JPH0283316A - Sustained release tablet - Google Patents
Sustained release tabletInfo
- Publication number
- JPH0283316A JPH0283316A JP23535988A JP23535988A JPH0283316A JP H0283316 A JPH0283316 A JP H0283316A JP 23535988 A JP23535988 A JP 23535988A JP 23535988 A JP23535988 A JP 23535988A JP H0283316 A JPH0283316 A JP H0283316A
- Authority
- JP
- Japan
- Prior art keywords
- water
- drug
- sustained
- release
- coating
- 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.)
- Pending
Links
- 239000007939 sustained release tablet Substances 0.000 title claims abstract description 15
- 239000003814 drug Substances 0.000 claims abstract description 34
- 229940079593 drug Drugs 0.000 claims abstract description 34
- 239000011248 coating agent Substances 0.000 claims abstract description 23
- 238000000576 coating method Methods 0.000 claims abstract description 21
- 238000013268 sustained release Methods 0.000 claims abstract description 20
- 239000012730 sustained-release form Substances 0.000 claims abstract description 20
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 14
- 239000000017 hydrogel Substances 0.000 claims abstract description 10
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims abstract description 8
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims abstract description 7
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims abstract description 7
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229920003169 water-soluble polymer Polymers 0.000 claims description 19
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 5
- 229920000609 methyl cellulose Polymers 0.000 claims description 5
- 239000001923 methylcellulose Substances 0.000 claims description 5
- 235000010981 methylcellulose Nutrition 0.000 claims description 5
- 239000002202 Polyethylene glycol Substances 0.000 claims description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 2
- 229920001223 polyethylene glycol Polymers 0.000 claims description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract description 17
- 239000003826 tablet Substances 0.000 abstract description 16
- 238000000034 method Methods 0.000 abstract description 11
- 239000000499 gel Substances 0.000 abstract description 10
- 238000002156 mixing Methods 0.000 abstract description 5
- SKZKKFZAGNVIMN-UHFFFAOYSA-N Salicilamide Chemical compound NC(=O)C1=CC=CC=C1O SKZKKFZAGNVIMN-UHFFFAOYSA-N 0.000 abstract description 4
- 229960000581 salicylamide Drugs 0.000 abstract description 4
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 abstract description 4
- 230000001079 digestive effect Effects 0.000 abstract description 3
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 abstract description 2
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 abstract description 2
- 229960002009 naproxen Drugs 0.000 abstract description 2
- 229960000278 theophylline Drugs 0.000 abstract description 2
- 229920000642 polymer Polymers 0.000 abstract 5
- 239000006185 dispersion Substances 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 description 9
- 238000004090 dissolution Methods 0.000 description 7
- 230000000052 comparative effect Effects 0.000 description 6
- 238000007922 dissolution test Methods 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 238000010828 elution Methods 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- 239000007864 aqueous solution Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 229920002678 cellulose Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000007888 film coating Substances 0.000 description 2
- 238000009501 film coating Methods 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000002667 nucleating agent Substances 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 description 1
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000003125 aqueous solvent Substances 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229960001476 pentoxifylline Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 238000005498 polishing Methods 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
Abstract
Description
【発明の詳細な説明】
（産業上の利用分野）
本発明は、徐放性錠剤、とくには初期の薬物の放出を抑
制し、水あるいは消化液に接して、より早く安定なゲル
層を形成することのできる徐放性錠剤に関するものであ
る。Detailed Description of the Invention (Field of Industrial Application) The present invention is a sustained-release tablet, particularly one that suppresses initial drug release and quickly forms a stable gel layer when in contact with water or digestive fluids. This invention relates to sustained-release tablets that can be used as tablets.
