JPS5838211A - release rate control material - Google Patents
release rate control materialInfo
- Publication number
- JPS5838211A JPS5838211A JP13728081A JP13728081A JPS5838211A JP S5838211 A JPS5838211 A JP S5838211A JP 13728081 A JP13728081 A JP 13728081A JP 13728081 A JP13728081 A JP 13728081A JP S5838211 A JPS5838211 A JP S5838211A
- Authority
- JP
- Japan
- Prior art keywords
- ethylene
- release rate
- vinyl alcohol
- alcohol copolymer
- copolymer
- 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
- 239000000463 material Substances 0.000 title claims abstract description 32
- 239000000126 substance Substances 0.000 claims abstract description 20
- 229920000219 Ethylene vinyl alcohol Polymers 0.000 claims abstract description 15
- 239000003814 drug Substances 0.000 claims abstract description 11
- 238000007127 saponification reaction Methods 0.000 claims abstract description 9
- 229940079593 drug Drugs 0.000 claims abstract description 8
- 239000003905 agrochemical Substances 0.000 claims abstract description 4
- 239000003205 fragrance Substances 0.000 claims description 2
- 239000003094 microcapsule Substances 0.000 claims description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 abstract description 12
- 239000005977 Ethylene Substances 0.000 abstract description 12
- 229920001577 copolymer Polymers 0.000 abstract description 8
- 238000006116 polymerization reaction Methods 0.000 abstract description 3
- 238000000354 decomposition reaction Methods 0.000 abstract 1
- 239000012633 leachable Substances 0.000 abstract 1
- 239000002304 perfume Substances 0.000 abstract 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 description 8
- 229960002949 fluorouracil Drugs 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 5
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 238000000465 moulding Methods 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 238000013268 sustained release Methods 0.000 description 4
- 239000012730 sustained-release form Substances 0.000 description 4
- -1 acrylic ester Chemical class 0.000 description 3
- 239000007864 aqueous solution Substances 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000035699 permeability Effects 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 238000010828 elution Methods 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 239000000186 progesterone Substances 0.000 description 2
- 229960003387 progesterone Drugs 0.000 description 2
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 2
- 239000011347 resin Substances 0.000 description 2
- 229920005989 resin Polymers 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 238000007789 sealing Methods 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 description 1
- 206010011224 Cough Diseases 0.000 description 1
- SXRSQZLOMIGNAQ-UHFFFAOYSA-N Glutaraldehyde Chemical compound O=CCCCC=O SXRSQZLOMIGNAQ-UHFFFAOYSA-N 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 229940009456 adriamycin Drugs 0.000 description 1
- 229940034982 antineoplastic agent Drugs 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 238000006243 chemical reaction Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- 239000003246 corticosteroid Substances 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 230000007423 decrease Effects 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 208000002925 dental caries Diseases 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960005309 estradiol Drugs 0.000 description 1
- 229930182833 estradiol Natural products 0.000 description 1
- PROQIPRRNZUXQM-ZXXIGWHRSA-N estriol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)C4)O)[C@@H]4[C@@H]3CCC2=C1 PROQIPRRNZUXQM-ZXXIGWHRSA-N 0.000 description 1
- 229960001348 estriol Drugs 0.000 description 1
- 229940011871 estrogen Drugs 0.000 description 1
- 239000000262 estrogen Substances 0.000 description 1
- 239000004715 ethylene vinyl alcohol Substances 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 208000030533 eye disease Diseases 0.000 description 1
- 239000003337 fertilizer Substances 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000010408 film Substances 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- RZXDTJIXPSCHCI-UHFFFAOYSA-N hexa-1,5-diene-2,5-diol Chemical compound OC(=C)CCC(O)=C RZXDTJIXPSCHCI-UHFFFAOYSA-N 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 229920001477 hydrophilic polymer Polymers 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 239000012046 mixed solvent Substances 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
Abstract
Description
【発明の詳細な説明】 本発明は新規な放出速度制御材料に関するものである。[Detailed description of the invention] FIELD OF THE INVENTION This invention relates to novel release rate controlled materials.
医薬や農薬等の化学物質を必要な時に必要な量だけ必要
な場所に限って放出させることにより、該化学物質を有
効に利用する方法は、特に医薬の分野を中心に徐放性製
剤として、研究、活用されている。A method of effectively utilizing chemical substances such as medicines and agricultural chemicals by releasing them only in the necessary amount and in the necessary place when and where they are needed is mainly used in the pharmaceutical field as sustained-release preparations. Researched and utilized.
