JP2002326927A - Quick-releasing tablet containing metformin hydrochloride - Google Patents
Quick-releasing tablet containing metformin hydrochlorideInfo
- Publication number
- JP2002326927A JP2002326927A JP2001136873A JP2001136873A JP2002326927A JP 2002326927 A JP2002326927 A JP 2002326927A JP 2001136873 A JP2001136873 A JP 2001136873A JP 2001136873 A JP2001136873 A JP 2001136873A JP 2002326927 A JP2002326927 A JP 2002326927A
- Authority
- JP
- Japan
- Prior art keywords
- metformin hydrochloride
- immediate
- release tablet
- tablets
- viscosity
- 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
Abstract
Description
【０００１】[0001]
【発明の属する技術分野】本発明は、糖尿病用薬である
塩酸メトホルミンの速放性錠剤及びその製造方法に関す
る。The present invention relates to a quick-release tablet of metformin hydrochloride, a drug for diabetes, and a method for producing the same.
【０００２】[0002]
【従来の技術】塩酸メトホルミンはビグアナイド系の血
糖降下剤であり、２型糖尿病に対する経口糖尿病用薬と
して臨床の場で使用されている。さらに、近年米国にお
いて肥満２型糖尿病のインスリン抵抗性を有する患者に
対し第一選択薬として汎用されたことから、国内におい
ても塩酸メトホルミン製剤の需要が高まっている。2. Description of the Related Art Metformin hydrochloride is a biguanide hypoglycemic agent and is used in clinical practice as an oral diabetes drug for type 2 diabetes. Furthermore, in recent years, since it has been widely used as a first-line drug in patients with insulin resistance of obese type 2 diabetes in the United States, the demand for metformin hydrochloride preparations has been increasing in Japan.
【０００３】ところで、国内においては、塩酸メトホル
ミン２５０ｍｇを含有する普通錠が２品目販売されてお
り、これらは１錠あたりの重量が３５０ｍｇ又は３８０
ｍｇと大きく、服用に際して好ましいものとはいえなか
った。[0003] In Japan, two types of ordinary tablets containing 250 mg of metformin hydrochloride are sold, and these tablets weigh 350 mg or 380 per tablet.
mg, which was not preferable when taken.
【０００４】また、特表平１０−５０５６０４号には、
有効成分として塩酸メトホルミンと、遅延剤としてヒド
ロキシプロピルセルロースなどのハイドロコロイド形成
剤を含有してなる医薬調製物が開示されている。ここ
で、遅延剤は、錠剤からの塩酸メトホルミンの放出を４
時間（０．５〜１０時間）にわたり、コントロールしつ
つ遅延させることを目的に添加されている。さらに、打
錠前の組成物の残留水分が０．５％未満であるときに
は、キャッピングが起き、打錠ができなかったことも記
載されている。[0004] In addition, Japanese Patent Publication No. Hei 10-505604 discloses that
Pharmaceutical preparations containing metformin hydrochloride as an active ingredient and a hydrocolloid-forming agent such as hydroxypropylcellulose as a retarder are disclosed. Here, the retarder reduces the release of metformin hydrochloride from the tablet by 4%.
It is added for the purpose of controlling and delaying over a period of time (0.5 to 10 hours). Furthermore, it is described that when the residual water content of the composition before tableting was less than 0.5%, capping occurred and tableting was not possible.
