OA10636A - Phytodrug for management of peptic ulcer and methods of preparing and using same - Google Patents
Phytodrug for management of peptic ulcer and methods of preparing and using same Download PDFInfo
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- OA10636A OA10636A OA70137A OA70137A OA10636A OA 10636 A OA10636 A OA 10636A OA 70137 A OA70137 A OA 70137A OA 70137 A OA70137 A OA 70137A OA 10636 A OA10636 A OA 10636A
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- 238000000034 method Methods 0.000 title claims description 8
- 208000008469 Peptic Ulcer Diseases 0.000 title description 20
- 208000011906 peptic ulcer disease Diseases 0.000 title description 18
- 244000140916 Indigofera arrecta Species 0.000 claims description 31
- 239000000203 mixture Substances 0.000 claims description 15
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 9
- 239000000463 material Substances 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 239000002904 solvent Substances 0.000 claims description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 7
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 6
- 239000000454 talc Substances 0.000 claims description 6
- 229910052623 talc Inorganic materials 0.000 claims description 6
- 241000196324 Embryophyta Species 0.000 claims description 4
- 229920002472 Starch Polymers 0.000 claims description 4
- 235000019698 starch Nutrition 0.000 claims description 4
- 239000008107 starch Substances 0.000 claims description 4
- 238000000605 extraction Methods 0.000 claims description 3
- 241001062009 Indigofera Species 0.000 claims description 2
- 238000004108 freeze drying Methods 0.000 claims description 2
- 230000001175 peptic effect Effects 0.000 claims description 2
- SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 description 11
- 208000000718 duodenal ulcer Diseases 0.000 description 9
- 208000002193 Pain Diseases 0.000 description 8
- 208000007107 Stomach Ulcer Diseases 0.000 description 8
- 208000025865 Ulcer Diseases 0.000 description 8
- 230000036407 pain Effects 0.000 description 8
- 231100000397 ulcer Toxicity 0.000 description 8
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 7
- 230000002496 gastric effect Effects 0.000 description 6
- 239000002775 capsule Substances 0.000 description 5
- 239000011780 sodium chloride Substances 0.000 description 5
- 230000001965 increasing effect Effects 0.000 description 4
- 238000007912 intraperitoneal administration Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 229920002261 Corn starch Polymers 0.000 description 3
- 235000019759 Maize starch Nutrition 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 241000700159 Rattus Species 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 210000004211 gastric acid Anatomy 0.000 description 3
- 201000005917 gastric ulcer Diseases 0.000 description 3
- 210000001187 pylorus Anatomy 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 2
- 235000014469 Bacillus subtilis Nutrition 0.000 description 2
- 241000894006 Bacteria Species 0.000 description 2
- 241000588724 Escherichia coli Species 0.000 description 2
- 102100021022 Gastrin Human genes 0.000 description 2
- 108010052343 Gastrins Proteins 0.000 description 2
- 208000032843 Hemorrhage Diseases 0.000 description 2
- NTYJJOPFIAHURM-UHFFFAOYSA-N Histamine Chemical compound NCCC1=CN=CN1 NTYJJOPFIAHURM-UHFFFAOYSA-N 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 206010047700 Vomiting Diseases 0.000 description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 229940069428 antacid Drugs 0.000 description 2
- 239000003159 antacid agent Substances 0.000 description 2
- AOXOCDRNSPFDPE-UKEONUMOSA-N chembl413654 Chemical compound C([C@H](C(=O)NCC(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H]1N(CCC1)C(=O)CNC(=O)[C@@H](N)CCC(O)=O)C1=CC=C(O)C=C1 AOXOCDRNSPFDPE-UKEONUMOSA-N 0.000 description 2
- 230000034994 death Effects 0.000 description 2
- 231100000517 death Toxicity 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 230000000968 intestinal effect Effects 0.000 description 2
- 210000003734 kidney Anatomy 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 235000012054 meals Nutrition 0.000 description 2
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 2
- 230000002829 reductive effect Effects 0.000 description 2
- 229920005989 resin Polymers 0.000 description 2
- 239000011347 resin Substances 0.000 description 2
- 229930182490 saponin Natural products 0.000 description 2
- 150000007949 saponins Chemical class 0.000 description 2
- 235000017709 saponins Nutrition 0.000 description 2
- 210000002460 smooth muscle Anatomy 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 229920001864 tannin Polymers 0.000 description 2
- 239000001648 tannin Substances 0.000 description 2
- 235000018553 tannin Nutrition 0.000 description 2
