Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
  • A61K31/732—Pectin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
  • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
  • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
  • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P5/00—Drugs for disorders of the endocrine system
  • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones

Definitions

• the present invention relates to a pharmaceutical composition comprising pectin effective in inhibiting the male reproductive toxicity.
• Endocrin system disturbing materials so-called “environmental hormones'" which have recently become an issue and been watched with keen interest in the U.S., Europe. Japan, etc., are chemical materials disturbing the function of the endocrin system and having similar activities as hormones in the body.
• Examples of such materials are various chemical products for industry, agricultural chemicals such as insecticides and herbicides, organic heavy metals, dioxins generated in an incinerator, hormone analogues such as phytoestrogen, synthetic estrogens useful as medicines such as diethylstilbestrol, and other food or food additives. A particular concern is given to dioxins among such materials.
• Dioxin is an organic compound having two benzene rings chemically bonded to two oxygen atoms.
• a generally available dioxin is dioxin chloride wherein a hydrogen within benzene rings is substituted with a chloride.
• dioxin chloride wherein a hydrogen within benzene rings is substituted with a chloride.
• the most toxic and stable dioxin is 2,3,7,8-TCIJD (tetrachloriodibenzo-p-dioxin) having four substituted chlorides. Because the dioxi/i is easily generated during the burning-out of domestic garbage or the softening of gasoline, it is more dangerous to the environment (see S. Alex, villalobos, Michael J Anderson, and Peter Kelley, 1996. "Dioxinline Properties of a Trichloroethylene Combustion-Generated Aerosol, Environmental Health Perspectives, 104. p734-p743).
• Dioxins are generally absorbed through the digestive duct, skin and respirator. The absorption rates vary depending on species, solvent, dioxin homologue and isomer, materials taken together, administered amount, and age. The absorbed dioxins are generally accumulated in the liver and adipose tissues, and hardly excreted out of the body.
• dioxins cause skin diseases, and toxicity, carcinogenicity and malformation of the liver. Recent experiments on humans also substantiated the harmfulness of dioxins. Particularly, dioxins cause unbalanced hormone secretion, reduced reproductivity and immunity, malformation of genitals, inhibition of growth, and cancers.
• U.S. Patent Nos. 5,834,442 and 5,895,784 disclose a method of inhibiting the transition of a primary tumor by orally administrating a citrus pectin of a modified pH to a recipient.
• WO 9710727 discloses a method of reducing separation of serum, using an enzyme, from an aqueous vehicle containing a pectin.
• WO 9631239 discloses a medicament useful in the prevention and treatment of catharsis and stomach ulcer in a mammal, comprising a mixture of a pectin and a phospholipid
• Pectins are contained in large amounts in primary cell walls and intermediate lamella of a plant
• the main physiological activity of pectins is to connect and protect cell structures and to affect the water retention power
• a pectin consists of partial methyl esters of acids of polysaccharide and their sodium, potassium, calcium and ammonium
• the methyl ester group which is closely related to the functionality of the pectin can be easily hydrolyzed by alkali, and has various functions according to the rate of hydrolysis
• a pectin is easily hydrated and has a strong moisture absorbency
• a pectin forms a hydrophilic colloid solution in water and apparently has a high viscosity
• Pectins are currently used in many industries such as confectionery, food additives, dairy food and cosmetics
• One of the discovered activities of pectin is the prevention of poisoning by a heavy metal or a radioactive metal
• a pectin has an ability to form a superior complex with a heavy metal such as lead, Mercury, cadmium, molybdenum and manganese, and with a radioactive metal such as cobalt, strontium, cesium, zirconium and ruthenium Therefore, a pectin prevents metal poisoning and produces a superior effect during a long- term accumulation of metals within the body
• a pectin reduces cholesterol in serum and expedites the peristalsis of intestines, thereby removing constipation It also reduces the blood glucose level in a patient suffering from diabetes, and is effective in reducing weight and treating gastrointestinal disorders Such effects have been proven by experiments.
• pectins are used in the above indications and other applications of pectins are being studied
• the present invention can use pectins extracted from citruses, lemons, oranges, apples or the like, but is not limited to those pectins only. It is preferred to use a pectin extracted from a citrus.
• the chemical equation of a citrus pectin is given by [Equation 1 ]
• pectin for medical use used in this application is distinguished from a general lower pectin, and hereinafter refers to a pectin having the esterification degree (degree of methyl esterification of organic acids of a pectin) of less than 50.
• esterification degree degree of methyl esterification of organic acids of a pectin
• present invention is not to be limited to the medical use of a pectin (i.e., inhibition of a male's reproductive toxicity).
• the pectin used in the present invention can be prepared by a method disclosed in the applicant's earlier application, Korean Patent Application No. 10-1999-45200 (filed on October 19, 1999).
• a pectin is obtained by drying shells of a citrus, apple, orange, lemon or the like, cutting the dried shells into minute pieces, hydrolyzing and extracting a pectin, and concentrating and drying it by a membrane filler.
• the method also comprises the purifying step of treating the pectin sequentially with alkali and acid and removing moisture with alcohol.
• the present invention using a highly purified pectin prepared by the above method, can produce a superior effect in inhibiting a male's reproductive toxicity caused by environmental hormones including dioxins.
• male's reproductive toxicity used in this application means reduction of the reproductivity of a male such as reduction of the number of sperms, reduction of seminal fluid, decrease of the concentration of testosterone, reduced motility of sperms, increase of the number of modified sperms, genital malformation, prostate diseases, and other problems of the tissues relating to reproduction.
• a pharmaceutical composition comprising a pectin, more preferably, a pectin for medical use, is provided.
• a preferred example of the invention provides an oral pharmaceutical composition comprising a pectin for use in inhibiting a male's reproductive toxicity caused by environmental hormones. Therefore, a composition comprising a pectin can be prepared in a liquid formulation form such as gel, solution or suspension, or in a solid unit dose form such as a compressed tablet or a capsule. Methods of preparing such a composition in a liquid formulation or a solid unit dose form and vehicles used for the methods are publicly known in the relevant art. A dispersing agent, emulsifier, surfactant, flow controlling agent, preservative, modifier or the like can be additionally used within the scope of the present invention.
• the pharmaceutical composition of the present invention be preferably in an oral administration form
• nothing described in this application should be interpreted to narrow the administration path of the pharmaceutical composition
• a combined therapy is considered in the present invention. That is, it is possible to administer a pectin together with ingredients (e.g., ginseng extracts and green tea extracts) known to be effective in protecting reproductivity from environmental hormones.
• the pectin used in the present invention can be administered with a pharmaceutically acceptable carrier, preferably with a non-toxic carrier suitable for a particular administration method.
• the pectin can be formulated to be suitable for a known administration.
• Pectins can be formulated in various forms other than the above described medicament form, such as food including health supplement food and additives.
• formulations should contain a pectin in an amount sufficient to produce the inhibitory activity against a male's reproductive toxicity caused by environmental hormones including dioxins. Therefore, the pharmaceutical composition of the present invention can contain a pectin in an amount of l ⁇ m to 1000 mg per 1kg weight.
• the therapeutically effective amount of pectin is determined depending on the recipient's age, sex, state, diet, etc.
• the "therapeutically effective amount” means an amount effective to obtain a desired result according to the present invention without any pharmacologically adverse side effects.
• the desired result is the inhibition of the weight loss of epididymis, reduction of the number or motility of sperms, etc.
• the pectin can be administered in a single unit dose form or a divided multiple dose form.
• FIG. 1 is a graph illustrating the experimental groups.
• FIG. 2 is a graph illustrating the weight of epididymis showing the protective effect of a pectin against a male's reproductive toxicity caused by TCDD.
• FIG. 3 is a graph illustrating the weight of seminal vesicle showing the protective effect of a pectin against a male's reproductive toxicity caused by TCDD.
• FIG. 4 is a graph illustrating the motility of sperms showing the protective effect of a pectin against a male's reproductive toxicity caused by TCDD.
• FIG. 5 is a graph illustrating the number of sperms showing the protective effect of a pectin against a male's reproductive toxicity caused by TCDD.
• TCDD 2,3,7,8-tetrachlorodibenzo-p-dioxin
• the experimental groups consists of group (A) to which a pectin was administered from one week before the administration of TCDD, group (B) to which TCDD only was administered, and group (C) to which a physiological saline only was administered. These groups are shown in detail in FIG. 1. Analysis and Results
• the groups to which TCDD was administered showed the reduced ratio of prostate and seminal vesicle to the body weight when compared to the control group.
• the prostate was recovered by 31.2%.
• the right didymus with its skin peeled off was weighed, and put into a conical tube. 20 ml of sterile distilled water was poured into the tube. The didymus was homogenized and treated with ultrasonic for 5 minutes. 2 ml was taken and diluted five times by adding 8 ml of sterile distilled water. The diluted didymus was moved to a hemocytometer, and the number of sperms was counted through an optical microscope at x400. The expression is: number of sperms x square factor x hemocytometer factor x dilution factor/weight of didymus
• TCDD is known as the strongest environmental hormone among dioxins This test also showed that administration of TCDD results in remarkable reduction of the number of sperms, decrease of sperm motility, and weight loss of seminal vesicle and prostate
• a pectin inhibited the function of TCDD as an environmental hormone, and increased the number and motility of sperms and weight of seminal vesicle and prostate Therefore, it is clear that a pectin effectively protects the decrease of a male's reproductivity due to environmental hormones including dioxins
• a pectin has an inhibitory or prophylactic effect with respect to the weight loss of seminal vesicle and prostate and the reduction of the motility and number of sperms due to poisoning by dioxins Therefore, a pectin can be used as a prophylactic/therapeutic agent against the decrease of a male's reproductivity caused by environmental hormones including dioxins.

