Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
  • A61K36/18—Magnoliophyta (angiosperms)
  • A61K36/185—Magnoliopsida (dicotyledons)
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K38/00—Medicinal preparations containing peptides
  • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
  • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
  • A61K38/46—Hydrolases (3)
  • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
  • A61K38/4873—Cysteine endopeptidases (3.4.22), e.g. stem bromelain, papain, ficin, cathepsin H
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • C—CHEMISTRY; METALLURGY
  • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
  • C12Y—ENZYMES
  • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
  • C12Y304/22—Cysteine endopeptidases (3.4.22)
  • C12Y304/22002—Papain (3.4.22.2)

Definitions

• This invention relates to a composition for treating the symptoms of excess gastric acid secretion, such as heartburn, sour stomach, acid indigestion and upset stomach.
• the composition of this invention is a combination of: 1) one or more compositions that reduce gastric acidity; and, 2) papaya extract.
• compositions that provide relief from gastric hyperacidity. These compositions include, but are not limited to, compositions that reduce intragastric hydrogen ion concentration by chemical neutralization such as calcium carbonate (e.g. Turns®), magnesium hydroxide (e.g. Mylanta®), a combination of calcium carbonate and magnesium hydroxide (e.g.
• H 2 receptor antagonists such as ranitidine (e.g. Zantac®), cimetidine (e.g. Tagemet®), and the like; proton-pump inhibitors such as omeprazole; bismuth compounds; prostaglandins; sucralfate; and, dopamine antagonists such as cisapride.
• compositions are effective, some are not long lasting, while others have a delayed onset of action. More specifically, compositions such as Turns®, Mylanta®, and Rolaids® are not long lasting, whereas H 2 receptor antagonists, proton-pump inhibitors, and others do not have a rapid onset of action (i.e. less than one minute). A composition capable of overcoming these disadvantages is therefore desired.
• papaya a fruit of the melon tree Carica papaya Linn has been known for centuries. Studies have shown the juice from the fruit, also referred to as latex, contains proteolytic enzymes, which have been identified as papain, chymopapain and papaya proteinase III. Papain is the most characterized among the three. Its approximate molecular weight is 21,000, and it contains 18 different amino acids in a sequence of 211 amino acids.
• the present invention is directed to a composition comprising: 1) one or more compositions that reduce stomach acidity; and, 2) a composition extracted from papaya, preferably comprising one or more proteolytic enzymes, including but not limited to, papain, chymopapain and papaya proteinase III.
• This composition can be used to provide improved, convenient relief from gastric distress resulting from excess gastric acid secretion.
• the present invention is further directed to a method of preparing a composition comprising: 1) one or more compositions that reduce stomach acidity; and, 2) a composition extracted from papaya, preferably comprising one or more proteolytic enzymes, including but not limited to, papain, chymopapain and papaya proteinase III.
• the present invention is further directed to a method of using a composition
• a composition comprising: 1) one or more compositions that reduce stomach acidity; and, 2) a composition extracted from papaya, preferably comprising one or more proteolytic enzymes, including but not limited to, papain, chymopapain and papaya proteinase
• the present invention is directed to a composition for relieving stomach distress comprising: 1) one or more compositions that reduce gastric acidity; and, 2) a composition extracted from papaya, preferably comprising one or more proteolytic enzymes, including but not limited to, papain, chymopapain and papaya proteinase III.
• This composition can be used to provide improved, convenient relief from gastric distress resulting from excess gastric acid secretion.
• This invention is further directed to a method of preparing and a method of using such a composition for providing improved relief of gastric distress.
• the amounts of the ingredients that can be used in this composition are generally the ordinary dosages required to obtain the desired result.
• the amount of the first component that reduces gastric acidity is present in an amount of from about 10 mg/dose to about 1500 mg/dose and the amount of the papaya extract is present in an amount of from about 50 mg/dose to about 3000 mg/dose.
• compositions that reduce gastric acidity may be any of the following: compositions that reduce intragastric hydrogen ion concentration by chemical neturalization; H 2 receptor antagonists; proton-pump inhibitors: bismuth compounds; prostaglandins; sucralfate; and dopamine antagonists. These compositions are herewith defined as "antacids.”
• the composition of this invention may comprise one or more than one of these antacids.
