Description:FIELD OF THE INVENTION
The present invention relates to the field of pharmaceutical formulations and drug delivery systems, specifically to the development of oral disintegrating films (ODFs) utilizing pineapple (Ananas comosus) waste as a natural, sustainable, and eco-friendly excipient. The invention further pertains to the utilization of agricultural and fruit processing waste for the preparation of fast-dissolving oral dosage forms, thereby promoting waste valorization and environmentally sustainable pharmaceutical practices.
BACKGROUND OF THE INVENTION
References which are cited in the present disclosure are not necessarily prior art and therefore their citation does not constitute an admission that such references are prior art in any jurisdiction. All publications, patents and patent applications herein are incorporated by reference to the same extent as if each individual or patent application was specifically and individually indicated to be incorporated by reference.
The increasing emphasis on patient-friendly drug delivery systems has led to the development of novel dosage forms that improve patient compliance and therapeutic effectiveness. Traditional solid dosage forms, such as tablets and capsules, can be difficult to swallow, particularly for children, elderly individuals, and patients suffering from dysphagia or other swallowing disorders. These limitations have driven the need for alternative dosage forms that are easy to administer, convenient, and require no water for consumption.
Oral disintegrating films (ODFs) have emerged as a promising solution due to their thin, flexible, and rapidly dissolving nature, which allows them to disintegrate quickly in the oral cavity. This makes them highly suitable for on-the-go administration and for patients with conditions such as motion sickness, recurrent diarrhea, mental health irregularities, and other ailments where immediate relief is desired.
Pineapple (Ananas comosus), a tropical fruit, is an abundant source of bioactive compounds, including the enzyme bromelain, known for its anti-inflammatory, proteolytic, and digestive properties. Additionally, pineapple contains essential phytonutrients and vitamins, such as vitamin C, which contribute to its therapeutic benefits. Although pineapple extract has been used in both traditional and modern medicine, its application in oral film technology remains underexplored.
The present invention aims to utilize pineapple waste, a readily available biological byproduct of fruit processing industries, as a sustainable source for developing oral disintegrating films. This approach not only promotes waste valorization and environmental sustainability but also provides a natural, effective, and palatable dosage form for delivering the beneficial compounds of pineapple. The formulation incorporates active ingredients, film-forming polymers, plasticizers, sweeteners, flavoring agents, and saliva-stimulating agents, resulting in a cost-effective and user-friendly pharmaceutical product with enhanced therapeutic potential.
Several patents issued for eatable film but none of these are related to the present invention. Patent US20120269742A1 relates to orally consumable film composition for delivering breath freshening agents to the oral cavity which is rapidly dissolvable or dispersible in the oral cavity, the composition being comprised of a homogeneous mixture of a water dispersible film forming polymer and an enzyme. An orally consumable film composition for delivering breath freshening agents to the oral cavity which rapidly dissolves or disintegrates when applied in the oral cavity, the composition being comprised of a homogeneous mixture of an enzyme and a water soluble or dispersible film forming polymer.
Another patent US7267718B2 relates to compositions based on pullulan and a setting system for the use in pharmaceutical, veterinary, food, cosmetic or other products like films for wrapping food, aspics or jellies, preferably for predosed formulations like soft or hard capsules. The composition preferably further contains a surfactant. By using aqueous solution of the inventive compositions, the hard pullulan capsules are produced by a conventional dipping moulding process under the same process condition range than conventional gelatine capsules.
Another patent KR101383430B1 relates to film-forming compositions and film-like pharmaceutical preparations thereof which improve the properties of fast disintegrating films in the oral cavity. The invention provides a film-forming composition containing Pullulan and Hydroxypropyl Pea Starch and a fast-disintegrating film-like pharmaceutical preparation containing oral drug. Intraoral fast disintegrating film-forming composition according to the present invention is very excellent in film properties, can produce a film formulation that can exhibit a rapid intraoral disintegration rate, the fast disintegrating film-type pharmaceutical preparation of the present invention is an excipient By suppressing the drug content is limited by, and can be prepared in the oral disintegrating film formulations containing the drug in the PDE5 series, it improves the dosage compliance and convenience of taking the drug.
