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Instant gel rubber of timolol maleate for eyes

A technology of timolol maleate and gel, which is applied in the field of medicine, can solve the problems of short retention time, large loss of eye drops, and restrict the wide use of the curative effect of timolol maleate eye drops, etc. Residence time, no adverse irritant reactions, enrichment of the effect of drug dosage forms

Inactive Publication Date: 2009-01-14
肖正连
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Timolol maleate eye drops is a commonly used ophthalmic preparation, but clinically there is a large loss of eye drops dropped into the eye and a short residence time. These problems limit the use of timolol maleate eye drops. Efficacy and wider use of eye drops

Method used

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  • Instant gel rubber of timolol maleate for eyes
  • Instant gel rubber of timolol maleate for eyes
  • Instant gel rubber of timolol maleate for eyes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Prescription: Timolol maleate 1 g hydrochloric acid (0.05mol / L) 400 ml

[0030] Sodium Citrate 7.2g Methylcellulose 5.0g Phenylethyl Alcohol 0.5g

[0031] Ethanol 5ml Sodium Chloride 1.0g PEG-1000 20g

[0032] PEG-400 5g water for injection appropriate amount

[0033] Preparation method: Heat water for injection to boil, cool to 80°C, add timolol maleate, dissolve phenylethyl alcohol in ethanol, add dropwise to the above solution while stirring, add sodium citrate, stir for more than 30 minutes, Then add hydrochloric acid and stir, filter through a microporous membrane (0.22 μm), heat the filtrate to 40°C, add sodium chloride, methylcellulose, PEG-1000 and PEG-400 while it is hot, and stir to room temperature (18 -25°C), add water for injection to make up the weight to 1000 ml, stir to form a uniform gel, and then aseptically pack it.

Embodiment 2

[0035] Prescription: 1.2 grams of timolol maleate, 200 milliliters of sulfuric acid (0.05mol / L)

[0036] Sodium Citrate 7.2g Methylcellulose 5.0g Benzyl Alcohol 0.5g

[0037] Ethanol 5ml Sodium Chloride 2.0g PEG-1000 70g

[0038] Appropriate amount of water for injection

[0039]Preparation method: heat water for injection to boil, cool to 80°C, add timolol maleate, dissolve benzyl alcohol in ethanol, add dropwise to the above solution while stirring, add sodium citrate, stir for more than 30 minutes, then Stir after adding sulfuric acid, filter through a microporous membrane (0.22μm), heat the filtrate at 40°C, add sodium chloride, methylcellulose and PEG-1000 while hot, stir to room temperature (18-25°C), and then Add water for injection to make up the weight to 1000 ml, stir to make it form a uniform gel, and aseptically pack it.

Embodiment 3

[0041] Prescription: Timolol Maleate 1.4g Sodium Hydroxide (0.1mol / L) 200ml

[0042] Boric acid 5.6g Methylcellulose 5.0g Sodium benzoate 0.5g

[0043] Ethanol 5ml Sodium Chloride 5.0g PEG-4000 100g

[0044] Appropriate amount of water for injection

[0045] Preparation method: heat water for injection to boil, cool to 80°C, add timolol maleate, add sodium citrate, sodium hydroxide and sodium benzoate, stir for more than 30 minutes, then add boric acid and stir, pass through microporous filter Filter through membrane (0.22μm), heat the filtrate to 40°C, add PEG-4000 and methylcellulose while hot, stir to room temperature (18-25°C), add water for injection to make up the weight to 1000ml, stir to make it Form a uniform gel and dispense aseptically.

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Abstract

The invention discloses an immediate type ophthalmic gelatin of timolol maleate and a preparation method thereof. 100 milliliters of the immediate type ophthalmic gelatin of timolol maleate contains 1 to 1.5 grams of the timolol maleate, 0.05 to 1 gram of preservative, 1.0 to 7.5 grams of permeation pressure conditioning agent and 30 to 150 grams of gelatin substrate. Remaining components are acid-base buffer regent and water for injection. The invention enriches the dosage forms of the timolol maleate by optimizing auxiliary materials and improving technology so that lag time in eyes is greatly prolonged and a curative effect is improved without adverse stimulus reaction.

Description

【Technical field】 [0001] The invention belongs to the technical field of medicines, and in particular relates to a timolol maleate instant ophthalmic gel. 【Background technique】 [0002] Ophthalmic instant gel is also called ophthalmic in-situ gel or ophthalmic in-situ gel. Its preparation is liquid when placed at room temperature. Gel-like, it can stay in the eye for a long time, so as to prolong the treatment time, enhance the treatment effect and reduce the loss of medicine. [0003] Instant ophthalmic gel is not yet a very mature pharmaceutical preparation, and instant ophthalmic gel, which depends on the principles of temperature, pH value and ionic strength, is not yet mature in commercialization, because the dosage form is not only It requires fine technology, appropriate excipients, and the proper matching of drugs, processes and excipients in ophthalmic ready-to-use gels. Otherwise, it cannot be placed in a liquid state at room temperature, and it will be transform...

Claims

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Application Information

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IPC IPC(8): A61K31/5355A61K9/00A61K47/32A61K47/34A61K47/38A61P27/06A61K47/10
Inventor 肖正连
Owner 肖正连
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