Note: Descriptions are shown in the official language in which they were submitted.
2129919
FIZ 0101 PCA
PHARMACEUTICAL COMPOSITION HAVING
ANTmRAL AND ANTIBACTERIAL ACTIVITY
AND METHOD OF ADMINISTRATION
Technic~l Field
The present invention relates to a composition
of matter for general immunostimulation. More particu-
larly, the present invention relates to a novel composi-
tion that is particularly adapted for the treatment of
a variety of selected amounts of chlorambucil, procarb-
azine and cyclophosphamide. Melphalan and liothyronine
are principal options. Calcium may be included as a
supplement.
Back~round Art
A method of stimulating the body's immunologic
system in response to various pathogens has been sought
by researches for some time. While various pharmaceuti-
cal drugs have proven effective against bacteria, ideal
responses to such pathogens are wanting. Effective
responses to viral infection are even less available.
Particularly, those bacterial and viral
infections that manifest themselves in diseases such as
pneumonia, pneumonitis, chronic purulent bronchitis,
bronchiectasis, different viremias, and other diseases
of bacterial or viral etiology are ideal targets for
such immunostimulation.
The common strand giving strength to these
various diseases is a compromised immune system. In
response, and to overcome the effects of these patho-
-
z ~ ~99 ~ 9
gens, two possible routes can be taken. The first is to
introduce antibacterial and antiviral agents into the
blood of the afflicted person, thereby bypassing the
person's own immune system. This course has the com-
bined advantages of directness and efficiency, butsuffers from negative side effects to the body of the
host.
The second method is directed to stimulating
the host's immunological system to fight the pathogen.
This method is desired because it minimizes the risk of
side effects. This method is also preferred because it
allows the host's natural processes to act against the
pathogen, thereby eliminating the need to fight the
toxin directly and rendering unnecessary the introduc-
tion of chemical agents that may secondarily harm thebody while fighting the disease.
However, the processes involved in immuno-
stimulation have not been as well-studied as agents to
directly disable bacteria and viruses, and methods of
stimulating the body's own defense system are not well
known. Accordingly, effective immunostimulating compo-
sitions do not exist for overcoming the above-noted
dlseases .
S-lmm~ry Of The Invention
The present invention is directed to a compo-
sition of matter useful for general immunostimu-
lation. More particularly, the present invention
relates to a novel composition that is particularly
adapted for the treatment of a variety of bacterial and
viral diseases.
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3 71087-374
The immunostimulating composition of the present
invention comprises a multi-component formula. The result is a
pharmaceutical product that includes quantities of chlorambucil,
procarbazine and cyclophosphamide. Preferably, the active
components are contained in a non-homogeneous pharmaceutically
acceptable matrix. Two other components, melphalan and
liothyronine, are principal options. Calcium is a preferred
part of the product as a supplement.
When the components are in the non-homogeneous matrix,
each component is released from the matrix separately by means
of a time release mechanism one by one with proper timing and
according to a selected sequence.
Normally, chlorambucil, melphalan, procarbazine and
cyclophosphamide are indicated as being cyto-toxic and
immunosuppressing. However, the observed positive results of
the composition according to the present invention contradict
the conventional wisdom regarding these chemicals. In the
combination according to the quantity ranges specified and in
the prescription of the present invention, these chemicals have
the opposite effect.
- Administration of the formula is followed by and
coupled with a specific dietary and work regimen comprising, for
the most part, rest. While not a vaccine in the traditional
sense, the effects of the administration of the composition
according to the prescribed plan appear to mimic a vaccine.
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Detailed Description of the Preferred Embodiments
As briefly noted, two options are principally
available in fighting bacteria or viruses. The patho-
gens can be attacked directly by antibacterial or
antiviral drugs, or the body's immune system can be
stimulated to respond by producing antibodies to attack
the foreign bodies.
The present invention is directed to a pharma-
ceutical composition that follows the latter course by
stimulating the production and proliferation of antibod-
ies from lymphocytes and other components of the immune
system.
The composition of the present invention is
directed to the activation of deficient immune systems
to overcome difficult or poorly managed diseases. The
composition of the present invention includes, as its
basic ingredients, chlorambucil, procàrbazine HCL and
cyclophosphamide. Melphalan and liothyronine Na are
principal options and, when included, assure optimum
results and hastened improvement. Calcium is a pre-
ferred supplement as it provides many known advantages.
The components are known and are readily
available. Particularly, chlorambucil is a nitrogen
mustard derivative that is slightly soluble water and is
often used in medicines. Procarbazine is well-known by
oncologists as an anti-cancer drug.
