WO2008052432A1 - Médicament pour améliorer la qualité du sperme et traiter la stérilité chez l'homme - Google Patents

Médicament pour améliorer la qualité du sperme et traiter la stérilité chez l'homme Download PDF

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Publication number
WO2008052432A1
WO2008052432A1 PCT/CN2007/003048 CN2007003048W WO2008052432A1 WO 2008052432 A1 WO2008052432 A1 WO 2008052432A1 CN 2007003048 W CN2007003048 W CN 2007003048W WO 2008052432 A1 WO2008052432 A1 WO 2008052432A1
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WIPO (PCT)
Prior art keywords
vitamin
sperm
medicament
male infertility
quality
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PCT/CN2007/003048
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English (en)
Chinese (zh)
Inventor
Shengxian Huang
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Shengxian Huang
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Publication of WO2008052432A1 publication Critical patent/WO2008052432A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/07—Retinol compounds, e.g. vitamin A
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355—Tocopherols, e.g. vitamin E
    • 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
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/04—Sulfur, selenium or tellurium; Compounds thereof
    • 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

Definitions

  • the invention relates to a medicine for improving sperm quality and treating male infertility, in particular to a substance consisting of L-carnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomiphene, selenium citrate, A drug consisting of vitamin A acetate for improving sperm quality and treating male infertility.
  • a medicine for improving sperm quality and treating male infertility in particular to a substance consisting of L-carnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomiphene, selenium citrate, A drug consisting of vitamin A acetate for improving sperm quality and treating male infertility.
  • Li Gang and others of Chengdu Family Planning Technical Guidance Institute published a survey of sperm quality and anti-sperm antibodies in college students in Chengdu, after completing a survey of 295 college students in 12 colleges and universities in Chengdu.
  • the paper reveals that 99 people with abnormal sperm quality accounted for 33.56%; after expanding the scope to 549 college students in 14 colleges and universities, in the December 2003 issue of "Chinese Men's Science” published "549 students in Chengdu area”
  • the paper of the Quality Survey revealed that 204 people accounted for 37.16% of the abnormal sperm quality, and exclaimed that "the incidence of infertility in the future may be higher than the current report of 12%-16%, or even more than 1/3" .
  • the quality of sperm is reduced to the main reasons for male infertility:
  • underwear is too tight or wear tight leather pants, which not only oppress the male reproductive organs, affecting the normal development of the testicles, but also affect the sperm survival due to airtightness, no heat dissipation.
  • hot bath, suitable for sperm development is about 34 °C
  • high lake sperm development has adverse effects, therefore, should be careful to stay at high temperature for 4» hot bath, sauna, summer without air conditioning and long drive Wait.
  • sexual dysfunction such as impotence, premature ejaculation, no ejaculation, retrograde ejaculation, etc. will also affect male fertility.
  • An object of the present invention is to provide a medicament for improving sperm quality and treating male infertility, which is effective, convenient to take, and free from toxic side effects.
  • the medicament of the present invention is composed of the following components: L-carnitine, arginine, vitamin E, nucleotides, zinc gluconate, clomiphene, selenium citrate, vitamin A acetate.
  • the ratio of L-carnitine, arginine, vitamin E, nucleotide, glucose, clomiphene, selenium citrate, and vitamin A acetate in the legs of the present invention is from 140: 140: 7: 7: 3.5: 1 : 1 to 80: 80: 4: 4: 4: 2: 1: 1, the specific ratio can be 140: 140: 7: 7: 7: 3.5: 1: 1 to 100: 100: 5: 5: 5: 2.5 : 1: 1, can also be from 80: 80: 4: 4: 4: 2: 1: 1 to 100: 100: 5: 5: 5: 2.5: 1: 1.
  • the method for preparing the above-mentioned medicine for improving sperm quality and treating male infertility is constituted by the following steps: (1) according to L-carnitine, arginine, vitamin E, nucleotide, glucose art, clomiphene, lemon The ratio of acid selenium and vitamin A acetate is from 140: 140: 7: 7: 7: 3.5: 1: 1 to 80 ⁇ 80: 4: 4: 4: 2: 1: 1 Select qualified raw materials and mix the hooks (2) Adding U-shaped auxiliary symplectic _ «-mixed evenly; (3) After drying, it is made into an oral preparation.
  • the oral preparation of the fiber may be a tablet, a granule, a face lotion, or a soft capsule.
