JPH01258619A - Novel sodium picosulfate pharmaceutical having rapid intraintestinal diffusion - Google Patents
Novel sodium picosulfate pharmaceutical having rapid intraintestinal diffusionInfo
- Publication number
- JPH01258619A JPH01258619A JP8484888A JP8484888A JPH01258619A JP H01258619 A JPH01258619 A JP H01258619A JP 8484888 A JP8484888 A JP 8484888A JP 8484888 A JP8484888 A JP 8484888A JP H01258619 A JPH01258619 A JP H01258619A
- Authority
- JP
- Japan
- Prior art keywords
- sodium picosulfate
- polyethylene glycol
- pharmaceutical
- picosulfate
- polyhydric alcohol
- 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
- GOZDTZWAMGHLDY-UHFFFAOYSA-L sodium picosulfate Chemical compound [Na+].[Na+].C1=CC(OS(=O)(=O)[O-])=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS([O-])(=O)=O)C=C1 GOZDTZWAMGHLDY-UHFFFAOYSA-L 0.000 title claims abstract description 26
- 229960005077 sodium picosulfate Drugs 0.000 title claims abstract description 24
- 238000009792 diffusion process Methods 0.000 title abstract description 4
- 239000002202 Polyethylene glycol Substances 0.000 claims abstract description 7
- 229920001223 polyethylene glycol Polymers 0.000 claims abstract description 7
- 239000004094 surface-active agent Substances 0.000 claims abstract description 7
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 5
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 4
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims abstract description 3
- 229920000642 polymer Polymers 0.000 claims abstract description 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract 2
- 229930195729 fatty acid Natural products 0.000 claims abstract 2
- 239000000194 fatty acid Substances 0.000 claims abstract 2
- 150000004665 fatty acids Chemical class 0.000 claims abstract 2
- 239000007902 hard capsule Substances 0.000 claims description 21
- 238000002360 preparation method Methods 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 12
- 238000009472 formulation Methods 0.000 claims description 11
- 239000007901 soft capsule Substances 0.000 claims description 9
- 239000000829 suppository Substances 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 3
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims 1
- 239000006196 drop Substances 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 229910052938 sodium sulfate Inorganic materials 0.000 claims 1
- 235000011152 sodium sulphate Nutrition 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 abstract description 9
- 239000008141 laxative Substances 0.000 abstract description 6
- 229920003171 Poly (ethylene oxide) Polymers 0.000 abstract description 3
- 230000002475 laxative effect Effects 0.000 abstract description 3
- 238000002156 mixing Methods 0.000 abstract description 3
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 abstract description 2
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical class [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 abstract description 2
- 210000000936 intestine Anatomy 0.000 abstract description 2
- 229940035044 sorbitan monolaurate Drugs 0.000 abstract description 2
- 230000000857 drug effect Effects 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 230000001737 promoting effect Effects 0.000 abstract 1
- 239000007788 liquid Substances 0.000 description 11
- 238000000034 method Methods 0.000 description 11
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 9
- 229960003511 macrogol Drugs 0.000 description 9
- 239000000243 solution Substances 0.000 description 6
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 238000004090 dissolution Methods 0.000 description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 238000007922 dissolution test Methods 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 229940125722 laxative agent Drugs 0.000 description 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 108010010803 Gelatin Proteins 0.000 description 2
