AU2023203385A1 - Omeprazole based oral paste formulation having increased temperature stability and enhanced absorption - Google Patents
Omeprazole based oral paste formulation having increased temperature stability and enhanced absorption Download PDFInfo
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- AU2023203385A1 AU2023203385A1 AU2023203385A AU2023203385A AU2023203385A1 AU 2023203385 A1 AU2023203385 A1 AU 2023203385A1 AU 2023203385 A AU2023203385 A AU 2023203385A AU 2023203385 A AU2023203385 A AU 2023203385A AU 2023203385 A1 AU2023203385 A1 AU 2023203385A1
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- 239000000203 mixture Substances 0.000 title claims abstract description 69
- 238000009472 formulation Methods 0.000 title claims abstract description 54
- 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 title claims abstract description 38
- 229960000381 omeprazole Drugs 0.000 title claims abstract description 38
- 229940041667 oral paste Drugs 0.000 title claims abstract description 18
- 238000010521 absorption reaction Methods 0.000 title description 6
- 244000144725 Amygdalus communis Species 0.000 claims abstract description 16
- 235000011437 Amygdalus communis Nutrition 0.000 claims abstract description 16
- 235000012550 Pimpinella anisum Nutrition 0.000 claims abstract description 16
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- 235000019198 oils Nutrition 0.000 claims abstract description 16
- 241000283086 Equidae Species 0.000 claims abstract description 15
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- 201000010099 disease Diseases 0.000 claims abstract description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 12
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 claims abstract description 10
- 230000002265 prevention Effects 0.000 claims abstract description 10
- 239000004255 Butylated hydroxyanisole Substances 0.000 claims abstract description 9
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 claims abstract description 9
- 229940043253 butylated hydroxyanisole Drugs 0.000 claims abstract description 9
- 235000019282 butylated hydroxyanisole Nutrition 0.000 claims abstract description 9
- 239000004359 castor oil Substances 0.000 claims abstract description 9
- 235000019438 castor oil Nutrition 0.000 claims abstract description 9
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims abstract description 9
- 239000012051 hydrophobic carrier Substances 0.000 claims abstract description 8
- 239000003381 stabilizer Substances 0.000 claims abstract description 5
- 239000003963 antioxidant agent Substances 0.000 claims abstract description 3
- 239000002562 thickening agent Substances 0.000 claims abstract description 3
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 claims description 16
- 238000002156 mixing Methods 0.000 claims description 14
- 239000002245 particle Substances 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 10
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 8
- 229940081974 saccharin Drugs 0.000 claims description 8
- 235000019204 saccharin Nutrition 0.000 claims description 8
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 8
- 239000000843 powder Substances 0.000 claims description 6
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 238000004040 coloring Methods 0.000 claims description 2
- 235000003599 food sweetener Nutrition 0.000 claims description 2
- 239000003765 sweetening agent Substances 0.000 claims description 2
- 208000007107 Stomach Ulcer Diseases 0.000 description 7
- 241001465754 Metazoa Species 0.000 description 6
- 229920000333 poly(propyleneimine) Polymers 0.000 description 4
- 229940126409 proton pump inhibitor Drugs 0.000 description 4
- 239000000612 proton pump inhibitor Substances 0.000 description 4
- 239000013543 active substance Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- PSIREIZGKQBEEO-UHFFFAOYSA-N 2-(1h-benzimidazol-2-ylsulfinylmethyl)-n-methyl-n-(2-methylpropyl)aniline Chemical compound CC(C)CN(C)C1=CC=CC=C1CS(=O)C1=NC2=CC=CC=C2N1 PSIREIZGKQBEEO-UHFFFAOYSA-N 0.000 description 2
- 241000282414 Homo sapiens Species 0.000 description 2
- IQPSEEYGBUAQFF-UHFFFAOYSA-N Pantoprazole Chemical compound COC1=CC=NC(CS(=O)C=2NC3=CC=C(OC(F)F)C=C3N=2)=C1OC IQPSEEYGBUAQFF-UHFFFAOYSA-N 0.000 description 2
- 208000008469 Peptic Ulcer Diseases 0.000 description 2
- 208000025865 Ulcer Diseases 0.000 description 2
- 230000037396 body weight Effects 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 208000000718 duodenal ulcer Diseases 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229960004770 esomeprazole Drugs 0.000 description 2
- SUBDBMMJDZJVOS-DEOSSOPVSA-N esomeprazole Chemical compound C([S@](=O)C1=NC2=CC=C(C=C2N1)OC)C1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-DEOSSOPVSA-N 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 229960003174 lansoprazole Drugs 0.000 description 2
- MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 description 2
- 229950007395 leminoprazole Drugs 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 229960005019 pantoprazole Drugs 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 231100000397 ulcer Toxicity 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 1
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- 102000004190 Enzymes Human genes 0.000 description 1
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- 241000282326 Felis catus Species 0.000 description 1
- 241000590002 Helicobacter pylori Species 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
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- 230000006806 disease prevention Effects 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 210000004211 gastric acid Anatomy 0.000 description 1
- 230000027119 gastric acid secretion Effects 0.000 description 1
- 231100000029 gastro-duodenal ulcer Toxicity 0.000 description 1
- 208000021302 gastroesophageal reflux disease Diseases 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 230000035876 healing Effects 0.000 description 1
- GPRLSGONYQIRFK-UHFFFAOYSA-N hydron Chemical compound [H+] GPRLSGONYQIRFK-UHFFFAOYSA-N 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
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- 230000003389 potentiating effect Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- 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
- A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Zoology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
There is provided an omeprazole based oral paste formulation for the prevention and
treatment of disease conditions caused by excess stomach acid in horses that suffer stress.