【０００５】一方、米国では、塩酸メトホルミンを５０
０ｍｇ、８５０ｍｇ又は１０００ｍｇを含有するフィル
ムコーティング錠剤が販売されている。このうち、グル
コファージ錠（商品名、ブリストルマイヤーズ スクイ
ブ社）は、塩酸メトホルミン、ポリビニルピロリドン及
びステアリン酸マグネシウムからなる錠剤にヒドロキシ
プロピルメチルセルロースなどをコーティングしたもの
であり（Physicians'Desk Reference 55Editions 200
1）、もともとの塩酸メトホルミンの含有量は多いが、
賦形剤の添加を少なくすることにより、錠剤を小型化し
たものといえる。しかし、日本薬局方第１３改正の溶出
試験（パドル法、回転数５０ｒｐｍ、試験液 水）を行
うとき、試験開始後１５分時点における塩酸メトホルミ
ンの溶出率は６０％以下であり、その放出性は速やかと
はいえない。On the other hand, in the United States, metformin hydrochloride is used in 50
Film-coated tablets containing 0 mg, 850 mg or 1000 mg are sold. Glucophage tablets (trade name, Bristol-Myers Squibb) are tablets comprising metformin hydrochloride, polyvinylpyrrolidone and magnesium stearate coated with hydroxypropylmethylcellulose or the like (Physicians' Desk Reference 55 Editions 200 Edition).
1) Although the original content of metformin hydrochloride is large,
It can be said that the tablet was miniaturized by reducing the amount of the excipient added. However, when performing the dissolution test (Paddle method, rotation speed 50 rpm, test solution water) of the 13th revision of the Japanese Pharmacopoeia, the dissolution rate of metformin hydrochloride at 15 minutes after the start of the test is 60% or less, and its release property is Not immediately.
【０００６】塩酸メトホルミンを経口投与した場合、そ
の吸収部位は、小腸上部の狭い部分に限局しており、例
えば徐放性製剤とした場合に、塩酸メトホルミンの生体
利用率が低下することが知られている。このため、塩酸
メトホルミンの普通錠を設計する場合には、速放性を有
する錠剤とすることが生体利用率の面で好ましいと考え
られる。When metformin hydrochloride is orally administered, its absorption site is limited to a narrow part of the upper part of the small intestine. For example, when a sustained release preparation is used, the bioavailability of metformin hydrochloride is known to decrease. ing. Therefore, when designing a normal tablet of metformin hydrochloride, it is considered that a tablet having immediate release properties is preferable in terms of bioavailability.
【０００７】[0007]
【発明が解決しようとする課題】従って、本発明の目的
は、塩酸メトホルミンを速やかに溶出でき、錠剤を小型
化するとともに、製造性及び保存による安定性に優れた
錠剤を提供することにある。SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to provide a tablet capable of rapidly dissolving metformin hydrochloride, reducing the size of the tablet, and having excellent manufacturability and storage stability.
【０００８】[0008]
【課題を解決するための手段】本発明者らは、塩酸メト
ホルミンを有効成分とする錠剤について鋭意検討を重ね
た結果、結合剤として、特定の粘度を有するヒドロキシ
プロピルセルロースを使用することにより、崩壊剤など
の他の添加剤を特に加えることなく、塩酸メトホルミン
を速やかに溶出できる錠剤が得られることを見出し、本
発明を完成するに至った。Means for Solving the Problems The present inventors have conducted intensive studies on tablets containing metformin hydrochloride as an active ingredient. As a result, the use of hydroxypropylcellulose having a specific viscosity as a binder disintegrates. The present inventors have found that a tablet capable of rapidly dissolving metformin hydrochloride can be obtained without particularly adding other additives such as an agent, and have completed the present invention.
【０００９】すなわち、本発明は次の成分（Ａ）及び
（Ｂ）： （Ａ）塩酸メトホルミン、（Ｂ）２０℃における２質量
％水溶液の粘度が２．０〜１０．０mPasであるヒドロキ
シプロピルセルロースを含有することを特徴とする速放
性錠剤を提供するものである。また、本発明は、（Ａ）
塩酸メトホルミン及び（Ｂ）２０℃における２質量％水
溶液の粘度が２．０〜１０．０mPasであるヒドロキシプ
ロピルセルロースを含む製剤原料混合粉末を、エタノー
ルを用いて造粒、乾燥した後、（Ｃ）滑沢剤を加えて打
錠することを特徴とする速放性錠剤の製造方法を提供す
るものである。More specifically, the present invention provides the following components (A) and (B): (A) metformin hydrochloride, (B) hydroxypropyl cellulose having a 2% by mass aqueous solution at 20 ° C. having a viscosity of 2.0 to 10.0 mPas. The present invention provides an immediate release tablet characterized by containing Further, the present invention relates to (A)
A granulated raw material powder containing metformin hydrochloride and (B) a hydroxypropylcellulose having a viscosity of 2.0 to 10.0 mPas of a 2% by mass aqueous solution at 20 ° C. is granulated using ethanol, and dried (C). An object of the present invention is to provide a method for producing an immediate release tablet, which comprises adding a lubricant and compressing the tablet.
