• 专利附录
  • 专利说明
  • 权利要求
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  • 引用文献
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    • 专利摘要:
    Composition and its use to prepare a medicine for the treatment of acidity. The present invention relates to a formulation prepared from a composition comprising magnesium oxide, calcium oxide, lithium carbonate and potassium bicarbonate. The invention also relates to its use for preparing a medicament for the treatment of acidity in humans, especially the acidity of body fluids, excluding blood. (Machine-translation by Google Translate, not legally binding)
    公开号:ES2684437A1
    申请号:ES201730468
    申请日:2017-03-29
    公开日:2018-10-02
    发明作者:Manuel MATEOS DE VICENTE
    申请人:Manuel MATEOS DE VICENTE；
    IPC主号:
    专利说明:

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    DESCRIPTION
    Pharmaceutical formulation and its use to prepare a drug for the treatment of heartburn
    Field of the Invention
    The present invention relates to the chemical-pharmaceutical sector. More specifically, it refers to a pharmaceutical formulation and its preventive and therapeutic application as an antacid.
    Background of the invention
    Acidification is produced by the body's own functions and by an imbalance in diets, which are very acidifying, producing an acidification of cells, tissues and organs; also for certain moods. This imbalance can trigger diseases and pathologies of all kinds: physical, chronic and acute, since acids will negatively influence the pH balance of the body. For some authors, acidosis of body fluids and, as a result, tissue acidosis, is the cause or a factor that helps worsen many disorders and alterations. The stress of contemporary society has made it widespread (Rocco Palmisano et al., "Alkalizing and ionizing: to live healthier and longer", S.A.P.I.O, chapter 1 and 23. 2015).
    There are authors who have suggested that acidosis of body fluids has a negative influence on alterations such as the development of cramps, demineralization, skin rashes, migraines, allergies, colds, sinusitis ... There are those who even consider, as Dr Robert Young ( Robert O. Young et al., "The miraculous pH diet: get your natural balance", Obelisk, chapter 1, 2, 3 and 4. 2012) that acidosis is the cause of all chronic and degenerative diseases, since As the acidity spreads and the pH of the tissues becomes more acidic, the oxygen levels decrease and the cellular metabolism stops or alters. Therefore, our body cannot withstand an acid state and will be reflected with a loss of energy, sensitivity and irritation, mucus and congestion, inflammation, soft tissue hardening, ulceration and finally coronary heart disease, cancer, heart attack, AIDS, multiple sclerosis or diabetes. In 1931 they awarded the Nobel Prize to Otto H. Warburg because he found that cancer originates when the human body is acidic. Much of the rare diseases can have their origin in the acidity of the body, perhaps thousands of diseases because acidity destroys organic compounds, such as our body.
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    The circulatory system will attempt to remove acids in the form of gas or liquid, through the lungs or kidneys. If there is too much waste, it will deposit them in several organs: heart, pancreas, liver and colon, or in fatty tissue, including breasts, hips, thighs and abdomen and brain (Christopher Vasey, “Alkaline feeding: importance of basic health balance ”, Edaf, chapter 1 and 2. 2014).
    To prevent excess acidity in the body, the blood begins to remove alkaline minerals from the tissues to compensate, but it is not very effective because the blood maintains its pH very close to 7.4 plus 0.2. It is easy to find in pharmacies, even in other establishments, products based on proton pump inhibitors such as omeprazole under the brand name Omeprazole or lansoprazole under the brand name Lansoprazole, which inhibit the secretion of acid in the stomach, binding to the proton pump in the gastric parietal cell, inhibiting the transport of H + to the gastric lumen or histamine-2 blockers which reduce the amount of acid produced by the stomach, such as Zantac® or Famotidine® with ranitidine as a principle active. Some others such as Citiboides® for the symptomatic treatment of gastric hyperacidity, a combination of sodium bicarbonate and lithium carbonate, Rennie® which is a combination of magnesium carbonate and calcium carbonate for the symptomatic treatment of gastric acidity and hyperacidity associated with peptic ulcer or Almax® whose active substance is almagato. There are doctors who try to eliminate cancer based on sodium bicarbonate but this has the disadvantage that sodium, with its love of water molecules, is surrounded by layers and layers of H2O that is introduced into cells and swells them, with the consequent damages.
    It is also known that other compounds such as lithium carbonate, in addition to helping reduce stomach upset, generally alter sodium transport in nerve and muscle cells; Some lithium is recommended to produce optimism. Other compounds, such as potassium bicarbonate, can alkalize the gastric juice hydrochloric acid, similar to the way sodium bicarbonate does; However, potassium bicarbonate is hardly used for this purpose. The body needs some potassium because it is usually lacking in it. On the other hand, magnesium oxide and calcium oxide can act as protectors by increasing the pH, inactivating the proteolytic action of pepsin.
    As you can see, for the most part, all products that can have an effect to control pH are products mainly used to control gastric acidity.
