AU2006100743A4 - Capsule with expressable fill material - Google Patents

Description

INO

;Z 1 P/00/009A Section 29

AUSTRALIA

Patents Act 1990 INNOVATION PATENT SPECIFICATION Invention Title: CAPSULE WITH EXPRESSABLE FILL MATERIAL Applicant: CARDINAL HEALTH AUSTRALIA 401 PTY LTD The invention is described in the following statement: CAPSULE WITH EXPRESSABLE FILL MATERIAL Field of the Invention The present invention relates to capsules, in particular pharmaceutical soft capsules derived from non-animal sources, that allow the user to express the contents from the C, capsule for consumption. The capsule is designed to enable ingestible pharmaceutical or Scomplementary health fill materials to be expressed directly into the mouth of the user.

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O The pharmaceutical or complementary health fill materials may be diluted first, for example, by expressing the fill materials into a glass of water before consumption.

0 Background Art Pharmaceuticals in liquid dosage forms, such as bottled cough syrups, have been marketed for many years. However, they require patients to dispense the doses accurately by themselves, which can be difficult. Furthermore, repeated opening of the liquid containers poses risks of contamination of the remainder.

Thus encapsulated forms of the liquids are often used to supply individual doses.

Conventional oral pharmaceuticals such as soft capsules usually derived from mammalian gelatin (or "softgels") and hard capsules are designed for taking as a whole without the shells being broken in the mouth. The capsules are ingested and swallowed intact, and release their contents (the "fill material") in the stomach or other site within the gastrointestinal system. They are formulated specifically so that the capsule shells are not readily broken, and the fill material is not released until after swallowing. As well as delivering a metered dose, such capsules allow administration without exposing the user to the often unpleasant taste of the therapeutic agent. A particular advantage of a capsule however, is that the dosage of the active in the fill material, whether in powdered or liquid form can be regulated, and the user can accurately determine the dose of the active consumed.

Despite the well recognized advantages of presenting active fill materials in capsules, there are still problems associated with such capsules. They can lack appeal to children, who must swallow them without any enjoyable taste experience. For ease of swallowing, 2 capsule size must be limited to less than 22 to 24 minim (1.36 to 1.48 Even within a this limit, certain patients or aged people may still have difficulty swallowing the capsules.

0 ,N The size constraints in turn restrict the dosage that can be contained within a capsule.

t Therefore, several capsules may need to be taken at any one time, which can compound the problems.

Larger metered doses could be delivered if the user could release the contents from the capsules before ingestion. However, the shell formulations of conventional capsules do a not readily allow the user to open them. Furthermore, even if the user was to break them apart, the standard shapes of conventional softgels such as an elongate oval or oblong O are not suited to expressing the content manually without spillage.

There is thus a need for capsules that allow for greater ease of ingestion of the therapeutic agent by users; that are less subject to restrictions in size; and that are of improved appeal to users, particularly children.

In recent times, there has also been an aversion to consuming animal derived products.

Both soft and hard shell gelatin capsules are derived from mammalian gelatin and hence, there is a reluctance in the market place for consumers to purchase animal derived products. Capsules made from non-animal derived products such as natural and synthetic polymers, gums and starches are known and have commercial success. A soft shell made from modified starch and carrageenan, also known by the trade name Vegicaps®, and disclosed in Australian patent 735699 in the name of Cardinal Health, Inc., is an established non-animal derived soft capsule.

However, non-animal derived capsules are designed to be consumed whole and suffer the same difficulties referred to above. The present invention aims to overcome or at least alleviate the difficulties presented by having to swallow capsules whole to receive the beneficial effects of the ingestible pharmaceutical or complementary health fill material within the capsule, particularly as it relates to non-animal derived products.

Throughout the description and claims of this specification, use of the word "comprise" and variations of the word, such as "comprising" and "comprises", is not intended to exclude other additives, components, integers or steps.

The discussion of documents, acts, materials, devices, articles and the like is included in O this specification solely for the purpose of providing a context for the present invention. It 0 N is not suggested or represented that any or all of these matters formed part of the prior art Sbase or were common general knowledge in the field relevant to the present invention as it existed in Australia before the priority date of this application.

Summary of the Invention The present invention provides a capsule comprising: a shell made from a non-animal derived material having a chamber and a c"i detachable component; and (ii) an ingestible pharmaceutical or complementary health fill material encapsulated within the shell; wherein the detachable component of the shell may be detached leaving the fill material within the chamber of the shell, and able to be released from the chamber of the shell upon compression of the chamber.

The shell of the capsules of the present invention will generally have two distinct portions, a chamber and a detachable component, separated by a line of weakness. When the detachable component is detached, the contents of the capsule remain in the chamber and can be expressed into, for example the mouth by compression of the chamber, through an opening formed in the chamber when the detachable component is removed.