（従来技術とその問題点）
従来、ヒドロゲル形成能のある水溶性高分子を用いた徐
放性錠剤は、薬物と水溶性高分子を混合し、必要に応じ
てその他の賦形剤を添加して打錠されたもので、容易に
薬物の徐放化が達成できる優れたものとして知られてい
る。このような錠剤の溶出特性を改善する方法として、
例えば、水溶性高分子として数平均分子量が５０，００
０以下のヒドロキシプロピルメチルセルロース
ルボキシメチルセルロースナトリウム（ＣＭＣ−Ｎａ）
とを配合する方法（特開昭５８−１１０５１３号公報）
。(Prior art and its problems) Conventionally, sustained-release tablets using water-soluble polymers capable of forming hydrogels have been produced by mixing drugs and water-soluble polymers, and adding other excipients as necessary. It is known as an excellent product that can easily achieve sustained release of drugs. As a method to improve the dissolution characteristics of such tablets,
For example, as a water-soluble polymer, the number average molecular weight is 50,00.
0 or less hydroxypropyl methyl cellulose ruboxy methyl cellulose sodium (CMC-Na)
(Japanese Unexamined Patent Publication No. 110513/1983)
.
数平均分子量が５０ 、 ０００以上のＨ Ｐ Ｍ Ｃ
とＣＭＣ−Ｎａとを配合する方法（特開昭５８−１７４
３１１号公報）、あるいは錠剤の組成中のｉ（Ｐ Ｍ
Ｃについて湿潤処理を施す方法（特開昭５２−１４５５
１４号公報）、ＨＰ ＭＣに界面活性剤を配合する方法
（特開昭６０−２１８３２９号公報）などが提案されて
いる。HPM C with a number average molecular weight of 50,000 or more
Method of blending and CMC-Na
311), or i (P M
Method of performing wet treatment on C (Japanese Patent Application Laid-open No. 52-1455
14) and a method of blending a surfactant into HP MC (Japanese Patent Application Laid-Open No. 60-218329).
（発明が解決しようとする課題）
しかしながら、これらはいずれも徐放性錠剤の処方か、
あるいはヒドロゲル形成能のある水溶性高分子としての
Ｈ１’ＭＣの処理方法に基づく徐放性錠剤の製造方法に
関してのもので、安定な薬物の濃度勾配のついたゲル層
を形成させはするが、それまでに多くの時間を要するた
め、錠剤服用後の初期の薬物の放出が早く、過剰に薬物
を溶出してしまうという欠点があった。(Problem to be solved by the invention) However, these are all sustained release tablet formulations,
Alternatively, it relates to a method for manufacturing sustained-release tablets based on a method for treating H1'MC as a water-soluble polymer capable of forming a hydrogel, which forms a gel layer with a stable drug concentration gradient; Since it takes a lot of time to reach that point, the initial release of the drug after taking the tablet is rapid, resulting in excessive drug elution.
徐放性製剤は時間に対して一定比率で薬物を放出するも
のが望ましいが、従来の水溶性高分子を用いた徐放性錠
剤は薬物と水溶性高分子とを均一に混合して打錠したも
ののため、水あるいは消化液に接して表面に存在する過
剰な薬物を放出し安定なゲル層を形成するのに必要な時
間が１〜２時間であった。すなわち、薬物の放出挙動に
おいて初期の１〜２時間の溶出率は、それ以降の溶出率
と比べてずっと大きく、最初の１〜２時間で大勢が決ま
るという状態にあった。It is desirable for sustained-release preparations to release the drug at a constant rate over time, but conventional sustained-release tablets using water-soluble polymers are compressed by uniformly mixing the drug and water-soluble polymer. Therefore, the time required to release the excess drug present on the surface and form a stable gel layer upon contact with water or digestive fluid was 1 to 2 hours. That is, in terms of drug release behavior, the dissolution rate during the initial 1 to 2 hours was much higher than the subsequent dissolution rate, and most of the release behavior was determined in the first 1 to 2 hours.
