Bemeprost ophthalmic temperature-sensitive in-situ gel as well as preparation method and application thereof
A bimatoprost and ophthalmic technology, which is applied in the field of medicine, can solve the problems of no ophthalmic temperature-sensitive in-situ gel preparations, etc., to overcome poor spreadability, solve short residence time, and avoid eye irritation sexual effect
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Embodiment 1
[0057] Formula (by mass volume percent):
[0058]
[0059] Preparation process: accurately weigh bimatoprost powder, add it into Tween 80 for ultrasonic dissolution, and then add double distilled water to prepare a bimatoprost solution with a concentration of 0.03%. Then add poloxamer 407 and poloxamer 188 into the bimatoprost solution according to the above ratio, seal it and put it in a refrigerator at 4°C for 24 hours to make it fully absorb water and swell and gradually dissolve until the solution is clear to obtain bimatoprost A thermosensitive in-situ gel for ophthalmic use.
[0060] Determination of gelation temperature: take 4°C bimatoprost thermosensitive in situ gel and place it in a test tube (uniform heating, large heating area, good spatial fluidity), place the test tube in a beaker inserted into an electronic thermometer and heat it with a water bath way, at 0.5℃·min -1 Slowly raise the temperature of the water-bath beaker at a rate of 10 s, and tilt the tes...
Embodiment 2
[0064] Formula (by mass volume percent):
[0065]
[0066] Preparation process: accurately weigh bimatoprost powder, add it into Tween 80 for ultrasonic dissolution, and then add double distilled water to prepare a bimatoprost solution with a concentration of 0.03%. Then add poloxamer 407 and poloxamer 188 into the bimatoprost solution according to the above ratio, seal it and put it in a refrigerator at 4°C for 24 hours to make it fully absorb water and swell and gradually dissolve until the solution is clear to obtain bimatoprost A thermosensitive in-situ gel for ophthalmic use.
[0067] The determination of the gelation temperature was the same as in Example 1. The gelation temperature of the bimatoprost ophthalmic thermosensitive in-situ gel prepared in this example was about 32.16±0.127°C before dilution with artificial tears, and the gelation temperature after dilution with artificial tears The condensation temperature is about 37.54±0.366°C.
Embodiment 3
[0069] Formula (by mass volume percent):
[0070]
[0071]
[0072] Preparation process: accurately weigh bimatoprost powder, add it into Tween 80 for ultrasonic dissolution, and then add double distilled water to prepare a bimatoprost solution with a concentration of 0.03%. Then poloxamer 407 and poloxamer 188 were added to the bimatoprost solution according to the above ratio, sealed and placed in a refrigerator at 4°C for 24 hours to allow it to fully absorb water and swell and gradually dissolve until the solution was clear to obtain bimatoprost A thermosensitive in-situ gel for ophthalmic use.
[0073] The determination of the gelation temperature was the same as in Example 1. The gelation temperature of the bimatoprost ophthalmic thermosensitive in-situ gel prepared in this example was about 31.15±0.375°C before dilution with artificial tears, and the gelation temperature after dilution with artificial tears The condensation temperature is about 37.12±0.311°C.
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