- -1 Polyoxyethylene Polymers 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- UJIDKYTZIQTXPM-UHFFFAOYSA-N [4-[pyridin-2-yl-(4-sulfooxyphenyl)methyl]phenyl] hydrogen sulfate Chemical compound C1=CC(OS(=O)(=O)O)=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS(O)(=O)=O)C=C1 UJIDKYTZIQTXPM-UHFFFAOYSA-N 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 229920000159 gelatin Polymers 0.000 description 2
- 239000008273 gelatin Substances 0.000 description 2
- 235000019322 gelatine Nutrition 0.000 description 2
- 235000011852 gelatine desserts Nutrition 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 239000012669 liquid formulation Substances 0.000 description 2
- GSGDTSDELPUTKU-UHFFFAOYSA-N nonoxybenzene Chemical compound CCCCCCCCCOC1=CC=CC=C1 GSGDTSDELPUTKU-UHFFFAOYSA-N 0.000 description 2
- LYRFLYHAGKPMFH-UHFFFAOYSA-N octadecanamide Chemical compound CCCCCCCCCCCCCCCCCC(N)=O LYRFLYHAGKPMFH-UHFFFAOYSA-N 0.000 description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 2
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 2
- 230000000704 physical effect Effects 0.000 description 2
- 238000006116 polymerization reaction Methods 0.000 description 2
- 229960002920 sorbitol Drugs 0.000 description 2
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 description 1
- FDCJDKXCCYFOCV-UHFFFAOYSA-N 1-hexadecoxyhexadecane Chemical compound CCCCCCCCCCCCCCCCOCCCCCCCCCCCCCCCC FDCJDKXCCYFOCV-UHFFFAOYSA-N 0.000 description 1
- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- SMVRDGHCVNAOIN-UHFFFAOYSA-L disodium;1-dodecoxydodecane;sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O.CCCCCCCCCCCCOCCCCCCCCCCCC SMVRDGHCVNAOIN-UHFFFAOYSA-L 0.000 description 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000321 herbal drug Substances 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 229940105132 myristate Drugs 0.000 description 1
- TZBAVQKIEKDGFH-UHFFFAOYSA-N n-[2-(diethylamino)ethyl]-1-benzothiophene-2-carboxamide;hydrochloride Chemical compound [Cl-].C1=CC=C2SC(C(=O)NCC[NH+](CC)CC)=CC2=C1 TZBAVQKIEKDGFH-UHFFFAOYSA-N 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 229950004959 sorbitan oleate Drugs 0.000 description 1
- 229950003429 sorbitan palmitate Drugs 0.000 description 1
- 229950011392 sorbitan stearate Drugs 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
［産業上の利用分野］
本発明は公知の緩下剤ピコスルファートナトリウムを主
薬とする従来の製剤の薬効を更に高める［１的をもって
新たな基剤を採用したことに関するものである。[Detailed Description of the Invention] [Industrial Field of Application] The present invention further enhances the efficacy of conventional preparations based on the known laxative sodium picosulfate [1] This invention relates to the adoption of a new base. It is.
［従来の技術］
本発明の主薬であるピコスルファートナトリウム（Ｓｏ
ｄｉｕｍ Ｐｉｃｏｓｕｌｆａｔｅ）とは４．４′−
ジスルホキシジフェニル−（２−ピリジル）−メタン
ジナトリウム塩なる化学組成を有し、日本薬局方外医薬
晶晟分規格に収載された緩下剤として広く用いられてい
る薬品であるが、その投与剤形は液剤または軟カプセル
剤であることが殆どであって、その基剤（賦形剤）には
糖質水７ｆｊ液、例えばＤ−ソルビット液等、を用いる
のが普通であった。[Prior art] Sodium picosulfate (Sodium chloride), the main drug of the present invention
dium Picosulfate) is 4.4'-
Disulfoxydiphenyl-(2-pyridyl)-methane
It has a chemical composition of disodium salt, and is widely used as a laxative listed in the Japanese Pharmacopoeia Non-Pharmaceutical Standards, but its dosage form is mostly liquid or soft capsules. As the base (excipient), carbohydrate water 7fj liquid, such as D-sorbitol liquid, etc., has generally been used.
［発明が解決しようとする開題点］
しかし、一般に緩下剤とは服用後に速やかに消化器管を
経由して腸管へ拡散されるのが望ましいことは当然であ
って、この観点からすれば従来市販のピコスルファート
ナトリウム製剤の腸内拡散速度は充分とは言えないもの
であった。[Problem to be Solved by the Invention] However, in general, it is desirable for laxatives to diffuse into the intestinal tract via the gastrointestinal tract immediately after taking them, and from this point of view, conventional commercially available laxatives The intestinal diffusion rate of the sodium picosulfate preparation was not sufficient.
そこで、これらの間趙に鑑み、主薬であるピコスルファ
ートナトリウムを速やかに拡散させることが可能な製剤
の開発を試み、本発明をもって一応解決に到達した次第
である。Therefore, in view of these problems, we attempted to develop a formulation that can quickly diffuse the main drug, sodium picosulfate, and have finally reached a solution with the present invention.
