ
る。The values of a i of the additive examples that can be used in the present invention are as follows.
即ち、微結晶セルロース:1.0、低置換度ヒドロキシプロ
ピルセルロース:2.0、無晶形無水ケイ酸:1.0、トウモロ
コシデンプン:0.6、粉末乳糖（粒子径約12μ）:0.18、
ヒドロキシプロピルスターチ:0.5、アルギン酸:1.5、カ
ルボキシメチルセルロース:2.0、カルボキシメチルセル
ロースカルシウム:2.0、ステアリン酸マグネシウム：ほ
とんど無視し得る値、である。That is, microcrystalline cellulose: 1.0, low-substituted hydroxypropyl cellulose: 2.0, amorphous silicic acid anhydride: 1.0, corn starch: 0.6, powdered lactose (particle diameter about 12μ): 0.18,
Hydroxypropyl starch: 0.5, alginic acid: 1.5, carboxymethyl cellulose: 2.0, carboxymethyl cellulose calcium: 2.0, magnesium stearate: almost negligible value.
本発明に使用し得る添加物としては、医薬品としての特
性を損うものでなければ特に限定はなく、例えば上記に
加えてデキストリン、ヒドロキシプロピルセルロース、
ヒドロキシプロピルメチルセルロース、ヒドロキシエチ
ルセルロース、メチルセルロース、アミコール、プルラ
ン、マンニトール、白糖、デンプン類、サイクロデキス
トリン類、ポリビニルピロリドン、ポリビニルアルコー
ル、各種イオン交換樹脂等をあげることができる。The additive that can be used in the present invention is not particularly limited as long as it does not impair the properties as a medicine, and for example, in addition to the above, dextrin, hydroxypropyl cellulose,
Examples thereof include hydroxypropylmethyl cellulose, hydroxyethyl cellulose, methyl cellulose, amycol, pullulan, mannitol, sucrose, starches, cyclodextrins, polyvinylpyrrolidone, polyvinyl alcohol and various ion exchange resins.
なお、ロキソプロフエン・ナトリウムの粒度が小さくな
るほど、総吸水能の値が小さくても良好な製剤が得られ
る傾向があるが、最低1.7以上の総吸水能は必要であ
る。It should be noted that as the particle size of loxoprofen / sodium becomes smaller, a better preparation tends to be obtained even if the value of total water absorption capacity is smaller, but a total water absorption capacity of at least 1.7 is required.
本発明の適用対象は錠剤、カプセル剤、顆粒剤、散剤等
の全ての固形製剤である。The object of application of the present invention is all solid preparations such as tablets, capsules, granules and powders.
また、製剤の製法については特に限定はなく、乾式混
合、湿式混合等の公知のいかなる手段も使用できる。The method for producing the preparation is not particularly limited, and any known means such as dry mixing and wet mixing can be used.
次に実施例をあげて本発明を更に詳細に説明するが、本
発明はこれらに限定されるものではない。Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.
実施例１ （１） 製剤の製法 実施例１の製剤は次のようにして製造した。Example 1 (1) Manufacturing method of preparation The preparation of Example 1 was manufactured as follows.
下記の表１の処方に従つて、ロキソプロフエン・ナトリ
ウム、微結晶セルロース、乳糖および低置換度ヒドロキ
シプロピルセルロースを乳鉢で混合した後、これに適量
の水を加えて練合し、練合物を通気型乾燥機で60℃で60
分間乾燥した。乾燥品を30メツシユの篩を通して篩過
し、次いでこれにステアリン酸マグネシウムを加えてＶ
型ミキサーで10分間混合した。得られた混合物を直径7.
5mmの平杵を用いて打錠した。According to the formulation shown in Table 1 below, loxoprofen sodium, microcrystalline cellulose, lactose and low-substituted hydroxypropyl cellulose were mixed in a mortar, and then an appropriate amount of water was added and kneaded to obtain a kneaded product. Aeration type dryer at 60 ℃ 60
Dry for minutes. The dried product is sifted through a 30 mesh screen, then magnesium stearate is added to this and V
Mix for 10 minutes in a mold mixer. The resulting mixture has a diameter of 7.
The tablets were compressed using a 5 mm flat punch.
なお、対照例１の製剤も同様にして製造した。The formulation of Control Example 1 was also produced in the same manner.
（２） 結 果 実施例１の製剤は打錠できたが、対照例１の製剤は杵に
「くつつき」が生じ打錠不可能であつた。 (2) Results As a result, the preparation of Example 1 could be tableted, but the preparation of Control Example 1 could not be tableted due to "pecking" on the punch.
実施例２および３ （１） 製剤の製法 実施例２および３の製剤は次のようにして製造した。Examples 2 and 3 (1) Manufacturing method of preparations The preparations of Examples 2 and 3 were manufactured as follows.
