Tablet giving rapid release of nicotine for transmucosal...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C424S434000, C424S435000, C424S464000, C424S466000, C424S468000, C424S471000, C424S472000, C424S474000, C424S682000, C424S686000, C424S687000, C424S688000, C424S692000, C514S769000, C514S810000, C514S813000, C514S819000, C514S960000

Reexamination Certificate

active

06248760

ABSTRACT:

BACKGROUND
1. Field of Invention
The present invention relates to a tablet for transmucosal administration of a medicament. Specifically, it relates to a tablet that will give a rapid release of nicotine.
2. Description of Prior Art
Nicotine is the most widely distributed of the plant alkaloids. It occurs in two separate phyla of the plant kingdom, Pteridophytes and Spermatophytes. Despite its wide distribution, for practical purposes, nicotine is obtained from the
tabacum
and
rustica
species of the Nicotina genus. However, it is interesting that Australian Aboriginal people chewed “pituri”, a nicotine preparation made from
Duboisia hopoodi.
Nicotine can be isolated as an oily, volatile base with a sharp burning taste. Nicotine will form acid salts with most acids. Nicotine can be introduced into the body in many ways. The most popular way is by smoking cigarettes. When a cigarette is smoked, the partial oxidation of the tobacco causes the vaporizing of some of the nicotine. The nicotine vapor as well as nicotine adsorbed on partial oxidation products of the cigarette is quickly absorbed through the lungs. A dozen beats of the heart can carry nicotine from the lungs to the brain in less than 20 seconds.
Smoking cigarettes introduces many undesirable materials into the person smoking, as well as into the environment. Because of this, most smokers would like to quit smoking. However, a craving for nicotine, irritability, restlessness, difficulty in concentrating, headaches, an increase in weight, and anxiety often follow cessation of smoking. Supplying nicotine in an alternative way has been helpful in some cases of those wishing to quit smoking. Several alternative ways of delivering nicotine have been proposed.
Pomerleau (Psychopharmacology 1992, 108, 519-526) listed some of the criteria that should be met for an alternative nicotine dosing method to be considered satisfactory: 1) the method should be safe and easy to use; 2) specified doses should be accurately and reproducibly delivered; and 3) the pharmacokinetics should resemble those of cigarette smoking. The following is a review of the major alternative nicotine dosing methods and their drawbacks, i.e., how they fail or meet these criteria.
Frith (Life Sciences, 1967, 6, 321-326) described experiments where tablets containing 0.1 mg of nicotine were administered orally. The subjects were instructed to chew the tablets until the tablets were dissolved. These tablets had the nicotine distributed uniformly throughout the tablets. The pharmacokinetics did not resemble those of cigarette smoking.
Lennox M. Johnston and M. D. Glasg in the Dec. 19, 1942 edition of Lancet, p.742, described intravenous injection of nicotine. They reported that after several injections, an injection was preferred to a cigarette. Intravenous injection has continued to be used in scientific experimentation. See for example Lucchesi et al. (Clin. Pharm. Ther., 1967, 8, 789-96), Soria et al. (Psychopharmacology 1996, 128, 1000-1005), Benowitz et al. (J. of Pharmacol. Exp. Ther. 1990, 254, 1000-1005), and Rosenberg et al. (Clin. Pharmacol. Exp. Ther. 1980, 28, 516-22). However, intravenous injection is obviously not a suitable replacement for smoking in most situations.
Jarvik et al. (Clin. Pharm. Ther. 1970,11, 574-576) described experiments where 10 mg tablets of nicotine tartrate were swallowed at two hour intervals by several subjects. The idea was that although the ionic form of nicotine would not be absorbed in the stomach, it would be absorbed in the intestine. However, most of the nicotine absorbed in the intestine is metabolized by the liver before it reaches the nervous system. The large amounts of nicotine in these experiments, as compared with about 1 mg available in a cigarette, had only a small effect. (Actually the abstract of this paper states that 10 mg of nicotine tartrate per kilogram was administered, but this is an obvious error.) The pharmacokinetics of swallowed nicotine did not resemble smoking.