［問題点を解決するための手段］
本発明で用いる酸化エチレンと水との付加重合体とは具
体的には通常ポリエチレングリコール、日本薬局方名で
はマクロゴール、と呼ばれる化合物であって、両成分の
重合度によって段階的に物性を異にし、その各重合度の
ものの大体の分子量に従って２００，４００．−−−−
−６０００゜２００００等の数字を付けて商品を区別し
ており、本発明ではこれら全ての数字を付したマクロゴ
ールが適宜用いられる。[Means for Solving the Problems] The addition polymer of ethylene oxide and water used in the present invention is specifically a compound commonly called polyethylene glycol, or macrogol in the Japanese Pharmacopoeia name, and both components are The physical properties vary stepwise depending on the degree of polymerization, and the approximate molecular weight of each degree of polymerization is 200, 400. ------
Products are distinguished by numbers such as -6000°20000, and in the present invention, macrogoals with all these numbers are used as appropriate.
それで、マクロゴールの物性がこの様に多様であるので
本発明における基剤としてのマクロゴールと主薬ピコス
ルファートナトリウムとの適正な配合比を数字的に規定
するのは簡単ではないが、後記する本発明の処方及び実
験データの成績から推して一応主薬ピコスルファートナ
トリウム１重呈部に対してマクロゴール１０ないし６０
重厘部の範囲の配合で目的が達成出来ると認められる。Since the physical properties of macrogol are thus diverse, it is not easy to numerically define the appropriate blending ratio of macrogol as a base and the main drug sodium picosulfate in the present invention, but this will be described later. Based on the formulation of the present invention and the results of experimental data, it is assumed that macrogol is 10 to 60% per part of the active ingredient sodium picosulfate.
It is recognized that the objective can be achieved with a combination within a heavy range.
また、これら必須二成分に更に配合することが出来る多
価アルコール型界面活性剤としてはソルビタンのモノラ
ウレート、パルミテート、ステアレートやオレエート、
グリセリンのカブリレート、ミリステートやステアレー
トあるいはデカグリセリルモノステアレート、ジブカン
酸プロピレングリコール及びショ糖オレイン酸エステル
等の中から適宜選ばれ、ポリエチレングリコール型界面
活性剤としてはポリオキシエチレン（２）ラウリルエー
テル、同（５）フィトステロール、同（１）−ポリオキ
シプロピレン（４）セチルエーテル、同（２）ノニルフ
ェニルエーテル、同（６）ソルビットミツロウ、同（４
）ステアリン酸アミド、■（２）ラウリルエーテル硫酸
ナトリウム等の中のいずれかが選ばれる。In addition, polyhydric alcohol type surfactants that can be further added to these two essential components include sorbitan monolaurate, palmitate, stearate, and oleate.
The polyethylene glycol type surfactant is appropriately selected from glycerin cabrylate, myristate, stearate, decaglyceryl monostearate, propylene glycol dibucanate, sucrose oleate, etc. Polyoxyethylene (2) lauryl is a polyethylene glycol type surfactant. Ether, (5) phytosterol, (1) -polyoxypropylene (4) cetyl ether, (2) nonylphenyl ether, (6) sorbit beeswax, (4)
) stearic acid amide, (2) sodium lauryl ether sulfate, and the like.
これらのピコスルファートナトリウム配合物は当該技術
界の常法に従ってそれぞれ所期する剤形、例えば硬また
は軟カプセル剤、液剤、液剤または坐剤に製剤化すれば
よい。These sodium picosulfate formulations may be formulated into the respective desired dosage forms, such as hard or soft capsules, solutions, solutions or suppositories, according to conventional methods in the art.
［作用］
本発明製剤の溶出速度を市販のピコスルファートナトリ
ウム製剤のそれと比較するための実験を下記に行った：
Ａ、市販ピコスルファートナトリウム軟カプセル製剤
直径４間の球状軟カプセルでゼラチン皮膜中にピコスル
ファートナトリウム１．５ｍｇと７０％の濃Ｉｙ、Ｄ−
ソルビトール液とを包含している。[Effect] An experiment was conducted to compare the dissolution rate of the preparation of the present invention with that of a commercially available sodium picosulfate preparation: A. Commercially available sodium picosulfate soft capsule preparation A spherical soft capsule with a diameter of 4 mm and a gelatin coating. 1.5 mg of sodium picosulfate and 70% concentrated Iy, D-
sorbitol solution.
