WO2001074370A1 - Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera - Google Patents
Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera Download PDFInfo
- Publication number
- WO2001074370A1 WO2001074370A1 PCT/IN2000/000044 IN0000044W WO0174370A1 WO 2001074370 A1 WO2001074370 A1 WO 2001074370A1 IN 0000044 W IN0000044 W IN 0000044W WO 0174370 A1 WO0174370 A1 WO 0174370A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pharmaceutical composition
- feracrylum
- peptic
- treatment
- cholera
- Prior art date
Links
- 238000011282 treatment Methods 0.000 title claims abstract description 31
- 208000008469 Peptic Ulcer Diseases 0.000 title claims abstract description 25
- 206010008631 Cholera Diseases 0.000 title claims abstract description 24
- 208000000718 duodenal ulcer Diseases 0.000 title claims abstract description 24
- 230000001175 peptic effect Effects 0.000 title claims abstract description 22
- 208000011906 peptic ulcer disease Diseases 0.000 title claims description 11
- WNWBIDPJHFYYLM-UHFFFAOYSA-K iron(3+);prop-2-enoate Chemical group [Fe+3].[O-]C(=O)C=C.[O-]C(=O)C=C.[O-]C(=O)C=C WNWBIDPJHFYYLM-UHFFFAOYSA-K 0.000 title description 2
- 239000000203 mixture Substances 0.000 claims abstract description 31
- 238000000034 method Methods 0.000 claims abstract description 21
- 239000003814 drug Substances 0.000 claims abstract description 16
- 229940079593 drug Drugs 0.000 claims abstract description 15
- 241000607598 Vibrio Species 0.000 claims abstract description 9
- 239000002775 capsule Substances 0.000 claims abstract description 9
- 239000002671 adjuvant Substances 0.000 claims abstract description 6
- 239000006188 syrup Substances 0.000 claims abstract description 6
- 235000020357 syrup Nutrition 0.000 claims abstract description 6
- 239000003826 tablet Substances 0.000 claims abstract description 6
- 241000590002 Helicobacter pylori Species 0.000 claims abstract description 5
- 229940122957 Histamine H2 receptor antagonist Drugs 0.000 claims abstract description 5
- 229940126409 proton pump inhibitor Drugs 0.000 claims abstract description 5
- 239000000612 proton pump inhibitor Substances 0.000 claims abstract description 5
- 229940037467 helicobacter pylori Drugs 0.000 claims abstract description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 12
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 12
- 238000009472 formulation Methods 0.000 claims description 11
- 241000607626 Vibrio cholerae Species 0.000 claims description 9
- 150000002505 iron Chemical class 0.000 claims description 8
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium group Chemical group [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 7
- 235000003891 ferrous sulphate Nutrition 0.000 claims description 7
- 239000011790 ferrous sulphate Substances 0.000 claims description 7
- 239000003242 anti bacterial agent Substances 0.000 claims description 6
- 229940088710 antibiotic agent Drugs 0.000 claims description 6
- 239000007788 liquid Substances 0.000 claims description 4
- 239000002245 particle Substances 0.000 claims description 4
- 239000004159 Potassium persulphate Substances 0.000 claims description 3
- 239000003795 chemical substances by application Substances 0.000 claims description 3
- 239000003485 histamine H2 receptor antagonist Substances 0.000 claims description 3
- 239000012535 impurity Substances 0.000 claims description 3
- 239000003999 initiator Substances 0.000 claims description 3
- USHAGKDGDHPEEY-UHFFFAOYSA-L potassium persulfate Chemical compound [K+].[K+].[O-]S(=O)(=O)OOS([O-])(=O)=O USHAGKDGDHPEEY-UHFFFAOYSA-L 0.000 claims description 3
- 235000019394 potassium persulphate Nutrition 0.000 claims description 3
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- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 239000000470 constituent Substances 0.000 claims 1
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- 235000013355 food flavoring agent Nutrition 0.000 claims 1
