A kind of ophthalmic composition, its preparation method and application

A technology for ophthalmic compositions and eye drops, which is applied in the direction of drug combinations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve the problem of inability to improve bacteriostasis and decrease in the content of active ingredients in preservatives , impurity increase and other problems, to achieve good preventive or therapeutic effect, low eye irritation effect

Active Publication Date: 2021-11-19
SHENYANG XINGQI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are some researches on voriconazole freeze-dried powder injection. Among them, some studies have found that adding preservatives commonly used in ophthalmology (benzalkonium chloride, benzalkonium bromide, cetrimonium bromide, phenoxy After the preparation of ethanol, p-hydroxybenzoic acid lipids, chlorobutanol), there is almost no inhibitory effect on bacteria, which does not meet the bacteriostatic requirements of ophthalmic preparations. times), also can not improve the bacteriostasis; also research found that after adding preservative sorbic acid (5 times of conventional dosage) when preparing voriconazole freeze-dried eye drops, the bacteriostasis meets the requirements, but found that preservatives and The content of active ingredients has dropped significantly, and the impurities have increased significantly
So far, no preservative has been found that has antibacterial effect on voriconazole freeze-dried eye drops and does not affect the activity of the drug

Method used

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  • A kind of ophthalmic composition, its preparation method and application
  • A kind of ophthalmic composition, its preparation method and application
  • A kind of ophthalmic composition, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0119] Prepare the voriconazole eye drops of embodiment 1 by prescription in table 1, and its preparation method may further comprise the steps:

[0120] (1) Swell the polyvinyl alcohol of the prescribed amount with an appropriate amount of water for injection, heat and dissolve, and set aside;

[0121] (2) dissolving the glycine of the prescribed amount with an appropriate amount of water for injection for subsequent use to obtain a solution;

[0122] (3) disperse the hydroxypropyl beta cyclodextrin of the prescribed amount with an appropriate amount of water for injection, stir and dissolve to obtain a solution;

[0123] (4) Adjust the pH value of the solution obtained in step (3) to about 5.0 with an appropriate amount of hydrochloric acid, add sodium chloride in the prescribed amount, stir and dissolve, and obtain the solution;

[0124] (5) Add the prescribed amount of voriconazole into the solution in step (4), and continue to stir for 1-3 hours at room temperature until...

Embodiment 2～ Embodiment 4

[0129] The voriconazole eye drops of Examples 2-4 were prepared according to the prescription in Table 1.

[0130] The preparation method refers to Example 1, wherein sulfobutylbeta cyclodextrin is used in step (3) of Example 2, and no sodium chloride is added in step (4) of Example 4.

[0131] Table 1

[0132] Component Example 1 Example 2 Example 3 Example 4 Voriconazole 0.50g 1.00g 1.00g 2.00g Hydroxypropyl Beta Cyclodextrin 10g — 20g 25g sulfobutyl beta cyclodextrin — 20g — — polyvinyl alcohol 0.3g 0.6g 0.6g 1.0g Glycine 0.05g 0.1g 0.1g 0.3g hydrochloric acid Appropriate amount Appropriate amount Appropriate amount Appropriate amount Sodium chloride 0.45g 0.10g 0.10g — Add water for injection to 100g 100g 100g 100g

Embodiment 5～ Embodiment 8

[0134] The voriconazole eye drops of Examples 5-8 were prepared according to the prescription in Table 2.

[0135] The preparation method refers to Example 1, wherein step (2) and step (7) are omitted, and sulfobutylbeta cyclodextrin is used in step (3) of Example 6, step (4) of Example 8 Sodium chloride was not added.

[0136] Table 2

[0137]

[0138]

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Abstract

The invention belongs to the field of pharmaceutical preparations, and specifically relates to an ophthalmic composition, comprising the following components: 0.5-5 parts by weight of voriconazole and / or a pharmaceutically acceptable salt thereof, 8-35 parts by weight of a solubilizer, and 0.1-4 parts by weight of polyvinyl alcohol parts by weight. The present invention also relates to a method for preparing the ophthalmic composition and the use of the ophthalmic composition. The ophthalmic composition of the invention has high stability, low ocular irritation, no preservative, and good preventive or therapeutic effect on ocular fungal infectious diseases.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, specifically relates to an ophthalmic composition, and also relates to a preparation method and application of the ophthalmic composition. Background technique [0002] Ocular fungal infectious diseases include fungal keratitis, fungal conjunctivitis, fungal blepharitis, etc. Among them, fungal keratitis has a high incidence and blinding rate, and has become a common blinding eye disease in my country. The main pathogens are Fusarium and Aspergillus. Due to the long treatment cycle and easy recurrence after ocular fungal infection, there is an increasing demand for therapeutic drugs with good clinical efficacy and broad antibacterial spectrum. Currently, the commonly used topical antifungal drugs in ophthalmology include polyene antifungal drugs and triazole antifungal drugs. Among them, the product representative of polyene antifungal drugs is natamycin eye drops, which is the only a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/506A61K47/18A61K47/32A61P27/02A61P31/10A61P31/02
CPCA61K9/0048A61K9/08A61K31/506A61K47/183A61K47/32A61P27/02A61P31/02A61P31/10
Inventor 杨希琴杨强高坤刘继东
Owner SHENYANG XINGQI PHARM CO LTD
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