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Betaxolol hydrochloride ion-sensitive eye-use in-situ gel and preparation method thereof

A betaxolol hydrochloride, ion-sensitive technology, used in medical preparations containing active ingredients, sensory diseases, pharmaceutical formulations, etc., can solve the problems of foreign body sensation, central nervous system, cardiovascular and respiratory system side effects, etc., to ensure affinity , a wide range of sources, the effect of prolonging the residence time

Inactive Publication Date: 2012-10-17
GUIZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are very few betaxolol hydrochloride ophthalmic preparations on the market, and there are currently two main clinically used products: "Betaxol" produced by Alcon and "Nuomeixin" produced by Shandong Haishan Pharmaceutical Co., Ltd. , both of which are liquid suspension preparations of betaxolol hydrochloride, patients will experience discomfort such as foreign body sensation, tearing, and dryness after use
In addition, as a liquid preparation, a large amount of drugs are still absorbed into the systemic circulation through the nasal mucosa or digestive tract after eye administration, which may induce side effects in the central nervous system, cardiovascular system and respiratory system

Method used

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  • Betaxolol hydrochloride ion-sensitive eye-use in-situ gel and preparation method thereof
  • Betaxolol hydrochloride ion-sensitive eye-use in-situ gel and preparation method thereof
  • Betaxolol hydrochloride ion-sensitive eye-use in-situ gel and preparation method thereof

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Embodiment 1

[0016] Embodiment 1 of the present invention: preparation of betaxolol hydrochloride ion-sensitive ophthalmic in situ gel, calculated in parts by weight, first weigh 50 parts of mannitol and 0.3 part of ethylparaben, and add 667 parts of injection Heat and stir with water to completely dissolve mannitol and ethylparaben to obtain solution A; then add 2 parts of deacetylated gellan gum to solution A, continue heating and keep stirring until the deacetylated gellan gum is completely dissolved, and then Cool naturally to room temperature to obtain solution B; add 2.8 parts of betaxolol hydrochloride to solution B, stir to completely dissolve betaxolol hydrochloride, then add water for injection to the full amount, stir evenly, and filter through a microporous membrane Aseptically subpackaged to obtain a finished product with a pH value of 5.85 and a viscosity of 4.0 centipoise.

Embodiment 2

[0017] Embodiment 2 of the present invention: preparation of betaxolol hydrochloride ion-sensitive ophthalmic in situ gel, calculated by weight, first weigh 25 parts of glycerin and 0.3 part of ethylparaben, and add 550 parts of injection Heat and stir with water to completely dissolve ethylparaben to obtain solution A; then add 3 parts of deacetylated gellan gum to solution A, continue heating and keep stirring until the deacetylated gellan gum is completely dissolved, and then cool naturally to room temperature to obtain solution B; add 2.8 parts of betaxolol hydrochloride to solution B, stir to completely dissolve betaxolol hydrochloride, then add water for injection to the full amount, stir evenly, and perform aseptic Subpackage to obtain a finished product with a pH value of 6.04 and a viscosity of 8.2 centipoise.

Embodiment 3

[0018] Embodiment 3 of the present invention: preparation of betaxolol hydrochloride ion-sensitive ophthalmic in situ gel, calculated in parts by weight, first weigh 45 parts of sorbitol, 0.2 part of methylparaben and 0.1 part of paraben Gold propyl ester, and add 650 parts of water for injection, heat and stir to completely dissolve sorbitol, methylparaben and propylparaben, and obtain solution A; then add 4 parts of deacetylated gellan gum to solution A, continue Heating and keeping stirring until deacetylated gellan gum is completely dissolved, then naturally cooling to room temperature to obtain solution B; adding 2.8 parts of betaxolol hydrochloride to solution B, stirring to completely dissolve betaxolol hydrochloride, and then adding Add water for injection to the full amount, stir evenly, filter through a microporous membrane, and carry out aseptic sub-packaging to obtain a finished product with a pH value of 5.81 and a viscosity of 7.1 centipoise.

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Abstract

The invention discloses a betaxolol hydrochloride ion-sensitive eye-use in-situ gel. Every 1000 parts of a finished product of the gel comprise: 1-5 parts of betaxolol hydrochloride, 2-10 parts of an ion-sensitive gel material, 22-50 parts of an osmotic pressure conditioning agent, 0.1-5 parts of a bacteriostatic agent, and balance of injection water. Under an in-vitro condition, the eye-use in-situ gel provided by the invention is a solution which can flow freely. When the solution is dropped into eyes, the solution contacts cations such as Na<+>, K<+>, Ca<2+> and the like in tears, and the solution is subjected to gelatinization, such that a non-chemical-crosslinked semisolid preparation is formed. Therefore, the affinity of betaxolol hydrochloride and eye mucosal tissues is effectively ensured, and the retention time of the medicine in eyes is prolonged. Therefore, possible side effect caused by a large amount of medicine which is absorbed into systemic circulation through nasal mucosa or digestive tract is avoided.

Description

technical field [0001] The invention relates to the field of pharmaceutical sciences, in particular to a betaxolol hydrochloride ion-sensitive in-situ ophthalmic gel and a preparation method thereof. Background technique [0002] Eyes are the windows for human beings to perceive the world, and at the same time they are extremely sensitive organs. Intraconjunctival eye drops are the most common treatment for ocular disorders. However, studies have found that because the eyes have very effective protective mechanisms such as tearing and blinking reflex, the liquid medicine instilled into the eye is quickly eliminated from the precorneal area, so traditional eye drops have problems such as short residence time and low bioavailability. In addition, a large amount of drugs enter the nasal cavity or digestive tract through the nasolacrimal duct and are finally absorbed systemically, which increases the risk of side effects and toxicity. [0003] Ophthalmic in-situ gel refers to ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/138A61P27/06A61P27/02
Inventor 王慧娟郭东贵周英李俐
Owner GUIZHOU UNIV
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