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- QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 229940118696 vibrio cholerae Drugs 0.000 claims 1
- 238000002360 preparation method Methods 0.000 abstract description 13
- VMXUWOKSQNHOCA-LCYFTJDESA-N ranitidine Chemical compound [O-][N+](=O)/C=C(/NC)NCCSCC1=CC=C(CN(C)C)O1 VMXUWOKSQNHOCA-LCYFTJDESA-N 0.000 abstract description 3
- 229960000620 ranitidine Drugs 0.000 abstract description 3
- SUBDBMMJDZJVOS-UHFFFAOYSA-N 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole Chemical compound N=1C2=CC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-UHFFFAOYSA-N 0.000 abstract description 2
- XUFQPHANEAPEMJ-UHFFFAOYSA-N famotidine Chemical compound NC(N)=NC1=NC(CSCCC(N)=NS(N)(=O)=O)=CS1 XUFQPHANEAPEMJ-UHFFFAOYSA-N 0.000 abstract description 2
- 229960001596 famotidine Drugs 0.000 abstract description 2
- 229960000381 omeprazole Drugs 0.000 abstract description 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 239000000243 solution Substances 0.000 description 16
- 208000025865 Ulcer Diseases 0.000 description 6
- 230000001580 bacterial effect Effects 0.000 description 6
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- 239000000463 material Substances 0.000 description 4
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- 229960000282 metronidazole Drugs 0.000 description 4
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 description 4
- 241000894006 Bacteria Species 0.000 description 3
- 208000007107 Stomach Ulcer Diseases 0.000 description 3
- HJLSLZFTEKNLFI-UHFFFAOYSA-N Tinidazole Chemical compound CCS(=O)(=O)CCN1C(C)=NC=C1[N+]([O-])=O HJLSLZFTEKNLFI-UHFFFAOYSA-N 0.000 description 3
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- 230000002496 gastric effect Effects 0.000 description 3
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- 239000002253 acid Substances 0.000 description 2
- 229960003022 amoxicillin Drugs 0.000 description 2
- LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 description 2
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- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 description 2
- 229960002626 clarithromycin Drugs 0.000 description 2
- AGOYDEPGAOXOCK-KCBOHYOISA-N clarithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@](C)([C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)OC)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 AGOYDEPGAOXOCK-KCBOHYOISA-N 0.000 description 2
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- 230000000025 haemostatic effect Effects 0.000 description 2
- LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 description 2
- 229940111202 pepsin Drugs 0.000 description 2
- 230000035945 sensitivity Effects 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- 238000004659 sterilization and disinfection Methods 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
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- 230000001018 virulence Effects 0.000 description 2
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 1
- GSDSWSVVBLHKDQ-UHFFFAOYSA-N 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid Chemical compound FC1=CC(C(C(C(O)=O)=C2)=O)=C3N2C(C)COC3=C1N1CCN(C)CC1 GSDSWSVVBLHKDQ-UHFFFAOYSA-N 0.000 description 1
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- 208000034826 Genetic Predisposition to Disease Diseases 0.000 description 1
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- 241000293871 Salmonella enterica subsp. enterica serovar Typhi Species 0.000 description 1
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- 229960003722 doxycycline Drugs 0.000 description 1
- XQTWDDCIUJNLTR-CVHRZJFOSA-N doxycycline monohydrate Chemical compound O.O=C1C2=C(O)C=CC=C2[C@H](C)[C@@H]2C1=C(O)[C@]1(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@@H]1[C@H]2O XQTWDDCIUJNLTR-CVHRZJFOSA-N 0.000 description 1
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- PLHJDBGFXBMTGZ-WEVVVXLNSA-N furazolidone Chemical compound O1C([N+](=O)[O-])=CC=C1\C=N\N1C(=O)OCC1 PLHJDBGFXBMTGZ-WEVVVXLNSA-N 0.000 description 1
