GB2285923A - Pharmaceutical powder containing N-acetyl-cysteine - Google Patents
Pharmaceutical powder containing N-acetyl-cysteine Download PDFInfo
- Publication number
- GB2285923A GB2285923A GB9500764A GB9500764A GB2285923A GB 2285923 A GB2285923 A GB 2285923A GB 9500764 A GB9500764 A GB 9500764A GB 9500764 A GB9500764 A GB 9500764A GB 2285923 A GB2285923 A GB 2285923A
- Authority
- GB
- United Kingdom
- Prior art keywords
- composition according
- acetyl
- cysteine
- weight
- pharmaceutical composition
- 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
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 title claims description 7
- 229960004308 acetylcysteine Drugs 0.000 title claims description 7
- 239000000843 powder Substances 0.000 title claims description 4
- 239000000203 mixture Substances 0.000 claims description 12
- 239000006188 syrup Substances 0.000 claims description 9
- 235000020357 syrup Nutrition 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 6
- 229930006000 Sucrose Natural products 0.000 claims description 6
- 235000013681 dietary sucrose Nutrition 0.000 claims description 6
- 229960004793 sucrose Drugs 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 238000004090 dissolution Methods 0.000 claims description 5
- 239000001509 sodium citrate Substances 0.000 claims description 5
- 159000000000 sodium salts Chemical class 0.000 claims description 5
- 229940038773 trisodium citrate Drugs 0.000 claims description 5
- KCXVZYZYPLLWCC-UHFFFAOYSA-N EDTA Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims description 4
- 239000000654 additive Substances 0.000 claims description 4
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 claims description 4
- 239000002904 solvent Substances 0.000 claims description 3
- 239000000796 flavoring agent Substances 0.000 claims description 2
- 235000010268 sodium methyl p-hydroxybenzoate Nutrition 0.000 claims 1
- 239000004290 sodium methyl p-hydroxybenzoate Substances 0.000 claims 1
- PESXGULMKCKJCC-UHFFFAOYSA-M sodium;4-methoxycarbonylphenolate Chemical compound [Na+].COC(=O)C1=CC=C([O-])C=C1 PESXGULMKCKJCC-UHFFFAOYSA-M 0.000 claims 1
- 239000013543 active substance Substances 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 239000004615 ingredient Substances 0.000 description 2
- 230000000510 mucolytic effect Effects 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- QZKRHPLGUJDVAR-UHFFFAOYSA-K EDTA trisodium salt Chemical compound [Na+].[Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O QZKRHPLGUJDVAR-UHFFFAOYSA-K 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229960002433 cysteine Drugs 0.000 description 1
- 239000003172 expectorant agent Substances 0.000 description 1
- 230000003419 expectorant effect Effects 0.000 description 1
- 230000002349 favourable effect Effects 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000000873 masking effect Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 210000003097 mucus Anatomy 0.000 description 1
- 239000008063 pharmaceutical solvent Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 230000000241 respiratory effect Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000000126 substance Substances 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
Landscapes
- 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)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
2285923 TITLE:
Pharmaceutical compositions containing N-acetyl-eysteine DESCRIPTION:
Technical Field
N-acetyl-cysteine is a pharmaceutically active substance which is well known for its favourable properties in the fluidification of mucus. This substance advantageously fluidifies the secretions notably in cases of infection of the respiratory and mucoviscidory tracts. It is therefore called mucolytic or expectorant.
For its practical utilisation as a mucolytic, N-acetyl-eysteine can be taken via the buccal route in the form of an aqueous solution obtained by dissolution of an effervescent granulate or tablet, or in the form of a tablet or of a capsule for ingestion with water. The organoleptic properties of this active substance are most disagreeable. For the production of these formulations for administration by the buccal route, it is necessary to mask the repulsive taste of N-acetyl-cysteine. The formulations for absorption by the oral route are either taken with water followed by dissolution inside the body, or to absorb directly after dissolution.