- 239000000341 volatile oil Substances 0.000 description 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- 206010000087 Abdominal pain upper Diseases 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 208000000412 Avitaminosis Diseases 0.000 description 1
- 241000784713 Cupido Species 0.000 description 1
- 208000035859 Drug effect increased Diseases 0.000 description 1
- 208000007882 Gastritis Diseases 0.000 description 1
- 206010020601 Hyperchlorhydria Diseases 0.000 description 1
- 208000002720 Malnutrition Diseases 0.000 description 1
- 108010058846 Ovalbumin Proteins 0.000 description 1
- 208000000114 Pain Threshold Diseases 0.000 description 1
- 206010046274 Upper gastrointestinal haemorrhage Diseases 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 238000009825 accumulation Methods 0.000 description 1
- 229960000583 acetic acid Drugs 0.000 description 1
- 235000011054 acetic acid Nutrition 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 231100000215 acute (single dose) toxicity testing Toxicity 0.000 description 1
- 229930013930 alkaloid Natural products 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 238000001949 anaesthesia Methods 0.000 description 1
- 150000004056 anthraquinones Chemical class 0.000 description 1
- 230000001458 anti-acid effect Effects 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 230000002921 anti-spasmodic effect Effects 0.000 description 1
- 230000000767 anti-ulcer Effects 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 235000021152 breakfast Nutrition 0.000 description 1
- 239000012876 carrier material Substances 0.000 description 1
- 235000013339 cereals Nutrition 0.000 description 1
- 239000003610 charcoal Substances 0.000 description 1
- 239000000812 cholinergic antagonist Substances 0.000 description 1
- 208000023652 chronic gastritis Diseases 0.000 description 1
- 239000012141 concentrate Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000001066 destructive effect Effects 0.000 description 1
- 238000003113 dilution method Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 230000002183 duodenal effect Effects 0.000 description 1
- 230000001667 episodic effect Effects 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 230000000763 evoking effect Effects 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 210000001156 gastric mucosa Anatomy 0.000 description 1
- 230000036397 gastrointestinal physiology Effects 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 229930182470 glycoside Natural products 0.000 description 1
- 150000002338 glycosides Chemical class 0.000 description 1
- 230000035929 gnawing Effects 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000002489 hematologic effect Effects 0.000 description 1
- 241000411851 herbal medicine Species 0.000 description 1
- 229960001340 histamine Drugs 0.000 description 1
- 229920001461 hydrolysable tannin Polymers 0.000 description 1
- 206010020718 hyperplasia Diseases 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 208000003243 intestinal obstruction Diseases 0.000 description 1
- 238000011835 investigation Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 230000001071 malnutrition Effects 0.000 description 1
- 235000000824 malnutrition Nutrition 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 239000004570 mortar (masonry) Substances 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 238000006386 neutralization reaction Methods 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 208000015380 nutritional deficiency disease Diseases 0.000 description 1
- 230000037040 pain threshold Effects 0.000 description 1
- WEXRUCMBJFQVBZ-UHFFFAOYSA-N pentobarbital Chemical compound CCCC(C)C1(CC)C(=O)NC(=O)NC1=O WEXRUCMBJFQVBZ-UHFFFAOYSA-N 0.000 description 1
- 229960001412 pentobarbital Drugs 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 230000000750 progressive effect Effects 0.000 description 1
- 239000011241 protective layer Substances 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 239000002464 receptor antagonist Substances 0.000 description 1
- 229940044551 receptor antagonist Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000003248 secreting effect Effects 0.000 description 1
- 210000002027 skeletal muscle Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000001179 sorption measurement Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 230000001562 ulcerogenic effect Effects 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/143—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Mycology (AREA)
- Medicines Containing Plant Substances (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
1 010636
BACKGROUND OF THE INVENTION
This invention relates to a pharxnaceutical composition for managing pepticulcer conditions comprising an extract of Indigofera arrecta, and to niethodsof preparëng the extract.