  • the present invention has the beneficial effects that: the components of the drug are a combination of pharmacological complementarity synergistically selected by the inventors through long-term exploration, and have obvious effects and no toxic side effects.
  • the components of the drug are a combination of pharmacological complementarity synergistically selected by the inventors through long-term exploration, and have obvious effects and no toxic side effects.
  • it can improve the penile erection strength, improve sperm quality, stabilize the genetic information of sperm, treat male infertility caused by sperm quality and quantity, improve fetal quality, and have remarkable curative effect (X-inch sperm improvement rate) About 80%); and can greatly reduce the cost of treatment without hospitalization, does not affect daily work and life, can be widely shed.
  • the invention can provide efficacy for the following populations:
  • the medicament of the present invention is composed of the following weight ratio components:
  • the ratio of L-carnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomiphene citrate, selenium citrate, vitamin A acetate is from 140': 140: 7: 7: 7: 3.5: 1: 1 to 80: 80: 4: 4: 4: 2: 1: 1 .
  • the role of each component is:
  • L-carnitine The role of L-carnitine is: (1) participate in sperm metabolism, improve vitality; (2) participate in the formation of sperm cell membrane, improve sperm integrity and life; (3) increase the number of sperm.
  • arginine The role of arginine is: (1) involved in sperm production, improve sperm quality and quantity; (2) increase the energy required for sperm cell metabolism, improve sperm vitality, prolong its survival time; (3) regulate testosterone and other reproductive hormones , improve sexual function and the speed and quantity of sperm production; (4) improve sperm production and utilization of ATP, improve sperm motility; (5), generate N0, leg penis erection.
  • vitamin E acetate deficiency can degeneration of testicular seminiferous tubules, leading to spermatogenic disorders; (2) inhibition of the oxidation products of prostaglandins that cause inflammation of male accessory inverted springs, thus avoiding Low sperm motility; (3) Anti-oxidation, stable sperm membrane, improved sperm quality and survival rate.
  • nucleotides The role of nucleotides is to: (1) increase the energy required for sperm cell metabolism, improve sperm motility; (2) as a genetic material in sperm, such as ribonucleic acid and DNA raw materials, to stabilize the genetic information of sperm Interest.
  • the role of zinc gluconate is to: (1) interfere with the absorption of toxic substances such as copper and lead, thereby reducing the toxicity of sperm; (2) participate in the formation of ⁇ , improve the quality and quantity of sperm; (3) improve the vitality of sperm, anti- Oxidation, stabilize sperm membrane, improve sperm quality and survival rate; (4) immune regulation function, positive for sperm anti-sperm antibody positive, serum anti-sperm antibody positive infertility; (5) reduce inflammation, caused by seminal vesicle 3 ⁇ 4 seminal vesicle Infertility is effective.
  • clomiphene The effects of clomiphene are: (1) increase the secretion of gonadotropin-releasing hormone in the hypothalamus and increase the secretion of gonadotropin in the pituitary gland, thereby improving the spermatogenic ability of the testis, facilitating the production of sperm and increasing the number of sperm; (2) regulating testosterone, etc. Reproductive 3 ⁇ 43 ⁇ 4, improving sexual function and speed and quantity of sperm production.
  • Selenium is one of the essential trace elements in human growth and development. Selenium is mainly concentrated in the testis and prostatic vas deferens, and two kinds of sesame isoforms are produced. Selenium is used at home and abroad. The medical profession and the nutrition community respect it as "life fire”; (2) eliminate harmful substances in the body, protect tissues from toxic substances, and resist harmful metal elements in the body; (3) improve sperm motility. (4) Selenium can be excreted together with semen to cause selenium-deficient infertility, which must be supplemented.
  • the role of vitamin A is to promote sperm production and improve sperm motility.
  • the preparation of the medicament of the present invention should be carried out on the GMP-compliant oral preparation production line, and the steps are as follows: (1) According to L-carnitine, arginine, vitamin E, nucleotide, zinc gluconate, clomiphene, selenium citrate The ratio of vitamin A acetate is from 140: 140: 7: 7: 7: 3.5: 1: 1 to 80: 80: 4: 4: 4: 2: 1: 1 Select the qualified raw materials to mix and hook; (2) Adding the shaped auxiliary material and mixing again; (3) drying to prepare an oral preparation. Oral preparations are prepared into tablets, granules, vinegars, and soft capsules according to equipment and market needs.
  • the method of taking the medicament of the present invention is as follows: Each bed is warmed before going to bed, one dose at a time, and the course of treatment is 3 months.