Wesnes and Warburton (Psychopharmacology, 1984, 82, 147-150) described experiments where nicotine was added to dextrose tablets. They also (Psychopharmacology, 1986, 89, 55-59) used nicotine absorbed in magnesium hydroxide pills. In their experiments they covered the taste of nicotine with hot pepper sauce. The sauce is acidic. Travel (Ann. New York Ac. Sc., 1960, 80, 13-32) had found that nicotine is more readily absorbed in its base form rather than as its acid salts. Beckett et al. (J. of Pharmacy and Pharmacology, 1971, 24, 115-120) had found that solutions of nicotine were more rapidly absorbed in the buccal cavity if they had an alkaline pH. Under the conditions of the experiments by Wesnes and Warburton, the alkaline reaction of the basic magnesium hydroxide would be useful. In the experiments of Wesnes and Warbuton a dilute nicotine solution was allowed to soak into the dextrose or magnesium hydroxide pills. The subjects were requested to hold the pills in their mouths for 5 minutes before swallowing. The described pills did not give a rapid release of nicotine.
Shaw (U.S. Pat. No. 4,806,356, 1989) described a lozenge made by compression molding with nicotine distributed uniformly throughout. Shaw's lozenges will slowly release nicotine. Santus (U.S. Pat. No. 5,549,906, 1996) described nicotine-containing lozenges where the nicotine is uniformly distributed through a nonnutritive sweetener and an absorbent excipient. Santus discussed how the administration of nicotine is obtained by allowing the lozenge to completely dissolve in the mouth. Several nicotine lozenges have been commercialized and are available as over-the-counter products in the U.K. These contain 0.5 mg nicotine distributed uniformly throughout the lozenges. The pharmacokinetics of these methods of dosing is not like smoking.
Sahakian et al. (Brit. J. Psychiatry, 1989,154, 797-800) described using a subcutaneous injection of nicotine. While of possible use in scientific studies, this does not fill the need for the usual smoker. Under some conditions, such an injection can cause severe muscular irritation.
The absorption of drugs such as nitroglycerin and scopolamine through the skin is a common occurrence. The absorption of nicotine through the skin has also long been known. Workers coming into physical contact with dew on tobacco leaves can develop what is called “green tobacco sickness”. See for example Gehlbach et al. (J.A.M.A., 1974, 229, 1880-1883). The transdermal administration of nicotine has been the subject of many patents. For example, Baker et al. U.S. Pat. No. 4,839,174, 1989, U.S. Pat. No. 4,943,435, 1990, and U.S. Pat. No. 5,135,753, 1992. The commercial products based on these patents have turned out to be quite expensive. More importantly, the patches give a rather constant level of nicotine in the blood. Transdermal nicotine patches have another disadvantage in that it is difficult to administer nicotine at the rate required by different subjects. Benowitz et al. (J. Pharmacol. Exp. Ther., 1982, 21, 368-373) and Feyerabend et al. (Brit. J. Clin. Pharmacol. 1985, 19, 239-249) have found that there are up to four-fold variations in the rate nicotine is eliminated by smokers. It is also advantageous for users to be able to vary dosage to cope with times of intense craving.
Nicotine chewing gum is another way of administering nicotine. Ellis et al. (U.S. Pat. No. 865,026, 1907) provides an early example. More recent examples are Ferno et al. (U.S. Pat. No. 3,845,217, 1974) and Lichtneckert et al. (U.S. Pat. No. 3,877,468, 1975 and U.S. Pat. No. 3,901,248, 1975). Products of these patents are now being marketed on an international scale. These products combine a nicotine-containing cation exchange resin complex in a gum base. However, chewing gum is not socially acceptable in some circumstances. Some users of nicotine gum have complained about the effort required to chew it. Many users complain about the taste. The pharmacokinetics are different than smoking.
Much has been learned in recent years. Russell (Nicotine Replacement: A Critical

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