Pharmaceutical composotion of paracetamol in a water-soluble form in a hermetically sealed container for preparing a hot beverage

Abstract

The present invention refers to pharmaceutical compositions suitable for oral administration comprising paracetamol in a water-soluble form, preferably in effervescent form, which composition is into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, more preferably into a thermoformed capsule, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages.

Description

[0001] Pharmaceutical composition of paracetamol in a water-soluble form in a hermetically sealed container for preparing a hot beverage

[0002] Description of the invention

[0003] The present invention refers to pharmaceutical compositions suitable for oral administration comprising paracetamol in a water-soluble form, preferably in effervescent form, which composition is into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, more preferably into a thermoformed capsule, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages.

[0004] Paracetamol is the main active metabolite of phenacetin and acetanidii and exhibits analgesic and antipyretic properties, as well as a weak anti-inflammatory effect.

[0005] Paracetamol presents stability problems when it is exposed to environmental factors, especially in the presence of oxygen and moisture.

[0006] The administration of effervescent pharmaceutical forms is desirable in cases of difficulties to swallow, in elderly and paediatric patient populations. However, the storage of effervescent forms must be done in conditions that completely prevent contact with oxygen and moisture. The storage of the effervescent forms in packages referred to in the state of the art, such as for example in aluminium packages, polyethylene and / or aluminium tapes, sachets, presents problems of oxygen and moisture absorption from the environment, leading to stability problems.

[0007] The documents GR20100100363, CN102836138A, CN112121017A, CN102743366A, EP0011489A1 refer to compositions comprising effervescent tablets or granules of paracetamol, without however mentioning their inclusion into a hermetically sealed container, preferably a thermoformed capsule or pod or sachet, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages, in order to protect them from exposure to environmental factors and to prepare a hot drink. Despite of the achievements already mentioned in the state of the art, there is a continuing need to further improve the compliance of patients receiving paracetamol, in order to treat pain and fever more promptly and more effectively.

[0008] Moreover, there is a need to further improve the packaging and thus the stability of the effervescent forms comprising paracetamol during storage, both the stability of paracetamol as an active pharmaceutical ingredient, and the stability of the effervescent pharmaceutical forms and especially in the presence of oxygen and moisture.

[0009] However, in the state of the art, there is no mention about the inclusion of the effervescent form of an active pharmaceutical ingredient, specifically of paracetamol, into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages and indeed with a pleasant taste.

[0010] The present invention solves all the above problems of the state of the art, and in fact with unexpected, surprising results in terms of ease of administration of the pharmaceutical composition and in terms of stability, either through preservation for a long period of time before administration or through prolonging the time of administration after the preparation of the beverage, because the hermetically sealed containers, preferably the thermoformed capsules or pods or sachets, which containers are suitable to be used in an extraction machine for preparation of hot aqueous beverages, lead to the complete isolation of their contents from environmental conditions and especially oxygen and humidity, as well as in the easy and efficient preparation of the hot beverage.

[0011] More specifically, the present invention is defined by the following definitions:

[0012] Definition 1. Pharmaceutical composition suitable for oral administration comprising paracetamol in a water-soluble form, preferably in effervescent form, which composition is into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, more preferably into a thermoformed capsule, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages.

[0013] Definition 2. Pharmaceutical composition according to definition 1, wherein the amount of paracetamol ranges from 5 to 4000 mg per hermetically closed container, preferably from 500 to 2000 mg per hermetically closed container and more preferably at 1000 mg per hermetically closed container.

[0014] Definition 3, Pharmaceutical composition according to any of the definitions 1 to 2, wherein the effervescent water-soluble form is selected from tablets, granules or powder, preferably granules.

[0015] Definition 4. Pharmaceutical composition according to any of the definitions 1 to 3, which additionally comprises one or more active substances other than paracetamol, preferably vitamin C, caffeine, orphenadrine, pseudoephedrine, acetylcysteine, chlorphenamine, acetylsalicylic acid, hyoscine, ibuprofen or a pharmaceutically acceptable derivative thereof.

[0016] Definition 5. Pharmaceutical composition according to any of the definitions 1 to 4, which additionally comprises one or more non-pharmaceutical active substances, preferably propolis and / or one or more plant extracts selected from Clstus creticus, Primula veris, Olea europaea and Slderltis syrlaca.

[0017] Definition 6. Pharmaceutical composition according to any of the definitions 1 to 5, which comprises one or more effervescent agents, preferably ascorbic acid and / or anhydrous citric acid and / or anhydrous sodium bicarbonate.

[0018] Definition 7. Pharmaceutical composition according to any of the definitions 1 to 6, which additionally comprises one or more excipients, selected from one or more diluents and / or one or more lubricants and / or one or more binders and / or one or more sweetening agents and / or one or more flavouring agents.

