Pharmaceutical components for treatment of AIDS and killer almost virus

The invention is related to the ingredients used in alleviation and treatment of HIV, production process & application

Acquired Immune Deficiency Syndrome (AIDS) are discovered in Central America, South Africa, Africa, Europe, Middle East, South East Asia and South Pacific. According to World Health Organization, by July 1, 1993 over 14 million people are HIV-positive, and by the year 2000, this number will increase by around 40 to 100 million, most of which will be in Africa and Asia.


HIV is the harbinger of AIDS. (Laurence J. et al.; 1984, New England Medical Journal 311:1269). It is a retrovirus surrounded by lipoprotein. If some of these viruses enter human body, they will multiply themselves, and over a long period there will be enough of them to cause immune deficiency. HIV infection causes the loss of lymphocyte (lymphopenai), and consequently the deficiency in D4 + T-cells

In healthy human, the CD4: + CD2 ratio is approximately 2, but in AIDS patient it is reduced to only 0.5. CD4 + T Cells indicate the completeness of immunity. Deficiency in CD4 + T Cells will result in AIDS patient showing compensation reaction.

HIV can be contracted through physical contact. The disease can spread much faster by blood infusion of sharing of hypodermic needle. HIV’s are present in blood, bone marrow, kidneys, plasma, semen and all kinds of secretions. Therefore, HIV’s can only spread around by blood infusion, sharing of hypodermic needle and sexual intercourse.

A person infected with HIV usually has fever and feels arches & pains in the muscles during the first 3 to 6 weeks. These symptoms may last a few days up to a few weeks. During this time, the number of viruses in the blood will quickly multiply, ready to spread whenever there is a chance, and blood test will give positive result. At next stage, which is the progressive destruction of immune system, the patient will do longer response to any viruses. The incubation period varies from one patient to another. The disease may be asymptomatic for a few years, during which the patient will be fairly healthy, but his T cells will eventually reduce to a dangerous lever. By this time, he will be suffering from tumors and opportunistic diseases. Later, the diseases will develop into lymphadenopathy without any fever. At this stage, the lymph nodes show hyperplasia of the follicles in cortex and invasion of germinal center by CD3 + which leads to destruction of germinal center and contraction of follicles.


Rapid weight loss is quite phenomenal in AIDS patients. This is due to loss of appetite caused by change in protein level, metabolism, intestine’s ingestion ability and endocrine malfunction.


Full blown AIDS shows many symptoms, such as chronic fever and diarrhea, rapid loss of weight without other illnesses, opportunistic diseases caused by pathogens and protozoa such as pneumo cystis carinii;

Kaposi’s sarcoma, toxoplasma, gondii and cryptosporidium muris; different types of viruses, e.g. cytomegalovirus and herpes zoster; bacteria, such as mycobacterium avium and fungi such as Cryptococcus and histoplasma. These germs cannot harm healthy human, but they can kill AIDS patients.

For the time being there is no cure of even vaccine for HIV/AIDS. US Food & Drug Administration has allowed three types of drugs to be used on AIDS patients. They are Azidothymidine, didioxycytidine and dideoxyinosine. These drugs intervene the RNA genome reversal process and prevent the HIV multiplication. Normally, the DNA chain will expand by linking nucleotides with hydrozy with 3 tips to form chains. The drugs are nucleotide. It can blend with the DNA chain, but it lacks the property called 3’ hydroxyl group. So, it breaks the chains and prevents production of DNA in normal cells. Therefore, these antiviral drugs are harmful to the body too.


To combat these special viruses, new drugs and treatment strategies are being developed continuously. In 1995, the US Food & Drug Administration approved Saquinavir or Invarase which are the first protease inhibitors. Later, many more protease inhibitors are sold on the market. Therefore, the use of *concoction* or combination of many drugs such as protese inhibitors, reverse transcriptase inhibitors and nucleotide analogs is likely to be more effective than the use of just one single drug (Carpenter et al. 1996 Jama 276:146-154).

The existing drugs and treatment strategies can only prevent HIV from turning into AIDS while maintaining patient in good health, but none of them is the cure for AIDS. The aim of this research is to find the drugs which for the time being can alleviate the suffering and retard the development of AIDS in the hope to find the new drugs which can help HIV patient fully recover.