The formulation includes omeprazole, a hydrophobic carrier including sweet almond oil and
aniseed oil, a stabilizing agent including triethanolamine, a thickening agent including
hydrogenated castor oil, and an antioxidant agent including butylated hydroxyanisole. The
omeprazole is in an amount from about 30% to about 45% w/w of the formulation. The
hydrophobic carrier is in an amount from about 50% to about 70% w/w of the formulation.
The weight ratio of sweet almond oil to aniseed oil is from about 6:1 to about 4:1.
Description
The present invention relates to an improved oral paste formulation containing a proton pump inhibitor and, in particular, to an omeprazole based oral paste formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress.
Omeprazole is a well known proton pump inhibitor (PPI) that decreases the amount of acid produced in the stomach, and so is widely used (in appropriate dose strength) to treat, as well as prevent, symptoms of gastroesophageal reflux disease, gastric and duodenal ulcers and other disease conditions caused by excess stomach acid. Omeprazole is also used to treat stomach infections caused by Helicobacter pylori bacteria.
As well as in human medicine, omeprazole is used in veterinary medicine to treat and prevent gastric and duodenal ulcers in horses, dogs, cats and some other companion animals.
Although the preferred PPI used in the present invention is omeprazole, there are other known PPIs which may be used, such as esomeprazole, lansoprazole, pantoprazole and leminoprazole. Methods for their preparation may be found in the literature. For example, in the patent literature, omeprazole is disclosed in EP 5129, esomeprazole is disclosed in US 5,714,504, lansoprazole in EP 174,726, pantoprazole in EP 166,287 and leminoprazole in GB 2,163,747.
Horses, and especially race horses, are prone to developing gastric ulcers (also referred to as stomach ulcers) during times of stress, such as when they are training, competing,
30/05/23 being transported in a horse float or trailer, or confined in a stall or small paddock. Foals may also develop such stress induced ulcers during weaning.
PPIs are potent inhibitors of gastric acid secretion by inhibiting H+K-ATPase, the enzyme involved in the final step of hydrogen ion production in the parietal cells. Hence, PPIs have been used in the treatment of gastric acid related diseases in humans. Peptic ulcers are common also in some animals, particularly in horses. Although the aetiology of gastro-duodenal ulcers in horses has not been ascertained, it appears that stress plays an important role in some cases.
PPIs are highly acid labile and hence oral formulations are enteric coated. Enteric coated formulations are expensive and time consuming to manufacture, and require elaborate technology and equipment. Another disadvantage of an enteric coated formulation is its moisture sensitivity.
W094/25070 discloses an oral composition containing a proton pump inhibitor in the form of enteric coated dry particles mixed with a dry gelling agent. The mixture may then be made into a paste-like gel prior to administration. The composition therefore requires enteric coating, with the aforementioned disadvantages associated with such formulation. Furthermore, because such a moist gel is not stable during long term storage at room temperature it cannot be manufactured and sold as a ready-to-use formulation. Rather, it must be prepared, without preparation, at the time of administration, making it inconvenient to use.
The formulation described herein is a stable, ready-to-use paste formulation containing a proton pump inhibitor suitable for administering to animals such as horses, cattle, pigs etc, and human beings, which may have difficulty swallowing solid dosage forms such as tablets and capsules. The present invention can be easily administered to horses and is readily accepted by these animals. The formulation of the present invention has increased temperature stability during long term storage at room temperature, and has enhanced absorption.
30/05/23
It is, therefore, a preferred object of the present invention to provide an omeprazole based oral paste formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress.
It is another preferred object of the present invention that the aforementioned formulation has increased temperature stability and enhanced absorption by a horse that is at risk of suffering stress, or is suffering stress, over well known omeprazole based oral paste formulations and solid dosage forms.
