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Ophthalmologic intraocular pressure reduction drug for external use

A drug and intraocular pressure technology, which is applied in the field of topical ocular preparations, can solve the problems of limited curative effect, low drug concentration, and short drug effect maintenance time, and achieve reliable curative effect, long-lasting drug effect, and reduce the number of drops

Inactive Publication Date: 2013-04-17
GUANGDONG WHOLEWIN TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this timolol ophthalmic preparation has poor intraocular penetration and relatively low drug concentration in ocular tissue, so its curative effect is limited
Furthermore, the drug effect of the existing timolol ophthalmic preparations is maintained for a short time after administration, resulting in large fluctuations in intraocular pressure, which can easily cause various ocular adverse reactions
If the number of daily doses is increased, the toxicity of the drug itself and preservatives to ocular tissues is increased

Method used

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  • Ophthalmologic intraocular pressure reduction drug for external use
  • Ophthalmologic intraocular pressure reduction drug for external use
  • Ophthalmologic intraocular pressure reduction drug for external use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-3

[0017] Embodiment 1-3 prepares timolol maleate eye drops by the inventive method

[0018] The used raw material components and consumption are listed in the following table:

[0019]

[0020] The preparation method is as follows: dissolve the full amount of timolol maleate with an appropriate amount of water for injection, add potassium sorbate and stir to dissolve, disperse the thickener with water for injection and let it cool, and then dissolve the pH regulator and osmotic pressure regulator with water for injection agent, bacteriostatic agent, stir well and filter, combine the two liquids, then add the dissolved timolol maleate, add water for injection to the full amount, filter, subpackage, and obtain. A pH regulator is used to adjust the pH value of the finished eye drops to 6.0-8.0.

Embodiment 4-6

[0021] Example 4-6 Preparation of Timolol Maleate Eye Drops Containing Tanshinone IIA

[0022] The used raw material components and consumption are listed in the following table:

[0023]

[0024]

[0025] The preparation method is as follows: dissolve the full amount of timolol maleate with an appropriate amount of water for injection, add potassium sorbate and stir to dissolve, then add tanshinone ⅡA and stir to dissolve, disperse the thickener with water for injection and let it cool, then dissolve it with water for injection Mix the pH regulator, osmotic pressure regulator and bacteriostatic agent, stir well and filter, combine the two liquids, then add the dissolved timolol maleate, add water for injection to the full amount, filter, subpackage, and get ready. A pH regulator is used to adjust the pH value of the finished eye drops to 6.0-8.0.

Embodiment 7-9

[0026] Example 7-9 Preparation of Timolol Maleate Eye Drops Containing Tanshinone IIA

[0027] The used raw material components and consumption are listed in the following table:

[0028]

[0029]

[0030] The preparation method is as follows: dissolve the full amount of timolol maleate with an appropriate amount of water for injection, add potassium sorbate and stir to dissolve, then add tanshinone ⅡA and stir to dissolve, disperse the thickener with water for injection and let it cool, then dissolve it with water for injection Mix the pH regulator, osmotic pressure regulator and bacteriostatic agent, stir well and filter, combine the two liquids, then add the dissolved timolol maleate, add water for injection to the full amount, filter, subpackage, and get ready. A pH regulator is used to adjust the pH value of the finished eye drops to 6.0-8.0.

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PUM

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Abstract

The invention discloses an ophthalmologic intraocular pressure reduction drug for external use. The drug takes timolol maleate as an active pharmaceutical ingredient; and the drug further comprises potassium sorbate, and the potassium sorbate is added according to the ratio that timolol maleate:potassium sorbate equals to 1:(0.1-5.0). The drug also takes tanshinone IIA as the active pharmaceutical ingredient, and the tanshinone IIA is added according to the ratio that timolol maleate:tanshinone IIA equals to 1:(0.1-5.0). The potassium sorbate-containing timolol maleate eye drops have a lasting medicinal effect, and the frequency for dropping the eye drops can be reduced.

Description

technical field [0001] The present invention relates to medical preparations, in particular to ocular topical preparations for lowering intraocular pressure. Background technique [0002] Timolol preparation is a known drug for lowering intraocular pressure, and its maleate salt is commonly used. The effect of lowering intraocular pressure after instillation is quick, and the intraocular pressure begins to drop about 20 minutes after instillation, and 1 to 2 hours then dropped to the maximum. The timolol ophthalmic preparations currently on the market are timolol maleate eye drops and timolol maleate ophthalmic gel administered twice a day. However, this timolol ophthalmic preparation has poor intraocular penetration and relatively low drug concentration in ocular tissues, so its curative effect is limited. Furthermore, the duration of the drug effect of the existing timolol ophthalmic preparation is short after administration, which leads to large fluctuations in intraocu...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K47/12A61K31/58A61P27/02
Inventor 王延东吴绮峰
Owner GUANGDONG WHOLEWIN TECH
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