Landscapes

• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Molecular Biology (AREA)
• General Chemical & Material Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Reproductive Health (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Endocrinology (AREA)
• Epidemiology (AREA)
• Gynecology & Obstetrics (AREA)
• Pregnancy & Childbirth (AREA)
• Diabetes (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Priority Applications (4)

Applications Claiming Priority (2)

Publications (1)

Family

ID=19629145

Family Applications (1)

Country Status (7)

Cited By (3)

Families Citing this family (3)

Citations (1)

Family Cites Families (4)

• 1999
  • 1999-12-24 KR KR10-1999-0061538A patent/KR100401456B1/ko not_active IP Right Cessation
  • 1999-12-30 EP EP99962539A patent/EP1248637A4/en not_active Withdrawn
  • 1999-12-30 AU AU18954/00A patent/AU1895400A/en not_active Abandoned
  • 1999-12-30 BR BR9917601-7A patent/BR9917601A/pt not_active IP Right Cessation
  • 1999-12-30 JP JP2001548124A patent/JP2003518502A/ja active Pending
  • 1999-12-30 WO PCT/KR1999/000837 patent/WO2001047531A1/en not_active Application Discontinuation
  • 1999-12-30 CN CN99817060A patent/CN1398186A/zh active Pending

Patent Citations (1)

Non-Patent Citations (4)

Also Published As

Similar Documents

Legal Events