WO1996003980A1 - Improved effervescent delivery system - Google Patents
Improved effervescent delivery system Download PDFInfo
- Publication number
- WO1996003980A1 WO1996003980A1 PCT/US1995/009540 US9509540W WO9603980A1 WO 1996003980 A1 WO1996003980 A1 WO 1996003980A1 US 9509540 W US9509540 W US 9509540W WO 9603980 A1 WO9603980 A1 WO 9603980A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- composition
- acid
- bicarbonate
- tablet
- weight
- Prior art date
Links
- 239000003826 tablet Substances 0.000 claims abstract description 18
- BVKZGUZCCUSVTD-UHFFFAOYSA-M Bicarbonate Chemical compound OC([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-M 0.000 claims abstract description 14
- 239000000796 flavoring agent Substances 0.000 claims abstract description 12
- 235000019634 flavors Nutrition 0.000 claims abstract description 12
- 239000002253 acid Substances 0.000 claims abstract description 11
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 9
- 239000003765 sweetening agent Substances 0.000 claims abstract description 9
- 239000007938 effervescent tablet Substances 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 21
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 7
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 7
- 239000002245 particle Substances 0.000 claims description 6
- -1 alkali metal bicarbonate Chemical class 0.000 claims description 5
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims description 4
- 229910052783 alkali metal Inorganic materials 0.000 claims description 4
- 150000007524 organic acids Chemical class 0.000 claims description 4
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 2
- 235000019204 saccharin Nutrition 0.000 claims description 2
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 2
- 229940081974 saccharin Drugs 0.000 claims description 2
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 2
- 239000003381 stabilizer Substances 0.000 claims description 2
- 235000000346 sugar Nutrition 0.000 claims description 2
- 229960001295 tocopherol Drugs 0.000 claims description 2
- 229930003799 tocopherol Natural products 0.000 claims description 2
- 235000010384 tocopherol Nutrition 0.000 claims description 2
- 239000011732 tocopherol Substances 0.000 claims description 2
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 2
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 238000009472 formulation Methods 0.000 description 5
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 4
- 108010011485 Aspartame Proteins 0.000 description 3
- 239000000605 aspartame Substances 0.000 description 3
- 235000010357 aspartame Nutrition 0.000 description 3
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 3
- 229960003438 aspartame Drugs 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 3
- 150000001340 alkali metals Chemical class 0.000 description 2
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 description 2
- 229910000029 sodium carbonate Inorganic materials 0.000 description 2
- BSYNRYMUTXBXSQ-FOQJRBATSA-N 59096-14-9 Chemical compound CC(=O)OC1=CC=CC=C1[14C](O)=O BSYNRYMUTXBXSQ-FOQJRBATSA-N 0.000 description 1
- 150000005323 carbonate salts Chemical class 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 235000019223 lemon-lime Nutrition 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000000820 nonprescription drug Substances 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
- 150000003444 succinic acids Chemical class 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 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
- A61K31/60—Salicylic acid; Derivatives thereof
- A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
- A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
Definitions
- Effervescent tablets containing medicinal or nutritional supplements are marketed worldwide as over-the-counter products. These tablets are added to water and dissolved with a characteristic effervescence, prior to ingestion. Although these formulations have the advantage of delivering medication in solution, they have the additional problem of requiring a high degree of flavoring to mask the taste of the incorporated medications or supplements. In addition, because of the high reactivity of the effervescent components the tablet is prone to stability problems and can also be very difficult to compress into a suitably hard tablet for packaging and sale. This invention provides a formulation which solves the latter problem.
- the preferred particle size of the acetylsalicylic acid is such that not more than 5% passes through a 40 mesh screen and not more than 20% passes through a 100 mesh screen, ie a normal distribution of particles between about 100 and 450 microns.
- Flavors are an important component of effervescent formulations. It has been found that high intensity flavors, containing tocopherol as a stabilizing agent provide better and more prolonged flavor stability in the composition of the invention. Such flavors are available from Firmenich Incorporated, Princeton, NJ. Preferably such flavors are incorporated at levels between 0.156 to about 0.5% of the tablet weight.