It is yet another preferred object of the present invention to provide an omeprazole based oral paste formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress and which overcomes, or at least ameliorates the shortcomings of the prior art, or at least provides a useful alternative.
According to one aspect of the present invention, there is provided an omeprazole based oral paste formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress, the formulation comprising omeprazole, a hydrophobic carrier comprising sweet almond oil and aniseed oil, a stabilizing agent comprising triethanolamine, a thickening agent comprising hydrogenated castor oil, and an antioxidant agent comprising butylated hydroxyanisole, wherein the omeprazole is in an amount from about 30% to about 45% w/w of the formulation, the hydrophobic carrier is in an amount from about 50% to about 70% w/w of the formulation, and wherein the weight ratio of sweet almond oil to aniseed oil is from about 6:1 to about 4:1.
Preferably, the omeprazole is in the form of a powder of micronized particles in which about 90% of the particles have a maximum particle diameter of about 1,000 micrometers, and about 10% of the particles have a maximum particle diameter of less than about 800 micrometers.
In a preferred form, the stabilizing agent provides a pH of greater than 9 to the formulation.
The formulation may further comprise a sweetening agent comprising saccharin, and/or a colouring agent comprising iron oxide.
In a particularly preferred embodiment, the formulation comprises 37% w/w omeprazole, 50.14% w/w sweet almond oil, 10% w/w aniseed oil, 1% w/w triethanolamine, 1.5% w/w hydrogenated castor oil, 0.01% w/w butylated hydroxyanisole, 0.2% w/w saccharin, and 0.15% w/w high purity yellow iron oxide.
According to another aspect of the present invention, there is provided a process for preparing the above oral paste formulation, comprising the steps of: (a) mixing sweet almond oil, aniseed oil and triethanolamine until the mixture is uniform, (b) adding saccharin to the mixture from step (a) and mixing until uniform, (c) adding butylated hydroxyanisole to the mixture from step (b) and mixing until completely dissolved, (d) adding omeprazole in micronized powder form and high purity yellow iron oxide to the mixture from step (c) and mixing until completely dispersed, and (e) adding hydrogenated castor oil to the mixture from step (d) and mixing until a uniform and thickened paste forms.
According to yet another aspect of the present invention, there is provided a method for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress, the method comprising orally administering to a horse in need thereof a pharmaceutically effective amount of the above oral paste formulation.
There has been thus outlined, rather broadly, the more important features of the invention in order that the detailed description thereof that follows may be better understood and put into practical effect, and in order that the present contribution to the art may be better appreciated.
There are additional features of the invention that will be described hereinafter. As such, those skilled in the art will appreciate that the conception, upon which the disclosure is based, may be readily utilized as the basis for designing other formulations, process steps and methods of prevention and treatment for carrying out the objects of the present invention. It is important, therefore, that the broad outline of the invention described above be regarded as including such equivalent features insofar as they do not depart from the spirit and scope of the present invention.
EXAMPLE 1
The composition of the formulation used in this Example is as follows:
Omeprazole powder 370 g Sweet almond oil 501.4 g Aniseed oil 100 g Triethanolamine 10g Hydrogenated castor oil 15 g Butylated hydroxyanisole 0.1 g Saccharin 2g High purity yellow iron oxide 1.5 g
Using the above quantities, sweet almond oil, aniseed oil and triethanolamine are mixed until the mixture is uniform. Saccharin is then added with mixing until uniform. Butylated hydroxyanisole is then added with mixing until completely dissolved. Omeprazole powder form (as micronized particles and yellow iron oxide (in high purity) are then added with mixing until completely dispersed. Finally, hydrogenated castor oil is added and mixing continues for about 30 minutes until a uniform and thickened paste forms that is suitable for administration as an oral paste.
The pH of the formulation according to this Example is greater than 9, which is largely attributable to the basifying effect of triethanolamine, to provide a buffered and stable non-acidic environment for the highly acid labile omeprazole.
The temperature stability of this formulation is greater than that of well known omeprazole based oral paste formulations. Without wishing to be bound by theory, this increased temperature stability of the active agent omeprazole is considered to be due to the selection of sweet almond oil and aniseed oil as the hydrophobic carrier in the weight ratio of sweet almond oil to aniseed oil of about 5:1.
EXAMPLE 2
The paste formulation prepared in Example 1 is used to fill paste dosing syringes which are to be used to orally administer a pharmaceutically effective amount of the paste to a horse that is diagnosed with stomach ulcers.
The paste, in a dose strength of omeprazole appropriate for the weight, age and condition of the horse, is deposited on the dorsal part of the affected horse's tongue. Normally, a dose strength range of from about 0.2 mg/kg body weight to about 20 mg/kg body weight may be used.
