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Latanoprost-containing aqueous eye drops and method for inhibiting adsorption of latanoprost to resin

A technology for latanoprost and eye drops, which is applied in the field of inhibiting the adsorption of latanoprost to resin, can solve problems such as insufficient inhibition effect, and achieve the effects of improving thermal stability and inhibiting adsorption

Inactive Publication Date: 2012-05-30
SENJU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in these prior arts, the stabilization of latanoprost in an aqueous solution and the inhibitory effect of the adsorption of latanoprost to a resin container in an aqueous solvent are insufficient, and improvement is desired.

Method used

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  • Latanoprost-containing aqueous eye drops and method for inhibiting adsorption of latanoprost to resin
  • Latanoprost-containing aqueous eye drops and method for inhibiting adsorption of latanoprost to resin
  • Latanoprost-containing aqueous eye drops and method for inhibiting adsorption of latanoprost to resin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0163] [Example 1] Aqueous eye drops

[0164] The formulation of the aqueous eye drops of Example 1 is shown in Table 1 together with the formulations of the aqueous eye drops of Comparative Examples 1 and 2. For their preparation, first, (1) in Table 1 was added to (8) (10% benzalkonium chloride solution), stirred and dissolved at about 50° C. to prepare a stock solution of latanoprost. Add (2)-(7) and an appropriate amount of (11) into another container, stir to dissolve, and prepare a base stock solution. Add all the basic stock solution to the latanoprost stock solution, stir well, add (9) and (10) to adjust the pH to 6.7, add (11) to make the total amount 1L.

[0165] 【Table 1】

[0166]

Embodiment 2～6

[0197] [Examples 2-6] Aqueous eye drops

[0198] The formulations of the aqueous eye drops of Examples 2 to 6 are shown in Table 5 together with the formulation of the aqueous eye drops of Comparative Example 3. In Table 5, the numerical values ​​for each component are represented by content ((w / v)%). "Appropriate amount" means the amount required to make the pH of the aqueous eye drops 6.7 for hydrochloric acid and sodium hydroxide, and means the amount to make the total amount 100 (w / v)% for purified water. These aqueous eye drops were prepared in the same manner as in Example 1.

Embodiment 7～11

[0203] [Examples 7-11] Aqueous eye drops

[0204] In this example, in order to more accurately evaluate the effect of surfactants and sorbic acid on inhibiting the adsorption of latanoprost to the resin, a formulation without benzalkonium chloride interacting with sorbic acid was applied.

[0205] Table 6 shows the formulations of the aqueous eye drops of Examples 7-11 and Comparative Examples 10-13. In Table 7, the numerical values ​​for each component are represented by content (w / v%).

[0206] The aqueous eye drops of Examples 7 to 11 and Comparative Examples 10 to 13 were prepared as follows: (1) to (10) in Table 6 were added to (14), stirred at about 80°C, and after dissolving, added to (12) and (13) Adjust the pH to 6.7, and use (14) to make the total amount 200 mL.

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PUM

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Abstract

Provided is a formulation of latanoprost-containing aqueous eye drops wherein decreases in effective latanoprost concentration due to adsorption to resin are inhibited and the stability of the latanoprost is improved. Also provided is a method for inhibiting adsorption of latanoprost to resin. The provided aqueous eye drops contain latanoprost, a surfactant, and a C3-10 aliphatic mono- or di-carboxylic acid or a salt thereof. The inclusion of a surfactant and either a C3-10 aliphatic mono- or di-carboxylic acid or a salt thereof allows the provision of a method for inhibiting the adsorption to resin of latanoprost in an aqueous solution.

Description

technical field [0001] The present invention relates to aqueous eye drops containing latanoprost. The present invention additionally relates to methods of inhibiting the adsorption of latanoprost to resins. Background technique [0002] Glaucoma, at least in part, is a group of ocular diseases characterized by progressive optic nerve disturbance due to elevated intraocular pressure (IOP). In Japan, glaucoma is the second leading cause of blindness after diabetic retinopathy. [0003] prostaglandin F 2α Latanoprost, a derivative, has high selectivity for prostaglandin receptors, namely FP receptors, and has the effect of increasing uveoscleral outflow of aqueous humor and reducing intraocular pressure. Side effects such as conjunctival hyperemia may be observed with latanoprost, but these are mostly mild and transient, and are widely used as eye drops for glaucoma treatment because once-a-day eye drops are effective. [0004] However, latanoprost is particularly easily ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5575A61K9/08A61K31/5377A61K47/12A61K47/22A61K47/34A61P27/06
CPCA61K9/0048A61K47/14A61K9/08A61K47/44A61K47/12A61K31/5575A61K47/26A61K47/10A61K31/5377A61P27/02A61P27/06A61P43/00A61K2300/00
Inventor 中岛朋子朝山和喜子多鹿哲也
Owner SENJU PHARMA CO LTD
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