Ｂ、市販ピコスルファートナトリウム液剤ピコスルファ
ートナトリウムを１ ｍｇ ／ ｍｌの割合でＤ−ソル
ビット液中溶解している。B. Commercial sodium picosulfate solution Sodium picosulfate is dissolved in D-sorbitol solution at a ratio of 1 mg/ml.
なお、現在市販品に硬カプセル剤としての坐剤は見当た
らない。Note that there are currently no suppositories available as hard capsules on the market.
以下は本溶出試験に使用した本発明の処方例である：
処方例１ （Ｃ−１）；硬カプセル剤
（イ）皮膜部処方
ゼラチン ｉｏｏ重量部濃グリセリン
３０ ノＩ合計
１３０重量部
（ロ）内容液処方
マクロゴール６００ ４８．５重員部マクロゴール
２００ ５０．Ｏｕ
ピコスルフアート
一ナトリウム １．５ ｌ１
合ｆｌ゛１００重１部
処方例２ （Ｃ−２）；硬カプセル剤
（イ）皮膜部処方；Ｃ−１の（イ）と同じ（ロ）内容液
処方
マクロゴール１５００ １６．２重量部マクロゴール
２００ ４０．ＯＩＩデカグリセリル
一モノステアレート ２３．８／／
（佑トに曳匂へｔ七り
ポリオキシエチレン（２）
一ラウリルエーテル １８．５重量部ピコスルファー
１〜
処方例３ （ＤＣ−１及びＤＣ−２）；液（滴）躬それ
ぞれ前記のＣ−１及びＣ−２処方例の（ロ）の内容液処
方のみの液剤
処方例４（Ｅ−１）；硬カプセル剤
（イ）皮膜部処方二日本薬局方の硬カプセルを使用
（ロ）内容液処方：Ｃ−１（ロ）と同じ処方例５ （Ｅ
−２）；硬カプセル剤
（イ）皮膜部処方二日本薬局方の硬カプセルを使用
（ロ）内容液処方：Ｃ−２の（ロ）と同じ処方例６（Ｆ
）；生薬
マクロゴール６０００ ２０．５重量部マクロゴール
４０００ ７８．５ ツノピコスルファ−１・
［発明の効果コ
上記した処方例１〜６の製剤を、その硬カプセル剤の場
合には４カプセル、液剤の場合には４滴が有効成分ピコ
スルファートナトリウムの６■を含有するように予め調
製しておき、その−同量６■をもって日本薬局方記載の
溶出試験の第２法（パドル法）を行った結果は本明細８
に添付の図面に表１〜４として示される通りであるが、
■ｐＨ１，２で行った試験の場合に本発明の前記Ｃ−１
及びＣ−２の硬カプセル剤は共に３分以内に有効成分の
１００％溶出を見たのに対し、対照品の市販ピコスルフ
ァートナトリウム軟カプセル剤（前記Ａ品）では約２０
分を要し、■ｐＨ１，２でシンカー無しのパドル法試験
を行った場合には、本発明の前記ＤＣ−１及びＤＣ−２
の液剤（液剤）は共に有効成分が完全に溶出するのが５
分以下であったのに対し、対照品の市販ピコスルフアー
トナトリウム液製剤（前記８品）では完全溶出に約８分
を要し、そして■ｐ８１．２のパドル法試験において硬
カプセル剤の皮膜部に日本薬局方のそれを用いた本発明
の硬カプセル剤（Ｅ−１及びＥ−２品）では約５分後に
有効成分は１００％溶出し、さらに■ｐＨ６，８で行っ
たパドル試験では本発明の坐剤（前記Ｆ品）は約５分後
に有効成分の完全溶出を見た。The following is a formulation example of the present invention used in this dissolution test: Formulation Example 1 (C-1); Hard capsule (a) Film part formulation Gelatin ioo parts by weight Concentrated glycerin 30 noI total
130 parts by weight (b) Contents liquid prescription Macrogol 600 48.5 parts by weight Macrogol 200 50. Ou Monosodium picosulfate 1.5 l1 100 weight 1 part Prescription example 2 (C-2); Hard capsule (a) Coating part prescription; Same as C-1 (a) (b) Contents liquid Prescription Macrogol 1500 16.2 parts by weight Macrogol 200 40. OII Decaglyceryl monostearate 23.8// (Polyoxyethylene (2)) Monolauryl ether 18.5 parts by weight Picosulfur 1 - Formulation example 3 (DC-1 and DC-2 ); Liquid formulation example 4 (E-1) with only the content liquid formulation of the above C-1 and C-2 formulation examples (B); Hard capsule (A) Film formulation 2 Japan Using pharmacopoeia hard capsules (b) Liquid content prescription: Same prescription example 5 as C-1 (b) (E