Pepdc ulcer has been defined as a benign lésion of gastric or duodenalmucosa occurring at a site where the mucosal epithelium is exposed to acidand pepsiza. It is a gastro-intestinal problem that is prévalent in society.The occurrence of the disease has been associated with over-indulgence,inacproprùate habits, anxiety and stress. Considérable energy and resourceshâve been expended towards relieving symptoms of peptic ulcer which 010636 2 usually manifests as an excruciating pain, especially in the upper abdomen.For centuries neutralization of gastric acid sécrétion with antacids and 112-receptor antagonists, provided the only relief from the pains of peptic ulcer.These crugs are generally expensive. Consequently, the socio-economicimpact of peptic ulcer disease on society can only be imagined.
In the foregoing assertion, efforts hâve been made to find a suitablepalliative andOr curative agent for the treatment of peptic ulcer conditionsfrom médicinal plants.
It is esrimated that approximately 10% of most populations globally willdsvelop severe peptic ulcer conditions at some time during their lifetime.The lésions occur at ail âges and affect both sexes.
Authorixies estimate that at least five million people suffer from activepeptic ulcers each year, and approximately 350,000 to 500,000 new casesare diasnosed annually in the United States of America alone. More than600,000 patients are hospitalized in the US each year for severe épisodes.In approximately one-third of these cases serious complications occur,includicg intestinal obstruction, upper gastrointestinal haemorrhage andperforation. Furthermore, each year, over 6,000 deaths in the US aredirectly caused by ulcer disorder. In addition, peptic ulcer conditions hâvebeen implicated as an indirect contributing factor in an additional 11,000deaths each year.
In Nigeria, peptic ulcer conditions general afflict persons between the âgesof 21 and 51. Duodenal ulcers hâve their greatest impact in middle âgewhile gastric ulcers become increasingly more frequent with advancing âge. 01 0636 3
Peptic ulcération reflects on imbalance between the aggressive action of acidpeptic sécrétions and the défensive forces that protect the inucosa. Gastriculcers resuit from lowered défensive mechanisms and duodenal ulcers arethe conséquence of the destructive action of increased acid-peptic sécrétions. 5 Duodenal ulcers occur when gastric mucosa sécrétés substantial amounts ofacid. Although some patients with duodenal ulcers hâve normal levels ofacid sécrétion, on the average they are hyperchlorhydrie. Gastric acid hastwo phases, viz; (1) a cephalic phase (vagally mediated) in which direct cholinesgic £0 stimulation of pariétal cells induces gastrin release from the antrum, and (2) a less powerful antral phase when food enters the stomach,causing libération of more gastrin from the antral mucosa.
Evidence that patients with duodenal ulcers hâve increased pariétal cell mass15 also suggests a genetic prédisposition even though experimental data indicate that parental cell hyperplasia can be acquired.
Gastric ulcération results from lowering of the gastric mucosal résistance.Principal among the défensive influences is mucous sécrétion. Theincreased frequency of gastric ulcers with advancing âge might be 20 compatible with progressive inability to secrete a protective layer ofmucous. Chronic gastritis is a frequent concomitant of gastric ulcer, isassociaced with impaired mucous sécrétion and is also age-related. Inexperimental animais, it has been demonstrated that protein déplétion,avitaminoses and general malnutrition increase the susceptibility to gastric 25 ulcération. 01 06 36 4
There is now growing evidence that Helicobactor pylori. a bacterium, maybe the cause of duodenal ulcer. The evidence linking Helicobactor pyloriwith benign gastric ulcer is less convincing than duodenal ulcer. However,the consensus now is that the organism is probably important in thepathogenesis of 70% of gastric ulcers not attributable to the use of non-steroidal anti-inflammatory drugs (NSAIDs).
The symptoms evoked by peptic ulcers are exceedingly variable; someulcers being virtually asymptomatic. Nausea and vomiting may be producedby either duodenal or gastric ulcers, but particularly by the latter. The mostconsistent manifestation is epigastric pain described variably as buming,gnawing or boring. Classically, the duodenal ulcer pain becomes mosts.evere two or three hours after the last meal and persists until it is relievedty food or antacids. For this reason, the pain recurs in the middle of therJght acid requires a glass of milk or antiacid for its relief. Such episodicpain may last for weeks or months only to abate, usually with regulateddtetary regimen and therapy. Récurrence is often triggered by dietaryindiscrétions or stress and is usually very rapid and sometimes dramatic,pnesenting with haemorrhage or perforation. Death from peptic ulcer isusually due to bleeding or perforation. In addition, a high proportion ofpatients who die or whose ulcers bleed or perforate hâve no warningsinnals.
