Methods for treating pruritus
An anti-pruritic and drug technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc.
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Embodiment 1-3
[0214] Three sustained release delivery systems were prepared by dry blending xanthan gum, locust bean gum, calcium sulfate dihydrate, and mannitol in a high speed mixer / granulator for 3 minutes. While the chopper / impeller was running, the dry blend was sprayed with water and regranulated for 6 minutes. The granulation process was then stopped and the mixer / granulation disk removed. While running the chopper / impeller, mix the granules for an additional 1 minute. After checking the consistency of the granules, while running the chopper / impeller, add additional water to the granules and re-granulate for 3.5 minutes. The granules are then dried to a LOD (loss on drying) of less than about 4 wt%. The granules were then ground using a No. 1521-0033 sieve. The relative amounts of the ingredients are listed in Table 1.
[0215] Table 1
[0216]
[0217]
Embodiment 4-7
[0219] A series of tablets containing different amounts of gum were prepared using the sustained release delivery system of Example 3. The amounts of ingredients per tablet are listed in Table 2.
[0220] Table 2
[0221]
[0222] Tablets are prepared by mixing nalbuphine and the sustained release delivery system in a mixer. The magnesium stearate was passed through a #30 mesh separator screen and then mixed with the dry blend containing nalbuphine and the sustained release delivery system. The lubricated blend was compressed using the dies specified in Table 2 to yield tablets with the indicated total weight.
[0223] The tablets of Examples 4-7 were tested for in vitro % release rate according to USP Procedure Drug Release General Chapter Dissolution using an instrument USP Type III / 250 mL. The test was performed in 100 mM ammonium phosphate buffer at pH 6.8, 37°C. / 15 dpm (dips per minute). The results are shown in Table 3.
[0224] table 3
[0225]
[0226] ...
Embodiment 8-10
[0228] A series of tablets containing different amounts of gum and different sustained release delivery systems were prepared using the sustained release delivery systems of Examples 1 and 2. The amounts of ingredients per tablet are listed in Table 4.
[0229] Table 4
[0230]
[0231] Tablets were prepared by first mixing nalbuphine with the sustained release delivery system in the mixer of example 8 and in the high shear granulator of examples 9 and 10. For Examples 9 and 10, the blend was then granulated with water until consistent granules were obtained, followed by drying in a fluid bed dryer at 70°C for 30 minutes. The dried granules were then passed through a Fitzmill using a 1521-0050 sieve at 2500 rpm. Magnesium stearate was passed through a #30 mesh screen, then mixed with the pulverized granules of Examples 9 and 10 and with the dry blend of Example 8 for 5 minutes. The lubricated blend was compressed using the dies specified in Table 4 to yield tablets with ...
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