-2); Hard capsules (a) Film prescription 2 Use hard capsules from the Japanese Pharmacopoeia (b) Contents liquid prescription: Same prescription example 6 (F) as in C-2 (b)
); Herbal drug Macrogol 6000 20.5 parts by weight Macrogol 4000 78.5 Tsunopicosulfa-1 [Effects of the invention] The formulations of the above-mentioned Prescription Examples 1 to 6 are prepared in the form of 4 capsules in the case of hard capsules and 4 capsules in the case of liquid preparation. In this case, prepare in advance so that 4 drops contain 6 parts of the active ingredient sodium picosulfate, and use the same amount of 6 parts to perform the second dissolution test method (paddle method) described in the Japanese Pharmacopoeia. The results are shown in this specification 8.
As shown in Tables 1 to 4 in the accompanying drawings,
■ In the case of the test conducted at pH 1, 2, the above C-1 of the present invention
Both Hard Capsules and C-2 showed 100% dissolution of the active ingredient within 3 minutes, whereas the control commercially available sodium picosulfate soft capsules (Product A above) released approximately 20% of the active ingredient within 3 minutes.
(1) When the paddle method test without a sinker was conducted at pH 1 and 2, the DC-1 and DC-2 of the present invention
For both liquid preparations, the active ingredient is completely eluted at 5.
In contrast, it took about 8 minutes for complete dissolution with the control commercially available sodium picosulfate liquid preparations (8 products above), and in the paddle method test on page 81.2, the coating of the hard capsule In the hard capsules of the present invention (Products E-1 and E-2) using the Japanese Pharmacopoeia for the part, 100% of the active ingredient was eluted after about 5 minutes, and furthermore, in the paddle test conducted at pH 6 and 8, In the suppository of the present invention (product F), the active ingredient was completely dissolved after about 5 minutes.
かくして、本発明の硬カプセル剤、液剤や坐剤は従来市
販のピコスルファートナトリウム製剤に比べて腸内にお
ける有効成分の拡散が明らかに促進されていることが実
証され、緩下剤として望ましい効果を発揮するものであ
ることが判明した。Thus, it has been demonstrated that the hard capsules, liquids, and suppositories of the present invention clearly promote the diffusion of the active ingredient in the intestine compared to conventionally commercially available sodium picosulfate preparations, and exhibit desirable effects as laxatives. It turned out that it does.