Complete revelation of invention;
This newly invented drug is made up of the following essential ingredients:
•flavonoid & anthocyanin
•beta-sitosterol & stigmasterol
•tannins
•triterpene


Analysis of ground extracts by means of 75-micron sieve:-
•Phytochemical tests:
Tests of constitution of extracts by Farmworth N.R. 1981 method gave the following results:


Determination of constitution:
Flavonoid: by Shinoda test
Phenolic compounds: by ferric chloride
Anthraquinone: by Dregendorff’s method
Cardiac glycocide: by Kedde’s & Raymond’s reagent methods
Tannins: Symposium on the Chemistry of Vegetable
Tannins, Soc leader, Trades Chemists, Croydon 1956


1956
B-sitosterol, Stigmasterol: Misra D.R. et al. Phytochemical Reports, 1973 Triterpene: Liebermann Burchard Test – showing signs but verification cannot be made


Flavonoid (light yellow), tannins, triterpene, b-sitosterol-stigmasterol can be found at the root and trunk of Antidesma, Acidum Retz, Stilaginaceae. Anthraquinone or Anthocyanin (red) can be found at its seeds.

About 5-16% of tannins can be present in the compound, but the ideal quantity is 6.07-11.49% when measured by UV Spectophotometry (Report 2)


Beta-sitosterol and Stigmasterol used in the product should have maximum wave length at 0.375-20.497 nm. About 0.7-1.4% of them can be present in the compound, but the ideal quantity is 0.93-1.1%. By being dissolved in chloroform, it can reveal the composition of this product by general means. For example, all the ingredients with such properties, which are commercially available or produced, can be mixed together in the said proportion all in one go or step by step, dried and purified.

An alternative method is to grind the plant named Antidesma Acidum Retz, Stilaginaceae into powder with ethyl alcohol with concentration at 60-80% --ideal concentration is 70% -- for 5-12 days – ideal time is 7 days. Leave the extract to settle. The quantity obtained is 3.5-13.5% -- by weight. By recycling method, separated the alcohol, and heat the extract at 60-90o C, but ideal temperature is at 70-80o C to make water evaporate. Then, the extract should be ground and put through 75-micro


This composition can be used in the alleviation and treatment of HIV/AIDS as described in some of the examples.
The extract can be made into many different forms, e.g. tablets, powder, solution, converted powder, etc. It can also be mixed other agents in the formula.


The plant extract can be mixed with pure water. Air can be used as oxidizing agent. This can be achieved by air pump for 2-3 weeks. Let the solution settle. Add light yellow agent and blow with ozone (O3) for an hour. Sterilize and leave to settle once more.


Pour light yellow, tasteless and odorless liquid. The amounts of Flavonoid and Tannins can be determined, because they can dissolve in water. By weight, there is 18.15% of tannins and 81.85% of flavonoid.


The other three components, namely b-sitosterol, stigmasterol, triterpene, etc. and dissolve will in alcohol. The quantity is about 16.1%, as they contain fatty elements.
In the extract of plant by water, quality control can be achieved by heating at 150o C. The right quantity of flavonoid and tannins can be obtained – 9 mg per tablespoon or 15 cc.

The dosage depends on various factors such as patient’s health based on CD4+, opportunistic infections and the number of viruses per 1 ml.
In the beginning of 1995, this product was tested on animals and patients based on the white blood cells count (WBC) with the unit of cells per mm3.


With advances of technology, we found more accurate methods viral load count by Amplicor HIV I Monitor with the unit of copied per ml of plasma RNA, CD4+ measurement with the unit of cells mm3 are used in conjunction.


Best method of production:
Please refer to the complete revelation of invention.
Drug tests:
13 male patients
19 female patients
Use of potion: 20-160 cc or 15-120 mg per day
(4 times before meal and bedtime)
Use of tablets: 80-20 tablets or 138-320 mg.
(4 times before meal and bedtime)


Effects:
80% of the patients had higher CD4 + and lower HIV’s. The results of blood tests before and after using the drug for 3-5 months are shown in the graph attached herewith. None of them suffered from side effects.


Relationships:
1.Going through full course, talking the drug regularly every day.
2.Disease at different levels of severity, e.g. patients with immunity not 50% below normal which is around 300-400 cells/mm3, with viral load of not greater than 150,000 copies or RNA/ml, not suffering from opportunistic infections


3.Blood tests before and after using the drug revealed that the patients’ conditions have improved. AIDS/HIV reverted to HIV infection stage, which means the immune system is normal or almost normal.
4. Only small amount of HIV’s are present – around
1,000 copies of RNA/ml. It means further treatment
can lead to complete recovery.


5.With patients suffering from severe opportunistic infections, such as toxoplasmosis encephalitis, tuberculosis, pneumonia, etc. , the use of drug did not alleviate the symptoms. However, with treatment of opportunistic infections by modern medicine in conjunction, these patients still have the change to revert to the stage mentioned in C1.2.
6.Most patients suffer from mental disorders known as Power HIV(PWHIV). Mental therapy or meditation can help improve their conditions.


Therefore, this traditional, drug, which is the extract of Antidesma Acidum Retz. Stilaginaceae, has to be used in conjunction with modern medicine in order to deal effectively with the opportunistic diseases. The natural plant extract has no toxic synthetic substances.

It does not produce any side effects