JP2007167358A - Intraocular drug administration appliance - Google Patents

Intraocular drug administration appliance Download PDF

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JP2007167358A
JP2007167358A JP2005369217A JP2005369217A JP2007167358A JP 2007167358 A JP2007167358 A JP 2007167358A JP 2005369217 A JP2005369217 A JP 2005369217A JP 2005369217 A JP2005369217 A JP 2005369217A JP 2007167358 A JP2007167358 A JP 2007167358A
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drug
hydrogel material
drug administration
intraocular
administration device
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Taketoshi Suzuki
武敏 鈴木
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Abstract

<P>PROBLEM TO BE SOLVED: To provide an intraocular drug administration appliance solving problems with conventional pharmacological treatment using contact lens made of a hydrogel material, responding to many patients without any trouble caused by a long-time lens wearing such as oxygen deficit conditions of the cornea, and being advantageous in the price. <P>SOLUTION: A drug agent support appliance 1 has an annular or C-shaped plane formed of drug sustained-release hydrogel material incorporating a large quantity of drug and controllable of drug releasing speed. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

本発明は、薬物放出速度を制御し得る薬物徐放可能なヒドロゲル材料を用いた眼内用の薬剤投与具に関するものである。   The present invention relates to an intraocular drug administration device using a hydrogel material capable of sustained drug release capable of controlling the drug release rate.

従来、眼科医療において、ドライアイ、緑内障、結膜炎あるいは角膜上皮障害などの疾患に対する薬剤治療に際して、取扱いが簡単なことや効果の面から点眼薬が用いられいる。   Conventionally, in ophthalmic medicine, eye drops are used from the viewpoint of easy handling and effectiveness in drug treatment for diseases such as dry eye, glaucoma, conjunctivitis or corneal epithelial disorder.

ところが、眼内に投与された点眼薬は、眼瞼の瞬きや涙液置換などによりを長時間にわたって眼内に保持しておくことはきわめて困難であり、その殆ど(90%以上)が短時間の内に涙液によって洗い流されてしまう。   However, eye drops administered into the eye are extremely difficult to keep in the eye for a long time by blinking the eyelids or replacing tears, and most of them (90% or more) are short-term. It is washed away by tears.

そのため、点眼薬による薬効を上げるためには比較的、短周期で投与し続けることが必要であるが、患者において一定時間毎に頻繁な点眼は難しく、特に、睡眠中は流亡が減少する反面、長時間にわたって投与ができないという事態か生じる。   Therefore, in order to increase the efficacy of eye drops, it is necessary to continue administration in a relatively short cycle, but frequent instillation is difficult at a certain time in patients, especially while sleep is reduced during sleep, A situation occurs where administration cannot be performed for a long time.

また、逆に、処方を越えた点眼は涙成分の減少に繋がることになり、症状の悪化や角膜上皮障害を発生するなどの弊害があり、更に、余分な薬剤が吸収されてしまうことから眼内の局所に疾患や人体に副作用が生じる場合があり、好ましくない。   Conversely, instillation beyond the prescription will lead to a decrease in tear components, which may cause adverse effects such as worsening of symptoms and corneal epithelial disorder, and absorption of excess drugs. It is not preferable because there may be side effects on the human body or disease.

そこで、例えば、特開2005−218780号公報、特開2005−314338号公報などに、薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放可能なヒドロゲル材料により作られたコンタクトレンズ および眼内レンズが提示されている。   Therefore, for example, JP 2005-218780 A, JP 2005-314338 A, etc., contact lenses made of a hydrogel material capable of sustained drug release with a large drug uptake amount and capable of controlling the drug release rate. And an intraocular lens.

従って、前記公報に提示されているヒドロゲル材料により作られたコンタクトレンズ を用いると、薬物放出速度を制御し得る薬物徐放が可能であり、長期にわたって適量の薬物を投与可能であり、効果のある治療が期待できる。   Therefore, by using a contact lens made of the hydrogel material presented in the above publication, it is possible to control the drug release rate and to administer an appropriate amount of drug over a long period of time. Treatment can be expected.

しかしながら、前記薬剤治療はコンタクトレンズの長期装用により行われる。そのため、角膜が酸素欠乏状態などの長期装用による障害が発生する心配がある。また、コンタクトレンズの不適応の患者は使用することができないなどの問題点がある。
特開2005−218780号公報 特開2005−314338号公報
However, the drug treatment is performed by long-term wearing of contact lenses. For this reason, there is a concern that the cornea may be damaged due to long-term wearing such as an oxygen-deficient state. In addition, there is a problem that a patient who is inadequate for contact lenses cannot be used.
JP 2005-218780 A JP 2005-314338 A

本発明は前記の実情に鑑みてなされたものであり、従来のヒドロゲル材料により作られたコンタクトレンズ を用いる薬物治療の問題点を解決して、角膜が酸素欠乏状態などの長期装用による障害が発生せずに多くの患者に対応可能であるばかりか、価格的にも有利な眼内用の薬剤投与具を提供するものである。   The present invention has been made in view of the above circumstances, and solves the problem of drug treatment using a contact lens made of a conventional hydrogel material, and the cornea is damaged due to long-term wearing such as an oxygen-deficient state. Therefore, the present invention provides an intraocular drug administration device that can be applied to many patients without cost and is also advantageous in price.