第１図は市販ピコスルファートナトリウム製剤Ａと本発
明Ｃ−１及びＣ−２硬カプセル剤、第２図は市販ピコス
ルファートナトリウム製剤Ｂと本発明のＤＣ−１及びＤ
Ｃ−２硬カプセル剤、第３図は本発明のＥ−１及びＥ−
２滴剤、そして第４図は本発明のＦ坐剤の、それぞれ日
本薬局方記載の溶出試験第２法（パドル法）による溶出
速度を示す線図である。
ただし、第３図のパドル法はシンカー無しで行った。ま
た、第１図、第２図、第３図および第４図のパドル法は
、それぞれｐＨ１，２、ｐＨ１゜２、ｐＨ１，２および
ｐＨ６，８の条件下で行った。
（特許出願人 東洋カプセル株式会社）（代理人 弁理
士 糟谷 安）
図面の、）、η（内容に変更なし）
名 第１図
老 第３図
モ
溶 第４図
七
手続ネ市正四（方式）
％式％
２、発明の名称
３、補正をする者
事件との関係 特許出願人
名 称 東洋カプセル株式会社
４、代理人
住 所 大阪市中央区淡路町２丁目１番１３号弘栄ビ
ル 電話（０６） ２２２．−０５４７氏名 （６０
３６）弁理士赤岡辿夫
５、 補正命令の日付
平成１年３月７日発送
６、補正の対象
図面
７、補正の内容
手続補正書
特許庁長官 殿 平成 １年 ４月グ日２、発
明の名称
３、補正をする者
事件との関係 特許出願人
名 称 東洋カプセル株式会社
４、代理人
住 所 大阪市中央区淡路町２丁目１番１３号弘栄ビ
ル 電話（０６） ２２２−０５４７氏名 （６０３
６）弁理士赤岡辿夫
５、補正命令の日付
自 発
６、補正の対象
発明の詳細な説明、図面の簡単な説明
７、補正の内容
別紙のとおり
補 正 の 内 容
１．、明細書第６頁第３行および第１４行、第８真下か
ら４行、第１０頁第１行の［硬カプセル剤Ｊをそれぞれ
「軟カプセル剤」に訂正する。
２、 同第８頁第８行の「その」を「軟カプセル剤及
び」に訂正する。
３７ 同第９頁第７行の「硬カプセル剤の皮膜部に
」を「硬カプセルとして」に訂正する。
４、 同第９頁第１３行のｒ本発明の」の次に「軟カ
プセル剤、」を挿入する。
５、 同第１０頁第３行の「硬カプセル剤」を「消削
」に訂正し、第４行の「消削」を「硬カプセル剤」に訂
正する。Figure 1 shows commercially available sodium picosulfate preparation A and hard capsules of the present invention C-1 and C-2, and Figure 2 shows commercially available sodium picosulfate preparation B and DC-1 and D of the present invention.
C-2 hard capsules, Figure 3 shows E-1 and E- of the present invention.
FIG. 4 is a diagram showing the dissolution rate of the 2-drop preparation and the F suppository of the present invention, respectively, according to the second dissolution test method (paddle method) described in the Japanese Pharmacopoeia. However, the paddle method shown in Figure 3 was performed without a sinker. Further, the paddle method shown in FIGS. 1, 2, 3, and 4 was performed under conditions of pH 1.2, pH 1.2, pH 1.2, and pH 6.8, respectively. (Patent applicant: Toyo Capsule Co., Ltd.) (Agent: Patent attorney: Yasushi Kasuya) Drawings, ), η (no change in content) Name: Figure 1: Figure 3: Molyo: Figure 4: Seven procedures (Method) % formula % 2. Name of the invention 3. Relationship with the person making the amendment Patent applicant name Toyo Capsule Co., Ltd. 4 Agent address Koei Building, 2-1-13 Awajicho, Chuo-ku, Osaka Telephone (06) 222. -0547 Name (60
36) Patent attorney Takuo Akaoka 5, Date of amendment order sent on March 7, 1999 6, Drawing subject to amendment 7, Contents of amendment, Procedures for amendment, Commissioner of the Patent Office, April 1, 1999 date 2, Invention Name 3. Relationship with the person making the amendment Patent applicant name Name Toyo Capsule Co., Ltd. 4 Agent address Koei Building, 2-1-13 Awajicho, Chuo-ku, Osaka Phone: (06) 222-0547 Name (603)
6) Patent attorney Takuo Akaoka5, date of the amendment order6, detailed explanation of the invention subject to the amendment, brief explanation of the drawings7, content of the amendment as shown in the appendix 1. , page 6, lines 3 and 14, line 8, line 4 from the bottom, page 10, line 1 [Hard capsule J is corrected to "soft capsule", respectively. 2. On page 8, line 8, "the" is corrected to "soft capsules and". 37 On page 9, line 7 of the same document, "in the coating of the hard capsule" is corrected to "as a hard capsule." 4. On page 9, line 13, insert "soft capsules," after "r of the present invention." 5. On page 10, line 3, "hard capsules" is corrected to "erasure", and line 4, "erasure" is corrected to "hard capsules".