【００１０】[0010]
【発明の実施の形態】本発明においては、成分（Ａ）の
塩酸メトホルミンは、１錠中に２５０〜１０００ｍｇを
含有することができるが、錠剤の服用感をよくするため
に、錠剤はできる限り小型であることが望ましい。この
とき、錠剤中の塩酸メトホルミンの濃度は高く設定する
こととなり、８５〜９７．５質量％、特に９０〜９５質
量％が好ましい。例えば、１錠中に塩酸メトホルミンを
２５０ｍｇ含有する錠剤の場合、錠剤の重量は、８５質
量％のときは約２９４ｍｇ、９０質量％のときは約２７
８ｍｇとなり、小型化され、服用感が改善された錠剤と
することができる。BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, the metformin hydrochloride of the component (A) can contain 250 to 1000 mg per tablet, but in order to improve the feeling of taking the tablet, the tablet should be as small as possible. It is desirable to be small. At this time, the concentration of metformin hydrochloride in the tablet is set to be high, and is preferably 85 to 97.5% by mass, particularly preferably 90 to 95% by mass. For example, in the case of a tablet containing 250 mg of metformin hydrochloride in one tablet, the weight of the tablet is about 294 mg at 85% by mass and about 27% at 90% by mass.
8 mg, resulting in a tablet that is reduced in size and has an improved feeling of taking.
【００１１】本発明に用いられる成分（Ｂ）の２０℃に
おける２質量％水溶液の粘度が２．０〜１０．０mPasで
あるヒドロキシプロピルセルロースは、結合剤として作
用するものである。粘度の測定はＢ型粘度計を用いて行
なわれる。粘度が２．０〜１０．０mPasの範囲であるヒ
ドロキシプロピルセルロースを使用すると、塩酸メトホ
ルミンの溶出はいずれの場合も速やかであるが、粘度の
低いヒドロキシプロピルセルロースを用いる方が、より
速やかな溶出を得ることができる。このため、なかでも
粘度が２．０〜５．９mPasのヒドロキシプロピルセルロ
ースを使用するのが好ましく、さらに、粘度が２．０〜
２．９mPasのヒドロキシプロピルセルロースを使用する
のがより好ましい。例えば、粘度が２．０〜２．９mPas
のヒドロキシプロピルセルロースとして、ＨＰＣ−ＳＳ
Ｌ（日本曹達）、粘度が３．０〜５．９mPasのヒドロキ
シプロピルセルロースとして、ＨＰＣ−ＳＬ（日本曹
達）、粘度が６．０〜１０．０mPasのヒドロキシプロピ
ルセルロースとして、ＨＰＣ−Ｌ（日本曹達）を使用す
ることができる。Hydroxypropylcellulose having a viscosity of 2.0 to 10.0 mPas of a 2% by weight aqueous solution of the component (B) at 20 ° C. used in the present invention acts as a binder. The viscosity is measured using a B-type viscometer. When using hydroxypropylcellulose having a viscosity in the range of 2.0 to 10.0 mPas, the elution of metformin hydrochloride is rapid in any case, but using hydroxypropylcellulose with low viscosity results in more rapid elution. Obtainable. For this reason, it is preferable to use hydroxypropylcellulose having a viscosity of 2.0 to 5.9 mPas.