前記課題を解決するために、本発明である眼内用の薬剤投与具は、薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放性ヒドロゲル材料により形成された平面が環状を呈することを特徴とし、特に、全体が結膜嚢に装着可能な大きさであると好ましい。   In order to solve the above-mentioned problems, the intraocular drug administration device of the present invention has a ring-shaped plane formed by a sustained-release drug hydrogel material that has a large amount of drug uptake and can control the drug release rate. In particular, it is preferable that the entire size is attachable to the conjunctival sac.

本発明である眼内用の薬剤投与具は環状を呈するので、ほぼ全体を結膜嚢に嵌め込んで使用するので医師において装着が確実で、並びに脱着容易であり、特に、中央環状部に空所が形成されているので、コンタクトレンズと異なり角膜部分が露出するので角膜の酸素欠乏、ドライアイや塵埃、雑菌の混入による障害などが発生しないばかりか、コンタクトレンズの装用が不適応の患者にも対応でき、全体としてコンタクトレンズに比べて表面積が少ないので高価な材料費も安くて済み経済性にも優れている。   Since the intraocular drug administration device according to the present invention has an annular shape, it is used by being almost entirely fitted in the conjunctival sac, so that it can be attached and removed easily by a doctor, and is particularly vacant in the central annular portion. Unlike the contact lens, the cornea is exposed, so the cornea is not deficient in oxygen and is not damaged by dry eye, dust, or germs. As a whole, the surface area is smaller than that of a contact lens, so that expensive material costs are low and the economy is excellent.

また、本発明において、薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放性ヒドロゲル材料により形成された平面がC形状を呈する場合には、前記環状形のものに比べて外径並びに内径に許容度があるので、装着する患者の結膜嚢の径に対応し易い。   Further, in the present invention, when the plane formed by the drug sustained-release hydrogel material having a large amount of drug uptake and capable of controlling the drug release rate has a C shape, it is outside of the annular shape. Since there is tolerance in the diameter and the inner diameter, it is easy to cope with the diameter of the conjunctival sac of the patient to be worn.

更に、本発明において、内周縁の一部に内方向への突出部が形成されている場合には、前記突出部を掴んで、結膜嚢に装着し、或いは離脱させることができるので脱着操作が容易である。   Furthermore, in the present invention, when an inward protruding portion is formed on a part of the inner peripheral edge, the protruding portion can be grasped and attached to or removed from the conjunctival sac. Easy.

本発明によると、眼内に投与した薬剤が長期にわたって適量を患部に投与することが可能で充分な治療効果を期待できる。また、コンタクトレンズのように角膜の表面を覆うことがないので、角膜酸欠や各種の装着による障害を生じる心配がなく、コンタクトレンズの装用が不適応の患者にも対応でき、全体として取り扱いが容易で、経済性も高い。   According to the present invention, it is possible to administer an appropriate amount of a drug administered into the eye to the affected area over a long period of time, and a sufficient therapeutic effect can be expected. In addition, because it does not cover the surface of the cornea unlike a contact lens, there is no fear of corneal oxygen deficiency or various damage caused by wearing, and it can be used for patients who are inappropriate for wearing contact lenses. Easy and economical.

次に本発明の実施の形態について図面を参照して説明する。  Next, embodiments of the present invention will be described with reference to the drawings.

図1は本発明である眼内用の薬剤投与具1を示すものであり、薬剤投与具1は全体が環状を呈し、前記例えば、特開2005−218780号公報、特開2005−314338号公報などに提示されているように、薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放可能なヒドロゲル材料により作られたコンタクトレンズ とほぼ同一材料により同一の方法に製造される。   FIG. 1 shows an intraocular drug administration device 1 according to the present invention. The drug administration device 1 has an annular shape as a whole. For example, JP 2005-218780 A, JP 2005-314338 A, and the like. As shown in the above, a contact lens made of a hydrogel material capable of sustained drug release, which has a large amount of drug uptake and can control the drug release rate, is manufactured in substantially the same manner using the same material.

