WO2000010562A1 - Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production - Google Patents

Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production Download PDF

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Publication number
WO2000010562A1
WO2000010562A1 PCT/RU1998/000269 RU9800269W WO0010562A1 WO 2000010562 A1 WO2000010562 A1 WO 2000010562A1 RU 9800269 W RU9800269 W RU 9800269W WO 0010562 A1 WO0010562 A1 WO 0010562A1
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WO
WIPO (PCT)
Prior art keywords
ranitidine
ρaniτidina
gidροχlορida
πρi
ray
Prior art date
Application number
PCT/RU1998/000269
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English (en)
Russian (ru)
Other versions
WO2000010562A8 (fr
Inventor
Nikolai Borisovich Leonidov
Svetlana Igorevna Uspenskaya
Alexandr Borisovich Krasnokutsky
Original Assignee
Leonidov Nikolai B
Svetlana Igorevna Uspenskaya
Krasnokutsky Alexandr Borisovi
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 Leonidov Nikolai B, Svetlana Igorevna Uspenskaya, Krasnokutsky Alexandr Borisovi filed Critical Leonidov Nikolai B
Priority to RU2001105137/14A priority Critical patent/RU2203048C2/ru
Priority to PCT/RU1998/000269 priority patent/WO2000010562A1/fr
Priority to AU15136/99A priority patent/AU1513699A/en
Priority to RU2001105137/15K priority patent/RU2385155C2/ru
Publication of WO2000010562A1 publication Critical patent/WO2000010562A1/fr
Publication of WO2000010562A8 publication Critical patent/WO2000010562A8/fr