More preferably, 2.9 mPas of hydroxypropylcellulose is used. For example, the viscosity is 2.0 to 2.9 mPas
HPC-SS as hydroxypropyl cellulose
L (Nippon Soda), as a hydroxypropyl cellulose having a viscosity of 3.0 to 5.9 mPas, HPC-SL (Nippon Soda), and as a hydroxypropyl cellulose having a viscosity of 6.0 to 10.0 mPas, HPC-L (Nippon Soda) ) Can be used.
【００１２】一方、粘度が１０．０mPasより高いヒドロ
キシプロピルセルロースとしては、１５０〜４００mPas
であるＨＰＣ−Ｍ（日本曹達）、１０００〜４０００mP
asであるＨＰＣ−Ｈ（日本曹達）などが挙げられるが、
これらの使用は、特表平１０−５０５６０４号に開示さ
れたように、錠剤からの塩酸メトホルミンの溶出を遅延
させる結果が得られたほか、打錠する際にキャッピング
の打錠障害が認められた。On the other hand, hydroxypropylcellulose having a viscosity higher than 10.0 mPas is 150 to 400 mPas.
HPC-M (Nippon Soda), 1000-4000 mP
HPC-H (Nippon Soda), which is as,
These uses, as disclosed in JP-T-10-505604, not only resulted in delaying the dissolution of metformin hydrochloride from the tablets, but also found tableting impairment of capping during tableting. .
【００１３】本発明において、成分（Ｂ）のヒドロキシ
プロピルセルロースは、塩酸メトホルミンと混合したと
き、良好な造粒及び打錠の製造性が得られるものであ
り、その錠剤中の濃度は、２〜１０質量％、特に４〜９
質量％が好ましい。In the present invention, the hydroxypropylcellulose of the component (B), when mixed with metformin hydrochloride, provides good granulation and tableting manufacturability. 10% by weight, especially 4 to 9
% By mass is preferred.
【００１４】また、本発明においては、良好な打錠性を
確保するために、成分（Ａ）及び成分（Ｂ）を含む造粒
物に、タルク、ステアリン酸マグネシウムなどの滑沢剤
（Ｃ）を１種又は２種以上を混合した後、打錠操作を行
うのが好ましい。錠剤中の滑沢剤の濃度は、０．５〜３
質量％、特に１〜２質量％が好ましい。In the present invention, in order to ensure good tableting properties, the granulated product containing the component (A) and the component (B) is added to a lubricant (C) such as talc or magnesium stearate. It is preferable to perform a tableting operation after mixing one or two or more. The concentration of the lubricant in the tablet is 0.5-3
% By weight, especially 1-2% by weight, is preferred.
【００１５】さらに、本発明では、成分（Ａ）、（Ｂ）
及び（Ｃ）の量的な関係を充足する限り、所望により他
の添加剤を含んでもよい。他の添加剤としては、乳糖、
マンニトール、バレイショデンプン、トウモロコシデン
プン、無水リン酸水素カルシウムなどが挙げられる。Further, in the present invention, the components (A) and (B)
If desired, other additives may be included as long as the quantitative relationship of (C) and (C) is satisfied. Other additives include lactose,
Mannitol, potato starch, corn starch, anhydrous calcium hydrogen phosphate and the like.
【００１６】本発明の速放性錠剤は、例えば成分（Ａ）
及び成分（Ｂ）を含む製剤原料混合粉末を、エタノール
で造粒、乾燥した後、滑沢剤を加えて打錠することによ
って製造することができる。この際の圧縮成形に使用す
る打錠機としては、通常の回転式打錠機を用いることが
できる。The immediate-release tablet of the present invention comprises, for example, the component (A)
The mixture can be produced by granulating and drying the raw material mixture powder containing the component (B) with ethanol, adding a lubricant, and tableting. As a tableting machine used for compression molding at this time, a normal rotary tableting machine can be used.
【００１７】なお、本発明によれば、打錠前の組成物の
残留水分が０．５％未満（カールフィシャー法）である
場合でも、良好に打錠することができる。According to the present invention, even if the residual water content of the composition before tableting is less than 0.5% (Karl Fischer method), tableting can be performed well.