ここでは、その詳細な説明については省略するが、例えば、ターゲット薬剤、該ターゲット薬剤と物理的架橋構造を形成できる特定官能基を有するモノマーおよび架橋剤からなり、かつ下記式(1)を満たすモノマー混合液を重合して得られるヒドロゲル材料からなる。
y≦0.277x−10 (1)
(ここで、xは特定官能基を有するモノマーのモル濃度(mM)、yはターゲット薬剤のモル濃度(mM)を表わす。ただし、xは50〜800である。)
また、ヒドロゲル材料に表面改質を施すことにより、取り込むことの可能な薬物量が多く、単位体積あたりのゲルへの薬物の取り込み量を大幅に改善して薬効を得るために充分な量の薬物をゲル内に確保するとともに、取り込んだ薬物をゆっくり放出させることが可能である目的にあったものが得られる。
Here, although detailed description thereof is omitted, for example, a target drug, a monomer having a specific functional group capable of forming a physical cross-linking structure with the target drug, and a cross-linking agent and satisfying the following formula (1) It consists of hydrogel material obtained by superposing | polymerizing a liquid mixture.
y ≦ 0.277x−10 (1)
(Here, x represents the molar concentration (mM) of the monomer having a specific functional group, and y represents the molar concentration (mM) of the target drug. However, x is 50 to 800.)
In addition, by applying surface modification to the hydrogel material, the amount of drug that can be incorporated is large, and a sufficient amount of drug to obtain a medicinal effect by greatly improving the amount of drug incorporated into the gel per unit volume. Can be obtained in the gel and the incorporated drug can be released slowly.

尚、前記薬物放出速度を制御し得る薬物徐放可能なヒドロゲル材料に含有させる薬物としては、抗生物質、抗ウィルス剤、抗炎症剤、ステロイド、ペプチド、ポリペプチド、抗アレルギー剤、α−アドレナリン遮断剤、β−アドレナリン遮断剤、抗白内障剤、緑内障治療剤、眼薬、涙液分泌亢進剤、眼の局部的または部分的麻酔薬などがあげられる。   The drug contained in the hydrogel material capable of controlled drug release that can control the drug release rate includes antibiotics, antiviral agents, anti-inflammatory agents, steroids, peptides, polypeptides, antiallergic agents, α-adrenergic blocking. Agents, β-adrenergic blockers, anti-cataract agents, glaucoma therapeutic agents, ophthalmic agents, lacrimal secretion enhancers, local or partial anesthetics of the eye and the like.

また、本実施の形態は、全体がコンタクトレンズのような薄板状を呈しており、全体の大きさが図2に示す人体の眼窩部2に眼瞼3と眼球4との間に形成される結膜嚢5に嵌め込まれる大きさを呈している。   Further, in the present embodiment, the whole has a thin plate shape like a contact lens, and the overall size is a conjunctiva formed between the eyelid 3 and the eyeball 4 in the eye socket 2 of the human body shown in FIG. The size is fitted into the sac 5.

このように構成される本実施の形態である薬剤投与具1は、図3に示すように、結膜嚢5の部分に嵌め込まれて使用される。このように結膜嚢5に嵌め込まれた薬剤投与具1から適量の薬物が長期にわたって眼内に放出される。   The drug administration device 1 according to the present embodiment configured as described above is used by being fitted into the conjunctival sac 5 as shown in FIG. An appropriate amount of drug is thus released into the eye over a long period of time from the drug administration device 1 fitted in the conjunctival sac 5.

このとき、本発明の薬剤投与具1は角膜6の部分には触れないのでコンタクトレンズを装着しているような装着感がなく、また、角膜6における酸欠や異物の混入などによるコンタクトレンズを着用していることによる違和感も生じないばかりか、長期の装用も問題を生じない。   At this time, since the drug administration device 1 of the present invention does not touch the cornea 6, there is no feeling of wearing the contact lens, and the contact lens due to lack of oxygen or contamination of the cornea 6 is not used. Not only does it cause discomfort due to wearing, but long-term wearing does not cause any problems.

尚、本実施の形態における薬剤投与具1は全体として円形の場合を示したが、必ずしも円形でなくてもよく、例えば、適宜の横長楕円形でもよい(図示せず)。横長楕円形の場合には、一部が結膜嚢5に嵌め込まれるので装着や離脱の際の作業が容易であるとともに、一部が直接、角膜6の部分に接触するので薬物を角膜6の部分に直接投与する場合などに適している。   In addition, although the case where the medicine administration device 1 in this Embodiment was circular as a whole was shown, it does not necessarily need to be circular, for example, an appropriate horizontally long ellipse may be used (not shown). In the case of a horizontally long oval shape, a part of the cornea sac is fitted into the conjunctival sac 5 so that it is easy to attach and detach, and a part directly contacts the cornea 6 part. It is suitable for direct administration.

