Preparation and application of gatifloxacin temperature and pH sensitive ophthalmic gel

Abstract

The invention relates to the technical field of medicaments and a new gatifloxacin ophthalmic formulation, in particular to the preparation and application of gatifloxacin temperature and pH sensitive ophthalmic gel. The invention is characterized in that: the formulation is solution in a non-physiological state and is converted into gel in a physiological state through phase variation. The temperature sensitive ophthalmic gel is prepared by performing systematic observation on an auxiliary material and using poloxamer 407 and poloxamer 188 in a proper ratio. The pH sensitive ophthalmic gel is prepared by regulating the using amount of poloxamer 980 and hydroxypropyl methyl cellulose (HPMC). Due to the adoption of the formulation, the detention time of the medicaments on eyes is greatly prolonged, the bioavailability is enhanced and the curative effect is improved; and the formulation has ideal application prospects.

Description

technical field

[0001] The present invention relates to a new dosage form of ophthalmic medicine, which is a solution in a non-physiological state, and the preparation and application of a gel in a physiological state. Specifically, it is sensitive to temperature and pH of gatifloxacin (abbreviated as GAT). Preparation method and clinical indication of ophthalmic gel. The preparation greatly prolongs the residence time of the drug in the eyes, improves the bioavailability, improves the curative effect, and has an ideal application prospect. Background technique

[0002] The gatifloxacin ophthalmic preparations currently on the market are mainly eye drops. There are eye ointment and eye gel in preparation. Among them, after the eye drops are used, due to eyelid blinking and tear dilution, the eye drops are quickly eliminated through the nasolacrimal duct, and their bioavailability is often less than 1%. It is necessary to increase the number of administrations to maintain t...

Examples

Embodiment 1

[0072] The preparation of embodiment 1 gatifloxacin thermosensitive ophthalmic gel

[0073] 【Prescription】Gatifloxacin 0.3g

[0074] Brogeramine (Benzalkonium Bromide) 0.02g

[0075] F127 21.4g

[0076] F68 9.6g

[0077] Add isotonic phosphate buffer (pH7.4) to the full amount of 100g

[0078] [Preparation method] Dissolve gatifloxacin and bromogeramine in 60% sterile isotonic phosphate buffer (pH7.4) in the prescribed amount, slowly add the prescribed amount of F127 and F68 under stirring conditions, add isotonic phosphate buffer To a sufficient amount, store in cold storage at low temperature to fully swell until a clear and uniform solution is formed.

Embodiment 2

[0079] Embodiment 2 Preparation of gatifloxacin thermosensitive ophthalmic gel

[0080] 【Prescription】Gatifloxacin 0.3g

[0081] Brogeramine (Benzalkonium Bromide) 0.02g

[0082] F127 21.4g

[0083] F68 9.6g

[0084] NaCl 0.9g

[0085] Add distilled water to the full amount of 100g

[0086] [Preparation method] Dissolve gatifloxacin, 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

[0087] Embodiment 3 Preparation of gatifloxacin temperature-sensitive ophthalmic gel

[0088] 【Prescription】Gatifloxacin 0.15g

[0089] Brogeramine (Benzalkonium Bromide) 0.02g

[0090] F127 21.4g

[0091] F68 9.6g

[0092] Mannitol 5g

[0093] Add distilled water to the full amount of 100g

[0094] [Preparation method] Dissolve gatifloxacin, bromogeramine, 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.

technical field

[0001] The present invention relates to a new dosage form of ophthalmic medicine, which is a solution in a non-physiological state, and the preparation and application of a gel in a physiological state. Specifically, it is sensitive to temperature and pH of gatifloxacin (abbreviated as GAT). Preparation method and clinical indication of ophthalmic gel. The preparation greatly prolongs the residence time of the drug in the eyes, improves the bioavailability, improves the curative effect, and has an ideal application prospect. Background technique

[0002] The gatifloxacin ophthalmic preparations currently on the market are mainly eye drops. There are eye ointment and eye gel in preparation. Among them, after the eye drops are used, due to eyelid blinking and tear dilution, the eye drops are quickly eliminated through the nasolacrimal duct, and their bioavailability is often less than 1%. It is necessary to increase the number of administrations to maintain t...

Examples

Embodiment 1

[0072] The preparation of embodiment 1 gatifloxacin thermosensitive ophthalmic gel

[0073] 【Prescription】Gatifloxacin 0.3g

[0074] Brogeramine (Benzalkonium Bromide) 0.02g

[0075] F127 21.4g

[0076] F68 9.6g

[0077] Add isotonic phosphate buffer (pH7.4) to the full amount of 100g

[0078] [Preparation method] Dissolve gatifloxacin and bromogeramine in 60% sterile isotonic phosphate buffer (pH7.4) in the prescribed amount, slowly add the prescribed amount of F127 and F68 under stirring conditions, add isotonic phosphate buffer To a sufficient amount, store in cold storage at low temperature to fully swell until a clear and uniform solution is formed.

Embodiment 2

[0079] Embodiment 2 Preparation of gatifloxacin thermosensitive ophthalmic gel

[0080] 【Prescription】Gatifloxacin 0.3g

[0081] Brogeramine (Benzalkonium Bromide) 0.02g

[0082] F127 21.4g

[0083] F68 9.6g

[0084] NaCl 0.9g

[0085] Add distilled water to the full amount of 100g

[0086] [Preparation method] Dissolve gatifloxacin, 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

[0087] Embodiment 3 Preparation of gatifloxacin temperature-sensitive ophthalmic gel

[0088] 【Prescription】Gatifloxacin 0.15g

[0089] Brogeramine (Benzalkonium Bromide) 0.02g

[0090] F127 21.4g

[0091] F68 9.6g

[0092] Mannitol 5g

[0093] Add distilled water to the full amount of 100g

[0094] [Preparation method] Dissolve gatifloxacin, bromogeramine, 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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