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- 239000002731 stomach secretion inhibitor Substances 0.000 description 1
- MNQYNQBOVCBZIQ-JQOFMKNESA-A sucralfate Chemical compound O[Al](O)OS(=O)(=O)O[C@@H]1[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](COS(=O)(=O)O[Al](O)O)O[C@H]1O[C@@]1(COS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)[C@H](OS(=O)(=O)O[Al](O)O)[C@@H](OS(=O)(=O)O[Al](O)O)O1 MNQYNQBOVCBZIQ-JQOFMKNESA-A 0.000 description 1
- 229960004291 sucralfate Drugs 0.000 description 1
- 229960005404 sulfamethoxazole Drugs 0.000 description 1
- JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 description 1
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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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K31/74—Synthetic polymeric materials
- A61K31/765—Polymers containing oxygen
- A61K31/78—Polymers containing oxygen of acrylic acid or derivatives thereof
-
- 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
- A61K33/24—Heavy metals; Compounds thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P31/04—Antibacterial agents
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Definitions
- This invention relates to a novel preparation for the treatment of peptic/duodenal ulcers and/or cholera. More particularly the invention relates to a preparation of feracrylum for the treatment of peptic and duodenal ulcers caused by the bacteria Helicobacter Pylori (H. Pylori) and/or the treatment of cholera caused by the strains of Vibrio.cholerae.
- the preparation can be formulated as a syrup, capsule and tablet form or it can be administered alone with proton pump inhibitors like Omeprazole or H2 antagonists like ranitidine, famotidine, etc.
- the invention also provides a novel method to treat peptic and duodenal ulcers and cholera.
- Peptic and duodenal ulcers are most common disease. Until the 1980s, the cause of peptic ulcer disease was thought to be due to excess secretion of acid and pepsin by the gastric mucosa or the diminished ability of the gastro-duodenal mucosal barrier to protect against the digestive properties of the acid-pepsin complex.
- H. pylori Helicobacter pylori by Warren and Marshall in 1982 has, however, revolutionized our view of the gastric environment, the disease associated with it and the appropriate treatment regimen. In most cases, peptic ulcer is now considered to be a consequence of H. Pylori infection and can be cured by the eradication of this enteric pathogen. With its emergence into clinical consciousness, exceptional attention is being devoted and vast amount of research is being carried out to unravel the biology of H.pylori. H. pylori is one of the most genetically diverse of the bacterial species and the important challenge is to elucidate its pattern of transmission in human population, it adaptation during long time colonization and its contribution to infection.
- H pylori infects about half of the world population, only 10 to 15% of those infected develop the disease. Of those infected, who will develop the disease is influenced by bacterial genotypes and the virulence of the infecting strains, the genetic susceptibility of the host and the environmental cofactors. Of these, bacterial genotypes have been the most intensively studied. (Simanti Data et al in the article entitled "Diversity in the genetic makeup of H. Pylori).
- H. Pylori is gram negative rods colonizing in mucous on the luminal surface of the gastric epithelium. H. Pylori has several genotypes and pathogenicity depends on virulence of these strains. These organisms are gram negative, spiral, microaerophilic bacteria specifically infecting the stomach and thus is the most prevalent infection of civilization in ulceration. It causes gastritis and is a putative contributor to peptic ulcer disease, gastric lymphoma, gastric carcinoma and adrenocarcinoma. (Ref : Blaster and Parsonnet, 1994 and Peterson, 1994, Symposium through Goodman and Gilman, The Pharmacological Basis of Therapeutics, 9 th edition).
