WO1994013289A1 - Compose pharmaceutique a proprietes antiulcereuses - Google Patents

Compose pharmaceutique a proprietes antiulcereuses Download PDF

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Publication number
WO1994013289A1
WO1994013289A1 PCT/RU1992/000235 RU9200235W WO9413289A1 WO 1994013289 A1 WO1994013289 A1 WO 1994013289A1 RU 9200235 W RU9200235 W RU 9200235W WO 9413289 A1 WO9413289 A1 WO 9413289A1
Authority
WO
WIPO (PCT)
Prior art keywords
drug
cimetidine
ulcers
stomach
gastric
Prior art date
Application number
PCT/RU1992/000235
Other languages
English (en)
Russian (ru)
Inventor
Mikhail Emmanuilovich Kaminka
Svetlana Mikhailovna Tupikina
Mikhail Davydovich Mashkovsky
Semen Davidovich Groisman
Vladimir Grigorievich Kukes
Alexei Konstantinovich Starodubtsev
Vladimir Ioirovich Volchenok
Original Assignee
Tsentr Po Khimii Lekarstvennykh Sredstv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Tsentr Po Khimii Lekarstvennykh Sredstv filed Critical Tsentr Po Khimii Lekarstvennykh Sredstv
Priority to PCT/RU1992/000235 priority Critical patent/WO1994013289A1/fr
Publication of WO1994013289A1 publication Critical patent/WO1994013289A1/fr

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom

Definitions

  • the invention relates to the area of the medin, and more precisely to a new drug product
  • a wide range of drugs is known that are used in the treatment of peptic ulcer disease and duodenal ulcers, such as chronic disease; antacids (almagel, ⁇ costume ⁇ -
  • Cimetidine is considered to be the standard drug among the indicated. Cimetidine is a strong inhibitor of the gastric tract, it suppresses the effect of the secretion - pentagastrin, histamine. The endoscopic treatment of cimetidine showed that
  • the beneficial and antisense activity of the aforementioned substance is unknown.
  • the inventive drug is a new one and is not described in the literature.
  • the inventive drug can be used in any other pharmaceutical form.
  • Pre-10 is a good practice for using the claimed product in the form of a tablet.
  • the inventive product in the form of a tablet, according to the invention contains a valid substance in the amount of 0.025-0.05 g per one tablet. 15
  • the inventive preparation exhibits a high effective activity, due to the effectiveness and the effect of this is the result of a known harmful process. It also indicates an inhibitory effect on the gastric secretion, reduces the volume of the secretion and contains 20 free saline acids.
  • the claimed drug in the absence of cimetidine does not possess the "syndrome of reversal", that is, after its elimination, the disease is not observed.
  • the claimed ⁇ e- ⁇ a ⁇ a ⁇ ⁇ e ⁇ mendue ⁇ sya is ⁇ lz ⁇ va ⁇ for ⁇ e ⁇ a ⁇ ii and ⁇ i- 25 la ⁇ i ⁇ i v ⁇ s ⁇ ali ⁇ elny ⁇ , gem ⁇ giches ⁇ i ⁇ , e ⁇ zivny ⁇ ⁇ v ⁇ ezhdeny slizis ⁇ y ⁇ b ⁇ l ⁇ ch ⁇ i zhelud ⁇ chn ⁇ - ⁇ ishechn ⁇ g ⁇ ⁇ a ⁇ a and yazvenny ⁇ ⁇ v ⁇ ezhdeny slizis ⁇ y ⁇ b ⁇ l ⁇ ch ⁇ i ⁇ i- schev ⁇ da, and zhelud ⁇ a dvenadtsa ⁇ i ⁇ e ⁇ s ⁇ n ⁇ y ⁇ ish ⁇ i.
  • the inventive preparation was tested in experiment 30 on live and in the clinic for people.
  • the susceptible activity of the claimed drug was studied on different experimental models of gastric ulcer in mice and mice. For specific indicators of the effect of the claimed drug 5
  • ED 50 of the claimed preparation when administered internally is 6.4 mg / kg
  • ED 50 of cimetidine is 35 mg / kg internally.
  • the Declared drug or cimetidine was administered internally in the form of an aqueous suspension from tween-80 for the first hour before the introduction of serotonin (10 mg per round, internal tire). Each dose of the claimed drug or cimetidine was administered 10 times.
  • the target action is already at a dose of 25 mg / kg, when cimetidine exhibits such an effect only at a dose of 100 mg / kg.
  • ED 0 of the claimed formulation is 27 mg / kg internally, ED 0 of cimetidine is 100 mg / kg internally.
  • the claimed appliance is manufactured
  • Delivered Doses Average%% Delivered, erosion on alternate samples mg / kg live (in case of ulcer, 10 times less than 5 days ago)
  • test data are presented in table 7. - 12 -
  • ⁇ a ⁇ vidn ⁇ of ⁇ ablitsy 7 claimed ⁇ e ⁇ a ⁇ a ⁇ (in zavisim ⁇ s ⁇ i ⁇ d ⁇ z) ⁇ edu ⁇ ezhdae ⁇ ⁇ b ⁇ az ⁇ vanie ulcers are caused by a ⁇ imm ⁇ bilizatsiey s ⁇ che ⁇ anii with ⁇ l ⁇ d ⁇ m.
  • Cimetidine 10 18 27.4 + 3.799.2 ⁇ ⁇ , 65.0 + 0.65
  • the claimed preparation also, like cimetidine, accelerates the healing of the ulcerative 15 defect in comparison with the oncological group.
  • 25 or cimetidine was administered as 10 animals. After an ethereal rush, they opened an abdominal cavity and put a ligature on the patient’s stomach. After 4 hours after the operation, the animals were killed, the stomach was removed, they shared its volume and the presence of a free salt
  • the claimed invention does not indicate - 16 - impact on civils, does not change hematologic indices, does not affect the biological indicators of physical and urinary dynamics, does not cause any changes.
  • the receptor for cimetidine has a low toxicity; does not have expressed side effects; It does not possess an immune, allergenic, mutagenic sensitizing effect.
  • the inventive preparation was tested in a clinic for people with hepatic, erosive injuries of a mucous obstruction of the gastric tract; with the ulcerated niche of the stomach and duodenal ulcer.
  • the inventive preparation is manufactured by known methods.
  • the substance in question is claimed to be 35 (hiauklidil-3) -di- (thienyl-2) carbine or it may have been received by the following method. - 18 -
  • the essential product separates, the acidic product is alkalized and processed, the refrigerant is removed and the target product is isolated.
  • the inventive device may be used in any other medicinal form, for example in the form of a tablet, a payment, capsules and other.
  • the inventive preparation is preferable to use 15 tablets for meals inside (containing 0.025 or 0.05 grams of the preparation) 2-4 times a day before meals (last).
  • the daily dose of the drug is up to 0.3 g; Acupuncture treatment ⁇ 2 to 6 weeks. 20 Prophylactically or in a cost-effective manner, the claimed medication is prescribed
  • the inventive drug should not be used for pregnancy, glaucoma, adenoma of the prostate gland.
  • the inventive product may be used in conjunction with alkalizing and enhancing substances (30 active sedative components do not amplify the claimed medicinal product).
  • the inventive drug is used in medicine for the treatment and treatment of erosion of the mucous membrane of the stomach and intestine, which develops due to the incidence of the disease.
  • the inventive product possesses a high active activity. Due to the efficiency and speed of the process, it eliminates the known preparation of cimetidine. It indicates an inhibitory effect on the biliary tract, reduces the content of free salt.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Composé pharmaceutique à propriétés antiulcéreuses, consistant en une substance active, le (quinuclidile-3)-di-(thiényl-2)carbinol, de la formule (I) ou sels de cette substance, en combinaison avec un excipient pharmaceutique. Ce composé se révèle utile pour prévenir et traiter les inflammations, les hémorragies ou les affections érosives de la membrane muqueuse des parties supérieures de l'appareil gastrointestinal et les affections ulcéreuses de l'estomac et du duodénum.
PCT/RU1992/000235 1992-12-10 1992-12-10 Compose pharmaceutique a proprietes antiulcereuses WO1994013289A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/RU1992/000235 WO1994013289A1 (fr) 1992-12-10 1992-12-10 Compose pharmaceutique a proprietes antiulcereuses