従来、この種の化学物質の放出速度を制御する素材とし
ては、種々の特殊な高分子重合体が知られており、例え
ば、ポリビニルアルコール、ポリアクリル酸、ポリ（メ
タ）アクリル酸エステル、特にヒドロキシ（又はプロピ
ル）（メタ）アクリレート、ｌリビニルピロリドン、ポ
リアクリルアミド等の親水性樹脂が特公昭４２−１７３
２４−号、特開１１１１ｓ１−１１５９１０号、同１４
２５２３号、特開昭５３−５２４１７号、特開１ｉ１３
５４−４４６３０号などにより多数知られている。しか
るにこれらの従来方法はいずれも、それらの樹脂の単独
の制御性能のみ開示しており、その放出速度を自由に制
御する方法に対する開示はない。Conventionally, various special polymers have been known as materials that control the release rate of this type of chemical substance, such as polyvinyl alcohol, polyacrylic acid, poly(meth)acrylic ester, especially hydroxyl. Hydrophilic resins such as (or propyl) (meth)acrylate, l-vinylpyrrolidone, and polyacrylamide were
No. 24-, JP-A No. 1111s1-115910, No. 14
No. 2523, JP 53-52417, JP 1i13
Many are known, such as No. 54-44630. However, all of these conventional methods disclose only the ability to control the resin alone, and do not disclose a method for freely controlling the release rate.
本発明者らはケン化度９０モル％以上のエチレンビニル
アルコール共重合体が、この棚の徐放性素材として優れ
ていることを見い出し、しかもこの共重合体においては
、エチレン含有量の僅かな相違により、放出速度が大幅
に変化し、放出速度制御材料として極めて優れているこ
とを認め、本発明に至った。The present inventors have discovered that an ethylene vinyl alcohol copolymer with a degree of saponification of 90 mol% or more is excellent as a sustained release material for this shelf. Due to the difference, the release rate changes significantly, and it has been recognized that it is extremely excellent as a release rate controlling material, leading to the present invention.
即ち本発明はケン化度９０モル％以上のエチレンビニル
アルコール共重合体成形物よりなる放出速度制御材料で
ある。That is, the present invention is a release rate controlling material made of a molded ethylene vinyl alcohol copolymer having a degree of saponification of 90 mol% or more.
一般に放出速度制御材料としては、化学物質放出速度の
速いものから遅いものまで、目的により種々のものが要
求される。この点、本発明の放出速度制御材料はエチレ
ンビニルアルコール共重合体中のエチレン含有量を変化
させることにより容易に所望の放出速度の徐放材料が得
られる。In general, various release rate controlling materials are required depending on the purpose, ranging from those with fast chemical substance release rates to those with slow chemical substance release rates. In this regard, in the release rate controlling material of the present invention, a sustained release material having a desired release rate can be easily obtained by changing the ethylene content in the ethylene vinyl alcohol copolymer.
また、化学物質の性質、例えば親水性、疎水性により、
放出速度は大きく異なるが、本発明の制御材料はエチレ
ン含有量を変化させることにより親水性と疎水性のバラ
ンスを大きく変化させることが可能であり、この点にお
いても所望の放出速度が得られるという利点がある。Also, depending on the properties of the chemical substance, such as hydrophilicity or hydrophobicity,
Although the release rate varies greatly, the balance between hydrophilicity and hydrophobicity can be greatly changed by changing the ethylene content of the controlled material of the present invention, and the desired release rate can also be obtained in this respect. There are advantages.
本発明の放出速度制御材料は、特に反応などにより不都
合を生ずる場合を除いて、広く化学物質（天然物を含む
）の放出速度制御材料として使用が可能であり、例えば
医薬、農薬の分野にとどまらず、肥料、香料などの徐放
材料として使用可能である。またその形層も顆粒状、錠
剤状、マイクロカプセル状、膜状、フィルム状、棒状、
繊維状など自由に選択できる。さらに化学物質を粉末状
、液体状、固体状、溶液状などの状態で本発明の材料に
より被覆したり、或は化学物質を材料内部に埋没して使
用することも可能で、例えば、化学物質をそのまま、或
は増量剤、粘着剤、溶媒などにより形態を整えた後に、
エチレンビニルアルコール共重合体のフィルムにより外
周をヒートシールなどにより囲んだり、公知のマイクロ
カプセル化法により内部に化学物質を包含した状態でマ
イクロカプセル化したり、或は化学物質と共重合体を、
好ましくは共通溶媒に混合溶解した後に、一体成形する
ことにより、化学物質が均一に材料中に分敢埋没した状
態での任意の形状の成形物を得ることができる。The release rate controlling material of the present invention can be widely used as a release rate controlling material for chemical substances (including natural products), except in cases where inconveniences arise due to reactions, etc., and for example, it can be used not only in the fields of medicine and agricultural chemicals. It can also be used as a sustained release material for fertilizers, fragrances, etc. In addition, its shape can be granules, tablets, microcapsules, membranes, films, rods, etc.