Claims (3)
酸化エチレンと水との付加重合体の１０乃至６０重量部
を基剤として配合したことを特徴とするピコスルファー
トナトリウム製剤。(1) A sodium picosulfate preparation, characterized in that 10 to 60 parts by weight of an addition polymer of ethylene oxide and water is blended as a base to 1 part by weight of sodium picosulfate, the main drug.
結合させた多価アルコール型界面活性剤またはポリエチ
レングリコール型界面活性剤を配合して成ることを特徴
とする特許請求の範囲第１項記載のピコスルファートナ
トリウム製剤。(2) Claim 1, characterized in that the base is further blended with a polyhydric alcohol type surfactant or a polyethylene glycol type surfactant in which a polyhydric alcohol and a fatty acid are ester bonded. sodium picosulfate formulation.
なる群より選ばれたいずれかであることを特徴とする特
許請求の範囲第１項および特許請求の範囲第２項記載の
ピコスルファートナトリウム製剤。(3) Pico according to claim 1 and claim 2, wherein the dosage form is any one selected from the group consisting of hard capsules, soft capsules, drops, and suppositories. Sodium sulfate preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63084848A JP2764581B2 (en) | 1988-04-05 | 1988-04-05 | A novel sodium picosulfate formulation with fast intestinal diffusion |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63084848A JP2764581B2 (en) | 1988-04-05 | 1988-04-05 | A novel sodium picosulfate formulation with fast intestinal diffusion |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH01258619A true JPH01258619A (en) | 1989-10-16 |
| JP2764581B2 JP2764581B2 (en) | 1998-06-11 |
Family
ID=13842222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63084848A Expired - Fee Related JP2764581B2 (en) | 1988-04-05 | 1988-04-05 | A novel sodium picosulfate formulation with fast intestinal diffusion |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2764581B2 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01283222A (en) * | 1988-05-10 | 1989-11-14 | Tokai Kapuseru Kk | Soft capsule agent of sodium picosulfate |
| WO1995011024A1 (en) * | 1993-10-19 | 1995-04-27 | The Procter & Gamble Company | Picosulphate dosage form |
| EP0682946A2 (en) * | 1994-05-19 | 1995-11-22 | Euro-Celtique S.A. | Laxative compositions |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57131727A (en) * | 1981-02-09 | 1982-08-14 | Sumitomo Chem Co Ltd | Suppository base |
| JPS62249922A (en) * | 1986-04-23 | 1987-10-30 | Toyo Kapuseru Kk | Method for freely controlling dissolution time of active component from gelatin-encapsulated preparation |
| JPS62255424A (en) * | 1986-04-05 | 1987-11-07 | ドロールギエツト ゲーエムベーハー ウント コ． カーゲー | Preparation of hymecromone and manufacture |
-
1988
- 1988-04-05 JP JP63084848A patent/JP2764581B2/en not_active Expired - Fee Related
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS57131727A (en) * | 1981-02-09 | 1982-08-14 | Sumitomo Chem Co Ltd | Suppository base |
| JPS62255424A (en) * | 1986-04-05 | 1987-11-07 | ドロールギエツト ゲーエムベーハー ウント コ． カーゲー | Preparation of hymecromone and manufacture |
| JPS62249922A (en) * | 1986-04-23 | 1987-10-30 | Toyo Kapuseru Kk | Method for freely controlling dissolution time of active component from gelatin-encapsulated preparation |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH01283222A (en) * | 1988-05-10 | 1989-11-14 | Tokai Kapuseru Kk | Soft capsule agent of sodium picosulfate |
| WO1995011024A1 (en) * | 1993-10-19 | 1995-04-27 | The Procter & Gamble Company | Picosulphate dosage form |
| US5631022A (en) * | 1993-10-19 | 1997-05-20 | The Procter & Gamble Company | Picosulfate dosage form |
| EP0682946A2 (en) * | 1994-05-19 | 1995-11-22 | Euro-Celtique S.A. | Laxative compositions |
| EP0682946A3 (en) * | 1994-05-19 | 1996-05-29 | Euro Celtique Sa | Laxative compositions. |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2764581B2 (en) | 1998-06-11 |
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