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU1992/000235 WO1994013289A1 (fr) 1992-12-10 1992-12-10 Compose pharmaceutique a proprietes antiulcereuses

Publications (1)

Publication Number Publication Date
WO1994013289A1 true WO1994013289A1 (fr) 1994-06-23

Family

ID=20129741

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/RU1992/000235 WO1994013289A1 (fr) 1992-12-10 1992-12-10 Compose pharmaceutique a proprietes antiulcereuses

Country Status (1)

Country Link
WO (1) WO1994013289A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2390956A1 (fr) * 1977-05-16 1978-12-15 Hokuriku Pharmaceutical Derives substitues de la quinolizidine et de l'indolizidine, leur procede de preparation et agents therapeutiques contenant lesdits derives
FR2531955A1 (fr) * 1982-08-17 1984-02-24 Pharmuka Lab Nouveau procede de preparation de derives de la quinuclidine substitues en position 3
US4650804A (en) * 1984-03-30 1987-03-17 Fujisawa Pharmaceutical Co., Ltd. Quinolizinone compounds and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents
US4843074A (en) * 1988-05-17 1989-06-27 Marion Laboratories, Inc. 1-azabicyclo[2.2.2]octan-3-yl 2-aryl-3-azacyclo-2-hydroxypropionates and their quaternary salts

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2390956A1 (fr) * 1977-05-16 1978-12-15 Hokuriku Pharmaceutical Derives substitues de la quinolizidine et de l'indolizidine, leur procede de preparation et agents therapeutiques contenant lesdits derives
FR2531955A1 (fr) * 1982-08-17 1984-02-24 Pharmuka Lab Nouveau procede de preparation de derives de la quinuclidine substitues en position 3
US4650804A (en) * 1984-03-30 1987-03-17 Fujisawa Pharmaceutical Co., Ltd. Quinolizinone compounds and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents
US4843074A (en) * 1988-05-17 1989-06-27 Marion Laboratories, Inc. 1-azabicyclo[2.2.2]octan-3-yl 2-aryl-3-azacyclo-2-hydroxypropionates and their quaternary salts

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