【００１８】また、本発明の速放性錠剤は、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
ースなどの水溶性皮膜を施して、フィルムコーティング
錠とすることができる。フィルムコーティング方法は、
例えば、パンコーティング装置などを用いて、通常この
分野で用いられる方法により行うことができる。The immediate-release tablet of the present invention can be formed into a film-coated tablet by applying a water-soluble coating such as hydroxypropylcellulose or hydroxypropylmethylcellulose. The film coating method is
For example, it can be performed using a pan coating apparatus or the like and a method usually used in this field.
【００１９】本発明の速放性錠剤としては、第１３改正
日本薬局方による溶出試験法（パドル法、回転数５０ｒ
ｐｍ、試験液 水）により試験するとき、試験開始後１
５分時点で塩酸メトホルミンの溶出率が８５％以上とな
るのが好ましい。The immediate-release tablets of the present invention include a dissolution test method (paddle method, rotation speed of 50
pm, test liquid water), 1
It is preferable that the dissolution rate of metformin hydrochloride be 85% or more at 5 minutes.
【実施例】次に、本発明を実施例によりさらに詳細に説
明するが、本発明は、これらの例によって何ら限定され
るものではない。EXAMPLES Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.
【００２０】［実施例１］錠剤の成分分量及び錠剤中の
成分の濃度を表１に示す。Example 1 Table 1 shows the component amounts of the tablets and the concentrations of the components in the tablets.
【００２１】[0021]
【表１】 [Table 1]
【００２２】塩酸メトホルミン２３１．５ｇ及び粘度
２．０〜２．９mPasのヒドロキシプロピルセルロース
（ＨＰＣ−ＳＳＬ）１６．０ｇをハイスピードミキサー
（深江工業）中で混合した後、エタノールで造粒した。
造粒物を棚式乾燥機に移し、４５℃で６時間乾燥した。
乾燥した造粒物は 目開き５９０ μｍの篩を用いて篩過
した。これに、タルク１．２５ｇ及びステアリン酸マグ
ネシウム１．２５ ｇを添加して混合した後、高速回転
式打錠機（畑鐡工所）で、１錠重量を２７０ｍｇとし
て、打錠し、１錠中に塩酸メトホルミンを２５０m含有
する錠剤を製造した。造粒性及び打錠性のいずれも良好
であった。なお、打錠前の造粒物及び錠剤の残留水分
は、いずれも約０．３％であった。231.5 g of metformin hydrochloride and 16.0 g of hydroxypropylcellulose (HPC-SSL) having a viscosity of 2.0 to 2.9 mPas were mixed in a high speed mixer (Fukae Kogyo), and then granulated with ethanol.
The granulated product was transferred to a tray dryer and dried at 45 ° C. for 6 hours.
The dried granules were sieved using a sieve having a mesh size of 590 μm. To this, 1.25 g of talc and 1.25 g of magnesium stearate were added and mixed, and the mixture was tableted with a high-speed rotary tableting machine (Hata Iron Works) to a weight of 270 mg for one tablet and tableted. Tablets containing 250 m of metformin hydrochloride therein were produced. Both granulation properties and tableting properties were good. In addition, the residual moisture of the granules and tablets before tableting was about 0.3%.
【００２３】［実施例２］錠剤の成分分量及び錠剤中の
成分の濃度を表２に示す。Example 2 Table 2 shows the component amounts of the tablets and the concentrations of the components in the tablets.
【００２４】[0024]
【表２】 [Table 2]
【００２５】粘度３．０〜５．９mPasのヒドロキシプロ
ピルセルロース（ＨＰＣ−ＳＬ）を用いた以外は、実施
例１と同様に製造した。造粒性及び打錠性のいずれも良
好であった。The same procedure was followed as in Example 1 except that hydroxypropylcellulose (HPC-SL) having a viscosity of 3.0 to 5.9 mPas was used. Both granulation properties and tableting properties were good.
