Adapalene vesicle and its preparation and preparation method
A technology of vesicles and preparations, applied in anti-inflammatory agents, pharmaceutical formulations, aerosol delivery, etc., which can solve problems such as skin allergies, adverse reactions, and poor transdermal effects
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[0093] 1.1 Preparation of mouse skin
[0094] SD male rats, 240-260g, were sacrificed by decapitating the cervical vertebrae. The hair on the abdomen and surrounding areas was removed with a razor, and the whole rat skin of the depilated part was peeled off with dissecting scissors, and placed in normal saline to stretch out (need 2-3min), use the filter paper to spread the mouse skin naturally, place the upper cover of the transdermal cup on the peeled skin, cut the mouse skin together with the filter paper (to ensure the natural shape of the mouse skin) and cut it out of the transdermal cup Put the small disc with a slightly larger layer into the prepared normal saline, cut off the fat tissue and mucosal tissue in the inner layer of the mouse skin with ophthalmic curved scissors (you can also scrape it with a blade), and the treated mouse skin Wash it with normal saline, store it in a watch glass filled with filter paper moistened with normal saline, wrap it with plastic wra...
Embodiment 1
[0117] Take adapalene 7.5mg, Span 60 45mg, polyethylene glycol monostearate 225㎎, sodium stearate 37.5㎎, cholesterol 131.25mg, add it to an appropriate amount of 95% ethanol, and heat it in a water bath at 85°C. After it is completely dissolved, inject it into an appropriate amount of water, stir at a constant temperature of 85°C for 30 minutes, lower the temperature to 55°C and continue stirring for hydration, evaporate the ethanol, add water to the prescribed amount, and shake well to obtain a vesicle suspension.
[0118] Carbomer 980 100㎎ add water to swell, ethyl paraben 10㎎ is dispersed with 1000㎎ 10% glycerin, anhydrous sodium sulfite 50㎎ is dissolved in water, all are added to Carbomer 980, swell together overnight, add appropriate amount of hydrogen The pH of the sodium oxide solution was adjusted to 7.3 to obtain a gel matrix.
[0119] Mix the vesicle suspension with the gel matrix and stir evenly to obtain the vesicle gel.
Embodiment 2
[0121] Take Span 80 50㎎, Tween 60 100㎎, Cholesterol 100㎎, Adapalene 0.5㎎ dissolved in an appropriate amount of dichloromethane, heated to dissolve, and the solution is ready for use; under constant temperature stirring at 15°C, take the above solution and inject it into tartaric acid buffer at a constant speed solution (pH7.2), continue stirring after adding, until dichloromethane evaporates, add tartrate buffer solution (pH7.2) to the full amount, and process once with a high-pressure milk homogenizer to obtain a vesicle suspension.
[0122] Carbomer 971 10㎎ add water to swell, benzyl alcohol 80㎎ use 1800mg hyaluronic acid: isopropanol (1:2) mixture to disperse, tert-butyl p-hydroxyanisole 15㎎ add water to dissolve, all add to carbomer Mu 971, co-swell overnight, add an appropriate amount of sodium hydroxide solution to adjust the pH to 7.2, to obtain a gel matrix.
[0123] Mix the vesicle suspension with the gel matrix and stir evenly to obtain the vesicle gel.
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