CA2594185A1 - Solid dosage forms comprising a substituted benzimidazole derivative and a buffer - Google Patents
Solid dosage forms comprising a substituted benzimidazole derivative and a buffer Download PDFInfo
- Publication number
- CA2594185A1 CA2594185A1 CA002594185A CA2594185A CA2594185A1 CA 2594185 A1 CA2594185 A1 CA 2594185A1 CA 002594185 A CA002594185 A CA 002594185A CA 2594185 A CA2594185 A CA 2594185A CA 2594185 A1 CA2594185 A1 CA 2594185A1
- Authority
- CA
- Canada
- Prior art keywords
- pharmaceutical composition
- oral pharmaceutical
- tablet
- recited
- proton pump
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 title 1
- 239000007909 solid dosage form Substances 0.000 title 1
- 239000006172 buffering agent Substances 0.000 claims abstract 13
- 210000004211 gastric acid Anatomy 0.000 claims abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 2
- 239000008203 oral pharmaceutical composition Substances 0.000 claims 18
- 229940126409 proton pump inhibitor Drugs 0.000 claims 13
- 239000000612 proton pump inhibitor Substances 0.000 claims 13
- 239000007788 liquid Substances 0.000 claims 10
- 239000003826 tablet Substances 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 239000012190 activator Substances 0.000 claims 6
- 239000007787 solid Substances 0.000 claims 6
- 210000001711 oxyntic cell Anatomy 0.000 claims 5
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical group [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims 4
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 4
- 239000000843 powder Substances 0.000 claims 4
- YAPQBXQYLJRXSA-UHFFFAOYSA-N theobromine Chemical compound CN1C(=O)NC(=O)C2=C1N=CN2C YAPQBXQYLJRXSA-UHFFFAOYSA-N 0.000 claims 4
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims 4
- 239000007938 effervescent tablet Substances 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- YREYEVIYCVEVJK-UHFFFAOYSA-N rabeprazole Chemical compound COCCCOC1=CC=NC(CS(=O)C=2NC3=CC=CC=C3N=2)=C1C YREYEVIYCVEVJK-UHFFFAOYSA-N 0.000 claims 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 claims 2
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims 2
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims 2
- 244000269722 Thea sinensis Species 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 239000002518 antifoaming agent Substances 0.000 claims 2
- 229960001948 caffeine Drugs 0.000 claims 2
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims 2
- 159000000007 calcium salts Chemical class 0.000 claims 2
- 239000002775 capsule Substances 0.000 claims 2
- 239000007910 chewable tablet Substances 0.000 claims 2
- 229940068682 chewable tablet Drugs 0.000 claims 2
- 235000019219 chocolate Nutrition 0.000 claims 2
- -1 dontoprazole Chemical compound 0.000 claims 2
- 239000007911 effervescent powder Substances 0.000 claims 2
- 239000000796 flavoring agent Substances 0.000 claims 2
- 235000013355 food flavoring agent Nutrition 0.000 claims 2
- 239000008187 granular material Substances 0.000 claims 2
- 229960003174 lansoprazole Drugs 0.000 claims 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 claims 2
- 239000001525 mentha piperita l. herb oil Substances 0.000 claims 2
- 239000001683 mentha spicata herb oil Substances 0.000 claims 2
- 229960000381 omeprazole Drugs 0.000 claims 2
- 239000008188 pellet Substances 0.000 claims 2
- 235000019477 peppermint oil Nutrition 0.000 claims 2
- 229960004157 rabeprazole Drugs 0.000 claims 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims 2
- 235000017557 sodium bicarbonate Nutrition 0.000 claims 2
- 235000019721 spearmint oil Nutrition 0.000 claims 2
- 239000007916 tablet composition Substances 0.000 claims 2
- 229960004559 theobromine Drugs 0.000 claims 2
- 229960000278 theophylline Drugs 0.000 claims 2
- 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 claims 1
- 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 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000002708 enhancing effect Effects 0.000 claims 1
- KWORUUGOSLYAGD-YPPDDXJESA-N esomeprazole magnesium Chemical compound [Mg+2].C([S@](=O)C=1[N-]C2=CC=C(C=C2N=1)OC)C1=NC=C(C)C(OC)=C1C.C([S@](=O)C=1[N-]C2=CC=C(C=C2N=1)OC)C1=NC=C(C)C(OC)=C1C KWORUUGOSLYAGD-YPPDDXJESA-N 0.000 claims 1
- 239000008240 homogeneous mixture Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 229950007395 leminoprazole Drugs 0.000 claims 1
- 229960005019 pantoprazole Drugs 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
New pharmaceutical composition comprising a PPI and a buffering agent in treating gastric acid disorders.
Claims (22)
1. A liquid oral pharmaceutical composition, comprising:
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein if said proton pump inhibitor is omeprazole, it must be present in a concentration greater than 1.2 mg/ml, and if said inhibitor is lansoprazole, it must be present in a concentration greater than 0.3 mg/ml.
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein if said proton pump inhibitor is omeprazole, it must be present in a concentration greater than 1.2 mg/ml, and if said inhibitor is lansoprazole, it must be present in a concentration greater than 0.3 mg/ml.
2. The liquid oral pharmaceutical composition as recited in Claim 1 further comprising a parietal cell activator.
3. The liquid oral pharmaceutical composition as recited in Claim 2 wherein said activator is selected from the group consisting of chocolate, sodium bicarbonate, a calcium salt, peppermint oil, spearmint oil, coffee, tea, cola, caffeine, theophylline, theobromine, at least one amino acid, and combinations thereof.