とくに薬物の水溶性が大きい場合には、形成される薬物
の濃度勾配の認められるゲル層が厚くなり、安定なゲル
層を形成するまでの間、薬物が溶出液と接触し、溶解度
の小さい薬物と比べて、より多量に溶出してしまうので
、その適用範囲や処方が制約される欠点があった。また
逆に薬物の水溶性が小さい場合には、水溶性高分子とし
て高粘度のものを少量用いる処方が有利になるが、溶出
初期の錠剤表面の部分的な崩壊により溶出速度が早くな
る欠点があった。なお安定なゲル層の形成後は錠剤の調
製方法の影響が殆どなく一定した速度で薬物を放出する
。In particular, when the drug has a high water solubility, the gel layer that forms where the concentration gradient of the drug is observed becomes thick, and the drug comes into contact with the eluate until a stable gel layer is formed, and the drug with low solubility becomes thicker. Since it elutes in a larger amount than that of other methods, it has the disadvantage that its application range and formulation are restricted. On the other hand, if the water solubility of the drug is low, it is advantageous to use a small amount of a high viscosity water-soluble polymer in a formulation, but this has the disadvantage that the dissolution rate becomes faster due to partial collapse of the tablet surface at the initial stage of dissolution. there were. Once a stable gel layer is formed, the drug is released at a constant rate, with little influence from the tablet preparation method.
本発明は、通常の水溶性高分子によるフィルムコーティ
ングに比へてコーティング量を多くすると、水溶性の高
い薬物の場合には安定したゲル層を形成するまでの時間
を短くし、より０次に近い放出特性を持たせることがで
きる、また水溶性の小さい薬物の場合には、核となる徐
放性薬剤がゆっくりと水に濡れるため、錠剤の部分的崩
壊が抑制されバラツキの小さい製剤が得られる、という
利点のあることに着目して達成されたものである。In the present invention, when the amount of coating is increased compared to ordinary film coating with water-soluble polymers, the time required to form a stable gel layer is shortened in the case of highly water-soluble drugs, and the zero-order In the case of drugs with low water solubility, the core sustained-release drug is slowly wetted by water, which suppresses partial disintegration of the tablet and produces a formulation with less variation. This was achieved by focusing on the advantage of being able to
したがって、本発明の目的は良好な放出特性を有する徐
放性錠剤を堤供するにある。Therefore, it is an object of the present invention to provide sustained release tablets with good release properties.
（問題点を解決するための手段）
本発明による徐放性錠剤は、薬物とヒドロゲル形成能の
ある水溶性高分子を主体とする徐放性核剤に、水溶性高
分子をコーティングしてなるものとしたことを要旨とす
るものである。(Means for Solving the Problems) The sustained-release tablet of the present invention is made by coating a sustained-release core agent containing a drug and a water-soluble polymer capable of forming a hydrogel with a water-soluble polymer. The main point is that
これをさらに詳細に説明すると、本発明において用いら
れる徐放性核剤はヒドロゲル形成能のある水溶性高分子
を薬物と共に均一に混合したものである。ここで使用さ
れるヒドロゲル形成能のある水溶性高分子としては、ヒ
ドロキシプロピルメチルセルロース、ヒドロキシプロピ
ルセルロース、およびメチルセルロースなどの１種また
は２種以上の組合せが挙げられる。薬物の種類としては
、水に対して比較的溶解性が小さいか、あるいは難溶性
のものが好ましく、例えばサリチルアミド、ナプロキセ
ン、テオフィリン、ペントキシフィリンなどが好適であ
る。To explain this in more detail, the sustained-release core agent used in the present invention is a mixture of a water-soluble polymer capable of forming a hydrogel and a drug homogeneously. Examples of the water-soluble polymer capable of forming a hydrogel used here include one or a combination of two or more of hydroxypropyl methylcellulose, hydroxypropylcellulose, and methylcellulose. The type of drug is preferably one that has relatively low solubility in water or is poorly soluble in water, such as salicylamide, naproxen, theophylline, pentoxifylline, and the like.
徐放性核剤にコーチインタする水溶性高分子は、水に溶
けて粘性を発現するか、ヒドロゲルを形成するものひあ
ればよく、これには例えばヒドロキシプロピルメチルセ
ルロース、ヒドロキシプロピルセルロース、メチルセル
ロースなどのセルロース誘導体、ポリエチレングリコー
ル、ポリビニルピロリドン、およびポリビニルアルコー
ルなどの合成水溶性高分子などが挙げられ、これらは１
種または２種以上の組合せで使用される。これらの内で
は、コーティング剤として広く使われているセルロース
誘導体が好ましい。The water-soluble polymer to be coached into the sustained-release nucleating agent may be one that dissolves in water to develop viscosity or form a hydrogel, such as hydroxypropylmethylcellulose, hydroxypropylcellulose, methylcellulose, etc. Synthetic water-soluble polymers such as cellulose derivatives, polyethylene glycol, polyvinylpyrrolidone, and polyvinyl alcohol are included;
Used in species or in combination of two or more species. Among these, cellulose derivatives, which are widely used as coating agents, are preferred.