All the fill material should remain in the chamber once the detachable component has been removed.

Preferably, the detachable component of the shell is detached by a twisting action as that is less likely to disrupt the contents of the chamber, but it may be designed so that it is detached by a snapping or pulling action. As the capsules do not need to be swallowed, they are not restricted in size, and therefore a single dose can be contained within one capsule.

The shapes of the shells of the capsules of the invention differ from those of conventional oral capsules. They are designed to break easily at a specific point, generally at one end of the capsule, when a manual force is applied separating the capsule into the chamber 0 and the detachable component.

In a preferred embodiment, the present invention resides in a capsule comprising: a shell made from a non-animal derived material having a chamber and a detachable component; and an ingestible pharmaceutical or complementary health fill material encapsulated within the shell; wherein the shell is configured to have at least two distinct components, a chamber and a detachable component separated by a line of weakness extending circumferentially around the shell whereby, the shell can be broken along the line of weakness by the application of a force to separate the detachable component from the chamber.

More preferably, the capsule is of an elongate shape and the line of weakness is a thinning in the shape of the shell such that the line of weakness is a narrow band around the circumference of the shell separating the detachable component from the chamber.

Alternatively, the line of weakness may be a thinning in the thickness of the shell material extending in a band around at least a portion of the elongate capsule. The line of weakness will generally be near one end of the elongate shape of the capsule. The shell is formed such that when a force is applied at either side of the line of weakness, the capsule will break with the ingestible pharmaceutical or complementary health fill material being retained in the chamber. The contents of the chamber can then be poured or expressed out through an opening formed at one end of the chamber when the detachable component has been removed, generally by the application of pressure, such as squeezing the chamber.

Typically, the application of a twisting force where the detachable component of the shell is twisted in the opposite direction to the chamber either side of the line of weakness will be sufficient to break the capsule or if one component is held still while the other component is twisted. A typical arrangement may be where the capsule is shaped so that it has a thin neck which will allow the detachable component of the shell to be twisted off to leave the chamber with an opening at one end to allow the contents of the chamber to be released.

The neck of the shell may also be associated with a thinning at that point of the non-animal derived material that forms the shell of the capsule.

C The shapes of the capsules can be varied to simulate desirable and appealing images,

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N which still allow the convenience of removing the detachable component of the capsules so that the contents can be expressed out for example, a fish shape, where the tail can be broken off. The tail represents the detachable component while the remainder of the fish represents the chamber separated by a thin line of weakness between the tail and the remainder of the fish. The capsules can thus be made particularly to appeal to children.

The capsules of the invention constitute a single dose. The shell is disposable after each dose application which eliminates the risk of contamination, while the capsules themselves C are more appealing with regard to presentation (their shapes) and taste. The shell c material can be formed so that it may be swallowed and behave in the same manner as a conventional capsule will once swallowed, but the capsules of the invention are designed such that the shell material does not need to be swallowed.

The capsules are not limited to the usual sizes of oral softgels (that is, up to maximum of 22-24 minim (1.36 to 1.48 ml) as the capsules are not required to be swallowed. This advantage greatly expands the possible applications of the capsule dosage forms.

Thus, more variation in capsule sizes is available compared to conventional capsules, and capsules can be manufactured to suit the dosage requirement.

The shells of the new capsules can be made of any non-animal based formulation known to be suitable for conventional capsules for example, natural or synthetic polymers, gum and starches. The choice of shell material will depend to a certain extent upon the nature of the ingestible pharmaceutical or complementary health fill material. With a fill material that has components that have a high water solubility, the shell material would generally comprise either a hydrophobic polymer or gum or a combination of polymers or gums that lead to a composition that is hydrophobic in nature. In a preferred embodiment, carrageenan together with a controlled amount of a secondary polymer with a controlled extent of hydrophilicity such as a modified starch or hydroxypropylmethylcellulose is preferred. The carrageenan base can incorporate different proportions of iota kappa and lambda carrageenan. This product has a relatively balanced hydrophobic character and has been found to be stable, even in the presence of water soluble fill materials.

In a further preferred form of the shell material, the shell material comprises a combination 0 of carrageenan together with a secondary hydrophilic polymer such as hydroxypropyl c starch. Preferred amounts of carrageenan range from about 6% to 12% by weight of the Swet shell composition during formation. Preferably the preferred ratio between the carrageenan and the second polymer ranges from 1:1 to about 1:4.