The Invention The invention provides a pharmaceutical composition in the form of a powder comprising:
N-acetyl-eysteine 7 - 10 % by weight Trisodium citrate 7 - 10 % by weight Saccharose 80 - 86 % by weight.
Such compositions can be kept in the fluid state during a prolonged period, and will be stable to storage in normal temperature conditions. They maintain an agreeable taste, or the disagreeable organolyptic properties of the active substance is masked. They are suitable for extemporaneous preparation by dissolution at the appropriate moment through agitation in a compatible pharmaceutical solvent, for preference water, to prepare a syrup ready for use. The resulting syrup has a good taste, masking that of the N-ac etyl -cyst eine, and it keeps this good taste during the period of its utilization.
The composition may also contain minor quantities of additives commonly used in pharmacy, preferably in a global fraction of from 0.1 to 1% by weight. Such additives may comprise the sodium salt of EDTA, conservation agents, saponifying agents and/or flavourings.
The syrup can be put up in ampoules for unitary dosage posology containing a quantity of N-acetyl-eysteine from 100 to 600 mg, for preference from 100 to 200 mg, advantageously of 200 mg. A unique volume of syrup may be equal to several (for example 7) unitary posology doses. It may then be kept in a bottle for example of 100, 150 or 250 ml of syrup after addition of solvent. In these bottles, the concentration of N- acetyl-eysteine is such that each administration (for example an appropriate measure or a coffee spoon) contains a quantity of active substance of about 100 to about 600 mg, for preference of 100 to 200 mg.
Example 1
Composition of a syrup according to the invention.
Component Quantity % by weight N-acetyl-eysteine + excess (5%) Sodium salt of EDTA Trisodium citrate Sodium methylparahyroxybenzoate Saponifying agent Saccharose (ultra fine quality) 6.0 g 0.3 g 0.03 g 7.28 g 0.18 g 0.21 g 60 g 74 g 8.51 o.4 0.04 9.84 0.24 0.28 81.08 99.99 j The total is made up to 150 ml by adding water. The excess of 5% of N- acetyl-cysteine is added to balance the loss during the pot life of the reconstituted solution.
Example 2 Process for the production of the syrup described Example 11,
The following ingredients are sieved:
N-acetyl-eysteine 710 m Sodium salt of EDTA 125 m Trisodium citrate 315 m Sodium methylparahyroxybenzoate 125 m Saccharose 710 m and the appropriate quantities of sodium salt of EDTA, sodium methylparahydroxybenzxoate, saponifying agent and 10% of the saccharose are stirred together for 20 minutes at 70 revolutions/minutes. The other ingredients: trisodium citrate, N-acetyl-cysteine and 90% of the saccharose are added, and the stirring is continued for 30 minutes at 65 revolutions /minute. 74 g of the powder mixture is decanted into each of two bottles. During the production, the humidity rate does not exceed 30%.
After reconstitution, addition of water to the solution to make it up to 150 ml, the pH is 4.3 + 0-5-
Claims (10)
1. A pharmaceutical composition in the form of a powder comprising:
N-acetyl-cysteine 7 - 10 % by weight Trisodium citrate 7 - 10 % by weight Saccharose 8o - 86 % by weight.
2. A composition according to claim 1, containing additives commonly used in pharmacy in a global fraction of from 0.1 to 1% by weight.
3. A composition according to claim 2, in which the additives comprise the sodium salt of EDTA, conservation agents, saponifying agents andlor flavourings.
4. A composition according to claim 3 containing as a conservation agent sodium methylparahydroxybenzoate.
5. A pharmaceutical composition in the form of a syrup obtained by dissolution of a composition according to any preceding claim in a solvent.
6. A composition according to claim 5, in which the solvent is water.
7. A pharmaceutical composition according to claim 5 or claim 6 containing in unitary posological dose from 100 to 600 mg N-acetyl- cysteine.
8. A pharmaceutical composition according to claim 7 containing from 100 to 200 mg N-acetyl-eysteine.
9. A pharmaeutical composition according to claim 5, in the form of a unique volume of syrup equal to 7 unitary posological doses.