You can freely choose the fibrous form. Furthermore, it is also possible to coat the chemical substance in the form of powder, liquid, solid, solution, etc. with the material of the present invention, or to use the chemical substance by embedding it inside the material. as it is, or after adjusting the form with fillers, adhesives, solvents, etc.
Surrounding the outer periphery with a film of ethylene vinyl alcohol copolymer by heat sealing, etc., microencapsulating the chemical substance inside using a known microencapsulation method, or combining the chemical substance and copolymer,
Preferably, by mixing and dissolving in a common solvent and then integrally molding, it is possible to obtain a molded article of any shape in which the chemical substance is uniformly embedded in the material.
本発明のエチレンビニルアルコールを主体、！−スる放
出速度制御材料は、生体との親和性がよく、またポリビ
ニルアルコールなどの他の親水性重合体と比較して、可
溶成分が少なく安定であり、また生体内での非分解性に
優れているので、特に医薬としての成形物、即ち製剤と
して人体中への挿入、皮肩への貼付、埋め込みなどによ
り最も有効に利用される。Mainly based on ethylene vinyl alcohol of the present invention! - The release rate controlling material has good affinity with living organisms, and compared to other hydrophilic polymers such as polyvinyl alcohol, it is stable with less soluble components, and is non-degradable in living organisms. Because of its excellent properties, it is most effectively used as a pharmaceutical product, ie, as a preparation, by inserting it into the human body, pasting it on the skin, or implanting it.
本発明において用いられるエチレンビニルアルコール共
重合体としては、ケン化度が９０モル％以上のものが要
求される。ケン化度がこの範囲を越え低い場合には放出
速度の制御が十分でない。The ethylene vinyl alcohol copolymer used in the present invention is required to have a degree of saponification of 90 mol% or more. If the degree of saponification exceeds this range and is low, the release rate cannot be controlled sufficiently.
この意味におい昭、実質的に未ケン化部分の少ない共重
合体がよく、好ましくは９７モル％以上、特に９９モル
％以上のものがよい。In this sense, a copolymer having substantially less unsaponified portion is preferable, preferably 97 mol% or more, particularly 99 mol% or more.
共１合体中のエチレン含有量は前述したとおり、化学物
質の種類や所望の放出速度を考慮して選択されるべきで
あり特に限定はないが、５〜９５モル％の範囲において
、放出速度の制御が容易となる。より好ましいエチレン
含有量は１０〜８０モル％であるが、この共重合体は親
水性の材料として使用する時、即ちエチレン含有量にお
いて１０〜６０モル％の範囲においては特によい、この
範囲において、エチレン含有量のわずか１０モル％の変
化は化学物質放出速度を５倍以上、或は１０倍以上に変
化させることが可能である。As mentioned above, the ethylene content in the co-1 polymer should be selected in consideration of the type of chemical substance and the desired release rate, and is not particularly limited. Control becomes easier. The more preferred ethylene content is 10 to 80 mol%, but this copolymer is particularly good when used as a hydrophilic material, that is, when the ethylene content is in the range of 10 to 60 mol%. A change of as little as 10 mole percent in ethylene content can change the chemical release rate by more than 5 times, or even more than 10 times.
共重合体の重合度についても、特に制限はないが、成形
性、材料の安定性などから５００〜２０．Ｇｏｏ、特に
１，０００〜１０，０００がよい。There is no particular restriction on the degree of polymerization of the copolymer, but from the viewpoint of moldability, material stability, etc., it is between 500 and 20. Goo, especially 1,000 to 10,000.
本発明の徐放効果が有効に利用される化学物質としては
、前述のごとく制限はないが、例えば医薬においては、
コーチシン、ヒドロコーチシン、ラキサメサゾン、フレ
ドニゾロン等の副腎皮質ホルモン剤、５−フルオロウラ
シル、プレオマイシン、アドリアマイシンなどの抗悪性
腫瘍剤、エストラジオール、エストラトリオール、エス
トロゲンなどの卵胞ホルモン剤、プロゲステロンなどの
黄体ホルモン剤、ピロカルビンなどの眼病治療剤、フッ
素イオンなどのう歯予防剤、インシュリンなどの高分子
化合物系治療剤などがある。As mentioned above, there are no restrictions on the chemical substances for which the sustained release effect of the present invention can be effectively utilized, but for example, in pharmaceuticals,
corticosteroids such as cortiscin, hydrocortiscin, laxamethasone, and frednisolone; antineoplastic agents such as 5-fluorouracil, pleomycin, and adriamycin; follicle hormones such as estradiol, estratriol, and estrogen; progesterone agents such as progesterone; These include eye disease treatment agents such as pilocarbin, dental caries prevention agents such as fluoride ions, and polymer compound therapeutic agents such as insulin.