[0019] Definition 8. Pharmaceutical composition according to definition 7, wherein the diluent is one or more diluents selected from sorbitol, mannitol, erythritol and isomaltitol, preferably sorbitol, the lubricant is preferably polyethylene glycol 6000, the binder is preferably sorbitol, the sweetening agents are one or more sweetening agents selected from neohesperidin DC, sodium saccharin, sucrose and sodium cyclamate, preferably sodium saccharin and / or sucrose and / or sodium cyclamate and the flavouring agents are preferably lemon powder flavor and / or honey powder flavor and / or caramel flavor.

[0020] Additional excipients that could be used in the present invention are povidone (K-30), basic butylated methacrylate copolymer, sodium lauryl sulfate, stearic add, sucralose, povidone, maltodextrin, coffee aroma and flavor containing maltodextrin, benzyl alcohol, propylene glycol, gum arable, triacetin and silicon dioxide and other sweetening agents.

[0021] It was surprisingly found that there was an impressive improvement in patient, compliance due to the administration of a pleasant tasting hot beverage, which ied to more immediate and more effective treatment of pain and fever.

[0022] In addition, it was surprisingly found that there was an increased stability of paracetamol during long-term storage, due to inclusion into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, suitable to be used in an extraction machine for preparation of hot aqueous beverages, as the content is completely isolated and thus the exposure of paracetamol to environmental factors, especially oxygen and moisture, is completely avoided.

[0023] Furthermore, it was surprisingly found that there was an increased stability of the effervescent form during long-term storage, due to inclusion into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, suitable to be used in an extraction machine for preparation of hot aqueous beverages, as the content is completely isolated and thus the exposure of paracetamol to environmental factors, especially oxygen and moisture, is completely avoided.

[0024] It was also surprisingly found that there was an improved stability of the prepared hot beverage, so that it could be consumed slowly and not necessarily immediately, as a pleasant beverage, easy for the patient to be swallowed, as for example in the case of other hot beverages e.g. coffee.

[0025] Furthermore, it was surprisingly found that the more is restricted the scope of the claims, the more intense are the effects and the advantages of the present invention.

[0026] The compositions of the present invention can be prepared by methods already known in the state of art.

[0027] The extraction machine for preparation of hot aqueous beverages can be machines e.g. for coffee, such as Nespresso® or Delonghi® or any other similar.

[0028] The present invention is further described by the following indicative, but non-limiting example.

[0029] Example 1: In one embodiment the composition of the present invention comprises the following

[0030] The above composition is formulated into effervescent granules. Next, the prepared granules are enclosed into a hermetically sealed thermoformed capsule, suitable to be used in an extraction machine for preparation of hot aqueous beverages, which thermoformed capsule is hermetically sealed in order to avoid contact with environmental factors, such as oxygen and moisture. The composition of the present Example exhibits all the advantages of the present invention.

Claims

Claims1. Pharmaceutical composition suitable for oral administration comprising paracetamol in a water-soluble form, preferably in effervescent form, which composition is into a hermetically sealed container, preferably into a thermoformed capsule or pod or sachet, more preferably into a thermoformed capsule, which container is suitable to be used in an extraction machine for preparation of hot aqueous beverages.

2. Pharmaceutical composition according to claim 1, wherein the amount of paracetamol ranges from 5 to 4000 mg per hermetically closed container, preferably from 500 to 2000 mg per hermetically closed container and more preferably at 1000 mg per hermetically closed container.

3. Pharmaceutical composition according to any of the claims 1 to 2, wherein the effervescent water-soluble form is selected from tablets, granules or powder, preferably granules.

4. Pharmaceutical composition according to any of the claims 1 to 3, which additionally comprises one or more active substances other than paracetamol, preferably vitamin C, caffeine, orphenadrine, pseudoephedrine, acetylcysteine, chlorphenamine, acetylsalicylic acid, hyosclne, ibuprofen or a pharmaceutically acceptable derivative thereof.

5. Pharmaceutical composition according to any of the claims 1 to 4, which additionally comprises one or more non- pharmaceutical active substances, preferably propolis and / or one or more plant extracts selected from Ostus creticus, Primula veris, Olea europaea and Sideritis syriaca.6, Pharmaceutical composition according to any of the claims 1 to 5, which comprises one or more effervescent agents, preferably ascorbic acid and / or anhydrous citric add and / or anhydrous sodium bicarbonate.

7. Pharmaceutical composition according to any of the claims 1 to 6, which additionlally comprises one or more excipients, selected from one or more diluents and / or one or more lubricants and / or one or more binders and / or one or more sweetening agents and / or one or more flavouring agents.

8. Pharmaceutical composition according to claim 7, wherein the diluent is one or more diluents selected from sorbitol, mannitol, erythritol and isomaititol, preferably sorbitol, the lubricant is preferably polyethylene glycol 6000, the binder is preferably sorbitol, the sweetening agents are one or more sweetening agents selected from neohesperidin DC, sodium saccharin, sucrose and sodium cyclamate, preferably sodium saccharin and / or sucrose and / or sodium cyclamate and the flavouring agents are preferably lemon powder flavor and / or honey powder flavor and / or caramel flavor.

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