Z
10. A pharmaceutical composition substantially as herein described in Example 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BE9400104A BE1007926A3 (en) | 1994-01-31 | 1994-01-31 | Pharmaceutical composition containing n-acetyl-cysteine. |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| GB9500764D0 GB9500764D0 (en) | 1995-03-08 |
| GB2285923A true GB2285923A (en) | 1995-08-02 |
| GB2285923B GB2285923B (en) | 1997-11-19 |
Family
ID=3887927
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB9500764A Expired - Fee Related GB2285923B (en) | 1994-01-31 | 1995-01-16 | Pharmaceutical compositions containing N-acetal-cysteine |
Country Status (6)
| Country | Link |
|---|---|
| BE (1) | BE1007926A3 (en) |
| DE (1) | DE19502566A1 (en) |
| FR (1) | FR2715564B1 (en) |
| GB (1) | GB2285923B (en) |
| IT (1) | IT1272935B (en) |
| NL (1) | NL193607C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR1007236B (en) * | 2009-12-07 | 2011-04-08 | Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Αβεε Με Δ.Τ. Uni-Pharma Abee, | New pharmaceutical composition of n-acetylcysteine granules and production method thereof |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA963590B (en) * | 1995-05-10 | 1996-11-19 | Adcock Ingram Ltd | Pharmaceutical composition |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2192790A (en) * | 1986-07-24 | 1988-01-27 | Inpharzam Int Sa | Acetylcysteine compositions |
| GB2234171A (en) * | 1989-07-27 | 1991-01-30 | Zambon Spa | Composition containing N-acetyl-cysteine of enhanced bioavailability |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH666814A5 (en) * | 1986-07-24 | 1988-08-31 | Inpharzam Int Sa | WATER-SOLUBLE PHARMACEUTICAL COMPOSITION CONTAINING N-ACETYL-CISTEIN. |
| IT1234194B (en) * | 1988-05-31 | 1992-05-06 | Magis Farmaceutici | SYRUP PHARMACEUTICAL COMPOSITIONS CONTAINING PENTITLES AS VEHICULATING AGENTS |
-
1994
- 1994-01-31 BE BE9400104A patent/BE1007926A3/en not_active IP Right Cessation
-
1995
- 1995-01-09 FR FR9500150A patent/FR2715564B1/en not_active Expired - Fee Related
- 1995-01-16 GB GB9500764A patent/GB2285923B/en not_active Expired - Fee Related
- 1995-01-23 NL NL9500120A patent/NL193607C/en not_active IP Right Cessation
- 1995-01-25 IT ITMI950120A patent/IT1272935B/en active IP Right Grant
- 1995-01-27 DE DE19502566A patent/DE19502566A1/en not_active Ceased
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2192790A (en) * | 1986-07-24 | 1988-01-27 | Inpharzam Int Sa | Acetylcysteine compositions |
| GB2234171A (en) * | 1989-07-27 | 1991-01-30 | Zambon Spa | Composition containing N-acetyl-cysteine of enhanced bioavailability |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GR1007236B (en) * | 2009-12-07 | 2011-04-08 | Uni-Pharma Κλεων Τσετης Φαρμακευτικα Εργαστηρια Αβεε Με Δ.Τ. Uni-Pharma Abee, | New pharmaceutical composition of n-acetylcysteine granules and production method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| BE1007926A3 (en) | 1995-11-21 |
| DE19502566A1 (en) | 1995-08-03 |
| GB2285923B (en) | 1997-11-19 |
| NL193607B (en) | 1999-12-01 |
| IT1272935B (en) | 1997-07-01 |
| FR2715564A1 (en) | 1995-08-04 |
| GB9500764D0 (en) | 1995-03-08 |
| NL193607C (en) | 2000-04-04 |
| NL9500120A (en) | 1995-09-01 |
| ITMI950120A1 (en) | 1996-07-25 |
| FR2715564B1 (en) | 1996-08-02 |
| ITMI950120A0 (en) | 1995-01-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PCNP | Patent ceased through non-payment of renewal fee |
Effective date: 20110116 |