Homatropine hydrobromide in-situ gel rubber preparations for dripping eyes and preparation method thereof

The technology of homatropine hydrobromide and in-situ gel is applied in the directions of pharmaceutical formulation, drug delivery, sensory diseases, etc., and can solve the problems of large fluctuation of blood drug concentration, easy occurrence of adverse reactions, frequent administration times, etc. To achieve the effect of reducing the number of eye drops, reducing the loss of drugs, and good biocompatibility

Inactive Publication Date: 2008-05-21
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Commonly used preparations are generally 1% to 5% eye drops or 2% eye ointment. The frequency of administration is relatively frequent, and the blood concentration fluctuates greatly, which is prone to adverse reactions and low bioavailability. Therefore, it is necessary to use new preparations Technology to reduce the number of doses, reduce side effects, facilitate medication for patients, and improve patient compliance

Method used

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  • Homatropine hydrobromide in-situ gel rubber preparations for dripping eyes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Component Content (by mass)

[0030] Homatropine Hydrobromide 1%

[0031] Gellan Gum 0.5%

[0032] Benzalkonium Chloride 0.01%

[0033] 10% sodium hydroxide solution to adjust the pH value to 6.5-7.2

[0034] Mannitol 3.5%

[0035] Ultrapure water balance

[0036] Take 80g of deionized water, add 0.5g of gellan gum dispersedly while stirring, and stir at about 90°C for about 15 minutes to completely dissolve the gellan gum to form a transparent solution, cool to room temperature, then add 1g of hydrobromic acid and immediately Tropin, 0.01g benzalkonium chloride, and 3.5g mannitol were stirred and dissolved, and the pH was adjusted to 6.5-7.2 by adding 10% sodium hydroxide solution, and ultrapure water was added to 100g.

Embodiment 2

[0038] Component Content (by mass)

[0039] Homatropine Hydrobromide 1%

[0040] Gellan Gum 0.6%

[0041] Benzalkonium Bromide 0.01%

[0042] 10% sodium hydroxide solution to adjust the pH value to 6.5-7.2

[0043] Sucrose 6%

[0044] Ultrapure water balance

[0045] Take 60g of deionized water, add 0.6g of gellan gum dispersedly while stirring, and stir at about 90°C for about 15 minutes to completely dissolve the gellan gum to form a transparent solution, cool to room temperature, then add 1g of hydrobromic acid, and immediately Tropin, 0.01g benzalkonium bromide, 6g sucrose, stirred and dissolved, adjusted pH to 6.5-7.2 by adding 10% sodium hydroxide solution, supplemented with ultrapure water to 100g.

Embodiment 3

[0047] Component Content (by mass)

[0048] Homatropine Hydrobromide 2%

[0049] Gellan Gum 0.4%

[0050] Methylparaben 0.02%

[0051] Propylparaben 0.01%

[0052] 10% sodium hydroxide solution to adjust the pH value to 6.5-7.2

[0053] Glycerol 2%

[0054] Ultrapure water balance

[0055] Take 80g of deionized water, add 0.4g of gellan gum dispersedly while stirring, and stir at about 90°C for about 15min to completely dissolve the gellan gum to form a transparent solution, cool to room temperature, then add 2g of hydrobromic acid and immediately Tropin, 0.02g methylparaben, 0.01g propylparaben, 2g glycerol, after stirring and dissolving, adjust the pH to 6.5-7.2 by adding 10% sodium hydroxide solution, and add ultra-pure water to 100g .

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Abstract

The invention discloses a homatropine hydrobromide in situ gel preparation for eye dripping and the preparation method thereof, which relates to an ion sensitive eye in situ gel preparation and the preparation method thereof. The eye in situ gel takes homatropine hydrobromide as the active ingredient, gellan gum as the gel matrix and preservative, isotonic regulator, pH regulator and ultra-pure water as the assistants for the preparation. The in situ gel preparation of the invention makes use of complex of gel matrix, gellan gum and Ca<2+>, Na<+>, K<+> and other metal ions in tear to form stable hydrogen bonds, so as to be in the gel state. The in situ gel preparation is in liquid state in vitro and is in gel state when the invention is dripped in eye. The preparation combines the advantages of eye drops and eye ointments or gels and at the same time avoids the shortcomings of the two. Furthermore, the usage is convenient, the drug loss is reduced and the local bioavailability is improved.

Description

technical field [0001] The invention relates to an ion-sensitive homatropine hydrobromide in-situ gel preparation with gellan gum as a matrix and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] At present, most of the ophthalmic preparations on the market are eye drops and ointments, which are very popular among patients because of their convenient use and low price. However, eye drops are generally a solution of a drug. After administration, due to the rapid blinking of the eyelids and the continuous secretion of tears in the conjunctival sac, the eye drops are quickly eliminated through the nasolacrimal duct, resulting in biological damage to the eye drops. Utilization is low (often lower than 10%), and in order to achieve therapeutic effect, frequent administration is needed; Although eye ointment can prolong the retention time of medicine in the cornea and improve local bioavailability, it is easy to caus...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/46A61P27/08
Inventor 孙柏旺戴建方姜新东韩苹
Owner SOUTHEAST UNIV
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