- Sweeteners are generally used in effervescent formulations. The preferred range for a sweetener in this composition is from about 0.4 lo 1.0 percent of the tablet weight. Any sweetener which imparts the necessary flavor may be used. Among the suggested sweeteners are sugar, aspartame and saccharin. Aspartame is a preferred sweetener.
- composition of the invention is further illustrated by the following example.
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
Abstract
An improved effervescent tablet is provided. The tablet contains acetylisylic acid, a critical ratio of bicarbonate to acid, flavors, sweeteners, tableting aids, and optionally other medicinals. The tablet has improved hardness and stability and can be readily compressed into a relatively small (by weight and diameter) effervescent tablet.
Description
IMPROVED EFFERVESCENT DELIVERY SYSTEM
FIELD OF THE INVENTION
The invention relates in general to effervescent compositions and in particular to effervescent compositions containing acelylsalicylic acid provided in tablet form.
BACKGROUND OF THE INVENTION
Effervescent tablets containing medicinal or nutritional supplements are marketed worldwide as over-the-counter products. These tablets are added to water and dissolved with a characteristic effervescence, prior to ingestion. Although these formulations have the advantage of delivering medication in solution, they have the additional problem of requiring a high degree of flavoring to mask the taste of the incorporated medications or supplements. In addition, because of the high reactivity of the effervescent components the tablet is prone to stability problems and can also be very difficult to compress into a suitably hard tablet for packaging and sale. This invention provides a formulation which solves the latter problem.
SUMMARY OF THE INVENTION
Disclosed herein is a composition containing between 0 lo 13 % (by weight) of acelylsalicylic acid and an effervescent component. In order to provide suitable tablet compressibility, it has been found that the ratio of bicarbonate component to acid, should be in the range between 1.5 and 1.0. The bicarbonate component is
composed of 80 to 90% bicarbonate and 10 to 20% carbonate. The remainder of the tablet composition is composed of sweetener, flavors, and tableting aids. Additional medications may be added.
DESCRIPTION OF THE INVENTION
The invention disclosed herein provides an improved effervescent tablet containing acetylsalicylic acid and optionally other medicinals. The acetylsallcylic acid is present in a range between about 8 and 13 percent of the tablet and is generally sufficient to provide good lablet lubrication. The weight percentages given are based on a tablet weight range of from about 2000 to about 2400 mg for an effervescent tablet having a tablet diameter of about 19 millimeters (mm) to 22.5 mm. The weight range is preferably from about 2950 to about 3200 mg.
The effervescent component of the formulation is composed of an alkali metal bicarbonate component and an organic acid useful for consumption in medicinals. The alkali metal or alkaline earth metal bicarbonate component (referred to herein as the "bicarbonate component") is actually a combination of 80 to 90% by weight of bicarbonate and 10 - 20% by weight carbonate salt. It has been found that the ratio of bicarbonate component to organic acid is critical to provide suitable tablet hardness The ratio of bicaibonate component to acid is critical to provide improved tablet compressibility wiiile maintaining a low tablet weight and is between about 1.5 to about 1.8.
Sodium bicarbonate and sodium carbonate are the preferred ingredients of the bicarbonate component. But other alkali metal or alkaline earth metal salts, may be used as is well known in the art. Although any of a number of organic acids,
including citric, malic, lartaric and succinic acids may be used, citric acid is preferred.
The preferred particle size of the acetylsalicylic acid is such that not more than 5% passes through a 40 mesh screen and not more than 20% passes through a 100 mesh screen, ie a normal distribution of particles between about 100 and 450 microns.
Flavors are an important component of effervescent formulations. It has been found that high intensity flavors, containing tocopherol as a stabilizing agent provide better and more prolonged flavor stability in the composition of the invention. Such flavors are available from Firmenich Incorporated, Princeton, NJ. Preferably such flavors are incorporated at levels between 0.156 to about 0.5% of the tablet weight.
Sweeteners are generally used in effervescent formulations. The preferred range for a sweetener in this composition is from about 0.4 lo 1.0 percent of the tablet weight. Any sweetener which imparts the necessary flavor may be used. Among the suggested sweeteners are sugar, aspartame and saccharin. Aspartame is a preferred sweetener.
It has been found that the composition described above allows the delivery of suitable amounts of acetylsalicylic acid, and optionally other medical components sometimes used in combination with acetylsalicylic acid.