【００２６】［実施例３］錠剤の成分分量及び錠剤中の
成分の濃度を表３に示す。Example 3 Table 3 shows the component amounts of the tablets and the concentrations of the components in the tablets.
【００２７】[0027]
【表３】 [Table 3]
【００２８】粘度６．０〜１０．０mPasのヒドロキシプ
ロピルセルロース（ＨＰＣ−Ｌ）を用いた以外は、実施
例１と同様に製造した。造粒性及び打錠性のいずれも良
好であった。The same procedure was followed as in Example 1 except that hydroxypropylcellulose (HPC-L) having a viscosity of 6.0 to 10.0 mPas was used. Both granulation properties and tableting properties were good.
【００２９】［比較例１］錠剤の成分分量及び錠剤中の
成分の濃度を表４に示す。Comparative Example 1 The component amounts of the tablets and the concentrations of the components in the tablets are shown in Table 4.
【００３０】[0030]
【表４】 [Table 4]
【００３１】粘度１５０〜４００mPasのヒドロキシプロ
ピルセルロース（ＨＰＣ−M ）を用いた以外は、実施例
１と同様に製造したが、キャッピングの打錠障害が見ら
れた。The same procedure was followed as in Example 1 except that hydroxypropylcellulose (HPC-M) having a viscosity of 150 to 400 mPas was used, but tableting trouble due to capping was observed.
【００３２】［試験例１］溶出試験 実施例１〜３の錠剤について、試験液として３７℃に加
温した水９００ｍLを用い、第１３改正日本薬局方によ
る溶出試験法第２法（パドル法）により、毎分５０回転
で試験を行なった（ｎ＝３）。溶出試験開始後５、１
０、及び１５分後に、試験液１０ｍLを採取し、ＨＰＬ
Ｃ法（カラム：ＯＤＳ、移動相：１−ヘプタンスルホン
酸ナトリウム・リン酸水素二カリウム／水・アセトニト
リル混液、検出：紫外吸収２３２ｎｍ）により測定し
た。図１に示すように、いずれの錠剤も、試験開始後１
５分時点における塩酸メトホルミンの溶出率は８５％以
上であり、良好な速放性を示した。[Test Example 1] Dissolution test The tablets of Examples 1 to 3 were tested using 900 mL of water heated to 37 ° C. as a test solution, and the second method (Paddle method) of the 13th revised Japanese Pharmacopoeia. The test was performed at 50 revolutions per minute (n = 3). 5, 1 after starting dissolution test
After 0 and 15 minutes, 10 mL of the test solution was collected and HPL was collected.
It was measured by the method C (column: ODS, mobile phase: a mixture of sodium 1-heptanesulfonate / dipotassium hydrogen phosphate / water / acetonitrile, detection: ultraviolet absorption 232 nm). As shown in FIG.
The dissolution rate of metformin hydrochloride at 5 minutes was 85% or more, indicating good rapid release.
【００３３】［試験例２］保存安定性試験 実施例１及び２の錠剤について、ＰＴＰ包装し４０℃７
５％ＲＨに２箇月間保存し、試験例1の溶出試験を行な
った（ｎ＝３）。いずれの錠剤についても、錠剤外観に
も変化はなかった。さらに、試験開始後１５分時点にお
ける塩酸メトホルミンの溶出率は８５％以上であった。
このことから、保存安定性は良好であった。[Test Example 2] Storage stability test The tablets of Examples 1 and 2 were PTP-packaged and packed at 40 ° C.
After storing at 5% RH for 2 months, the dissolution test of Test Example 1 was performed (n = 3). There was no change in the tablet appearance for any of the tablets. Further, the dissolution rate of metformin hydrochloride at 15 minutes after the start of the test was 85% or more.
From this, the storage stability was good.
