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Preparation and application of olopatadine in-situ gel

A technology of in-situ gel and olopatadine, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, respiratory diseases, etc., can solve the problem of high acid carbomer concentration, discomfort, and eye problems Irritation and other issues

Inactive Publication Date: 2011-02-09
胡容峰
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the large concentration of acidic carbomer required to form a stable gel, it is not easy to be neutralized and irritating, so it is not suitable for use as a matrix for in-situ gel alone, and it is irritating to the eyes

Method used

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  • Preparation and application of olopatadine in-situ gel
  • Preparation and application of olopatadine in-situ gel
  • Preparation and application of olopatadine in-situ gel

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] Embodiment 1 Preparation of olopatadine thermosensitive eye (or nasal cavity) gel

[0098] [Prescription] Olopatadine 0.15g

[0099] Brogeramine (Benzalkonium Bromide) 0.02g

[0100] F127 21.4g

[0101] F68 9.6g

[0102] Add isotonic phosphate buffer (pH7.4) to the full amount of 100g

[0103] [Preparation method] Take olopatadine and dissolve it in 60% sterile isotonic phosphate buffer (pH7.4) with prescribed amount of bromogeramine, slowly add the prescribed amount of F127 and F68 under stirring condition, add isotonic phosphate buffered saline To a sufficient amount, store in cold storage at low temperature to fully swell until a clear and uniform solution is formed.

Embodiment 2

[0104] Embodiment 2 Preparation of olopatadine thermosensitive ophthalmic (or nasal cavity) gel

[0105] [Prescription] Olopatadine 0.1g

[0106] Brogeramine (Benzalkonium Bromide) 0.02g

[0107] F127 21.4g

[0108] F68 9.6g

[0109] NaCl 0.9g

[0110] Add distilled water to the full amount of 100g

[0111] [Preparation method] Dissolve olopatadine, brogeramine, and NaCl in 60% distilled water of the prescribed amount, slowly add the prescribed amount of F127 and F68 under stirring conditions, add distilled water to a sufficient amount, and store in low temperature refrigeration to fully swell until it becomes clear homogeneous solution.

Embodiment 3

[0112] Embodiment 3 Preparation of olopatadine thermosensitive ophthalmic (or nasal cavity) gel

[0113] [Prescription] Olopatadine 0.3g

[0114] Brogeramine (Benzalkonium Bromide) 0.02g

[0115] F127 21.4g

[0116] F68 9.6g

[0117] Mannitol 5g

[0118] Add distilled water to the full amount of 100g

[0119] [Preparation method] Dissolve olopatadine, brogeramine, and mannitol in 60% distilled water of the prescribed amount, slowly add the prescribed amount of F127 and F68 under stirring conditions, add distilled water to a sufficient amount, and store in low temperature refrigeration to fully swell until formed Clear homogeneous solution.

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Abstract

The invention relates to a new dosage form of olopatadine in the technical field of medicines, in particular to the preparation and an application of olopatadine in-situ gel. The invention is characterized in that the preparation is a solution in a non-physiological state and is converted into gel in a physical state. Olopatadine temperature-sensitive gel is prepared by systematically investigating shaft materials and properly proportioning poloxamer 407 (F127 for short) and poloxamer 188 (F68 for short). Olopatadine pH-sensitive gel is prepared by adjusting the consumption of carbomer 980 and hydroxypropyl methyl cellulose (HPMC). The preparations can be applied through the eyes or nasal cavity, the residence time of the drug in the administration parts is greatly prolonged, bioavailability is increased, curative effect is improved, and the preparation has ideal application prospects.

Description

technical field [0001] The present invention relates to a new dosage form of olopatadine for ophthalmic or nasal cavities, which is a solution in a non-physiological state, and the preparation and application of a gel in a physiological state. Specifically, it is the temperature and temperature of olopatadine Preparation method and clinical indication of pH sensitive gel. The preparation greatly prolongs the residence time of the drug in the eye (or nasal cavity), improves the bioavailability, improves the curative effect, and has an ideal application prospect. Background technique [0002] Olopatadine is a mast cell stabilizer and a relatively selective histamine H1-receptor antagonist. Both in vivo and in vitro experiments can inhibit type I immediate hypersensitivity reactions. Olopatadine has no effect on alpha-adrenergic receptors, dopamine receptors, muscarinic type I and type II receptors, and serotonin receptors. Currently, the olopatadine preparations on the mark...

Claims

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Application Information

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IPC IPC(8): A61K31/335A61K47/38A61K47/40A61K47/34A61P11/02A61K9/00A61P37/08A61P27/14A61K47/10
Inventor 胡容峰徐亚静
Owner 胡容峰
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