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Carteolol hydrochloride in-situ-forming eye gel

A hydrochloric acid card and gel technology, which is applied in the directions of medical preparations containing active ingredients, drug delivery, organic active ingredients, etc., can solve the problem of limiting the efficacy of carteolol hydrochloride eye drops, widely used, large loss of eye drops, and retention. Short time and other problems, to achieve the effect of enriching drug dosage forms, prolonging residence time, and improving curative effect

Inactive Publication Date: 2008-12-31
肖正连
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Carteolol hydrochloride 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 curative effect of carteolol hydrochloride eye drops and more widely used

Method used

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  • Carteolol hydrochloride in-situ-forming eye gel
  • Carteolol hydrochloride in-situ-forming eye gel

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Prescription: 5 grams of carteolol hydrochloride, 400 ml of hydrochloric acid (0.05mol / L)

[0025] Sodium Citrate 9.1g Methylcellulose 5.0g Phenylethyl Alcohol 0.5g

[0026] Ethanol 5ml Sodium Chloride 1.0g PEG-1000 20g

[0027] PEG-400 5g water for injection appropriate amount

[0028] Preparation method: Heat water for injection to boil, cool to 80°C, add carteolol hydrochloride, dissolve phenylethyl alcohol in ethanol, add dropwise to the above solution while stirring, add sodium citrate, stir for more than 30 minutes, then add Stir after hydrochloric acid, filter through a microporous membrane (0.22 μm), heat the filtrate to 40°C, add sodium chloride, methylcellulose, PEG-1000 and PEG-400 while hot, and stir to room temperature (18-25 ℃), add water for injection to make up the weight to 1000 milliliters, stir to make it form a uniform gel, and aseptically pack it.

Embodiment 2

[0030] Prescription: 10 grams of carteolol hydrochloride, 200 milliliters of sulfuric acid (0.05mol / L)

[0031] Sodium Citrate 9.1g Methylcellulose 5.0g Benzyl Alcohol 0.5g

[0032] Ethanol 5ml Sodium Chloride 2.0g PEG-1000 70g

[0033] Appropriate amount of water for injection

[0034] Preparation method: heat water for injection to boil, cool to 80°C, add carteolol hydrochloride, dissolve benzyl alcohol in ethanol, add dropwise to the above solution while stirring, add sodium citrate, stir for more than 30 minutes, then add Stir after sulfuric acid, filter through a microporous membrane (0.22μm), heat the filtrate to 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

[0036] Prescription: Carteolol Hydrochloride 20g Sodium Hydroxide (0.1mol / L) 200ml

[0037] Boric acid 5.6g Methylcellulose 5.0g Sodium benzoate 0.5g

[0038] Ethanol 5ml Sodium Chloride 1.0g PEG-4000 100g

[0039] Appropriate amount of water for injection

[0040] Preparation method: Heat water for injection to boil, cool to 80°C, add carteolol hydrochloride, sodium citrate, sodium hydroxide and sodium benzoate, stir for more than 30 minutes, then add boric acid and stir, pass through a microporous membrane (0.22μm) filtered, the filtrate was heated to 40°C, PEG-4000 and methylcellulose were added while it was hot, stirred to room temperature (18-25°C), and water for injection was added to make up the weight to 1000ml, and stirred to form Uniform gel, aseptically dispensed.

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Abstract

The present invention discloses a carteolol hydrochloride eye gel formed in situ and a preparation method thereof. 1,000ml of the carteolol hydrochloride eye gel formed in situ of the present invention contains 5 to 20g of carteolol hydrochloride, 0.05 to 1g of preservative, 1.0 to 7.5g of osmotic pressure regulator and 30 to 150g of gel substance, and the rest quantity is acid-base buffer and water for injection. The carteolol hydrochloride eye gel formed in situ uses the optimization of accessories and the improvement of technology to enrich the medicine preparation form of the carteolol hydrochloride, prolong the detention time of medicine in eyes and improve the curative effect, and cause no pessimal stimulation response.

Description

【Technical field】 [0001] The invention belongs to the technical field of traditional Chinese medicines, in particular to a carteolol hydrochloride ophthalmic instant 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 w...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4704A61P27/02A61P27/06
Inventor 肖正连
Owner 肖正连
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