WO2010125408A2 - Prostata-norm rectal suppositories for the treatment of prostatitis - Google Patents

Prostata-norm rectal suppositories for the treatment of prostatitis Download PDF

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Publication number
WO2010125408A2
WO2010125408A2 PCT/GE2010/000002 GE2010000002W WO2010125408A2 WO 2010125408 A2 WO2010125408 A2 WO 2010125408A2 GE 2010000002 W GE2010000002 W GE 2010000002W WO 2010125408 A2 WO2010125408 A2 WO 2010125408A2
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Prior art keywords
treatment
prostatitis
suppositories
prostata
norm
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PCT/GE2010/000002
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French (fr)
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WO2010125408A3 (en
Inventor
Giorgi Gogbaidze
Natalia Gogbaidze
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Giorgi Gogbaidze
Natalia Gogbaidze
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Publication of WO2010125408A2 publication Critical patent/WO2010125408A2/en
Publication of WO2010125408A3 publication Critical patent/WO2010125408A3/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0031Rectum, anus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/61Myrtaceae (Myrtle family), e.g. teatree or eucalyptus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/48Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482Serine endopeptidases (3.4.21)
    • A61K38/4826Trypsin (3.4.21.4) Chymotrypsin (3.4.21.1)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate

Definitions

  • the invention refers to medicine, in particular to urology and concerns rectal suppositories that are used for the treatment of prostatitis.
  • the ratio of active ingredients in grams per one suppositoiy up to 2 g is as follows: Dipotassium glycyrrhizinate 0.025 - 0.1
  • the unity of medicinal properties of said components makes it possible to create rectal suppositories of high therapeutic efficacy. It is characterized with a wide spectrum of biologic activities including anti-inflammatory, antibacterial, antiviral, immune modulating effects and is composed of organic, mostly natural substances, without known toxicity.
  • the process of preparing of suppositories comprises the following steps: first the three components - dipotassium glycyrrhizinate, chymotrypsin in crystalline form and tea tree oil are mixed together. Then the diphyllic base Witepsol H- 15 is added to the resulted mixture and stirred until substance becomes homogenous. As a final step the homogenous mass is poured into the preformed patterns to obtain suppositories.
  • composition in grams per one suppository up to 2 g.:
  • composition in grams per one suppository up to 2 g.: Dipotassium glycyrrhizinate 0.05
  • Chymotrypsin in crystalline form 0.015 Tea tree oil 0.025
  • composition in grams per one suppository up to 2 g.:
  • Tea tree oil 0.015 Witepsol H- 15 up to 2 Suppository has a yellowish color and has a smell characteristic of a tea tree oil, and it weighs about 1.5 -2 g. Suppositories can be kept for 2 years; they retain their biologic activity for this long if kept in cool place.
  • the trade name of the suppository is "PROSTATA-NORMA", it is registered in Georgia as a trade mark N° M 18263. Therapeutic efficacy of the drug was investigated in several hundreds of patients with prostatitis.
  • Example 1 Patient - male, of age 32, clinical diagnosis: chronic prostatitis of 4 years duration.
  • the patient was prescribed 20 suppositories PROSTATA-NORMA, 2 times a day for 10 days.
  • PRO ST AT A-NORM A is highly effective drug with prominent anti-inflammatory, antibacterial, antiviral and immune modulating activities. It also has high permeability in the prostate gland tissues.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Mycology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Microbiology (AREA)
  • Organic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

The invention refers to medicine, in particular to urology and concerns rectal suppositories that are used for the treatment of prostatitis. The technical result of this invention is widening of assortment of medicinal means for treatment of prostatitis and the reduction of treatment duration. The technical result is achieved in that suppositories contain dipotassium glycyrrhizinate, chymotrypsin in crystalline form, tea tree oil (pharmaceutical form) and diphyllic base.

