Eye-purposed in-vivo gel preparation prepared from pH (Potential Of Hydrogen) sensitive type baicalin

A body gel and ophthalmic technology, applied in the field of ophthalmic pharmaceutical preparations, can solve the problems of loss of baicalin and low bioavailability, and achieve the effects of reasonable composition, increased adhesion time, and increased effective drug concentration

Active Publication Date: 2014-08-20
北京汇诚瑞祥医药生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the shortcomings of the dosage form of eye drops and the physical and chemical properties of baicalin itself at different pH values, most of the baicalin instilled into the eyes is lost, and the bioavailability is low

Method used

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  • Eye-purposed in-vivo gel preparation prepared from pH (Potential Of Hydrogen) sensitive type baicalin
  • Eye-purposed in-vivo gel preparation prepared from pH (Potential Of Hydrogen) sensitive type baicalin
  • Eye-purposed in-vivo gel preparation prepared from pH (Potential Of Hydrogen) sensitive type baicalin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Preparation of Example 1pH Sensitive Baicalin Ophthalmic In-body Gel (1)

[0049] The composition of the drug prescription is: 0.1 part of baicalin, 0.3 part of carbomer 974PNF 974PNF), 0.6 parts of HPMCE4M, 0.9 parts of sodium chloride, 0.001 parts of benzalkonium bromide, and 94 parts of phosphate buffered saline (PBS) at pH 5.8.

[0050] The preparation method of the above-mentioned pH-sensitive ophthalmic in-body gel preparation comprises the following steps:

[0051] (1) preparation matrix: get the described ratio Add HPMCE4M to an appropriate amount of pH5.8 phosphate buffer under constant stirring, and stir evenly to obtain the matrix;

[0052] (2) Prepare the drug solution: take the baicalin, sodium chloride and benzalkonium bromide in the ratio, gradually add them to the phosphate buffer solution with pH 5.8, and mix evenly to obtain the drug solution;

[0053] (3) Mixing: Add the drug solution prepared in step (2) into the matrix obtained in step (1) unde...

Embodiment 2

[0054] Preparation of embodiment 2pH-sensitive baicalin ophthalmic in-body gel (2)

[0055] The composition of the drug prescription is: 0.1 part of baicalin, 0.3 part 980NF, 0.6 parts of HPMCF4M, 0.9 parts of sodium chloride, 0.001 parts of benzalkonium bromide, and 94 parts of phosphate buffered saline at pH 5.8.

[0056] The preparation method of the pH-sensitive ophthalmic in-body gel preparation is the same as that in Example 1.

Embodiment 3

[0057] Preparation of Example 3 pH Sensitive Baicalin Ophthalmic In-body Gel (3)

[0058] The composition of the drug prescription is: 0.1 part of baicalin, 0.3 part 934PNF, 0.6 parts of HPMCK4M, 0.9 parts of sodium chloride, 0.001 parts of benzalkonium bromide, and 94 parts of phosphate buffered saline at pH 5.8.

[0059] The preparation method of the pH-sensitive ophthalmic in-body gel preparation is the same as that in Example 1.

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Abstract

The invention relates to a pH-sensitive baicalin ophthalmic in-body gel preparation, which comprises the following components (by weight): 0.05-10 parts of baicalin, 0.1-3 parts of pH-sensitive materials, 0.1-10 parts of Thickener, 0.1-10 parts of isotonic regulator, 0.001-3 parts of preservative and 80-100 parts of buffer solution with pH5-6.2. The present invention also relates to the preparation method of the pH-sensitive baicalin ophthalmic in-body gel preparation and its use in the preparation of medicines for preventing and / or treating conjunctivitis, keratitis or cataract.

Description

technical field [0001] The present invention relates to an ophthalmic pharmaceutical preparation, in particular to an ophthalmic in-body gel preparation, especially a pH-sensitive baicalin ophthalmic in-body gel preparation, and the preparation method and application of the gel preparation . Background technique [0002] The traditional ophthalmic drug delivery method is often in the form of eye drops, but eye drops have problems such as short residence time and low bioavailability. Degrees are generally less than 10%. Therefore, the inherent deficiency of ophthalmic liquid preparations has prompted people to explore the development of ocular solid drug delivery systems with long residence time and slow and controlled release capabilities. Environmentally sensitive gel drug delivery system is a new dosage form born with the rapid development of pharmaceutical polymer material science, which improves patient compliance. Environmentally sensitive gel refers to a non-chemica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/7048A61K47/32A61K47/36A61K47/38A61P27/02A61P27/12
Inventor 刘志东武昊昀李琳李楠李佳玮
Owner 北京汇诚瑞祥医药生物科技有限公司
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