• improved relief from gastric distress can be either relief that has a longer duration of action and/or a faster onset of action than would occur from ingesting the antacid component alone of this inventive composition alone.
• compositions that reduce gastric acidity by chemical neutralization are: aluminum-containing active ingredients; bicarbonate-containing active ingredients; bismuth-containing active ingredients; calcium-containing active ingredients; citrate-containing active ingredients; glycine; magnesium-containing active ingredients; dried milk solids; phosphate-containing active ingredients; potassium-containing active ingredients; sodium-containing active ingredients; silicates and tartrate-containing active ingredients; and other compositions recognized by the U.S. Food and Drug Administration (FDA) as useful for the relief of heartburn, sour stomach, or acid indigestion and upset stomach.
• FDA U.S. Food and Drug Administration
• calcium carbonate and magnesium hydroxide are the preferred chemical neutralizing compositions. Calcium carbonate is the most preferred.
• Receptor antagonists reduce gastric acid secretion by blocking histamine receptors in the stomach lining. Histamine stimulates gastric secretion via H 2 receptors.
• H 2 receptor antagonists are: ranitidine, cimetidine, famotidine, mifentidine, roxatidine, and mizatidine.
• the amount of H 2 receptor antagonist that can be used in this invention is from about 10 mg/dose to about 800 mg/dose.
• ranitidine is the preferred H 2 receptor antagonist.
• the amount of ranitidine that can be used in this invention is from about 75 mg/dose to about 300 mg/dose.
• Proton pump inhibitors block the membrane pump on the parietal cells in the stomach that are responsible for exchanging potassium from the gastric lumen with hydrogen ions. Blocking this membrane pump inhibits gastric acid secretion.
• a nonlimiting example of a proton pump inhibitor is omeprazole.
• Bismuth compounds act in a number of ways to reduce gastrointestinal distress.
• a nonlimiting example of a bismuth compound is bismuth subcitrate, also known as tripotassium dicitrato bismuthate.
• Prostaglandins are lipid hormones found in virtually all tissues. It is believed that one effect of prostaglandins in the stomach is reduction of acid secretion. They may also enhance mucosal resistance to stomach irritation.
• Nonlimiting examples of prostaglandins are PGEi of which misoprostol is an analogue: PGE 2 , of which arabaprostil and enprostil are analogues; PGIi, and methyl analogs of prostaglandins of the E series.
• Sucralfate is a complex salt of polyaluminium hydroxide with a sulphated saccharide skeleton which has been proven clinically to be effective in the treatment of gastric and duodenal ulceration. It is a weak buffer with a pK of approximately 4.5.
• Dopamine antagonists are believed to relieve gastric distress by increasing gastrointestinal motility and decreasing transit time.
• Nonlimiting examples of dopamine antagonists are metoclopramide, domperidone. and cisapride.
• the amount of the foregoing compositions that reduce gastric acidity that are used in this invention may vary depending upon the therapeutic dosage recommended or permitted for the particular agent. In general, the amount of these compositions is the ordinary dosage required to obtain the desired result. In one embodiment of this invention the amount of compositions that reduce gastric acidity by chemical neutralization are present in an amount of from about 250 mg to about 1450 mg/dose.
• the dosage form may be a tablet, caplet, capsule, powder, troche, lozenge, elixir, and the like. Such dosages are known to the skilled practitioner in the medical arts. Preferred dosage forms are tablets and caplets.
• magnesium hydroxide is in an amount of from about 50 to about 800 mg/dose; preferably in an amount of from about 80 mg to about 600 mg/dose; and most preferably from about 100 mg to about 400 mg/dose.
• calcium carbonate is in an amount of about 200 to about 1250 mg/dose; preferably from about 400 mg to about 1000 mg/dose; and most preferably from about 500 mg to about 800 mg/dose.
• Another preferred embodiment of this invention contains both magnesium hydroxide and calcium carbonate in an amount of magnesium hydroxide of from about 50 mg to about 400 mg/dose and calcium carbonate in an amount of from about 200 mg to about 1250 mg/dose; preferably an amount of magnesium hydroxide of from about 80 mg to about 300 mg/dose and calcium carbonate in an amount of from about 400 mg to about 1000 mg/dose; and most preferably an amount of magnesium hydroxide of from about 100 mg to about 260 mg/dose and calcium carbonate in an amount of from about about 500 mg to about 800 mg/dose.
• the present invention further includes a composition extracted from the juice, pulp, or other parts of papaya.
• the composition extracted from papaya is defined as papaya extract.
• One embodiment of this invention comprises one or more proteolytic enzymes from papaya extract.