SUMMARY OF THE INVENTION
Accordicg to a first aspect of the invention there is provided apharmaceutical composition for managing peptic ulcer conditions comprisingan extracr. of Indigofera arrecta (family Papilionaeeae), preferably Indigofera
0î 063 G 5 arrecta plsnt lecves, the extract having been prepared using a suitable solvent.
The soivem is preferably water, more preferably hot water.
The solvent extract is preferably freeze-dried before used. 5 The phaoiaceurical composition of the invention may include as anexcipient for oral administration, a combination of magnésium carbonate,generaiiy heavy magnésium carbonate, a starch, for example dried maizestarch. talc and magnésium stéarate. In a preferred form, thepharmaceutical composition of the invention comprises about 8 parts toabout 12 pans by weight of the extract, about 170 pans to about 180 partsby weight of magnésium carbonate, about 100 parts to about 120 parts byweight of a starch, and about 4 parts to about 6 parts by weight of amixture of talc and magnésium stéarate.
The pharmaceuncal composition of the invention preferably comprises about2,6% to about 4,3% by weight of the extract by total weight of thecomposition.
The phannaceubcal composition of the invention is preferably fonnulatedas a capsule.
Accorcing te a second aspect of the invention there is provided a methodof preparung an extract of Indigofera arrecta. including the steps of: (i) reducing Indigofera arrecta plant material to a powder; and (îi) subieeting the powder to an extraction process using a suitable solvent.
0 1 0 6 3 G 6
The method of the invention may include an additional step of: (iii) freeze-drying the solvent extract.
The pharmaceutical composition of the invention is of particular use in themanagement of peptic ulcer conditions.
DESCRIPTION OF EMBODIMENTS
In accordance with the invention, a pharmaceutical composition for treatingand managing peptic ulcer conditions in humans is provided. Thecomposition is prepared by extracting effective peptic ulcer inhibitingChemicals from the powdered leaves of Indigofera arrecta plant. In apreferred form of the invention, the powdered leaves are subjected to a hotwater extraction process whereby the powdered leaves are contacted by hotwater for a period of hours. The extract may be combined with anexcipient carrier material to préparé an admixture which may beencapsulated for oral administration. The admixture, which may preferablycontain from about 2,6 to about 4,3% of the extract by weight, is preferablyadministered orally to a human patient afflicted by a peptic ulcer condition.
To préparé the extract, the leaves of Indigofera arrecta plant are dried andreduced to a fine powder by grinding with a mortar and pestle or bail mill.500 grams of the finely ground material are then macerated in 3 litres ofwater and heaied over a boiling water bath for about 4 hours. The résultantmixture is then filtered using filter paper and the filtrate is concentrated invacuo te a volume of about 800 mi. The concentrate is then freeze-driedfor about 48 hours using a Finn - Aqua Lyovac freeze dryer to provide adry powder œntaining the active drug materials extracted from the initial 010636 powdered leaf material. The typical yield of the extracted material is about14 to 15% based on the original weight of the crude ground leaf material.That is to say, the yield is about 70 to 75 grains when the starting batch isabout 500 grams. 5 Phvtochemical screening of the crude ground leaf material revealed thepresence of volatile oils, saponins, tannins and resins. However, onlytannins and saponins were found to be présent in the freeze dried extract.Glycosides, anthraquinones, alkaloids, hydrolysable tannins and resins wereail absent from the freeze-dried extract. The freeze-dried extract contains 10 about 0,02 to 0,04% by weight of volatile oils and about 7 to 9% by weightof tannins.
The Indigofera arrecta plant was selected as a possible candidate forsciencific investigation in the first place and its effectiveness against bacteriaknown to be associated with peptic ulcer conditions was evaluated using the 15 freeze-dried extract. The minimum inhibitory concentration and minimumbactericidal concentration of Indigofera arrecta extract againstPs. Aeruginosa, E. Coli, S. Aureus and B. Subtilis were determined usingthe sgar dilution method. Indigofera arrecta extract showed potentantimicrobial efficacy against ail of the tested commonly encountered 20 microbes. The minimum inhibitory concentrations were Ps, Aeruginosa.0,5 ng/ml: E. Coli. 1 mg/ml; S, Aureus, 1 mg/ml; and B. Subtilis,1 mg/ml. The minimum bactericidal concentrations were 1 mg/ml forPs. Aeruginosa and 2 mg/ml for the other three bacteria species.