4. The liquid oral pharmaceutical composition as recited in Claim 1 further comprising an anti-foaming agent.
5. The liquid oral pharmaceutical composition as recited in Claim 1 further comprising a flavoring agent.
6. A liquid oral pharmaceutical composition, comprising:
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein said proton pump inhibitor is selected from the group consisting of omeprazole (in a concentration greater than 1.2 mg/ml), lansoprazole (in a concentration greater than 0.3 mg/ml), pantoprazole, rabeprazole, dontoprazole, perprazole, habeprazole, ransoprazole, pariprazole, and leminoprazole.
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein said proton pump inhibitor is selected from the group consisting of omeprazole (in a concentration greater than 1.2 mg/ml), lansoprazole (in a concentration greater than 0.3 mg/ml), pantoprazole, rabeprazole, dontoprazole, perprazole, habeprazole, ransoprazole, pariprazole, and leminoprazole.
7. A solid oral pharmaceutical composition, comprising:
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein said composition is in a dosage form selected from the group consisting of a powder, a tablet, a suspension tablet, a chewable tablet, a capsule, an effervescent powder, an effervescent tablet, pellets and granules, and wherein said dosage form is not enteric coated or time-released.
a) a proton pump inhibitor; and b) at least one buffering agent;
wherein said composition is in a dosage form selected from the group consisting of a powder, a tablet, a suspension tablet, a chewable tablet, a capsule, an effervescent powder, an effervescent tablet, pellets and granules, and wherein said dosage form is not enteric coated or time-released.
8. The solid oral pharmaceutical composition as recited in Claim 7 further comprising a parietal cell activator.
9. The solid oral pharmaceutical composition as recited in Claim 7 further comprising an anti-foaming agent.
10. The solid oral pharmaceutical composition as recited in Claim 7 wherein said composition is in the form of a tablet, said tablet comprising a central core of said proton pump inhibitor uniformly surrounded by the at least one buffering agent.
11. The tablet composition as recited in Claim 10 wherein the buffering agent is sodium bicarbonate in an amount of approximately 1 mEq to approximately 25 mEq.
12. The solid oral pharmaceutical composition as recited in Claim 7 wherein said composition is in the form of a tablet, said tablet comprising a substantially homogeneous mixture of said proton pump inhibitor and said at least one buffering agent.
13. The tablet composition as recited in Claim 12 wherein the buffering agent is sodium bicarbonate in an amount of approximately 1 mEq to approximately 25 mEq.
14. The solid oral pharmaceutical composition as recited in Claim 7 wherein said composition is in the form of an effervescent tablet, said tablet further comprising an effervescing agent.
15. A method of treating gastric acid disorders comprising administering to a patient an oral pharmaceutical composition comprising a proton pump inhibitor and at least one buffering agent wherein said administering step comprises providing a patient with a single dose of the pharmaceutical composition without requiring further administration of the at least one buffering agent.
16. A kit for the preparation of a liquid oral pharmaceutical composition, comprising:
a) a powder comprising a proton pump inhibitor; and b) a liquid buffering agent to be mixed with said powder to form said liquid composition.
a) a powder comprising a proton pump inhibitor; and b) a liquid buffering agent to be mixed with said powder to form said liquid composition.
17. A kit for the preparation of a liquid oral pharmaceutical composition, comprising a proton pump inhibitor in combination with at least one buffering agent, said combination in a dry form, and a diluent to be mixed with said dry form to create said composition.
18. An oral pharmaceutical composition to be administered in combination with a proton pump inhibitor, comprising at least one buffering agent, wherein said composition is in a dosage form selected from the group consisting of a powder, a tablet, a chewable tablet, a capsule, an effervescent powder, an effervescent tablet, pellets and granules, and wherein said dosage form is not enteric coated or time-released.
19. The oral pharmaceutical composition of Claim 18 further comprising a parietal cell activator.
20. The oral pharmaceutical composition of Claim 18 further comprising a flavoring agent.
21. A method for enhancing the pharmacological activity of a proton pump inhibitor intravenously administered to a patient, comprising orally administering to the patient at least one parietal cell activator at a time interval selected from the group consisting of before, during and after the intravenous administration of the proton pump inhibitor.
22. The method as recited in claim 21 wherein the parietal cell activator is selected from the group consisting of chocolate, sodium bicarbonate, a calcium salt, peppermint oil, spearmint oil, coffee, tea, cola, caffeine, theophylline, theobromine, at least one amino acid, and combinations thereof.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/481,207 | 2000-01-11 | ||
| US09/481,207 US6489346B1 (en) | 1996-01-04 | 2000-01-11 | Substituted benzimidazole dosage forms and method of using same |
| CA002396159A CA2396159C (en) | 2000-01-11 | 2001-01-10 | Novel substituted benzimidazole dosage forms and method of using same |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002396159A Division CA2396159C (en) | 2000-01-11 | 2001-01-10 | Novel substituted benzimidazole dosage forms and method of using same |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2594185A1 true CA2594185A1 (en) | 2001-07-19 |
| CA2594185C CA2594185C (en) | 2011-08-23 |
Family
ID=38653228
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2594185A Expired - Fee Related CA2594185C (en) | 2000-01-11 | 2001-01-10 | Solid dosage forms comprising a substituted benzimidazole derivative and a buffer |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA2594185C (en) |
-
2001
- 2001-01-10 CA CA2594185A patent/CA2594185C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CA2594185C (en) | 2011-08-23 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20190110 |
|
| MKLA | Lapsed |
Effective date: 20190110 |