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Definitions

  • the invention is related to the field of medicine, in particular, for pharmaceutical chemistry.
  • a new stable x-ray form of ranitidine hydride, possessing the properties of ⁇ 2 - block is described.
  • the new format is physically stable and has a more pronounced, effective ulcerative effect compared to previously known crystalline forms.
  • ranitidine hydrochloride which is a patent of the United States, 45g4521431 and ⁇ 24672133, has been described and patented.
  • ⁇ vysheu ⁇ azanny ⁇ is ⁇ chni ⁇ a ⁇ ⁇ mechae ⁇ sya nev ⁇ zm ⁇ zhn ⁇ s ⁇ ⁇ izv ⁇ ds ⁇ va ⁇ is ⁇ alliches ⁇ y ⁇ my 1 ⁇ ani ⁇ idina gid ⁇ l ⁇ ida in ⁇ mme ⁇ ches ⁇ m massh ⁇ abe and b ⁇ lee ⁇ g ⁇ , ⁇ ma 1 yavlyae ⁇ sya nes ⁇ abiln ⁇ y and sam ⁇ izv ⁇ ln ⁇ ⁇ e ⁇ e ⁇ di ⁇ in s ⁇ abilnuyu ⁇ mu 2 ⁇ ichem ⁇ chen bys ⁇ .
  • the installation is carried out by the addition of an ethyl acetate.
  • This process is unsatisfactory due to its characteristics - from the aforementioned solvents (ethyl acetate and ethanol), the form 1 of ranitidine is hydrochloride. This makes the process indispensable for use on a commercial scale.
  • Pa ⁇ en ⁇ SSH ⁇ ⁇ .5338871 ⁇ isyvae ⁇ ⁇ ig ⁇ vlenie chis ⁇ y ⁇ my 1 ⁇ ani ⁇ idina gid ⁇ l ⁇ ida ⁇ u ⁇ em ⁇ as ⁇ v ⁇ eniya ⁇ ani ⁇ idina gid ⁇ l ⁇ ida in ⁇ as ⁇ v ⁇ i ⁇ eley mixture s ⁇ de ⁇ zhaschey least ⁇ dn ⁇ g ⁇ nizsheg ⁇ ali ⁇ a ⁇ iches ⁇ g ⁇ s ⁇ i ⁇ a, a ⁇ ma ⁇ iches ⁇ y uglev ⁇ d ⁇ d and initsia ⁇ ⁇ is ⁇ allizatsii as za ⁇ dyshevy ⁇ ⁇ is ⁇ all ⁇ v chis ⁇ y ⁇ my 1 ⁇ ani ⁇ idina gid ⁇ l ⁇ ida.
  • Patent ⁇ .562P20 describes various types of modifiers that differ in process characteristics - - Form 1, 2 Form 2, and standard.
  • the object of the invention is to produce a physically stable form of ranitidine hydroulhoid, possessing an increased activity of the drug.
  • the invention is also a method of obtaining a new X-ray framed form.
  • lower fatty alcohol in particular, ethyl alcohol.
  • ranitidine is hydrated in comparison with the previously known poliomyopathy and various compounds of the oversensitive
  • Fig. 1 The first-party x-ray of the declared x-ray form of ranitidine hydrochloride.
  • ranitidine hydride ( ⁇ XXIII ⁇ Brassss SWyssap ⁇ ) is dissolved in 470 g of distilled water at a temperature of 75 ° ⁇ and it is cooled to freeze the product.
  • the frozen mass is mechanically crushed and the temperature of the frozen food product is not more than 5 mm in size, and then it is dried at a pressure of "1 mm.
  • the X-ray analysis was carried out on an automated, simple diffractometer.
  • Shooting conditions CI ⁇ radiation, a large amount of video for quick start, corner angles from 4 to 64 2 °, step 0, 1, speed of scanning 2 ° / min.
  • the sample under study was placed in a quartet's cuvette, and the survey was sent to the taimen plyimernoy (maylarova) film.
  • the diffuse dispersion (amorphous galaxy) is characteristic of amorphous materials. Sguz ⁇ a ⁇ ga ⁇ ü. ⁇ Eg ⁇ at ⁇ ⁇ gez ⁇ . ⁇ .
  • the enthalpy ( ⁇ ) of the effect is equal to 0 81.49 J / g.
  • the distributor is distilled water, the temperature of the distributor 20 ° ⁇ .
  • the rate of dissolution of the comparable samples was separated, growing at 5.0 g of each sample in 10 ml of distilled water at 20 ° ⁇ , and the separator was separated.
  • the sample of ranitidine hydrated hydrophosphate is consumed within 47 seconds (the last of the 10 compounds), the sample is claimed to be transgenic hydrated 10 In general, the speed of production of the claimed sample in