The freeze-dried extract of Indigofera arrecta leaves was subjected to acutetoxicity testing by the intraperitoneal route in mice using standard 25 procedures. No remarkable adverse effect was observed. The LD5() was 8 01 0636 established as 245 ± 28 mg/kg i.p.
The target System in peptic ulcer disease is the gastrointestinal tract. Manyanti-uicer agents, especially those that interact with receptor Systems,influence gastrointestinal physiology and its response to ulcerogenic 5 substances. Based on this premise, the effect of the freeze-dried hot waterextract of Indigofera arrecta leaves and its interaction with acétylcholine(Ach> and histamine were investigated on both smooth muscles and skeletalmuscles. The results indicate that the extract of Indigofera arrecta leavesmay contain some anti-spasmodic principles which relax the smooth muscles 10 of the gastrointestinal tract.
In a preliminary study, the aspirin model of inducing experimental gastriculcer in rats was used to assess the anti-ulcer activity of the extract ofIndigofera arrecta leaves which is the subject of the invention. As shownin Table !, the extract of Indigofera arrecta leaves has a remarkable effect 15 against aspirin-induced ulcers. This effect increased with the dose of theextract as shown by the mean ulcer indices.
TABLE I
Dose of I. arrecta Extract Ulcer Index Normal saline solution 1,1 ± 0,07 250mg of extract/ml of saline 0,5 ±0,12 50ümg of extract/ml of saline 0,24 ± 0,02
Drugs that delay the small intestinal transit time hâve bénéficiai effects onulcer patients. The effect of the Indigofera arrecta extract on smallintestinal transit in mice was tested using the charcoal meal method. The 010636 9 results in Table II below show that intraperitoneal administration of theextract in mice significantly reduced small intestinal transit. The inhibition,however, did not seem to be dose-dependent.
TABLE II
Dose of Extract % DistanceTravelled % Inhibition Normal saline solution 92,38 ± 8,8 7,4 25Gmg/ml of saline 33,93 ± 1,2 66,07 50Cmg/ml of saline 61,16 ± 11,3 38,8 Noradrenaline 64,6 ± 9,0 .35,4
The Indigo fera arrecta extract of the invention showed little tendency to10 induce inflammation. In fact, during testing the extract was administered i.p. (200 mg/kg) for 1 hour before inflammation was induced. On the otherhand. the Indigofera arrecta extract at the dose tested did not exhibit potentanti-inflammatory activity. Significant (P < 0,05) anti-inflammatory activity was observed, however, 80 minutes after egg-albumin. 5
The analgésie effect of the Indigofera arrecta extract of the invention wastested in thermal pain (hot plate at 50,2 ± 1°C) and Chemical pain (aceticacid induced writhing). In the two models, it appeared that the Indigoferaarrecta extract was ineffective in increasing the pain threshold.
Anüsecretory activity of the Indigofera arrecta extract of the invention wasaise studied. This study was performed in pylorus - ligated (shay) rats.After 48 hours fasting with access to water ad libitum, the pylorus wasIigaited under pentobarbitone anaesthesia. Pylorus ligation of the rats for 6 01 06 36 ίο hours caused accumulation of gastric secretory volume and increased gastricacid output. As shown below in Table III, the Indigofera arrecta extract ofthe invention significantly decreased the volume and acidity of basal gastricsécrétions. The number and severity of ulcers were remajrkably reduced in 5 animais treated with the Indigofera arrecta extract of the invention.Moreover, it was determined that the effect of the extract was dosedépendent.
TABLE III
Treatment Dosage/Kg Volume ofGastric Sécrétion Acid Output(mEq/L) 40ml saline 3,6 ± 0,19 250 ± 16,4 50mg I. arrecta extract 2,6 ± 0,99 170 ± 6,8 lOOmz I. arrecta extract 2,3 ± 0,12 150 ± 8,2
The Indigofera arrecta plant leaf extract of the invention was standardisedand formulated into capsule dosage forms using World Health Organisation(WHO) guidelines. These guidelines clearly advise that when a plant based 15 product (e.g. herbal medicine) is safe and indicates efficacy, it can besu.bsequently standardised and formulated into suitable dosage for clinicaltrials. In accordance with accepted procedures it has been determined thatan appropriate daily dosage of the Indigofera arrecta plant leave extract ofthe présent invention is approximately 3 mg/kg of body weight administered 20 orally in two divided doses.
