Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2000-02-23
2001-09-11
Davenport, Avis M. (Department: 1653)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C514S012200, C514S021800, C424S184100, C424S185100
Reexamination Certificate
active
06288026
ABSTRACT:
FIELD OF INVENTION
The present invention relates to a process and composition for the treatment of various diseases with an oil-in-water emulsion.
BACKGROUND
U.S. Pat. No. 5,904,925 describes an oil-in-water emulsion as an incomplete and a complete adjuvant for antigens, which comprises from 0.01% to 30% of a polydimethylsiloxane, from 0.01 to 15% of a complex emulsifier with an HLB of 9016, from 45% to 99% of a pharmaceutically acceptable salt solution, from 0.01% to 10 of dimethylsulfoxide, and from 0.0001% to 1% of a chelating agent (the foregoing incomplete adjuvant of U.S. Pat. No. 5,904,925 being hereinafter referred to as “Paravac”). Peptidoglycans of species-specific
Staphylococcus aureus
strains and/or of other strains can be added to this incomplete adjuvant composition for immunization, in a concentration of from 0.00001 to 1 mg protein per ml adjuvant, and water soluble natural and/or synthetic polymers in a concentration of from 0.0001 to 10 mg/ml of the adjuvant. The patent also discloses the use of that adjuvant against a variety of diseases, and this application is a further development and a completion of that earlier invention. Thus any reference herein to a “Paravac” emulsion or composition, other than in the specific examples, is intended to encompass both the incomplete and the complete adjuvant compositions of U.S. Pat. No. 5,904,925.
That earlier invention provided adjuvancies which by combination with immunizing antigens or in combination with peptidoglycans into a pharmaceutically acceptable formulation will stimulate the defense mechanisms of the body to such an extent that in addition to the active immune prophylaxis also weak antigens produce a general and specific immunotherapy. Good results are obtained with this adjuvant in immunotherapy. It is a drawback that the preparation of the complete adjuvant, or the adding of proteins have relatively substantial requirements. The danger of an anaphylactic reaction in the host is a pathophysiological drawback of the complete adjuvant in the case of repeated use.
DESCRIPTION OF THE INVENTION
It is an object of the invention to provide a process for treating or for preventing the occurrence of certain diseases with an oil-in-water emulsion as an adjuvant for parenteral, especially intramuscular application, which is free from proteins as an incomplete adjuvant, by itself, or in combination with other parenterally applicable agents or in combination with a protein, in the for of a completre adjuvant. The diseases treated by the process of the present invention are systemic inflammatory response syndrome (SIRS), intensive care requiring conditions, viral diseases including hepatitis C and AIDS, Colitis ulcerosa, Crohn's disease, Parkinson's disease, Alzheimer's disease, multiple sclerosis, infectious hospital polyresistance conditions of viral and bacterial sources (infections hospitalismus), bronchial asthma, kidney and urethral infections, migraines, rheumatoid arthritis, osteoporosis Sudeck, acute and chronic inflammations, venal and arterial inflammations, acute and chronic exhaustion conditions, tumors, muscle shrinkage diseases, hemorrhoids, chemically induced heart diseases, hypertonia, aging phenomena, acute and chronic pain conditions, spastics, polyneuropathies, prostate neoplasms, hair loss, impotence, neurodermitis, cervical syndrome, tissue traumas, and amyotropic lateral sclerosis (Lou Gehrig's disease).
As used throughout the specification and the claims (other than in the specific treatment examples), any reference to the “treating” of any disease, is also meant to include prophylactic application against the disease.
It was found that the aforementioned oil-in-water Paravac emulsion produces upon parenteral, especially intramuscular or subcutaneous application surprisingly good effects for the enumerated and other indications, with durable improvements. It was also found that the duration of the treatment until initial effects can be observed, is substantially shorter than in the case of conventional, targeted medications for each of the specific indications. Furthermore, the total period of treatment, as well as until initial improvements are observed, can all be substantially reduced, and no side effects were observed.
Application of the present invention leads to desired results also in the case of indications which have been heretofore considered to be “uncurable.”, specifically in the case of hepatitis C, Parkinson's disease, Alzheimer's disease, multiple sclerosis, tumors, prostate neoplastics, and the like. In the case of patients for whom conventional drug therapy did not produce healing or relief and were considered refractory to conventional drug therapy, application of the present invention has frequently produced unexpected improved results.
The incomplete adjuvant Paravac is suitably formed into a silicone oil emulsion of an oil-in-water emulsion type, such as in g/ml of from about 0.01 to about 0.03 polydimethylsiloxane with a polymerization degree of from about 20 to about 400 and a kinematic viscosity of from about 20 to about 1300 mm
2/s
; from about 0.01 to about 0.03 dimethylsulfoxide; from about 0.03 to about 0.06 of a hydrophilic emulsifier such as from about 25 to about 35% sorbitantrioleate, from about 25 to about 35% cetylstearylalcohol, and from about 35 to about 45% polysorbate 80; and from about 0.86 to about 0.95 isotonic salt solution, and optionally from about 0.0001 to about 0.01 Na or Ca salt of EDTA as a chelating agent. The following embodiment of the Paravac emulsion was used in the following examples; wherein the components are given in mass proportions (g/ml emulsion):
0.015 dimethicone 200,
0.015 dimethylsulfoxide,
0.015 sorbitantrioleate,
0.015 cetylstearylalcohol,
0.02 Polysorbate 80,
0.0002 Na/CA salt of ethylenediaminetetraacetic acid, and
0.9 isotonic NaCl solution (0.9% NaCl in water).
In addition to the foregoing components, the emulsion can also contain 0.02 g/ml glycerol.
It was found that the oil-in-water Paravac emulsion when applied alone intramuscularly or subcutaneously, has produced surprisingly good results with the aforementioned diseases, and also produced a durable effect. When Paravac was applied in combination with other pharmacologically active ingredients, further surprising benefits were obtained. Thus the addition to Paravac of antibiotics, corticoids, antiparkinsonian agents, multiple sclerosis treating agents, neuro- and psychopharmaceutical agents, immunostimulants, and analgesics, can bring about a reduction of the conventional drug dose by up to 60%, and this permits a reduction of certain undesirable side effects of these agents.
The following examples further support and illustrate the process of the present invention. The Paravac composition that was used in the following examples was in mg/ml 0.015 dimethicone 200, 0.015 dimethylsulfoxide, 0.015 sorbitantrioleate, 0.015 cetylstearylalcohol, 0.02 Polysorbate 80, 0.0002 Na/CA salt of ethylenediaminetetraacetic acid, and 0.9 isotonic NaCl solution (0.9% NaCl in water).
The paravac composition was administered, depending on the nature of the treated disease, in 3-7, possibly 14 day intervals until stabilization of the health of the patient, and leukocytes, as well as CD4, CD8, NK, and TNF-&agr; values were stabilized at normal levels. These levels were generally achieved depending on the severity of the disease and the age of the patient, after two to four weeks of treatment.
After the application of the treatment for from about 3 to about 7 days, treatment was generally continued within a from about 7 to about 14 days time period of each other. After clinical stabilization was achieved, i.e. a stable clinically improved condition, the time period between applications was extended for a from about 4 to about 6 weeks period to about every 14 days. Multiple injections can be made few hours apart from each other in the initialization of treatment.
Restitution of damaged tissues required a treatment of at least 6 to 12 months, and in the case of b
Exner Heinrich
Klose Peter
Davenport Avis M.
Katona L.L.P. Gabriel P.
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