下記の表２の処方に従つて、ステアリン酸マグネシウム
を除く各成分を乳鉢で混合した後、混合末を乾式粉砕機
アトマイザー（不二電機（株）製サンプルミル）によ
り、φ＝1mmスクリーンを装着して粉砕混合した。得ら
れた粉砕物にステアリン酸マグネシウムを加えてＶ型ミ
キサーで15分間混合した。得られた混合物をカプセル充
填機（Hozliger社製、タイプGKF 700）によりカプセル
充填した。According to the prescription in Table 2 below, after mixing each component except magnesium stearate in a mortar, the mixed powder was attached to a φ = 1 mm screen by a dry pulverizer atomizer (Fuji Electric Co., Ltd. sample mill). And crushed and mixed. Magnesium stearate was added to the obtained pulverized product and mixed with a V-type mixer for 15 minutes. The obtained mixture was capsule-filled by a capsule filling machine (type GKF 700 manufactured by Hozliger).
なお、対照例２の製剤も同様にして製造した。The preparation of Control Example 2 was manufactured in the same manner.
（２） 結 果 実施例２および３の製剤は充填できたが、対照例２の製
剤は回転充填盤およびスピンドルに粉末が固着し、充填
機破損のおそれが生じ充填不可能であつた。 (2) Results Although the preparations of Examples 2 and 3 could be filled, the preparation of Control Example 2 could not be filled because powder adhered to the rotary filling machine and the spindle, which could damage the filling machine.
───────────────────────────────────────────────────── フロントページの続き (72)発明者 佐藤 雄紀 東京都品川区広町１丁目２番58号 三共株 式会社内 (56)参考文献 特開 昭61−268621（ＪＰ，Ａ) 特開 昭57−106617（ＪＰ，Ａ) 特公 昭58−4699（ＪＰ，Ｂ２) 三共研究所年報36（1984），Ｐ．１−43 内藤著「内藤俊一薬剤学体系▲ＩＩＩ▼ 「錠剤」」第２版 広川書店Ｐ．102〜103 （Ｓ50−４−１) ─────────────────────────────────────────────────── ─── Continuation of front page (72) Inventor Yuki Sato 1-2-58 Hiromachi, Shinagawa-ku, Tokyo Sankyo Co., Ltd. (56) References JP-A-61-268621 (JP, A) JP-A-SHO 57-106617 (JP, A) JP 58-4699 (JP, B2) Sankyo Research Institute Annual Report 36 (1984), p. 1-43 Naito, "Shunichi Naito Pharmaceutical System III:" Tablets "" Second Edition Hirokawa Shoten P. 102 ~ 103 (S50-4-1)
Claims (2)
対して添加物量が３重量部以下であり、且つ総吸水能が
1.7以上であるロキソプロフェン・ナトリウム含有製
剤。1. An additive amount of 3 parts by weight or less per 1 part by weight of loxoprofen sodium, and a total water absorption capacity.
A loxoprofen sodium-containing preparation of 1.7 or more.
対して添加物量が３重量部以下の添加物を加えて混合し
て得られる総吸水能が1.7以上である均質なロキソプロ
フェン・ナトリウム含有製剤の製法。2. A method for producing a homogeneous loxoprofen / sodium-containing preparation having a total water absorption capacity of 1.7 or more obtained by adding 3 parts by weight or less of an additive to 1 part by weight of loxoprofen / sodium and mixing them.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61085257A JPH0774153B2 (en) | 1986-04-14 | 1986-04-14 | Loxoprofen / sodium-containing preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP61085257A JPH0774153B2 (en) | 1986-04-14 | 1986-04-14 | Loxoprofen / sodium-containing preparation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP8133257A Division JP2669517B2 (en) | 1996-05-28 | 1996-05-28 | Loxoprofen sodium solid formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS62242616A JPS62242616A (en) | 1987-10-23 |
| JPH0774153B2 true JPH0774153B2 (en) | 1995-08-09 |
Family
ID=13853516
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP61085257A Expired - Lifetime JPH0774153B2 (en) | 1986-04-14 | 1986-04-14 | Loxoprofen / sodium-containing preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0774153B2 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012106973A (en) * | 2009-11-30 | 2012-06-07 | Kowa Co | Pharmaceutical composition containing loxoprofen |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20010014340A1 (en) | 1996-06-14 | 2001-08-16 | Motohiro Ohta | Intrabuccally rapidly disintegrating tablet |
| US8071128B2 (en) | 1996-06-14 | 2011-12-06 | Kyowa Hakko Kirin Co., Ltd. | Intrabuccally rapidly disintegrating tablet and a production method of the tablets |
| KR100481583B1 (en) * | 1996-06-14 | 2005-07-12 | 교와 핫꼬 고교 가부시끼가이샤 | Tablets disintegrate quickly in the oral cavity |