The composition of the invention is further illustrated by the following example.
Example: FLAVORED EFFERVESCENT TABLET bicarbonate component 1700. mg critic acid 1000. mg aspirin 330. mg aspartame 20 mg flavor (lemon lime) 8 mg tableting aids 1.5 mg
The bicarbonate component is composed of sodium bicarbonate and carbonate as described previously and prepared in a Huhn dryer. The acetylsalicylic acid is preferably in a particle size range from about 100 to about 450 microns. All components are weighed and mixed for about 10 to 20 minutes. The mixture is pan blended through a sifter using a suitable screen. The preferred particle size of acetylsalicylic acid is achieved by a distribution of particles not greater than 5% above 400 microns and not greater than 20% below 100 microns. After sifting the mixlure is returned to the mixer from from about 5 to 10 minutes. Finally the mixture is compress by standard methods in a tablet press.
It should be understood that many modifications and variations may be made in the proportions and components used herein without departing from the spirit and scope of the invention, which is solely defined by the claims.
Claims
1. An effervescent tablet composition, comprising: a. an effervescent couple, composed of an alkali metal bicarbonate and an organic acid chosen from the group consisling of citric, malic, succinc and lartaric acid wherein the ratio of bicarbonate component lo acid is in the range between about 1.5 to about 1.8; b. from aboul 8 to about 13% by weighl of acelylisalicyiic acid; c. from about 0.156 to about 0.5% by weight of a flavor component; d. from about 0.4% to about 1 % by weight of a sweetener; and e. tableting aids.
2. The composition of claim 1 , wherein the total tablet weight is in the range between 2,000 to 3,400 milligrams .
3. The composition of claim 2, wherein the tablet diameter is between about 19 and about 22.5 mm.
4. The composition of claim 1 wherein the bicarbonate component is composed of between about 80 to 90% by weight of bicarbonate and 10 to 20 % by weighl of carbonate.
5. The composition of claim 4 wherein the bicarbonate and carbonate both sodium salts.
6. The composition of claim 2 in which the particle size of acetylsalicylic acid is between aboul 100 and about 450 microns.
7. The composition of claim 1 in which the sweetener is selected from the group consisting of sugar, asparlame and saccharin.
8. The composilion of claim 1 in which the flavors are high intensity flavors containing tocopherol as a stabilizer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU31524/95A AU3152495A (en) | 1994-07-29 | 1995-07-28 | Improved effervescent delivery system |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US28305794A | 1994-07-29 | 1994-07-29 | |
| US08/283,057 | 1994-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1996003980A1 true WO1996003980A1 (en) | 1996-02-15 |
Family
ID=23084300
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1995/009540 WO1996003980A1 (en) | 1994-07-29 | 1995-07-28 | Improved effervescent delivery system |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU3152495A (en) |
| WO (1) | WO1996003980A1 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2189639A1 (en) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Aqueous medicinal composition containing dissolved acid consists of an oral medicine containing acetyl salicylic acid dissolved in water, with additives |
| WO2023182904A1 (en) * | 2022-03-21 | 2023-09-28 | Акционерное Общество "Производственная Фармацевтическая Компания Обновление" | Effervescent medicinal preparation for forming a solution and method of producing same |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2211485A (en) * | 1940-08-13 | Effervescent acetyl salicylic acid |
-
1995
- 1995-07-28 AU AU31524/95A patent/AU3152495A/en not_active Abandoned
- 1995-07-28 WO PCT/US1995/009540 patent/WO1996003980A1/en active Application Filing
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2211485A (en) * | 1940-08-13 | Effervescent acetyl salicylic acid |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2189639A1 (en) * | 2001-05-22 | 2003-07-01 | Cordon Jesus Angel Hernandez | Aqueous medicinal composition containing dissolved acid consists of an oral medicine containing acetyl salicylic acid dissolved in water, with additives |
| WO2023182904A1 (en) * | 2022-03-21 | 2023-09-28 | Акционерное Общество "Производственная Фармацевтическая Компания Обновление" | Effervescent medicinal preparation for forming a solution and method of producing same |
Also Published As
| Publication number | Publication date |
|---|---|
| AU3152495A (en) | 1996-03-04 |
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