【００３４】[0034]
【発明の効果】本発明によれば、２０℃における２質量
％水溶液の粘度が２．０〜１０．０mPasの範囲であるヒ
ドロキシプロピルセルロースを使用することにより、有
効成分である塩酸メトホルミンが速やかに溶出できる錠
剤が得られる。さらに、塩酸メトホルミンを８５質量％
以上含有して小型化した錠剤を得ることができる。ま
た、実生産性及び保存安定性に優れるなどの効果を奏す
る。According to the present invention, by using hydroxypropylcellulose having a 2% by mass aqueous solution at 20 ° C. having a viscosity in the range of 2.0 to 10.0 mPas, metformin hydrochloride as an active ingredient can be rapidly produced. A dissolvable tablet is obtained. Furthermore, metformin hydrochloride was 85% by mass.
Tablets containing the above and miniaturized can be obtained. In addition, it has effects such as excellent actual productivity and storage stability.
【図１】試験例１に記載した実施例１〜３の錠剤の溶出
試験結果を示す。1 shows the dissolution test results of the tablets of Examples 1 to 3 described in Test Example 1. FIG.
───────────────────────────────────────────────────── フロントページの続き Ｆターム(参考） 4C076 AA37 BB01 CC21 EE32 FF09 FF33 GG12 4C206 AA01 AA02 HA31 MA05 MA55 MA72 NA20 ZC35 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C076 AA37 BB01 CC21 EE32 FF09 FF33 GG12 4C206 AA01 AA02 HA31 MA05 MA55 MA72 NA20 ZC35
Claims (7)
％水溶液の粘度が２．０〜１０．０mPasであるヒドロキ
シプロピルセルロースを含有することを特徴とする速放
性錠剤。1. The following components (A) and (B): (A) Metformin hydrochloride, (B) Hydroxypropylcellulose having a 2% by mass aqueous solution at 20 ° C. having a viscosity of 2.0 to 10.0 mPas. An immediate release tablet characterized by the above-mentioned.
質量％である請求項１記載の速放性錠剤。2. The content of the component (A) is from 85 to 97.5.
The immediate-release tablet according to claim 1, which is in mass%.
である請求項１又は２記載の速放性錠剤。3. The content of the component (B) is 2 to 10% by mass.
The immediate-release tablet according to claim 1 or 2, wherein
〜３のいずれか１項記載の速放性錠剤。4. The method according to claim 1, further comprising (C) a lubricant.
The immediate-release tablet according to any one of claims 1 to 3.
合粉末を、エタノールを用いて造粒した後、打錠して得
られるものである請求項１〜４記載のいずれか１項記載
の速放性錠剤。5. The method according to claim 1, wherein the raw material mixture powder containing the components (A) and (B) is granulated with ethanol and then tableted. The immediate-release tablet of the above.
ル法、回転数５０ｒｐｍ、試験液 水）を行うとき、試
験開始後１５分時点における塩酸メトホルミンの溶出率
が８５％以上である請求項１〜５のいずれか１項記載の
速放性錠剤。6. The dissolution rate of metformin hydrochloride at 15 minutes after the start of the test when performing a dissolution test (paddle method, rotation speed 50 rpm, test liquid water) according to the Japanese Pharmacopoeia 13th Edition. The immediate-release tablet according to any one of claims 1 to 5.
℃における２質量％水溶液の粘度が２．０〜１０．０mP
asであるヒドロキシプロピルセルロースを含む製剤原料
混合粉末を、エタノールを用いて造粒、乾燥した後、
（Ｃ）滑沢剤を加えて打錠することを特徴とする速放性
錠剤の製造方法。(A) Metformin hydrochloride and (B) 20
The viscosity of a 2% by mass aqueous solution at 2.0 ° C is 2.0 to 10.0 mP
The drug substance mixed powder containing hydroxypropylcellulose which is as is granulated using ethanol and dried,
(C) A method for producing an immediate release tablet, which comprises adding a lubricant and tableting.
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| JP2001136873A JP4848558B2 (en) | 2001-05-08 | 2001-05-08 | Rapid-release tablets containing metformin hydrochloride |
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| EXPY | Cancellation because of completion of term |