Cyclophosphamide is an alkylating agent. It
is also a known anti-cancer drug. Melphalan (the
generic name for the hydrochloride) is also a nitrogen
mustard and is similarly used in medicines. Like
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FIZ 0101 PCA -5-
cyclophosphamide, melphalan is an alkylating agent.
Liothyronine is an iodothyronine hormone.
Calcium is an essential component of bones and
teeth. It is provided as a optional component, although
it is noted that too much of this component (beyond the
amounts recommended herein) results in a compromise of
the effects of the present composition.
In its preferred embodiment, the pharmaceuti-
cal composition of the present invention includes the
above-described components according to the following
approximate ranges:
Chlorambucil - 0.1 - 1.0 mg
Procarbazine HCL - 2.0 - 25.0 mg
Cyclophosphamide - 2.0 - 25.0 mg
Melphalan - 0.1 - 1.0 mg
Liothyronine Na - 1.5 ~g - 25.0 ~g
Calcium - 200.0 mg - 2000.0 mg
Preferably provided in a capsule, the individ-
ual components are mixed, but are provided in a matrix
whereby there is no chemical interaction between them.
An inert bonding agent may be used to maintain the
separation of the components.
For optimum effect, the components of the
present composition are released by conventional time-
release means according to a preselected schedule even
though the components are combined in the capsule.
Following ingestion, the following release schedule is
preferred:
Chlorambucil - within 2-4 hours after ingestion
Melphalan - after 6-8 hours
Procarbazine HCL - after 9-12 hours
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FIZ 0101 PCA -6-
Cyclophosphamide - after 12 hours
Liothyronine and calcium are released at any
time after ingestion. As noted, the release of the
components according to the preferred schedule is made
by conventional time-release mechanisms.
The preferred dosage is one treatment per day.
If all the ingredients are provided in one capsule or
tablet, then the dosage is once a day. Conversely, if,
for example, chlorambucil and melphalan are provided in
one capsule and procarbazine and cyclophosphamide are
provided in another, one dose of each per day is the
appropriate regimen. This latter procedure requires the
user to take the second dose at an appropriate time
interval after the first in accord with the preferred
release schedule. The conventional time release mecha-
nism is altered accordingly. The forms of the dosages
(that is, capsule, tablet, pill) are differentiated by
numerical or alphabetical markings, size or color.
This preferred dosage is administered between
eight and ten days. ~mi ni stration should begin at the
earliest sign of disease. During administration,
alcohol, cigarettes, corticosteroids and anti-flammatory
agents are avoid. Spicy foods are also avoided during
the treatment period. Other antibacterial or antiviral
medications may be taken concurrently unless contraindi-
cated by known undesirable interactions.
After the composition of the present invention
begins to stimulate the immunologic system, tolerance to
alcohol improves. Results vary according to the age of
the patient and the stage of the disease.
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7 71087-374
Once properly administered, the pharmaceutical
composition of the present invention typically provides the
patient with three to six months' protection against infectious
diseases. Unless otherwise indicated, failure of the
composition to produce the desired results can be corrected by
the readministration of the composition in the same dosage and
according to the same schedule as set forth above. Care should
be taken on subsequent administration to verify that no agents
are taken that would compromise the effectiveness of the
composition as noted above.
The pharmaceutical composition of the present
invention embodies the unique ability to stimulate in vivo the
production and proliferation of antibodies. Application of this
composition either alone or in conjunction with other antibiotic
or antiviral therapy appears likely to markedly reduce morbidity
and mortality rates due to infectious agents and prevent
complications due to chronic intractable infections.
As well known in the art, the pharmaceutical
composition of the present invention may be put in commercial
packages for practical use. Such commercial packages usually
carry instructions or indications that the pharmaceutical
composition should or can be used for the purposes disclosed in
this specification.
Example
As discussed, the pharmaceutical composition of the
present invention includes, as its base ingredients,
chlorambucil, melphalan, procarbazine HCL and cyclophosphamide.
According to the present and preferred example, the composition
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included 0.4 mg chlorambucil, 0.4 mg melphalan, 10.0 mg
procarbazine HCL and 10.0 mg cyclophosphamide. The primary
optional component liothyronine Na was provided in the amount of
10.0 ~g. Calcium was provided in the amount of 800.0 mg.
The invention thus being described, it will be obvious
that the same may be varied in many ways. Such
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FIZ 0101 PCA -8-
variations are not regarded as a departure from the
spirit and scope of the invention, and all such modifi-
cations are intended to be included within the scope of
the following claims.