• proteolytic enzymes are papain, chymopapain, and papaya proteinase III.
• the preferred enzyme is papain.
• the papaya extract of this invention may be in a variety of forms. Nonlimiting examples of these forms are: the dried powdered latex of papaya; freeze dried papaya powder; papaya juice powder; crystalline papain; and crystalline chymopapain.
• the preferred forms are freeze dried papaya powder and papaya juice powder.
• the amount of papaya extract in each dose of the composition of this invention is from about 50 mg to about 3000 mg.
• the preferred amount is from about 100 mg to about 1000 mg.
• the most preferred amount is from about 200 mg to about 800 mg.
• Another embodiment of this inventive composition contains one or more proteolytic enzymes found in papaya extract, including but not limited to papain, chymopapain, and papaya protease III. These enzymes may be relatively pure (i.e. of pharmaceutical grade), but preparations of less pure enzymes are also acceptable.
• the amount of the one or more proteolytic enzymes per dose in this embodiment is from about 0.5 to about 600 mg; preferably from about 1.5 mg to about 300 mg; and most preferably from about 2.5 mg to about 200 mg.
• composition of this invention may also contain other ingredients and excipients known to one skilled in the art.
• additional ingredients include excipients, binders, coloring, flavoring, sugars, starches and the like.
• the composition of this invention may be used in many distinct physical forms well known in the pharmaceutical art to provide an initial dosage of the inventive composition and/or a further time-release form of the inventive composition.
• such physical forms include tablets, caplets, capsules, powders, troches, lozenges, elixirs, and the like.
• composition of this invention is made by admixing one or more antacids of this invention with dried papaya extract as well as other dry ingredients such as excipients, binders, starches, sugars and the like. These ingredients are then blended thoroughly and prepared as powders, tablets, caplets, capsules, and the like according to skills known in the art.
• Another method of preparing the composition of this invention comprises thoroughly blending the dry ingredients then further combining them with liquid papaya extract and blending, then further combining with water, corn syrup, and the like in order to prepare a liquid form of the invention. By using additional methods known to one skilled in the art, this liquid form of the invention can then be prepared to form a lozenge, troche, and the like.
• This invention extends to methods for using the inventive composition.
• these methods employ ingesting the inventive composition in an amount and frequency sufficient to provide improved treatment of symptoms caused by excess gastric acid secretion.
• compositions according to this invention are provided to illustrate, but not limit, the claimed invention.
• the sugar, calcium carbonates, magnesium hydroxide, pregelatinized starch and polyethylene glycol were previously combined with water, and blended to from a uniform, dry, powdered composition. These ingredients were then blended with the papaya juice powder, flavor, starch 1500, and silica for twenty minutes using a half- quart P-K blender. The magnesium stearate is then added to this mixture and blended for five minutes.
• the blended composition is then compressed into hard, pleasant tasting tablets using conventional technology.
• the amount of papaya extract contained in each dose can range from about 50 mg to 3000 mg with about 100 mg to about 1000 mg preferred.
• the particular form of papaya extract used is not believed to be critical in the present invention, however, the purer the form used the less the amount of extract needed for each dose.

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• Natural Medicines & Medicinal Plants (AREA)
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• Chemical Kinetics & Catalysis (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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• Biochemistry (AREA)
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Applications Claiming Priority (3)

Publications (1)

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• 1998
  • 1998-07-08 EP EP98933290A patent/EP1001796A1/en not_active Withdrawn
  • 1998-07-08 AU AU82968/98A patent/AU8296898A/en not_active Abandoned
  • 1998-07-08 JP JP50751899A patent/JP2002509539A/ja active Pending
  • 1998-07-08 CA CA002286357A patent/CA2286357A1/en not_active Abandoned
  • 1998-07-08 BR BR9809419-0A patent/BR9809419A/pt not_active Application Discontinuation
  • 1998-07-08 WO PCT/US1998/014233 patent/WO1999003486A1/en not_active Application Discontinuation
  • 1998-07-14 ZA ZA986247A patent/ZA986247B/xx unknown
  • 1998-07-14 AR ARP980103405A patent/AR016514A1/es unknown
  • 1998-07-15 PE PE1998000622A patent/PE102699A1/es not_active Application Discontinuation

Non-Patent Citations (1)

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