Description

PROSTATA-NORM RECTAL SUPPOSITORIES FOR THE TREATMENT OF PROSTATITIS
The invention refers to medicine, in particular to urology and concerns rectal suppositories that are used for the treatment of prostatitis.
Currently, several medications are known, in the form of rectal suppositories that are used for the treatment of prostatitis, namely, "Vitaprost" and "Prostatilen" that are approved for clinical use in Russia by the Register of Medicinal Means of Russia (Register of Medicinal Means of Russia "LSP" Moscow, LSR, 2008, p. 293, 815). As an active ingredient these suppositories contain dry extract, obtained from prostate glands of sexually mature animals, that is free of androgen and estrogen hormones and proteins. These suppositories are not characterized with high therapeutic efficacy, possibly because they contain only one active component. There is also another medication, manufactured in Georgia, called "Suppositories for the treatment of prostatitis" (Georgian patent N° 4646, published in the Official Bulletin N°5 on 10.11.2008). This medication contains alcoholic extracts of Calendula and Achillea grisea virens, alcoholic solution of Propolis and Cocoa oil. The treatment by these suppositories is a lengthy process. The technical result of the present invention is widening of assortment of medicaments for treatment of prostatitis and reduction of treatment period. The technical result is achieved in that the medication contains dipotassium glycyrrhizinate , being the derivative of glycyrrhizinic acid, (M.D. Mashkovskyi, "Medicinal Remedies", Moscow, "Medicine", year 2008, Tl-2, pg. 359), chymotrypsin in crystalline form, (proteolytic enzyme) (M.D. Mashkovskyi, "Medicinal Remedies", Moscow, "Medicine", year 2008, Tl-2, pg. 651), tea tree oil (pharmaceutical form) and diphyllic base, thus as a diphyllic base is used Witepsol H-15.
The ratio of active ingredients in grams per one suppositoiy up to 2 g is as follows: Dipotassium glycyrrhizinate 0.025 - 0.1
Chymotrypsin, chrystalline form 0.01- 0.02 Tea tree oil (Melaleucae aetheroleum) 0.015 - 0.05 Witepsol H- 15 up to 2
The unity of medicinal properties of said components makes it possible to create rectal suppositories of high therapeutic efficacy. It is characterized with a wide spectrum of biologic activities including anti-inflammatory, antibacterial, antiviral, immune modulating effects and is composed of organic, mostly natural substances, without known toxicity.
This medicinal means has high permeability in prostate gland tissues in very short period of time. The process of preparing of suppositories comprises the following steps: first the three components - dipotassium glycyrrhizinate, chymotrypsin in crystalline form and tea tree oil are mixed together. Then the diphyllic base Witepsol H- 15 is added to the resulted mixture and stirred until substance becomes homogenous. As a final step the homogenous mass is poured into the preformed patterns to obtain suppositories. Specific examples of preparing suppositories:
Example 1
Composition in grams per one suppository up to 2 g.:
Dipotassium glycyrrhizinate 0.1
Chymotrypsin in chrystaline form 0.02 Tea tree oil 0.05
Witepsol H- 15 up to 2
Example 2
Composition in grams per one suppository up to 2 g.: Dipotassium glycyrrhizinate 0.05
Chymotrypsin in crystalline form 0.015 Tea tree oil 0.025
Witepsol H- 15 up to 2
Example 3
Composition in grams per one suppository up to 2 g.:
Dipotassium glycyrrhizinate 0.025
Chymotrypsin in crystalline form 0.01
Tea tree oil 0.015 Witepsol H- 15 up to 2 Suppository has a yellowish color and has a smell characteristic of a tea tree oil, and it weighs about 1.5 -2 g. Suppositories can be kept for 2 years; they retain their biologic activity for this long if kept in cool place. The trade name of the suppository is "PROSTATA-NORMA", it is registered in Georgia as a trade mark N° M 18263. Therapeutic efficacy of the drug was investigated in several hundreds of patients with prostatitis.
The obtained data analysis showed substantial improvement in 90% of research population and the obvious improvement in 10% of the study population.
In the course of the treatment there was significant reduction and in some cases the total disappearance of pain, disorders of urination, improvement of lab test results (urinalysis and analysis of prostate gland secretions), in many cases improvement of sexual functions were observed. The above stated results obviate the high therapeutic efficacy of this particular drug.
The real cases from clinical practice of treatment with PROSTAT A-NORM suppositories:
Example 1. Patient - male, of age 32, clinical diagnosis: chronic prostatitis of 4 years duration.
Chief complaints: pain in pubic and inguinal areas, pain is getting worse after sexual intercourse. Sexual dysfunction, in particular premature ejaculation and diminished arousal.
Frequent urination, pain at the end of urination, easy fatigability, anxiety and sleep disorders.
On physical examination: digital rectal examination of prostate gland resulted in enlarged, swollen and painful gland. Margins of the gland are irregular.
Microscopic analysis of prostate gland secretions: visual field is covered with leukocytes, there is marked reduction of lecithin granules and the amount of epithelial cells is increased.
Bacteriologic analysis of the prostate gland secretions: revealed abundant pathogenic E.coli in specimen.
The patient was prescribed 20 suppositories PROSTATA-NORMA, 2 times a day for 10 days.
In 5-7 days of treatment there was significant clinical improvement, pain and urination problems diminished, on the 10th day of treatment microscopic analysis of prostate gland secretions showed the normal range of leukocytes in the visual field (6-8 un the visual field). At the completion of the treatment course sexual function was significantly improved, duration of sexual intercourse increased to 5-8 minutes. One year has passed since the treatment completion and the patient feels healthy. Example 2. Patient - male, of age 41 , clinical diagnosis: chronic prostatitis of 7 years duration.
Chief complaints: pain in inguinal area, pain is referred to the right testis and sacrum. Frequent urination, 8 times a day in the daytime and 12 times a day in the nighttime, there is sticky, mucosal discharge from the urethra after defecation and during straining. Diminished arousal and decreased duration of sexual intercourse, that resulted in sexual disharmony between spouses and the frequency of sex decreased to one time in 2 weeks.
Patient tried many treatment options including antibiotic therapy, antibacterial drugs and prostate gland massage.
On physical examination: digital rectal examination of prostate gland resulted in enlarged, swollen and painful gland of non-homogenous consistency, with dense and softened areas. Microscopic analysis of prostate gland secretions: there is significant leukocytosis that is arranged in clusters prominent reduction of lecithin granules. Bacteriologic analysis of the prostate gland secretion: revealed abundant S. aureus in specimen. The combined multimodal approach to the treatment included suppositories PROSTATA- NORMA, 2 times a day for 10 days, specific physio-therapeutic procedures and antibacterial drugs. The patient's condition improved significantly, pain and prostatorrhea has disappeared, urination process became normal and on follow-up bacterial analysis S. aureus was not identified. On microscopy leukocytes are in normal range (5-7 in visual field), arousal quality is improved and duration is increased up to 10 min. To consolidate the positive results the second treatment course was administered. After one year the patient feels healthy and his sexual life is normal. Example 3. Patient - male, of age 28, clinical diagnosis: chronic prostatitis of 5 years duration. Chief complaints: pain in the perineal area, that is referred to the sacrum, frequent urination, sense of incomplete emptying of the bladder, diminished arousal, premature ejaculation, pain during orgasm, reduced libido. Because of the sexual problems patient developed "neurosis of anticipated failure", he attempted treatment several times but no desirable results were achieved. On physical examination: digital rectal examination of prostate gland resulted in enlarged, swollen and painful gland. Inter-lobar septum is evened out; there is a palpable density in the left lobe, of a size of a grain. Gland is of non-homogenous consistency.
Microscopic analysis of prostate gland secretions: visual field is completely covered with leukocytes. Bacteriologic analysis of the prostate gland secretions: revealed Proteus mirabillis vulgaris in specimen that was highly sensitive to most of antibiotics.
As a result of treatment, mainly including PRO ST AT A-NORM A suppositories and antibiotics and laser therapy patient improved significantly. Pain and urination problems were gone, sexual function and the quality of sexual intercourse normalized, that was of particular importance to the patient. Results of the follow-up microscopic and bacteriologic analysis revealed leukocytes in normal range and no pathogenic bacteria. After one year patient is healthy and there were no recurrences of the symptoms during this period.
According to these case reports we can conclude that PRO ST AT A-NORM A is highly effective drug with prominent anti-inflammatory, antibacterial, antiviral and immune modulating activities. It also has high permeability in the prostate gland tissues.

