Oral Antagonist Compositions For Nicotine Burning Relief

[0334]Oral Analgesic Compositions with or without Nicotine

TABLE 1Oral analgesic compositions. Amounts of raw materials are given in mg.(25-01)(25-02)(34-06)(34-04)(34-02)(25-07)Nicotine API*3.096.18————Na2CO35.010.0————Eucalyptol——10.0———Oleic Acid———10.0——Camphor————2.0—WS-12—————2.0Mannitol76.9168.8271.071.085.587.0Crospovidone8.08.07.57.57.57.5Syloid——10.010.00.5—Micro-5.05.0———2.5crystallinecellulose (MCC)Magnesium2.02.0————StearateSodium Stearyl——1.51.54.51.0FumarateTotal100.0100.0100.0100.0100.0100.0*The nicotine API used contains 32.4% nicotine implying that a formulation with 3.088 mg API contains 1 mg of nicotine

[0335]Examples of specific raw materials used in the table are as follows:

[0336]Nicotine may eg be nicotine bitartrate dihydrate (NBT)

[0337]Eucalyptol may eg be Eucalyptol Nat available from Symrise

[0338]Oleic acid may eg be NF-LQ-(MH) available from Croda Inc

[0339]Camphor may eg be Camphor USP available from Rochem International Inc

[0340]WS-12 may eg be Symcool WS-12

[0345]Fast Dissolving Tablets (FDT) with or without Nicotine

[0346]Fast disintegrating tablets (FDT) were prepared based on the compositions of Example 1. The tablets were prepared as follows:

[0347]Raw materials are weighed from bags or buckets into separate weighing containers. For formulations using Syloid, a premix is made by mixing Eucalyptus and Syloid XDP 3050, Camphor and Syloid 244 FP or Oleic acid and Syloid 244 FP respectively.

[0348]All excipients are sifted through an 800-micron sieve into a stainless steel or plastic bin in the following order:[0349]Half the filler / bulk sweetener[0350]The nicotine (if included) and all other excipients including premix, except magnesium stearate and sodium stearyl fumarate[0351]The remaining half of the filler / bulk sweetener

[0352]These are mixed in a Turbula mixer for 4-10 minutes at 25 RPM. Then lubricant, eg. magnesium stearate is sifted through an 800-micron sieve into the mixing bin, and the lubrication is conducted by additional mix

[0356]Preparation of Samples for Testing

[0357]Samples were prepared based on the tablets from Example 2.

[0358]Tablets with a content of nicotine (25-01) and (25-02) were evaluated in a sensory panel and used as standards for nicotine irritation under the tongue, in the oral cavity and in the throat. These samples were applied in test conditions in a weight of 100 mg, corresponding to the weight of the tablets of Example 2.

[0359]Additionally, tablets without a content of nicotine (34-06), (34-04), (34-02) and (25-07) were combined with the nicotine tablets (25-01) and (25-02) in various configurations.

[0360]In some configurations, one of each of these tablets without nicotine was combined with one of the nicotine tablets to give samples of a nicotine tablet and a single antagonist tablet for evaluation in a sensory panel for nicotine irritation under the tongue, in the oral cavity and in the throat.

[0361]In some other configurations, two of each of these tablets without nicotine were co