  • ranitidine hydrate Separation of stability during storage The resulting amorphous process of ranitidine hydrate was stored under normal conditions for 14 months and after the study was upgraded. For the first time, it provides a clean, “airy”, lightweight, amber, lightweight white with a slight yellow color.
  • the gastric and intraperitoneal injected the claimed drug in a physiological solution at a concentration of 0.1 mg / ml or 0.2 mg of body weight.
  • a lively business group was introduced into the physiological community. Ulcerative disorders of the mucous membrane of the stomach caused by the intramuscular injection of 6% suspension of acetylsalicylic acid in 1% of starch from the calculation of 5 ml / kg. After the introduction of a suspension of acetylsalicylic acid through the transfer of medical fluids, there were no live animals.
  • ⁇ iz ⁇ li ⁇ vannye zhelud ⁇ i with nal ⁇ zhennymi on ⁇ ischev ⁇ d and ⁇ iv ⁇ a ⁇ ni ⁇ liga ⁇ u ⁇ ami che ⁇ ez 10- millime ⁇ vy sh ⁇ its vv ⁇ dili 8 ml of 2% ⁇ as ⁇ v ⁇ ⁇ malina, ⁇ sle cheg ⁇ ⁇ e ⁇ a ⁇ a ⁇ y ⁇ meschali 10 minutes the 2% ⁇ as ⁇ v ⁇ ⁇ malina for ⁇ i ⁇ satsii s ⁇ en ⁇ i zhelud ⁇ a, zhelud ⁇ i ⁇ e ⁇ a ⁇ i ⁇ vali ⁇ b ⁇ lsh ⁇ y ⁇ ivizne.
  • the total length of ulcerative lesions of the mucous membrane of the stomach in each of the regions was measured at an 8-fold increase with the use of a biological measurement.
  • the ulcerative index was calculated as the sum of the length of the ulcerative lesions of the mucous membrane of the stomach of the gastric ulcer. ⁇ / ⁇ 8 / 00269
  • an acceptable decrease in the ulcerative index in the claimed drug is comparable with the known - pharmaceutical and hydrogen sulfate, compared with 1.5 mg, for 1 mg; ⁇ ⁇ 00/10562 ⁇ / ⁇ 8 / 00269
  • ranitidine hydrochloride ( ⁇ XXIII ⁇ solution) is dissolved in 470 g of distilled water at 70 ° C and it is cooled to freeze.
  • Zam ⁇ zhennuyu weight me ⁇ aniches ⁇ i izmelchayu ⁇ ⁇ i ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e zam ⁇ zhenn ⁇ g ⁇ ⁇ du ⁇ a d ⁇ ⁇ lucheniya chas ⁇ its ⁇ azme ⁇ m less than 5 mm and za ⁇ em vysushivayu ⁇ ⁇ i pressure Yu "1 mm. ⁇ .s ⁇ .
  • the product is well-prepared on the X-ray radiograph by an amorphous galaxy in the region of 15-30 20 °.
  • ranitidine hydride (corresponding to the first 1 parameter of the X-ray diffractor) is dispersed in a total of 470 g.
  • Zam ⁇ zhennuyu weight me ⁇ aniches ⁇ i izmelchayu ⁇ ⁇ i ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e zam ⁇ zhenn ⁇ g ⁇ ⁇ du ⁇ a d ⁇ ⁇ lucheniya chas ⁇ its ⁇ azme ⁇ m less than 5 mm and za ⁇ em vysushivayu ⁇ ⁇ i pressure of 10 '' mm. ⁇ .s ⁇ .
  • the product is processed at a random X-ray at an average of 15-30 °.
  • ranitidine hydrochloride (corresponding to a 2-parameter type of X-ray diffractor) is used in a total of 470 g of distilled water Zam ⁇ zhennuyu weight me ⁇ aniches ⁇ i izmelchayu ⁇ ⁇ i ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e zam ⁇ zhenn ⁇ g ⁇ ⁇ du ⁇ a d ⁇ ⁇ lucheniya chas ⁇ its ⁇ azme ⁇ m less than 5 mm and za ⁇ em vysushivayu ⁇ ⁇ i pressure of 10 "mm. ⁇ .s ⁇ .
  • ranitidine hydride ( ⁇ XXIII ⁇ solution) is consumed in 940 g of distilled water and 80 ° C and it is cooled to freeze.
  • Zam ⁇ zhennuyu weight me ⁇ aniches ⁇ i izmelchayu ⁇ ⁇ i ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e zam ⁇ zhenn ⁇ g ⁇ ⁇ du ⁇ a d ⁇ ⁇ lucheniya chas ⁇ its ⁇ azme ⁇ m less than 5 mm and za ⁇ em vysushivayu ⁇ ⁇ i pressure Yu "1 mm. ⁇ .s ⁇ .
  • ranitidine hydrochloride ( ⁇ XXIII ⁇ rescipas) is dissolved in 398 g of ethyl alcohol and temperature of 50 C and it is cooled ⁇ ⁇ 00/10562 ⁇ / ⁇ 8 / 00269
  • Zam ⁇ zhennuyu weight me ⁇ aniches ⁇ i izmelchayu ⁇ ⁇ i ⁇ em ⁇ e ⁇ a ⁇ u ⁇ e zam ⁇ zhenn ⁇ g ⁇ ⁇ du ⁇ a d ⁇ ⁇ lucheniya chas ⁇ its ⁇ azme ⁇ m less than 5 mm and za ⁇ em vysushivayu ⁇ ⁇ i pressure Yu "1 mm. ⁇ .s ⁇ .