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    However, as previously mentioned, it would be interesting to have preparations that were not primarily intended to control gastric acidity, but were intended to control acidity in different body fluids. And the stabilization of pH in body fluids is important because, although the blood has its own homeostasis system, which maintains its continuous pH at values close to 7.4, the same does not happen with other body fluids. And their acidification, as discussed above, seems to be involved in the development or worsening of different diseases.
    It would also be preferable if the composition comprised compounds that were easy to acquire and could be ingested continuously. Therefore, the problem that is intended to be solved with the present invention is the elimination of acidity from body fluids excluding blood, thereby stabilizing the pH to a value close to 7.4.
    The present application provides a solution to this problem.
    Description of the invention
    The main object of the present invention is to provide stability to body fluids by means of an antacid that allows easy preparation and easy obtaining of the desired or required dose, which helps cover a wide range of doses as needed. , allowing dose adjustments.
    The solution of the present invention is a composition based on combining lithium carbonate (U2CO3), potassium bicarbonate (KHCO3), magnesium oxide (MgO) and calcium oxide (CaO), which will be able to neutralize and detoxify harmful acids of the body.
    The combination of these four elements is not common in antacids, since these products are usually acquired and ingested when there are symptoms of gastric disturbances, acidity or esophageal reflux, but they are not usually ingested for the purpose of stabilizing the pH of the body fluids. And yet, one of the aspects of the present invention is the use of a formulation of the present invention to prepare a medicament for the treatment of acidity in humans, especially the acidity of body fluids other than blood.
    Specifically, the proposed pharmaceutical formulation for this product is as follows:
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    In a total of ten parts, the proportion of each compound would be:
    -calcium oxide: between 0.5 and 6 parts
    -Lithium carbonate: between 0.5 and 3 parts
    Potassium bicarbonate: between 0.5 and 2 parts, and, optionally,
    -Magnesium oxide: between 1 and 8 parts.
    Preferably, the pharmaceutical formulation comprises a combined composition comprising, for every ten parts:
    - magnesium oxide: between 1 and 8 parts
    -calcium oxide: between 0.5 and 6 parts
    -Lithium carbonate: between 0.5 and 3 parts
    - potassium bicarbonate: between 0.5 and 2 parts,
    the most preferable proportion being:
    - lithium carbonate: 1 part
    - potassium bicarbonate: 1 part
    - calcium oxide: 2 parts
    -Magnesium oxide: 6 parts.
    As used herein, "parts" are called amounts that have the same weight.
    Preferably, all components must be present, with magnesium oxide being especially preferable. The proportion can be adjusted according to the effect on the patient, since there are those who, for example, tolerate magnesium poorly because of diarrhea; in those cases, it would be convenient to decrease the amount of magnesium oxide, or even eliminate it, and increase the amount of either calcium oxide alone, or of calcium oxide, potassium bicarbonate or lithium carbonate, or combinations thereof. In any case, the fact that the preferred formulation of the invention combines four components, and the proportions chosen for them, decrease a possible risk of adverse side effects that, in the long term, could perhaps be observed if only one of the components was administered. , especially if administered in high amounts. Also for that reason, preferably, the formulation of the invention
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    It must be administered under the control of an expert, who controls the evolution of the subject and can vary the proportions according to the possible effects observed. Preferably, the modification of the proportions should be carried out by an expert in Chemistry.
    The preparation technique of this formulation would be as follows:
    The components of the composition are introduced into a container and removed until the components are well distributed throughout the mass.
    In this way it is stored and then used by dissolving in water the part you want to take.
    The pharmaceutical formulation may be presented in powder form, directly as a result of the previous mixture. It can also be prepared in other known forms of presentation, such as in the form of tablets, capsules or as a solution. For this, preferably, the above mixture will be mixed with some solvent, preferably water or an aqueous solution; Pharmaceutically authorized excipients may also be added to said solution, selected according to the pharmaceutical form of presentation chosen. In the case of tablets, binders, such as microcrystalline cellulose, polivilpyrrolidone, will preferably be added.
    hydroxypropyl methylcellulose, starch, or mixture thereof. Once well mixed, the final mixture obtained will be compressed to give rise to the final tablets.
    The formulation will preferably be taken orally. In the case of the powder mixture, it will preferably be taken dissolved in water, and never injected into the veins or arteries. Thus, it is one of the possible embodiments of the use of the formulation to prepare a medicament for the treatment of acidity in humans that the medicament is prepared to be administered orally, preferably dissolved in water.
    As mentioned above, in case the composition contained magnesium oxide and diarrhea symptoms were observed, the amount of magnesium oxide will be lowered by preferably replacing it with calcium oxide in the same proportion until the diarrhea is stopped.