本発明の制御材料は単独で使用することにより十分に効
果を出すが、他の材料と混合したり或は＊ｍｔ、、て使
用することも可能である。また例えばグルタルアルデヒ
ドにより架橋構造を導入することにより、より安定性を
増加させたり放出速度を制御することができる。Although the control material of the present invention is sufficiently effective when used alone, it is also possible to mix it with other materials or use it *mt. Furthermore, by introducing a crosslinked structure using, for example, glutaraldehyde, the stability can be further increased and the release rate can be controlled.
また、従来公知の他の材料と全く同様に、成形条件を種
々選択することにより膜の緻密度などを変化させ放出速
度を制御することも可能である。Further, just like other conventionally known materials, it is also possible to control the release rate by changing the density of the film and the like by selecting various molding conditions.
また、重合度、ケン化度を変化させることにより放出速
度および化学物質との組合せによる成形条件などを任意
に選択することができる。Furthermore, by changing the degree of polymerization and saponification, the release rate and molding conditions in combination with chemical substances can be arbitrarily selected.
以下、実施例により本発明をより具体的に説明する。EXAMPLES Hereinafter, the present invention will be explained in more detail with reference to Examples.
実施例１
エチレン含有量の異なるエチレンビニルアルコール共重
合体（ケン化度？ｔ５モル％）の溶融押出法により調製
したフィルムを用い透析用垂直膜型セルにより、薬物の
水溶液中での透過性を測定した。実験はドナー側に約２
０ｍｊの薬物飽和懸濁水溶液を満たし、３７＠Ｃで振盪
下におき、２４時間毎にアクセプター側の水を入れ換え
、ｓ’ａ量を分光光度計にて定量し、累積溶出量を測定
することにより行った。結果をまとめて表１に示した。Example 1 Using films prepared by melt extrusion of ethylene vinyl alcohol copolymers with different ethylene contents (saponification degree: t5 mol%), the permeability of drugs in aqueous solutions was measured using a vertical membrane cell for dialysis. It was measured. The experiment was conducted with approximately 2
Fill with 0mJ drug saturated suspension aqueous solution, shake at 37@C, replace the water on the acceptor side every 24 hours, quantify the amount of s'a with a spectrophotometer, and measure the cumulative elution amount. This was done by The results are summarized in Table 1.
表 １
表１の結果から明らかなように、エチレンビニルアルコ
ール共重合体フィルムは放出材料として使用可能であり
、またエチレン含有量が増大すると透過係数は大きく減
少し、咳共重合体が放出制御材料として優れていること
が認められた。Table 1 It is clear from the results in Table 1 that the ethylene vinyl alcohol copolymer film can be used as a release material, and as the ethylene content increases, the permeability coefficient decreases significantly, making the cough copolymer a controlled release material. It was recognized as being excellent.
実施例２
実施例１の薬剤に変え５−フルオロウラシルを用いて、
実施例１と同様な実験を行った。結果を表２に示したが
、実施例１と同様に共重合体中のエチレン含有量が異な
ると透過係数が大きく異なり、該共重合体が５−フルオ
ロウラシルに対する優れた放出制御材料であることが認
められた。Example 2 Using 5-fluorouracil instead of the drug in Example 1,
An experiment similar to Example 1 was conducted. The results are shown in Table 2, and as in Example 1, the permeability coefficient varies greatly when the ethylene content in the copolymer differs, indicating that the copolymer is an excellent release control material for 5-fluorouracil. Admitted.
表 ２
実施例３
厚す１５．ｃａｎのエチレンビニルアルコール共重合体
フィルム（エチレン含有１７１５２モル％）により、５
−フルオロウラシルの飽和懸濁水溶液の２０ｍｊを周囲
をヒートシールで成形した製剤を作った。Table 2 Example 3 Thickness 15. Can's ethylene vinyl alcohol copolymer film (ethylene content: 17152 mol%)
- A preparation was prepared by molding the periphery of 20 mj of a saturated aqueous suspension of fluorouracil by heat sealing.
該製剤を水中に投入したところ、５−フルオロウラシル
が長期間にわたり水溶液中に溶出してくることが確認さ
れた。When this preparation was poured into water, it was confirmed that 5-fluorouracil was eluted into the aqueous solution over a long period of time.