コーティングは従来公知の方法でよく、コーティングパ
ン中でコーティング剤の水溶液あるいは有機溶剤溶液、
または水−有機溶剤溶液をスプレすればよい。なお、こ
れらのコーティング液には必要に応じてタルク、酸化チ
タン等の通常添加される添加剤を加えてもよい。Coating may be done by a conventionally known method, including coating in an aqueous or organic solvent solution in a coating pan;
Alternatively, a water-organic solvent solution may be sprayed. Additionally, commonly used additives such as talc and titanium oxide may be added to these coating liquids as necessary.
このときのコーティング量としては徐放性核剤に対して
５重量％以上が好ましい。これが５％未満では錠剤の初
期の崩壊を抑える効果が不充分となる。コーティング量
はコーティング時間などの制約の許される範囲でできる
だけ多いことが望ましい。The coating amount at this time is preferably 5% by weight or more based on the sustained release core agent. If this is less than 5%, the effect of suppressing initial disintegration of the tablet will be insufficient. It is desirable that the amount of coating be as large as possible within the range allowed by constraints such as coating time.
以上のようにして得られた錠剤は、必要に応じて通常行
われるポリッシング等を施すことができる。The tablets obtained as described above can be subjected to conventional polishing and the like, if necessary.
（実施例）
以ト、本発明の具体的態様を実施例および比較例により
説明するが、本発明はこの実施例に限定されるものでは
ない。なお各例中、部および％はすべで重量部および重
量％を表わす。(Examples) Hereinafter, specific aspects of the present invention will be explained using Examples and Comparative Examples, but the present invention is not limited to these Examples. In each example, all parts and % represent parts by weight and % by weight.
実施例 １゜
（徐放性核剤の調ｌ２）
１錠当り、サリチルアミド（吉富製薬■製）を３００、
、ヒドロキシプロピルメチルセルロース９０Ｓ１ト１５
０００（信越化学工業■製、商品名＝２０℃における２
％水溶液の粘度が１４ 、７００ｃｐｓ）を５０■の割
合で均一に混合し、さらにステアリン酸マグネシウムを
１％混合し、 １０ｍｎ＋φの平型の杵を用いて打錠圧
２．５ｔで打錠した。Example 1゜ (Preparation 12 of sustained release core agent) 300% salicylamide (manufactured by Yoshitomi Pharmaceutical ■) per tablet,
, hydroxypropyl methylcellulose 90S1-15
000 (manufactured by Shin-Etsu Chemical Co., Ltd., product name = 2 at 20℃
% aqueous solution with a viscosity of 14.700 cps) was uniformly mixed at a ratio of 50 cm, and 1% of magnesium stearate was further mixed and tableted at a tableting pressure of 2.5 t using a flat punch of 10 mm + φ.
（コーティング液組成）
ヒドロキシプロピルメチルセルロースＴＣ−５５（信越
化学工業■製、商品名＝２０℃における２％水溶液の粘
度が１４．７ｃｐｓ） ・・・・・・５％精
製水 ・・・・・・９５％
上記組成のコーティング液を通気式のコーティング装置
を用いて一般のフィルムコーティングと同様にコーティ
ングした。コーティング量は徐放性核剤に対して２０％
とした。(Coating liquid composition) Hydroxypropyl methyl cellulose TC-55 (manufactured by Shin-Etsu Chemical Co., Ltd., trade name = viscosity of 2% aqueous solution at 20°C is 14.7 cps) ...5% purified water ... 95%
The coating solution having the above composition was coated using a vent-type coating device in the same manner as general film coating. Coating amount is 20% of sustained release core agent
And so.