    Each day a total of four grams can be taken at first, dissolved in water, which is the preferable daily dose until the pH of the body fluids is stabilized. Said daily dose can be taken in a single dose or divided into several doses. If you don't like the
    Taste can be sweetened with powdered sugar or with a liquid sweetener to increase the palatability of it.
    The acidity usually disappears in a few days, generally no more than 20. It is convenient to analyze the acids daily at the beginning and once the pH has stabilized in 7 adjust the 5 doses, which can continue to be daily or spacing them one or more days.
    Thus, once the balance of body fluids has been reached, the amount to be taken to keep the pH close to 7 or 7.5 will be reduced. However, the acidity of the body should be checked frequently so that it is not acidic again.
    In line with all this, it is also a possible embodiment of the use of the formulation to prepare a drug for the treatment of acidity in humans, compatible with the above, that the drug is prepared to be administered in a maximum total daily dose 4 grams per day, until the pH of the body fluids is stabilized, preferably in several doses. It is also a preferred embodiment that in which the medicament is prepared so that the total daily dose ingested can be less than 4 grams, which allows to achieve the objective indicated above: once the pH of the fluids in the fluids has stabilized body, reduce the amount until you find the balance with a neutral pH in the body fluids.
    The acidity control can be carried out using usual means for these purposes, such as litmus paper, soaking it with saliva to be able to be before taking any food or drink or by urine and preferably by getting out of bed by the morning. Preferably, litmus paper will be accompanied by a color scale that will indicate the pH value or pH range that corresponds to a certain color, to facilitate acidity control.
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    权利要求:
    Claims (13)
    [1]
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    1. A pharmaceutical formulation comprising a combined composition characterized in that it comprises, for every ten parts:
    - calcium oxide (CaO): between 0.5 and 6 parts
    - lithium carbonate (U2CO3): between 0.5 and 3 parts
    - potassium bicarbonate (KHCO3): between 0.5 and 2 parts, and, optionally,
    - magnesium oxide (MgO): between 1 and 8 parts.
    [2]
    2. The formulation according to claim 1, wherein the combined composition comprises, for every ten parts:
    - magnesium oxide (MgO): between 1 and 8 parts
    - calcium oxide (CaO): between 0.5 and 6 parts
    - lithium carbonate (U2CO3): between 0.5 and 3 parts
    - potassium bicarbonate (KHCO3): between 0.5 and 2 parts.
    [3]
    3. The formulation according to claim 2, wherein the combined composition comprises, for every ten parts:
    - magnesium oxide: 6 parts
    - calcium oxide: 2 parts
    - lithium carbonate: 1 part
    - potassium bicarbonate: 1 part.
    [4]
    4. The formulation according to any one of claims 1 to 3, which is in powder form.
    [5]
    5. The formulation according to any one of claims 1 to 4, which optionally also contains pharmaceutically acceptable excipients.
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    [6]
    6. The formulation according to any one of claims 1 to 5, which additionally also contains sugar or a sweetener.
    [7]
    7. Use of a formulation according to any one of claims 1 to 6, to prepare a medicament for the treatment of acidity in humans.
    [8]
    8. Use according to claim 7, wherein the acidity to be treated is acidity of body fluids except blood.
    [9]
    9. Use according to claim 7 or 8, wherein the medicament is prepared to be administered orally.
    [10]
    10. Use according to any one of claims 7 to 9, wherein the medicament is prepared to be administered dissolved in water.
    [11]
    11. Use according to any one of claims 7 to 10, wherein the
    Medication is prepared so that the composition is administered in a maximum total daily dose of 4 grams per day until the pH of the body fluids is stabilized and then lower the amount until a balance is found with a neutral pH in the body fluids.
    [12]
    12. Use according to claim 11, wherein the medicament is prepared in a manner
    that the maximum total daily dose of 4 grams per day be administered in several doses.
    [13]
    13. Use according to any one of claims 7 to 10, wherein the
    Medication is prepared so that the composition is administered in a total daily dose less than 4 grams per day that results in a balance with a neutral pH in the body fluids.
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    同族专利:
    公开号 | 公开日
    ES2684437B1|2019-08-22|
    引用文献:
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    WO2013111077A1|2012-01-27|2013-08-01|Institute Of Bioorganic Chemistry|Pharmaceutical composition as a substance for antireflux antacid drug|
    US20140255465A1|2013-03-08|2014-09-11|Cognate3 Llc|Process For The Preparation Of A Non-Corrosive Base Solution And Methods Of Using Same|
    CN103845734A|2014-03-20|2014-06-11|辽宁亿灵科创生物医药科技有限公司|Esomeprazole pharmaceutical composition and preparation thereof|
    法律状态:
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    ES201730468A|ES2684437B1|2017-03-29|2017-03-29|Pharmaceutical formulation and its use to prepare a drug for the treatment of heartburn|ES201730468A| ES2684437B1|2017-03-29|2017-03-29|Pharmaceutical formulation and its use to prepare a drug for the treatment of heartburn|
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