Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-09-13
2003-04-22
Padmanabhan, Sreeni (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S290000, C514S299000
Reexamination Certificate
active
06552035
ABSTRACT:
TECHNICAL FIELD
This invention relates to a composition for inducing smoking cessation comprising as active ingredient alkaloids from
Radix ipecauanhae.
More specifically, it relates to a composition comprising as active ingredient basic alkaloid fraction from
Radix ipecauanhae
or basic emetine, optionally in combination with one or more auxiliary agents selected from
Nicotiana tabacum,
Fructus Phyllanthus emblica,
Herba adenophorae, Herba leonuri, Herba foeniculi, Folia valerianae, Herba centellae
or
Circii herba.
The invention also provides a method for using the same.
BACKGROUND ART
Nicotiana tabacum
contains harmful ingredients to human body such as nicotine, tar, dioxin and the like in large quantities. It is a one's favorite known to increase incidence of diseases related lung and cancers through long-term smoking. Various kinds of smoking cessation medicines or aids have been hitherto developed for smoking cessation. However, they have frequently adverse effects on human body or fail to successfully induce smoking cessation. Accordingly, it is absolutely needed to develop more efficient smoking cessation method or smoking cessation aid.
Radix ipecauanhae,
as emetic, has been used for detoxification and the treatment of dysentery, and used as expectorant, depending upon its dosage (Deutsches Arzneibuch, British Herbal Pharmacopoeia, Gerhardt Madaus's Lehrbuch der Biologischen Heilmittel, Georg Olms 1976). However, it has never been used for inducing smoking cessation.
DISCLOSURE OF THE INVENTION
The present inventors carried out extensive studies to develop a novel efficient smoking cessation composition. As a result, they found that basic alkaloid fraction from
Radix ipecauanhae
of its constituent emetine can efficiently induce smoking cessation after various clinical trials and thus, completed the present invention.
Accordingly, a purpose of the present invention is to provide a composition for inducing smoking cessation comprising basic alkaloid fraction from
Radix ipecauanhae
or emetine as active ingredient.
Another purpose of the present invention is to provide the composition comprising basic alkaloid fraction from
Radix ipecauanhae
or emetine as active ingredient for smoking cessation, in combination with one or more selected from
Nicotiana tabacum,
Fructus Phyllanthus emblica,
Herba adenophorae, Herba leonuri, Herba foeniculi, Folia valerianae, Herba centellae
or
Circii herba.
In the composition of the present invention, alkaloid extract from
Radix ipecauanhae
(root of
Cephaelis ipecacuanha
), an emetic, is used as active ingredient.
Radix ipecauanhae,
one species of Rubiaceae, is known as emetic and anti-dysentery.
Radix ipecauanhae
contains 1.9-2.1% of total alkaloids (Deutsches Arzneibuch 9, Edition 1986; British Herbal Pharmacopoeia 1979). Emetine (6,7,10,11-tetramethoxyemethan) and cephaelin are main ingredients in the alkaloid fraction. In the present composition, ipecac extract is used in the form of basic alkaloid fraction or emetine.
A mechanism that emetine will induce vomiting is as follows: it stimulates gastrointestinal system thereby to transduce signal to 5-HT
3
(5-hydroxytryptamine-receptor) in chemo-receptor trigger zone of area postremia and solitary tract nucleus. Subsequently, the transduced signal stimulates vomiting center in Medulla oblongota and then, passes through nervus vagus, phrenic nerve and abdominal muscular nerve to reach nausea followed by vomiting (Goodman & Gilman, The Pharmacological Basis of Therapeutics, 9th Edition, 1996).
Alkaloids in
Radix ipecauanhae
are usually in the form of salt with acid and commercial emetine is emetine hydrochloride. If smoking this salt as is, acidic moiety will transform to gaseous acid to have harmful effects on oral cavity, bronchus and lung, etc. In particular, hydrochloride may react with herbal aromatic compounds, especially, phenol and phenolic compounds, which are secondarily formed during combustion, to form poisonous dioxins. Therefore, in the present composition, ipecac alkaloid salt or salt of emetine should be converted into basic alkaloid before its use.