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

Abstract

L'invention concerne un médicament pour améliorer la qualité du sperme et traiter la stérilité chez l'homme. Le médicament est composé de lévocarnitine, d'arginine, de vitamine E, de nucléotide, de gluconate de zinc, de clomifène, de citrate de sélénium et d'acétate de vitamine A, et le rapport de ces composants est de 140: 140: 7: 7: 7: 3,5: 1: 1 à 80: 80: 4: 4: 4: 2: 1: 1. Le procédé de préparation dudit médicament comprend les étapes consistant à : (1) mélanger les composants du médicament uniformément dans le rapport, (2) ajouter des excipients et mélanger à nouveau, (3) sécher et formuler en une préparation orale. Les composants du médicament ont un effet synergique.
PCT/CN2007/003048 2006-10-27 2007-10-26 Médicament pour améliorer la qualité du sperme et traiter la stérilité chez l'homme WO2008052432A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CNA2006101426609A CN101167735A (zh) 2006-10-27 2006-10-27 一种用于提高精子质量、治疗男性不育症的药物
CN200610142660.9 2006-10-27

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITTO20090515A1 (it) * 2009-07-09 2011-01-10 Mastelli S R L Composizione per il trattamento di infertilita' maschile
CN112544987A (zh) * 2020-12-03 2021-03-26 山东腾贵医药有限公司 一种提高精子活性的组合物及其制备方法和应用

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101953844A (zh) * 2010-02-28 2011-01-26 黄胜先 一种用于提高精子质量、治疗男性不育症的药物
CN104083468B (zh) * 2014-05-31 2016-06-29 山东欣希安药业股份有限公司 一种治疗男性少精弱精、提高精子质量的药物
CN106074598A (zh) * 2016-06-14 2016-11-09 奥格生物技术（六安）有限公司 一种治疗精液异常男性不育症的复方有机螯合微量元素组合物及其制备方法

Citations (2)

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JPS5793913A (en) * 1980-12-03 1982-06-11 Ajinomoto Co Inc Enhancing agent for spermous vital power
WO2003086080A1 (fr) * 2002-04-08 2003-10-23 The Daily Wellnes Company Procede et composition d'amelioration de la fertilite chez des humains et des animaux males et femelles

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
JPS5793913A (en) * 1980-12-03 1982-06-11 Ajinomoto Co Inc Enhancing agent for spermous vital power
WO2003086080A1 (fr) * 2002-04-08 2003-10-23 The Daily Wellnes Company Procede et composition d'amelioration de la fertilite chez des humains et des animaux males et femelles

Non-Patent Citations (9)

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Title
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IANNIELLO B. ET AL.: "Support therapy with integators after varicocelectomy", GIORNALE ITALIANO DI OSTETRICIA E GINECOLOGIA, vol. 26, no. 12, 2004, pages 469 - 472 *
LV H. ET AL.: "Clinical observation on levocarnitine in the treatment of asthenozoospermia and oligoashtenozoospermia", NATIONAL JOURNAL OF ANDROLOGY, vol. 11, no. 6, June 2005 (2005-06-01), pages 470 - 476 *
SHI Y. ET AL.: "Effects of Xinxibao on Sperm Quality in Oligosthenozoospermic Men", NATIONAL JOURNAL OF ANDROLOGY, vol. 10, no. 10, October 2004 (2004-10-01), pages 758 - 760 *
ZHANG D.-T. ET AL.: "Clinical study of Zn-complex glucose acid as an adjuvant drug for the treatment of the male infertility due to seemen of poor quality", CHINESE JOURNAL OF UROLOGY, vol. 24, no. 8, August 2003 (2003-08-01), pages 564 - 567 *
ZHAO H. ET AL.: "Advances in the nutritional and physiological effect of exogenous nucleotides", ACTA ZOONUTRIMENTA SINICA, vol. 15, no. 4, December 2003 (2003-12-01), pages 7 - 11 *
ZHOU Q. ET AL.: "Clinical observation on JING AN capsule in the treatment of male infertility (104 examples)", THE CHINESE JOURNAL OF HUMAN SEXUALITY, vol. 14, no. 4, April 2005 (2005-04-01), pages 21 - 23 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITTO20090515A1 (it) * 2009-07-09 2011-01-10 Mastelli S R L Composizione per il trattamento di infertilita' maschile
CN112544987A (zh) * 2020-12-03 2021-03-26 山东腾贵医药有限公司 一种提高精子活性的组合物及其制备方法和应用

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