Claims

Claims
1. Suppositories for the treatment of prostatitis comprising an active ingredient and the base, characterized in that as an active ingredient it contains dipotassium glycyrrhizinate, chymotrypsin in crystalline form, tea tree oil and diphyllic base.
2. Suppository according to Claim 1 characterized in that as a diphyllic base it contains Witepsol H-15.
3. Suppository for treatment of prostatitis according to claims 1 , 2 characterized in that it contains the components in the following ratio per one suppository of the weight 2g: Dipotassium glycyrrhizinate 0.025 - 0.1
Chymotrypsin in crystalline form 0.01- 0.02
Tea tree oil 0.015 - 0.05
Witepsol H-15 up to 2
PCT/GE2010/000002 2009-05-01 2010-04-23 Prostata-norm rectal suppositories for the treatment of prostatitis WO2010125408A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GEAP200911241A GEP20115319B (en) 2009-05-01 2009-05-01 Rectal suppositories for treatment of prostate “prostate-norm”
GEAP2009011241 2009-05-01

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WO2010125408A2 true WO2010125408A2 (en) 2010-11-04
WO2010125408A3 WO2010125408A3 (en) 2011-03-03

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Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0597680A (en) * 1991-10-04 1993-04-20 Sanwa Kagaku Kenkyusho Co Ltd Glycyrrhizin suppository
CN1134293A (en) * 1995-04-28 1996-10-30 丁志敏 Method for producing Chinese and western medicine synthetic injection for treating prostatitis and hyperplasia
CN1326780A (en) * 2001-06-02 2001-12-19 辛耀禄 Medicinal capsule for cuirng male sterility and its preparing process
CN1520842A (en) * 2003-01-29 2004-08-18 谢殿左 Liposoluble suppository for treating prostatitis
CN1562218A (en) * 2004-04-13 2005-01-12 云大科技股份有限公司 Medication combination of compound tea tree oil for preventing or curing inflammation of human genital tract
CN1317001C (en) * 2005-07-28 2007-05-23 谢作印 Compound essential oil for treating prostatitis

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
M.D. MASHKOVSKYI, MEDICINAL REMEDIES, vol. TI-2, 2008, pages 651
M.D. MASHKOVSKYI, MEDICINAL REMEDIES, vol. TL-2, 2008, pages 359
REGISTER OF MEDICINAL MEANS OF RUSSIA, 2008, pages 293815

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WO2010125408A3 (en) 2011-03-03

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