For conversion of salt into base, conventional alkaloid extraction method may be employed. That is, in the present invention, general alkaloid fractionation method is used for obtaining fraction, which contains mainly basic alkaloids. Specifically, the given amount of ipecac powder is degreased with hexane, and to the residual plant are added alkalis such as ammonium to basify. Subsequently, the resulting solution is extracted with water-immiscible solvent such as ether, etc. The obtained fraction contains 70-80% of total alkaloids. Further, emetine hydrochloride is dissolved in water and then, extracted with water-immiscible solvent such as ether, etc. to obtain emetine.
Generally, a daily dose of emetine for the halt of coughing and for the discharge of phlegm ranges about 1.0-1.5 mg of emetine hydrochloride. The daily dose of
Radix ipecauanhae
for the same purpose ranges about 0.03-0.15 g, and a single dose thereof for vomiting ranges about 0.5-1.0 g. In the present invention, it is important to adapt the dosage for inducing smoking cessation. That is,
Radix ipecauanhae
contained in the present composition has the practical purpose of nauseating rather than of vomiting and thus, vomiting is conversely regarded as an adverse event. In view of the fact that a single dose of
Radix ipecauanhae
for vomiting is 0.5-1.0 g, its amount for smoking cessation would be lesser than 0.5-1.0 g. Synergic effect with nicotine as described hereunder can lead to remarkable reduction of the inhalation amount of
Radix ipecauanhae
, i.e. alkaloids therefrom. In the present invention, ipecac alkaloid is preferably contained at 0.01 to 2 wt %, more preferably, 0.05 to 0.3 wt %, as basic alkaloid fraction, on the basis of the total weight of the composition. In another aspect, emetine, if employed as active ingredient, is preferably contained at 0.005 to 0.5 wt %, more preferably 0.005 to 0.15 wt %, on the basis of the total weight of the composition. In the present composition, nicotine, if employed as excipient, is contained at the residual amount excluding the active ingredient. For example, in case that the total weight of the composition is 100 g and the content of ipecac alkaloid is 2000 mg, 98 g of tobacco leaf is preferably added thereto.
If desired, the composition of the present invention may contain tobacco leaf having nicotinic ingredient. In the present composition, the tobacco leaf may not only function as excipient but also provide properties inherent in tobacco. Nicotine has complicated and unexpectable mechanism. It functions on various nerve transfer systems and further, stimulates or desensitizes receptor depending upon its dosage. Usually, nicotine inhaled into the body through smoking does not lead to desensitization, but causes stimulation and excitation of receptor. Nicotine displays vomiting effect via the same mechanism as emetine. Mechanism of vomiting in nicotine is as follows: It stimulates vomitive chemo-receptor trigger zone of area postremia in medulla oblongata thereby to activate vagal and spinal afferent which receive vomiting and reflex thereby to promote vomiting.
From the fact that emetine and nicotine pass through many common afferent areas through their reaction mechanism, these two substances are anticipated to have synergic or additive effect. Nicotine in the form of tobacco leaf may be comprised in the present composition at a conventional amount as excipient for the manufacture of tobacco. For example, in case that the total weight of the composition is 100 g and the content of emetine is 500 mg, 99.5 g of tobacco leaf may be contained. Such content of nicotine is sufficient for exhibiting synergic or additive effect.
A further aspect of the present invention is to provide a composition for inducing smoking cessation comprising smokable herbal materials instead of tobacco leaf. In this composition, as the bulk of herbal materials,
Herba adenophorae, Herba cente
Ahn Byung-Zun
Park Hwa-Mok
Birch & Stewart Kolasch & Birch, LLP
Hwa-Mok Park
Jiang S.
Padmanabhan Sreeni
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