| JP4293572B2 (en) * | 1998-06-30 | 2009-07-08 | 株式会社龍角散 | Loxoprofen sodium-containing tablets |
| US9358214B2 (en) | 2001-10-04 | 2016-06-07 | Adare Pharmaceuticals, Inc. | Timed, sustained release systems for propranolol |
| US7615269B2 (en) * | 2002-04-15 | 2009-11-10 | Multisorb Technologies, Inc. | Adsorbent compositions |
| JP4585220B2 (en) * | 2003-04-09 | 2010-11-24 | 第一三共株式会社 | Oral composition containing loxoprofen |
| JP5186540B2 (en) * | 2003-04-09 | 2013-04-17 | 第一三共株式会社 | Oral composition containing loxoprofen |
| US9884014B2 (en) | 2004-10-12 | 2018-02-06 | Adare Pharmaceuticals, Inc. | Taste-masked pharmaceutical compositions |
| NZ589750A (en) | 2004-10-21 | 2012-07-27 | Aptalis Pharmatech Inc | Taste-masked pharmaceutical compositions with gastrosoluble pore-formers |
| US9161918B2 (en) | 2005-05-02 | 2015-10-20 | Adare Pharmaceuticals, Inc. | Timed, pulsatile release systems |
| CA2782285A1 (en) | 2009-12-02 | 2011-06-09 | Luigi Mapelli | Fexofenadine microcapsules and compositions containing them |
| JP6008857B2 (en) * | 2011-07-29 | 2016-10-19 | 興和株式会社 | Pharmaceutical composition containing loxoprofen |
| WO2013018766A1 (en) * | 2011-07-29 | 2013-02-07 | 興和株式会社 | Stable pharmaceutical composition |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57106617A (en) * | 1980-12-23 | 1982-07-02 | Sankyo Co Ltd | Analgesic and anti-inflammatory agent |
-
1986
- 1986-04-14 JP JP61085257A patent/JPH0774153B2/en not_active Expired - Lifetime
Non-Patent Citations (2)
| Title |
|---|
| 三共研究所年報３６（１９８４），Ｐ．１−４３ |
| 内藤著「内藤俊一薬剤学体系▲ＩＩＩ▼「錠剤」」第２版広川書店Ｐ．１０２〜１０３（Ｓ５０−４−１） |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2012106973A (en) * | 2009-11-30 | 2012-06-07 | Kowa Co | Pharmaceutical composition containing loxoprofen |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS62242616A (en) | 1987-10-23 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP0330284B1 (en) | Process for the preparation of a pharmaceutical granulate | |
| EP0305051B1 (en) | Orally sustained-release acetaminophen formulation and process to obtain it | |
| JP4334616B2 (en) | Method for producing a dosage unit by wet granulation | |
| JPS58403B2 (en) | L- Ascorbine Sanseizaino Seizouhou | |
| JPH0774153B2 (en) | Loxoprofen / sodium-containing preparation | |
| HUT59588A (en) | Retarde composition and process for producing it | |
| JPS6191118A (en) | Granule of thiamine salt, its production, and tablet | |
| RU2300368C2 (en) | Ibuprofen-containing composition | |
| EP0324725B1 (en) | A pharmaceutical composition | |
| JP2669517B2 (en) | Loxoprofen sodium solid formulation | |
| WO1997033571A1 (en) | Rapid-release microdispersible ecadotril preparation | |
| JP4293572B2 (en) | Loxoprofen sodium-containing tablets | |
| JPS6320409B2 (en) | ||
| JPH029007B2 (en) | ||
| JPH08310969A (en) | Solid pharmaceutical composition and its preparation | |
| CA2782498C (en) | Tablet composition containing kampo medicinal extract and its manufacturing process | |
| KR100267525B1 (en) | Cytarabine ocfosfate hard capsule | |
| JP2003116966A (en) | Composition for direct tabletting and compounding method for supplement agent | |
| JP2000516601A (en) | Granules containing water-soluble compounds and cellulose | |
| JPH05139973A (en) | Production of nifedipin-containing solid preparation | |
| JPH05105636A (en) | Antacid agent composition | |
| KR20040047920A (en) | Solid pharmaceutical formulation for a piperazine urea derivative | |
| NZ251806A (en) | Making compressed tablets containing aminoguanidine or a salt thereof and a binder, by first spray-drying an aqueous solution to form a powder | |
| CN1049114C (en) | Method for prepn. of slowly-released medicaments preparation | |
| JPS6328414B2 (en) |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EXPY | Cancellation because of completion of term |