Novel eye drop composition for treating dry eye syndrome containing rebamipide and method for solubilizing and stabilizing same
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The technology of a special eye drop, rebamipide, is applied in the field of preparation of eye drop aqueous solution and its composition, which can solve problems such as biocompatibility and achieve minimal side effects, convenient use, and high bioavailability Effect
Active Publication Date: 2020-05-05
DAEWOO PHARMA IND
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[0031] In this regard, as there are no data on the use of cyclodextrins above 3% as pharmaceutical excipients, additional toxicity data are required
[0032] In addition, in the examples, the pH is more than 8, so it can be seen that there are still biocompatibility problems
[00
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Embodiment 9 to Embodiment 18
[0126] [Example 9 to Example 18] Preparation of 1.5% eye drops by solubilizing rebamipide
[0127] [table 5]
[0128]
[0129]
[0130] 1) Add the stabilizer corresponding to each example in 85ml of distilled water and stir to dissolve, then add the main component rebamipide and stir to suspend it.
[0131] 2) Add 1N NaOH solution as a solubilizer dropwise to the solution of 1) under stirring, adjust the pH to 10-11, and dissolve all the main components.
[0132] 3) Add the buffer corresponding to each example to the solution of 2) and stir to dissolve them all.
[0133] 4) Add the osmotic pressure regulator corresponding to each example to the solution of 3) and stir to adjust to a hypotonic range of 220 to 240 mOsmol / kg that can be used as eye drops.
[0134] 5) Add dropwise the 1N HCl solution corresponding to each embodiment as a pH regulator to the transparent solution obtained in the above 4), and adjust the pH to 7-8.
[0135] 6) Add distilled water to the tran...
Embodiment 19 to Embodiment 22
[0147] [Example 19 to Example 22] Preparation of 1.5% eye drops by solubilizing rebamipide
[0148] [Table 7]
[0149]
[0150]
[0151] 1) Add a stabilizer to 85ml of distilled water and stir to dissolve, then add the main component rebamipide and stir to suspend it.
[0152] 2) Add 1N NaOH solution as a solubilizer dropwise to the solution of 1) under stirring, adjust the pH to 10-11, and dissolve all the main components.
[0153] 3) Add the buffer corresponding to each example to the solution of 2) and stir to dissolve them all.
[0154] 4) Add the osmotic pressure regulator corresponding to each embodiment to the solution of 3) and stir to adjust to a hypotonic 170-190 mOsmol / kg.
[0155] 5) Add dropwise the 1N HCl solution corresponding to each embodiment as a pH regulator to the transparent solution obtained in the above 4), and adjust the pH to 7-8.
[0156] 6) Add distilled water to the transparent solution obtained in 5) to make the total volume 100 ml to obt...
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Abstract
The present invention relates to an eye drop composition for treating dry eye syndrome, characterized in that the eye drop composition remains stable during storage without precipitation occurring andcontains a safe ingredient for use as an eye drop, by solubilizing rebamipide that is a poorly soluble compound, and a method for producing the same. The eye drop composition for treating dry eye syndrome of the present invention includes a base for solubilizing rebamipide, and is characterized by containing a stabilizer for maintaining a supersaturated stabilized state, a specific type of bufferfor maintaining biocompatible pH of 7 to 8 and an osmotic agent. A method for producing the same comprises the steps of: adding a base to rebamipide or a pharmaceutically acceptable salt thereof anda stabilizer and dissolving the same in water to obtain an aqueous eye drop solution of pH of 10 to pH of 11; adding at least one osmotic agent selected from a buffer and a nonionic osmotic agent to the eye drop solution and dissolving the same; and after adjusting the pH to 7 to 8 with an acid, filtering the solution with a syringe filter to make the same sterile. The produced eye drop is in theform of an aqueous solution, is stable when frozen, refrigerated, and at room temperature, and includes a therapeutic agent for dry eye syndrome which is stable even when cross-stored in a refrigerator or at room temperature, or at a refrigerating temperature or room temperature.
Description
technical field [0001] The invention relates to the preparation and composition of an aqueous eye drop solution for treating dry eye, wherein rebamipide is stably solubilized, contains additive components safe to human body, and has excellent therapeutic effect. [0002] By utilizing the aqueous solution of the present invention, an eye drop composition for the purpose of treating dry eye can be provided. [0003] Eye drops in a completely aqueous state have high bioavailability, are non-resistance and convenient for users, and are economical and efficient in terms of aseptic preparation and quality control. [0004] Due to the characteristics of its preparation, eye drops have various storage forms in terms of distribution and use after preparation, such as refrigeration, room temperature and high temperature conditions, etc. [0005] Therefore, under these various conditions, the key to ensuring stability is to maintain the solution state which is the initially set mass sta...
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