（結 果）
得られた錠剤について日本薬局方溶出試験法に基づいて
溶出試験を行った。(Results) A dissolution test was conducted on the obtained tablets based on the Japanese Pharmacopoeia dissolution test method.
溶出液 第１液 ９００ｏ＋１ 錠剤１錠試験法 パ
ドル法（１００ｒρｍ）
温度 ３７℃
溶出量はサリチルアミドの３００ｎｍの極大吸収により
測定した。結果を第１図に示した。Eluate 1st solution 900o+1 Single tablet test method Paddle method (100rpm) Temperature 37°C The elution amount was measured by maximum absorption of salicylamide at 300nm. The results are shown in Figure 1.
実施例 ２゜ （徐放性核剤の調製） 前例と同一のものを使用した。Example 2゜ (Preparation of sustained release nuclear agent) I used the same one as in the previous example.
（コーティング液組成）
ヒドロキシプロピルセルロースＩＩＰｃ−ＬＰＧ（信越
化学工業■製、商品名：２０℃における２％水溶液の粘
度が７．４ｃρＳ） ・・・・・・５％精製水
・・・・・・９５％前例と
同様にして徐放性核剤に対して２０％コーティングした
。(Coating liquid composition) Hydroxypropyl cellulose IIPc-LPG (manufactured by Shin-Etsu Chemical Co., Ltd., trade name: viscosity of 2% aqueous solution at 20°C is 7.4cρS) ......5% purified water ... A 20% coating was applied to the sustained release core agent in the same manner as in the previous example.
（結 果）
前例と同一条件で溶出試験を行った。その結果を第１図
に示した。(Results) A dissolution test was conducted under the same conditions as in the previous example. The results are shown in Figure 1.
比較例 １゜
（コーティングしていない）実施例１で得られた徐放性
核剤について、前例と同様に溶出試験を行い、その結果
を第１図に示した。Comparative Example 1° (Uncoated) The sustained release nucleating agent obtained in Example 1 was subjected to a dissolution test in the same manner as in the previous example, and the results are shown in FIG.
比較例 ２゜
実施例１において、コーティング量を徐放性核剤に対し
て２％とした他は同様にして徐放性錠剤を調製し、同様
の試験を行い、その結果を第１図に示した。Comparative Example 2゜Sustained-release tablets were prepared in the same manner as in Example 1, except that the coating amount was changed to 2% of the sustained-release core agent, and the same test was conducted. The results are shown in Figure 1. Indicated.
徐放性核剤（比較例１）および２％コーティング剤（比
較例２）では溶出試験開始と同時に部分的な錠剤の崩壊
が認められ、初期の溶出速度が大きくなったのに対して
、各実施例ではいずれも初期の崩壊は認められなかった
。本発明のコーティング錠剤では溶出特性が０次に一層
近くなり改善された。With the sustained-release core agent (Comparative Example 1) and the 2% coating agent (Comparative Example 2), partial tablet disintegration was observed at the same time as the start of the dissolution test, and the initial dissolution rate was high. No initial collapse was observed in any of the Examples. The coated tablet of the present invention has an improved dissolution characteristic that is closer to zero order.
（発明の効果）
本発明の徐放性錠剤によれば、
■水溶性の高い薬物の場合には、安定したゲル層を形成
するまでの時間が短く、より０次に近い放出特性を備え
る。(Effects of the Invention) According to the sustained-release tablet of the present invention, (1) In the case of highly water-soluble drugs, the time required to form a stable gel layer is short, and the drug has release characteristics closer to zero-order.
■水溶性の小さい薬物の場合には、核となる徐放性薬剤
がゆっくりと水に濡れるため、錠剤の部分的崩壊が抑制
され、バラツキの小さい製剤となる、
という効果を奏する。■In the case of drugs with low water solubility, the core sustained-release drug is slowly wetted by water, which suppresses partial disintegration of the tablet and results in a formulation with less variation.