- H. Pylori Generally the treatment of ulcers caused by H. Pylori consists of the use of H2 Antagonist Receptors or Proton Pump Inhibitors and antibiotics like clarithromycin, amoxycillin, etc., and drugs like metronidazole, tinidazole, etc., which are active against non-specific anaerobic pathogens which are normally used in amoebiasis caused by Entamoeba histolytica and giardia lamblia. Drugs commonly used consist of metronidazole, tinidazole, ranitidine, cytoprotective drugs like sucralfate, colloidal bismuth derivatives, prostaglandin antagonists and antacids. Single drug therapy for H. Pylori is ineffective invivo and emergence of resistant strains is very common.
- Metronidazole and tinidazole as a therapy is also ineffective because of nitro reductase strains.
- Clarithromycin, amoxycillin, etc. are effective but because of emergent resistant strains, combination therapy along with metronidazole, bismuth salt, etc., are tried.
- antibiotics consisting of two or more antibiotics along with anti-secretory agents, is used for treatment of patients with H. Pylori.
- Cholera is another syndrome caused by strains of Vibrio.cholerae which causes acute secretory diarrhea. It can be associated with 2 serogroup of cholerae (l) 01 & (2) 0139 * .
- Serogroup 01 is further divided in to 2 biotypes, (classical and El Tor). Each has 3 serotypes. (Inaba, Oeawa and Hikojima).
- the genus vibrio includes a group of gram negative short and curved rods (comma Bacilli) having polar flagella.
- the pathogenecity is due to V. Cholerae and E 1 Tor vibrio species. It appears as epidemics in various parts of the globe. These organisms cause rice water stools with water and electrolyte imbalance in body. It enters the body through oral route and multiplies in intestine in alkaline environment. They multiply rapidly. It causes high mortality without proper treatment, death is caused because of dehydration and electrolyte imbalance, leading to irreversible shock.
- Vibrocholerae is with antibiotics like Doxycycline, Ciprofloxacin or Ofloxacin, Sulphamethoxazole & Trimethoprim, Furazolidane, Erthyromycin, Chloramphenicol with Furazolidone. Drug resistance is a common feature for V. cholerae strains.
- Another object of the present invention is to provide for novel formulation and cost effective short duration therapy regimen for treatment of cholera caused by strains of Vibrio.cholerae.
- feracrylum has been found to be not only haemostatic but also anti-infective against a number of gram positive and gram negative pathogenic, bacterial and fungus strains like Staphylococcus aureus, Streptococcus pyogenes, Corynebacterium diphtheriae, Salmonella typhi, Shigella dysentriae, Escherichia coli, Proteus Vulgaris, Pseudomanas aeruginosa, Trichoderma Viridae, Candida Albicans, Etc.
- Feracrylum when prepared by the novel process as described in our co- pending Application No. 467/BOM/99 could be processed to a solid form or solution in water. As mentioned this material is an excellent haemostatic and anti-infective.
- the present invention relates to a pharmaceutical composition
- a pharmaceutical composition comprising feracrylum in an amount of 1% w/v to 10% w/v of the composition for use in the treatment of peptic and duodenal ulcers caused by the bacteria H. Pylori and/or cholera caused by the bacteria V.cholerae.
- composition of the invention comprising feracrylum shows increased benefits when the feracrylum used in the composition is prepared by the process developed by the applicants and disclosed in co-pending application No. 467/BOM/99.
- the process of preparation of the pharmaceutical composition of the invention comprises :
- the ratio of acrylic acid to initiator is 166 to 186 : 1.0
- the ratio of acrylic acid to iron salt is 105- 115 : 1.0
- the iron salt is ammonium ferrous sulphate
- the ratio of acrylic acid to ammonium ferrous sulphate is 110 : 1.
- the present invention relates to the pharmaceutical composition comprising feracrylum and use of this composition for treatment of peptic/duodenal ulcers and/or cholera.
- the composition can be in form of oral liquid or in the form of tablets, capsules.
- the pH of the oral liquid composition is between 2.5 to 4.0 and preferably between 2.9 to 4.0.