実施例４
水：ｎ−プロパツールの４：６（体積比）混合溶媒１ｏ
Ｏｍｇに、エチレン含有量３２モル％のエチレンビニ
ルアルコール共重合体５ｇ及び５−フルオロウラシル２
００ｍｇをそれぞれ混合溶解後、ガラス板上に流延し、
乾燥後メルトブレス法により厚さ２．５ｍに製膜し、フ
ィルム内に薬物が混入されてなるフィルム状製剤を調製
した。Example 4 4:6 (volume ratio) mixed solvent of water:n-propanol 10
Omg, 5g of ethylene vinyl alcohol copolymer with an ethylene content of 32 mol% and 5-fluorouracil 2
After mixing and dissolving 00 mg of each, cast on a glass plate,
After drying, a film was formed to a thickness of 2.5 m by a melt breath method, and a drug was mixed into the film to prepare a film-like preparation.
溶出試験は５７°Ｃで５ｓｎｊの水中に上記フィルムの
α４ｇを入れ振とう下に２４時間毎に水を取り換え溶出
した５−フルオロウラシルを実施例２と同様の方法で測
定したが、長期間に渡って、定量的に５−フルオロウラ
シルが溶出されたことが確認された。これによりエチレ
ンビニルアルコール共重合体は薬剤を成形物中に埋没し
た形態にても使用できることが認められた。In the elution test, 4 g of the above film was placed in 5snj water at 57°C, and while shaking, the water was changed every 24 hours and the eluted 5-fluorouracil was measured in the same manner as in Example 2, but over a long period of time. It was confirmed that 5-fluorouracil was quantitatively eluted. As a result, it was recognized that ethylene vinyl alcohol copolymer can be used even in the form of a drug embedded in a molded article.
特許出願人 株式会社クラレ 代 理 人弁理士 本多 堅Patent applicant: Kuraray Co., Ltd. Representative Patent Attorney Ken Honda
Claims (4)
ール共重合体成形物よりなる化学物質の放出速度制御材
料。(1) A chemical substance release rate controlling material comprising a molded ethylene vinyl alcohol copolymer having a degree of saponification of 90 mol% or more.
ある特許請求の範囲第１項記載の材料。(2) The material according to claim 1, wherein the chemical substance is one selected from medicines, agricultural chemicals, and fragrances.
とする特許請求の範囲第２項記載の材料。(3) The material according to claim 2, wherein the chemical substance is embedded in the molded product.
徴とする特許請求の範囲第１項記載の材料。(4) The material according to claim 1, wherein the molded product is in the form of microcapsules.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13728081A JPS5838211A (en) | 1981-08-31 | 1981-08-31 | release rate control material |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP13728081A JPS5838211A (en) | 1981-08-31 | 1981-08-31 | release rate control material |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5838211A true JPS5838211A (en) | 1983-03-05 |
| JPS614814B2 JPS614814B2 (en) | 1986-02-13 |
Family
ID=15194982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP13728081A Granted JPS5838211A (en) | 1981-08-31 | 1981-08-31 | release rate control material |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5838211A (en) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6144238U (en) * | 1984-08-29 | 1986-03-24 | 宇部興産株式会社 | Vertical crusher |
| JPS61236723A (en) * | 1985-04-12 | 1986-10-22 | Fujimoto Seiyaku Kk | Long-acting nifedipin suppository |
| US5288501A (en) * | 1991-07-04 | 1994-02-22 | Merz + Co. Gmbh & Co. | Mechanically-stable, readily-disintegratable tablets made of small preformed particles containing active ingredients |
| WO2013069701A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
| WO2013069702A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
| WO2013069700A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
-
1981
- 1981-08-31 JP JP13728081A patent/JPS5838211A/en active Granted
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS6144238U (en) * | 1984-08-29 | 1986-03-24 | 宇部興産株式会社 | Vertical crusher |
| JPH029899Y2 (en) * | 1984-08-29 | 1990-03-12 | ||
| JPS61236723A (en) * | 1985-04-12 | 1986-10-22 | Fujimoto Seiyaku Kk | Long-acting nifedipin suppository |
| US5288501A (en) * | 1991-07-04 | 1994-02-22 | Merz + Co. Gmbh & Co. | Mechanically-stable, readily-disintegratable tablets made of small preformed particles containing active ingredients |
| WO2013069701A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
| WO2013069702A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
| WO2013069700A1 (en) * | 2011-11-07 | 2013-05-16 | 日信化学工業株式会社 | Water-dispersible vaporized active substance sustained release product |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS614814B2 (en) | 1986-02-13 |
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