第１図は本発明の実施例１〜２および比較例１〜２にお
いて得られた被覆薬剤についての溶出量の測定結果を示
すもので１図において縦軸は溶出率、横軸は経過時「ｆ
■である。FIG. 1 shows the measurement results of the elution amount of coated drugs obtained in Examples 1 to 2 of the present invention and Comparative Examples 1 to 2. In FIG. 1, the vertical axis is the elution rate, and the horizontal axis is the elapsed time. f
■It is.
Claims (1)
とする徐放性核剤に、水溶性高分子をコーティングして
なる徐放性錠剤。 ２、ヒドロゲル形成能のある水溶性高分子が、ヒドロキ
シプロピルメチルセルロース、ヒドロキシプロピルセル
ロース、およびメチルセルロースから選ばれる１種また
は２種以上の組合せである請求項１記載の徐放性錠剤。 ３、水溶性高分子が、ヒドロキシプロピルメチルセルロ
ース、ヒドロキシプロピルセルロース、メチルセルロー
ス、ポリエチレングリコール、ポリビニルピロリドン、
およびポリビニルアルコールから選ばれる１種または２
種以上の組合せである請求項１記載の徐放性錠剤。 ４、徐放性核剤に対する水溶性高分子のコーティング量
が、徐放性核剤の５重量％以上である請求項１記載の徐
放性錠剤。[Scope of Claims] 1. A sustained-release tablet formed by coating a sustained-release core agent containing a drug and a water-soluble polymer capable of forming a hydrogel with a water-soluble polymer. 2. The sustained release tablet according to claim 1, wherein the water-soluble polymer capable of forming a hydrogel is one or a combination of two or more selected from hydroxypropylmethylcellulose, hydroxypropylcellulose, and methylcellulose. 3. The water-soluble polymer is hydroxypropyl methylcellulose, hydroxypropylcellulose, methylcellulose, polyethylene glycol, polyvinylpyrrolidone,
and one or two selected from polyvinyl alcohol
The sustained release tablet according to claim 1, which is a combination of more than one kind. 4. The sustained-release tablet according to claim 1, wherein the amount of water-soluble polymer coating the sustained-release core agent is 5% by weight or more of the sustained-release core agent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23535988A JPH0283316A (en) | 1988-09-20 | 1988-09-20 | Sustained release tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP23535988A JPH0283316A (en) | 1988-09-20 | 1988-09-20 | Sustained release tablet |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH0283316A true JPH0283316A (en) | 1990-03-23 |
Family
ID=16984919
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP23535988A Pending JPH0283316A (en) | 1988-09-20 | 1988-09-20 | Sustained release tablet |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0283316A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001010951A (en) * | 1992-09-18 | 2001-01-16 | Yamanouchi Pharmaceut Co Ltd | Sustained release preparation of hydrogel |
| US6699503B1 (en) | 1992-09-18 | 2004-03-02 | Yamanuchi Pharmaceutical Co., Ltd. | Hydrogel-forming sustained-release preparation |
| US8303987B2 (en) | 2001-04-11 | 2012-11-06 | Novartis Ag | Pharmaceutical compositions comprising fluvastatin |
| CN106074426A (en) * | 2016-06-23 | 2016-11-09 | 南京华宽信息咨询中心 | A kind of Theo-Dur treating bronchial asthma and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63215620A (en) * | 1987-03-03 | 1988-09-08 | Nippon Soda Co Ltd | Sustained release preparation |
-
1988
- 1988-09-20 JP JP23535988A patent/JPH0283316A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS63215620A (en) * | 1987-03-03 | 1988-09-08 | Nippon Soda Co Ltd | Sustained release preparation |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001010951A (en) * | 1992-09-18 | 2001-01-16 | Yamanouchi Pharmaceut Co Ltd | Sustained release preparation of hydrogel |
| US6699503B1 (en) | 1992-09-18 | 2004-03-02 | Yamanuchi Pharmaceutical Co., Ltd. | Hydrogel-forming sustained-release preparation |
| US8303987B2 (en) | 2001-04-11 | 2012-11-06 | Novartis Ag | Pharmaceutical compositions comprising fluvastatin |
| CN106074426A (en) * | 2016-06-23 | 2016-11-09 | 南京华宽信息咨询中心 | A kind of Theo-Dur treating bronchial asthma and preparation method thereof |
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