The amount of the formulation to be administered may vary according to the particular animal species to be treated, the specific active ingredient (i.e. PPI) in the formulation, the severity of the disease, the physical condition of the afflicted animal, and other factors. A physician or veterinarian skilled in the art of ulcer treatment may readily determine the proper dosage for the specific host under treatment.
The omeprazole is absorbed by the affected horse more efficiently and in a greater proportion (at least a 4% enhancement) of the available omeprazole in the formulation than is the case in well known omeprazole based oral paste formulations. Without wishing to be bound by theory, this enhanced absorption of the active agent omeprazole
30/05/23 is considered to be due to the selection of sweet almond oil and aniseed oil as the hydrophobic carrier in the weight ratio of sweet almond oil to aniseed oil of about 5:1.
The stomach ulcers of the affected horse showed significant improvement and healing well within 28 days of orally administering the paste.
EXAMPLE 3
The unused paste dosing syringes filled with the paste formulation in Example 2 are used to orally administer a pharmaceutically effective amount of the paste to a horse that suffers stress and is in need of the prevention of disease conditions caused by excess stomach acid. The same administration procedure as that in Example 2 is followed, but with a reduced daily dose appropriate to the stress levels of the horse, and similarly enhanced absorption of the active agent omeprazole occurs.
Over a 28 day period during which the horse experienced numerous stressful events, no stomach ulcers developed in the horse.
It will be readily apparent to persons skilled in the art that various modifications may be made in details of the design of the omeprazole based oral paste formulation, of the process steps for its preparation, and of the methods which utilize any such formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress, without departing from the scope or ambit of the present invention.
The reference in this specification to any prior publication (or information derived from it), or to any matter which is known, is not, and should not be taken as an acknowledgement or admission or any form of suggestion that that prior publication (or information derived from it) or known matter forms part of the common general knowledge in the field of endeavour to which this specification relates before the filing date of this patent application.
Claims (7)
1. An omeprazole based oral paste formulation for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress, the formulation comprising omeprazole, a hydrophobic carrier comprising sweet almond oil and aniseed oil, a stabilizing agent comprising triethanolamine, a thickening agent comprising hydrogenated castor oil, and an antioxidant agent comprising butylated hydroxyanisole, wherein the omeprazole is in an amount from about 30% to about 45% w/w of the formulation, the hydrophobic carrier is in an amount from about 50% to about 70% w/w of the formulation, and wherein the weight ratio of sweet almond oil to aniseed oil is from about 6:1 to about 4:1.
2. The formulation of claim 1, wherein the omeprazole is in the form of a powder of micronized particles in which about 90% of the particles have a maximum particle diameter of about 1,000 micrometers, and about 10% of the particles have a maximum particle diameter of less than about 800 micrometers.
3. The formulation of claim 1 or claim 2, wherein the stabilizing agent provides a pH of greater than 9 to the formulation.
4. The formulation of any one of claims 1 to 3, further comprising a sweetening agent comprising saccharin, and/or a colouring agent comprising iron oxide.
5. The formulation of claim 4, wherein the formulation comprises 37% w/w omeprazole, 50.14% w/w sweet almond oil, 10% w/w aniseed oil, 1% w/w triethanolamine, 1.5% w/w hydrogenated castor oil, 0.01% w/w butylated hydroxyanisole, 0.2% w/w saccharin, and 0.15% w/w high purity yellow iron oxide.
6. A process for preparing the oral paste formulation of claim 5, comprising the steps of: (a) mixing sweet almond oil, aniseed oil and triethanolamine until the mixture is uniform, (b) adding saccharin to the mixture from step (a) and mixing until uniform, (c) adding butylated hydroxyanisole to the mixture from step (b) and mixing until completely dissolved,
(d) adding omeprazole in micronized powder form and high purity yellow iron oxide to the mixture from step (c) and mixing until completely dispersed, and (e) adding hydrogenated castor oil to the mixture from step (d) and mixing until a uniform and thickened paste forms.
7. A method for the prevention and treatment of disease conditions caused by excess stomach acid in horses that suffer stress, the method comprising orally administering to a horse in need thereof a pharmaceutically effective amount of the oral paste formulation of any one of claims I to 5.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2022902313 | 2022-08-15 | ||
| AU2022902313A AU2022902313A0 (en) | 2022-08-15 | Omeprazole Based Oral Paste Formulation Having Increased Temperature Stability and Enhanced Absorption |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2023203385A1 true AU2023203385A1 (en) | 2024-02-29 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2023203385A Pending AU2023203385A1 (en) | 2022-08-15 | 2023-05-30 | Omeprazole based oral paste formulation having increased temperature stability and enhanced absorption |
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| Country | Link |
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| AU (1) | AU2023203385A1 (en) |
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2023
- 2023-05-30 AU AU2023203385A patent/AU2023203385A1/en active Pending
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