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

Cette invention concerne une forme nouvelle et autrefois connue de ranitidine d'hydrochlorure qui possède des propriétés de blocage de H2. Cette forme est amorphe aux rayons X et, du fait de ses caractéristiques, se distingue sensiblement des modifications cristallines autrefois connues, et possède notamment un effet anti-ulcère plus prononcé. Cette forme amorphe aux rayons X est physiquement stable et peut être utilisée en médecine. Cette invention concerne également un procédé de production de cette forme amorphe aux rayons X à partir des modifications cristallines connues autrefois.
PCT/RU1998/000269 1998-08-18 1998-08-18 Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production WO2000010562A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
RU2001105137/14A RU2203048C2 (ru) 1998-08-18 1998-08-18 Физически устойчивая рентгеноаморфная форма ранитидина гидрохлорида с повышенной противоязвенной активностью и способ ее получения
PCT/RU1998/000269 WO2000010562A1 (fr) 1998-08-18 1998-08-18 Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production
AU15136/99A AU1513699A (en) 1998-08-18 1998-08-18 Physically stable and x-ray amorphous form of hydrochloride ranitidine having anincreased antitumoral activity and method for producing the same
RU2001105137/15K RU2385155C2 (ru) 1998-08-18 1998-08-18 Физически устойчивая рентгеноаморфная форма ранитидина гидрохлорида с повышенной противоязвенной активностью и способ ее получения

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/RU1998/000269 WO2000010562A1 (fr) 1998-08-18 1998-08-18 Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production

Publications (2)

Publication Number Publication Date
WO2000010562A1 true WO2000010562A1 (fr) 2000-03-02
WO2000010562A8 WO2000010562A8 (fr) 2001-03-15

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PCT/RU1998/000269 WO2000010562A1 (fr) 1998-08-18 1998-08-18 Forme physiquement stable et amorphe aux rayons x de ranitidine d'hydrochlorure ayant une action anti-ulcere accrue, et procede de production

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AU (1) AU1513699A (fr)
RU (2) RU2385155C2 (fr)
WO (1) WO2000010562A1 (fr)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0558779A1 (fr) * 1990-09-11 1993-09-08 Glaxo Group Limited Compositions contenant des sels de Ranitidine/carboxylates de Bismuth
US5665767A (en) * 1993-03-05 1997-09-09 Hexal Pharma Gmbh Crystalline cyclodextrin complexes of ranitidine hydrochloride, process for their preparation and pharmaceutical compositions containing the same
US5708021A (en) * 1994-12-17 1998-01-13 Roehm Gmbh Chemische Fabrik Debittered ranitidine preparation

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0558779A1 (fr) * 1990-09-11 1993-09-08 Glaxo Group Limited Compositions contenant des sels de Ranitidine/carboxylates de Bismuth
RU2108097C1 (ru) * 1990-09-11 1998-04-10 Глэксо Груп Лимитед Фармацевтическая композиция, содержащая соль ранитидина и карбоксилата висмута, и способ ее получения
US5665767A (en) * 1993-03-05 1997-09-09 Hexal Pharma Gmbh Crystalline cyclodextrin complexes of ranitidine hydrochloride, process for their preparation and pharmaceutical compositions containing the same
US5708021A (en) * 1994-12-17 1998-01-13 Roehm Gmbh Chemische Fabrik Debittered ranitidine preparation

Also Published As

Publication number Publication date
RU2385155C2 (ru) 2010-03-27
WO2000010562A8 (fr) 2001-03-15
AU1513699A (en) 2000-03-14
RU2203048C2 (ru) 2003-04-27

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