更に、図4は本発明の異なる実施の形態を示すものであり、材質並びに全体の構成は前記図1に示した実施の形態とほぼ同様であるが、全体が平面においてC形を呈している点が異なる。   Further, FIG. 4 shows a different embodiment of the present invention, and the material and the overall configuration are almost the same as those of the embodiment shown in FIG. 1, but the whole has a C shape in a plane. The point is different.

本実施の形態は、全体が平面においてC形を呈しているので、図2に示した結膜嚢5への装着時に、径が多少合わなくても、遊端部を拡縮させることにより大きさの異なる結膜嚢5に装着することが可能であり、汎用性に優れており、患者個々の結膜嚢の大きさに合わせて多数種類の径の異なるものを用意することを要しないので経済的である。   Since the present embodiment has a C shape as a whole in a plane, it can be sized by expanding and contracting the free end portion even when the diameters do not match somewhat when attached to the conjunctival sac 5 shown in FIG. It is possible to attach to different conjunctival sac 5 and is excellent in versatility, and it is economical because it is not necessary to prepare many different diameters according to the size of each patient's conjunctival sac. .

更にまた、図5に示すものは、本発明の更に異なる実施の形態を示すものであり、薬物支持体1の内周縁11の一部に内方向への突出部12が形成されている点が異なる。本実施の形態では、装着並びに離脱時に、前記突出部12をコンタクトレンズ用ののピンセットなどの操作具で掴むことにより容易に作業ができる。また、装着時に突出部12が角膜部分に接するので(図示せず)、直接的な角膜への薬物の投与効果も期待できる。   Furthermore, what is shown in FIG. 5 shows a further different embodiment of the present invention, in that an inward protruding portion 12 is formed on a part of the inner peripheral edge 11 of the drug support 1. Different. In the present embodiment, the work can be easily performed by gripping the protruding portion 12 with an operation tool such as tweezers for contact lenses at the time of mounting and dismounting. Moreover, since the protrusion 12 contacts with the corneal portion at the time of wearing (not shown), a direct administration effect of the drug to the cornea can be expected.

尚、前記実施の形態はいずれもコンタクトレンズのように薄板状に形成されているので装用が容易で目への負担も少ないという利点を有しているが、本発明は、断面が円形状であってもよく(図示せず)、この場合には断面積が増加する結果、薬剤の取り込み量を多くすることができ、長時間の投与がかのうになるという利点がある。   Each of the above embodiments has the advantage that it is easy to wear and less burden on the eyes because it is formed in a thin plate shape like a contact lens, but the present invention has a circular cross section. This may be present (not shown). In this case, the cross-sectional area is increased, so that the amount of the drug taken up can be increased, and there is an advantage that administration for a long time is prolonged.

本発明の好ましい実施の形態を示す平面図。The top view which shows preferable embodiment of this invention. 人体の眼窩部の断面概略図。The cross-sectional schematic of the eye socket of a human body. 図1に示した実施の形態の使用状態を示す説明図。Explanatory drawing which shows the use condition of embodiment shown in FIG. 本発明の異なる実施の形態を示す平面図。The top view which shows different embodiment of this invention. 本発明の更に異なる実施の形態を示す平面図。The top view which shows further another embodiment of this invention.

符号の説明Explanation of symbols

1 薬物支持体、 2 眼窩部、 3 眼瞼、 4 眼球、 5 結膜嚢、 11 内周縁、 12 突出部
DESCRIPTION OF SYMBOLS 1 Drug support body, 2 Orbit part, 3 Eyelid, 4 Eyeball, 5 Conjunctival sac, 11 Inner periphery, 12 Protrusion part

Claims (4)

薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放性ヒドロゲル材料により形成された平面が環状を呈することを特徴とする眼内用の薬剤投与具。   An intraocular drug administration device characterized in that a plane formed by a drug sustained-release hydrogel material having a large amount of drug uptake and capable of controlling the drug release rate has an annular shape. 薬物の取り込み量が多く、かつ薬物放出速度を制御しうる薬物徐放性ヒドロゲル材料により形成された平面がC形状を呈する眼内用の薬剤投与具。   An intraocular drug administration device in which a plane formed by a drug sustained-release hydrogel material having a large amount of drug uptake and capable of controlling the drug release rate has a C shape. 内周縁の一部に内方向への突出部が形成されている請求項1または2に記載の眼内用の薬剤投与具。   The intraocular drug administration device according to claim 1 or 2, wherein an inward projection is formed at a part of the inner peripheral edge. 全体が結膜嚢に装着可能な大きさである請求項1,2または3に記載の眼内用の薬剤投与具。
4. The intraocular drug administration device according to claim 1, 2 or 3, wherein the entire size is attachable to the conjunctival sac.
JP2005369217A 2005-12-22 2005-12-22 Intraocular drug administration appliance Withdrawn JP2007167358A (en)

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