Clinical trials for the Indigofera arrecta leaf extract of the inventioncommenced using volunteers. The clinical parameter of episodic pain,nsusea and vomiting as well as kidney and liver haematological status and 010636 11 function were assessed. The data obtained so far indicates the efficacy ofthe Indigofera arrecta plant leaf extract against peptic ulcers with nodétectable adverse effects on kidney, liver and blood chemistry. The valuesrecorded for these parameters fall within normal ranges. On the average 5 about 80% of those in the test groups hâve experienced relief from épisodesof pain since they entered the test program.
As a resuit of the testing to date, it has been determined that an appropriateand effective formulation of the Indigofera arrecta plant leaf extract of theinvention for oral administration to humans for managing peptic ulcer 10 conditions includes about 8 parts to about 12 parts by weight of the extractitself, about 170 parts to about 180 parts by weight of heavy magnésiumcarbonate, about 100 parts to about 120 parts by weight of dried maizestarch and about 4 parts to about 6 parts by weight of a mixture of talc andmagnésium stéarate. This formulation is prepared by adsorbing about 15 200 mg of the freeze-dried extract, which is a sticky solid mass, in about 20 to 25 ml of methanol. The mixture is subjected to évaporation over awater bath leaving a thick liquid mass. About 3 to 4 granis of heavymagnésium carbonate is added as an agent for adsorption, after which themixture is triturated to présent a homogenous mass. About 2 to 2,4 grams 20 of dried maize starch is then added and the mixture again triturated to forma uniform mixture. About 8 to 12 mg of a talc/magnesium stéarate mixtureis then added and again the mass is mixed until uniform. The material isthen fîlled into capsules such that each capsule contains from about 282 to306 mg of the uniform mixture. The daily dose of the Indigofera arrecta 25 plant leaf extract of the invention is then administered orally as two separate capsules, preferably one in the moming at breakfast tinte and the other inthe evening before bed time.
Claims (7)
- 010636 CLAIMS 1 A pharmaceutical composition for managing peptic ulcerconditions comprising an extract of lndigofera arrecta. theextract having been prepared using a suitable solvent.
- 2 A pharmaceutical composition according to daim 1 comprising 5 an extract of lndigofera arrecta plant leaves.
- 3 A pharmaceutical composition according to daim 1 or daim 2wherein the solvent is hot water.
- 4 A pharmaceutical composition according to any one of daims 1to 3 wherein the solvent extract is freeze-dried. 10
- 5 A pharmaceutical composition according to any one of daims 1 to 4 comprising as an excipient for oral administrationmagnésium carbonate, a starch, talc and magnésium stéarate.
- 6 A pharmaceutical composition according to daim 5 wherein diecomposition comprises about 8 parts to about 12 parts by weight 15 of die extract, about 170 parts to about 180 parts by weight of magnésium carbonate, about 100 parts to about 120 parts byweight of a starch and about 4 parts to about 6 parts by weightof a mixture of talc and magnésium stéarate.
- 7 A pharmaceutical composition according to any one of daims 1 20 to 5 comprising about 2,6% to about 4,3% by weight of the composition of the extract. 01 0636 10 10 12» A method for preparing an extract of Indigofera arrectaeomprising the steps of: (i) reducing Indigofera arrecta material to a powder;and (ii) subjecting the powder to an extraction processusing a suitable solvent. A method according to claim S wherein in step (ii) the water ishot water. A method according to either of daims 8 or 9 which includesthe step of (iii) freeze-drying the solvent extract.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| OA70137A OA10636A (en) | 1997-11-25 | 1997-11-25 | Phytodrug for management of peptic ulcer and methods of preparing and using same |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| OA70137A OA10636A (en) | 1997-11-25 | 1997-11-25 | Phytodrug for management of peptic ulcer and methods of preparing and using same |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| OA10636A true OA10636A (en) | 2001-04-24 |
Family
ID=32026329
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| OA70137A OA10636A (en) | 1997-11-25 | 1997-11-25 | Phytodrug for management of peptic ulcer and methods of preparing and using same |
Country Status (1)
| Country | Link |
|---|---|
| OA (1) | OA10636A (en) |
-
1997
- 1997-11-25 OA OA70137A patent/OA10636A/en unknown
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