Other shell materials which are far more hydrophilic in character may be used such as shells made by using cellulose derivatives such as hydroxypropyl cellulose in combination r'- C with a secondary polymer or gum such as guar gum. Such shell material is suitable for encapsulating oil soluble herbals such as Saw Palmetto.

c Most preferably, the shell material is a combination of modified starch and carrageenan, particularly iota carrageenan, also known by the trade name Vegicaps® and disclosed in Australian patent 735699 in the name of Cardinal Health, Inc.

The applicants of the present application have found that such materials lend themselves to the advantageous property that they can be formed into a soft capsule with a line of weakness, to allow the capsule to be broken, while retaining the property that allows a portion to be squeezed to express its contents.

The fill material may be any ingestible pharmaceutical or complementary health fill material compatible with the non-animal derived shell material. It should be flowable such that when the capsule has been broken, the fill material should be able to be expressed from the chamber of the shell, either by tipping the chamber containing the fill material, or by squeezing that portion. Most preferably the fill material is liquid or semi-liquid either as solutions or suspensions, or paste material, but may also be a flowable powder. As the contents are ingested directly into the mouth, the fills should be of palatable or pleasant flavour. Alternatively, in use the fill material may be diluted by expressing the contents into a glass of water that may allow the active fill material to be more readily consumed.

The fill material may be any suitable ingestible pharmaceutical that is compatible with nonanimal derived shell materials and includes over-the-counter and some prescription ingestibles such as cough/cold formulations, analgesics, anti-inflammatory and some antibiotic agents as well as products for oral care, for example toothpastes or gels for whitening or prevention of gum disease; sub-lingual medicines, or complementary health products including vitamin preparations, multi-vitamins and vitamin-like materials such as O Coenzyme Q10, minerals, herbal preparations glucosamine, fish oils and probiotics.

The capsule with an expressable fill material may also be appropriate for use in veterinary applications where an ingestible veterinary pharmaceutical is contained within the capsule r, and maybe expressed to the mouth of an animal in a specified dose.

SConventional fill formulations commonly do not have a pleasant taste, due to the nature of the therapeutic agents they contain. However, the fills of the new capsules of the invention may have taste and texture to mask the unpleasant taste of the therapeutic C agents. Suitable excipient combinations, such as flavours, sweeteners and texture agents, c- may be chosen.

The flavours of fills can be any type, such as, for example, fruit, herbal, or chocolate, so long as they taste pleasant and have the necessary flow characteristics for encapsulation.

The fills can further be formulated to impart additional properties apart from pleasant taste, such as water dispersability or self-emulsifying properties, and/or odour masking where the smell of the therapeutic agents may be objectionable (as is the case for some oils).

Odour masking of objectionable oils can be achieved to a degree by flavouring. The masking is more effective if a surfactant system is incorporated. With the addition of a surfactant system, the oils are emulsified into micelles in water. The vapour pressure of the volatile part, which produces the bad odour, is thus much reduced, as opposed to the situation where the oils float on top of water. The combination of flavour and surfactant set is more effective than either alone.

A particular advantage of presenting an active ingestible pharmaceutical or complementary health fill material in the capsule according to the present invention is the ability to accurately provide a metered dosage of the active material is retained, while overcoming the disadvantage of having to swallow the capsule as a whole.

A further advantage of the capsule according to the present invention is that as the ingestible pharmaceutical or complementary health fill material can be expressed into the mouth, it can be absorbed sublingually. This could have particular advantages for some medicaments and complementary health products, as a more rapid absorption can be 0 achieved in some circumstances.

Description of the Drawings Figure 1 discloses a capsule in accordance with the invention having a shell and a Sfill material The shell has two portions, a detachable component and a chamber C component separated by a thin neck at one end of the capsule. The shell is able to be broken about the thin portion by the application of force such as a twisting motion being

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0 applied to both portions of the shell. The contents of the chamber component of the shell c can be expelled through an opening in the chamber component of the shell once the detachable component has been removed, by squeezing the chamber component of the shell.

Figure 2 illustrates an alternative arrangement where there is a thinning in the thickness of the shell material around a band near one end of the capsule. The band of thinner material separates the shell of this embodiment into both a chamber component and a detachable component The above description is intended to be illustrative of the preferred embodiments of the present invention. Variations to the invention without departing from the spirit or ambit described herein should also be considered to form part of the invention.

Claims (2)

1. 3. A capsule according to claim 2 wherein the fill material is expressed through the opening upon application of a compression force applied to the chamber.
2. 4. A capsule according to claim 1 wherein the shell is made from a combination of modified starch and carrageenan. A capsule wherein the ingestible pharmaceutical and/or complementary health fill material is seleeted from one or more ofcough/cold formulations, analgesics, anti- inflammatories, vitamin preparations, multi-vitamins and vitamin-like materials, minerals, herbal extracts, glucoasimine, fish oils, probiotics, oral care products and antibiotic agents.