- the concentration of the feracrylum may vary from 1% w/v to 10% w/v of an aqueous composition, and composition may optionally contain other adjuvants used in oral preparations and drugs like proton pump inhibitors, H2 antagonist receptors, anaerobic organism inhibitors, antibiotics and anti secretive agents.
- the feracrylum solution prepared using the feracrylum by the process has strong characteristics for suitability of treatment of peptic/ duodenal ulcers and cholera.
- the use of feracrylum solution for the above treatment can be made by administering the compound in syrup or by admixing its tablets/ capsules.
- the formulation can be administered alone or in conjunction with other adjuvants.
- Fercrylum may be prepared in solution form in various concentrations preferably from 1%-10% w/v or w/w depending on the formulation. This solution prepared is limpid, stable and safe. The amount of water can be upto 90% v/v to 99% v/v by volume of the composition.
- Example 1 The composition of the invention including its preparation and efficacy will be illustrated and demonstrated with the help of examples which are non- limiting:
- Example 1 The composition of the invention including its preparation and efficacy will be illustrated and demonstrated with the help of examples which are non- limiting:
- 0.039 mole of potassium persulphate is taken in a vessel containing 14.3 L of distilled water and stirred for 3 minutes. 26.08 mole of acrylic acid solution is added which is previously dissolved in 1.2 L of distilled water. This is further mixed with 0.0592 mole of Ammonium Ferrous Sulphate dissolved in water. This is mixed thoroughly under continuous stirring for 3 to 4 hours. The mixture is diluted to 25 L and the whole mass is cooled to room temperature and kept for 2 hours. Resin is then added to remove impurities the mixture stirred for 30 minutes, filtered and evaporated under vacuum at 50°C to 60°C using rotary evaporator. The evaporated product is passed through a micronizer, which yields fine shining peach coloured crystals. These crystals have the characteristics of rapid solubility and meet the general pharmaceutical specifications.
- the feracrylum prepared by the applicant has the following specifications:
- the feracrylum thus prepared readily dissolves in water at 25°C, is easily filterable and can also be easily sterilized.
- Agar dilution method was used to determine the minimal concentration of Feracrylum required to inhibit the growth of Helicobacter Pylori.
- the drug was dissolved in minimum volume of sterile distilled water to get different Feracrylum concentrations used in this drug sensitivity study.
- H.pylori strains were selected for this study.
- the strains of category A are collected from the antral region of the stomach while those of category B are collected from the fundus region.
- the strains were collected from the Post graduate Medical Institute (PGMI), Calcutta.
- the sample numbers were also generated by the PGMI.
- Blood agar plates were prepared with brain-heart infusion agar containing 10% defibrinated sheep blood and a particular dilution of the drug added to each plate. Control plates with no Feracrylum were simultaneously prepared.
- the drug- supplemented as well as the control blood-agar plates were streak- inoculated with ⁇ 10 4 CFU of each H.pylori strain.
- the inoculated plates were incubated at 37°C under 10% CO2 and 5% O2 and were observed for the presence of bacterial growth initially at 48 hours and then daily for upto 10 days.
- H.pylori strains used 109A, 114A, 100A, 86A, 115B, 91A, 62A, 77A, 222B, 278A, 286B, 291B, 105A, 331A, 353A, 324B, 41B, 56B, 60A, 17A, 2 IB, 78B, l l lA and 27B.
- V. cholerae strains used 181, 175, 272, 285, 219, 186, 211
- feracrylum is an excellent agent for eradicating H.pylori bacteria which as mentioned hereinbefore is responsible for almost all cases of ulcers, peptic and duodenal. Also feracrylum is shown to be suitable for use in the treatment of cholera caused by Vibrio.cholerae.
- the animal model studies and other clinical studies further confirm that feracrylum when administered orally or intra peritoneally has no adverse effects in the systemic sense or in the physio-pathological sense and gives no adverse side effects whatsoever.
- the formulations having feracrylum for treatment of peptic/duodenal ulcer and/or cholera can be administered as syrup or in the form of tablets/capsules.
- the formulation can be administered alone or in conjunction with other adjuvants drugs.
- the formulations are stable as per ICH guidelines.
- the tablets can be obtained in varying strength ranging from 50 mg. to 2 gms. as per the needs of the patient and the gravity of the treatment required.
- the invention thus makes the treatment of peptic ulcers, duodenal ulcers, whether bleeding or non-bleeding, and cholera simple and cost effective by use of the novel formulation comprising the feracrylum.
- the formulation comprising feracrylum as detailed above is simple to manufacture and does not require special technology.
- the product can be easily administered and is therefore beneficial and highly advantageous for treatment of ulcer and/or cholera as discussed above.
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Abstract
Description
Claims
Priority Applications (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IN2000/000044 WO2001074370A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
EP00944210A EP1267895A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
AU2000258441A AU2000258441A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
CA002401112A CA2401112A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/IN2000/000044 WO2001074370A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
Publications (1)
Publication Number | Publication Date |
---|---|
WO2001074370A1 true WO2001074370A1 (en) | 2001-10-11 |
Family
ID=11076244
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IN2000/000044 WO2001074370A1 (en) | 2000-04-03 | 2000-04-03 | Use of feracryl for the treatment of peptic/duodenal ulcer and/or cholera |
Country Status (4)
Country | Link |
---|---|
EP (1) | EP1267895A1 (en) |
AU (1) | AU2000258441A1 (en) |
CA (1) | CA2401112A1 (en) |
WO (1) | WO2001074370A1 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2024013762A1 (en) * | 2022-07-11 | 2024-01-18 | Patel, Vishal | Improved process for feracrylum preparation |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4215106A (en) * | 1978-04-07 | 1980-07-29 | Annenkova Valentina M | Local hemostatic |
-
2000
- 2000-04-03 AU AU2000258441A patent/AU2000258441A1/en not_active Abandoned
- 2000-04-03 WO PCT/IN2000/000044 patent/WO2001074370A1/en not_active Application Discontinuation
- 2000-04-03 CA CA002401112A patent/CA2401112A1/en not_active Abandoned
- 2000-04-03 EP EP00944210A patent/EP1267895A1/en not_active Withdrawn
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4215106A (en) * | 1978-04-07 | 1980-07-29 | Annenkova Valentina M | Local hemostatic |
Non-Patent Citations (8)
Title |
---|
ANNENKOVA, V.E.: "Antibacterial and antifungal activity of Feracryl", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 31, no. 3, 1997, pages 39 - 40 * |
ANNENKOVA, V.Z. ET AL: "Ferakril--gemostatik mestnogo deistviia", FARMAKOLOGIIA I TOKSIKOLOGIIA, vol. 54, no. 5, 1991, pages 36 - 40 * |
ANNENKOVA, V.Z. ET AL: "Novel water soluble polymers having antimicrobial activity", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 24, no. 6, 1990, pages 34 - 36 * |
DATABASE BIOSIS BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; XP002156479 * |
DATABASE CAPLUS AMERICAN CHEMICAL SOCIETY; XP002147039 * |
DATABASE CHEMABS CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; XP002156481 * |
DATABASE MEDLINE US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; XP002156480 * |
ZHDANKOVICH, E.L. ET AL: "Metal-containing trisalt of polyacrylic acid with a high antimicrobial activity", KHIMIKO-FARMATSEVTICHESKII ZHURNAL, vol. 24, no. 9, 1990, pages 50 - 51 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2024013762A1 (en) * | 2022-07-11 | 2024-01-18 | Patel, Vishal | Improved process for feracrylum preparation |
Also Published As
Publication number | Publication date |
---|---|
EP1267895A1 (en) | 2003-01-02 |
CA2401112A1 (en) | 2001-10-11 |
AU2000258441A1 (en) | 2001-10-15 |
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