Another patent WO2007148951A1 relates to the field of biotechnology, and in particular to obtaining secondary metabolites, via induction, such as bromelain from plants of the genus Ananas spp., previously established in vitro. The subject of the invention is the development of an innovative process for extracting bromelain from the natural tissues of the pineapple (Ananas comosus (L) Merr) plant that have been established and induced in vitro with a higher proteolytic activity (200 to 600%) - and in high concentrations - as compared with the protein generated naturally in the plant and currently extracted using conventional methodologies. In this process, use is made of pineapple seedlings established and induced in vitro, which are macerated in a phosphate buffer for the purposes of their extraction. Later, they are subjected to filtering, centrifugation, freezing and lyophilization processes in order thus to obtain a crude bromelain extract characterized by high protein yields and specific activity.
Another patent US12127579B2 relates to aerosol generating material is disclosed containing a reconstituted cannabis material. The reconstituted material can contain extracted cannabis fibers in combination with web building fibers, such as softwood fibers. The reconstituted cannabis material is capable of generating an aerosol, such as a smoke, that can have a conventional cannabis taste with reduced amounts of irritants and harsh components. In one embodiment, the reconstituted cannabis material is formed from plants that are low in cannabinoids, such as THC. Cannabinoids, such as THC and/or CBD, can then be topically applied to the reconstituted plant material for not only controlling the amount of cannabinoids contained in an aerosol generated by the material but also for producing consistent and uniform deliveries.
OBJECTS OF THE INVENTION
Main object of the present invention is to develop an oral disintegrating film utilizing pineapple (Ananas comosus) waste as a natural source of bromelain and other bioactive compounds.
Another object of the present invention is to formulate a standardized dosage form containing 10–100 mg of bromelain per film for enhanced therapeutic benefits.
Another object of the present invention is to employ eco-friendly film-forming polymers such as Pullulan and HPMC for creating a stable and flexible film.
Another object of the present invention is to enhance patient compliance by incorporating natural flavors, sweeteners, and saliva-stimulating agents for improved taste and mouthfeel.
Another object of the present invention is to establish a sustainable process for valorizing pineapple waste into a value-added pharmaceutical product.
SUMMARY OF THE INVENTION
This summary is provided to introduce a selection of concepts, in a simplified format, that are further described in the detailed description of the invention.
This summary is neither intended to identify key or essential inventive concepts of the invention and nor is it intended for determining the scope of the invention.
To further clarify advantages and features of the present invention, a more particular description of the invention will be rendered by reference to specific embodiments thereof, which is illustrated in the appended drawings.
The present invention relates to the formulation and development of an oral disintegrating film (ODF) utilizing pineapple (Ananas comosus) waste as a natural source of bromelain and bioactive compounds. The invention addresses the challenges faced by patients who experience difficulty in swallowing conventional solid dosage forms, such as tablets and capsules, particularly children, elderly individuals, and patients with dysphagia, motion sickness, recurrent diarrhea, and mental health irregularities.
The oral disintegrating film is formulated using pullulan and hydroxypropyl methylcellulose (HPMC) as film-forming polymers, glycerine as a plasticizer to improve flexibility and mouthfeel, sucralose as a sweetener to enhance palatability, natural pineapple flavor or other fruit essences to improve taste, and citric acid as a saliva-stimulating agent and antioxidant. The formulation process involves solvent casting, where the polymers are dissolved in distilled water and stirred continuously, followed by the incorporation of plasticizer, standardized pineapple extract, and optional ingredients to form a homogeneous mixture. The solution is de-gassed to remove air bubbles, spread evenly on a Teflon-coated plate, and dried at 40–50°C for 12–24 hours. Once dried, the film is carefully peeled off and cut into unit doses containing 10–100 mg of bromelain per film.
The final product is packaged in moisture-resistant blister packs or sachets to maintain stability and effectiveness. This innovation not only offers a patient-friendly, fast-dissolving drug delivery system but also promotes environmental sustainability by converting fruit processing waste into a value-added pharmaceutical product.
Herein enclosed a method for preparing an oral disintegrating film utilizing pineapple (Ananas comosus) waste extract comprising the steps of:
Collecting pineapple juice and vacuum drying it at 40°C for three days to obtain a concentrated extract;
Grinding the dried extract into a fine powder;
Dissolving a film-forming polymer selected from the group consisting of Pullulan and Hydroxypropyl Methylcellulose (HPMC) in 100 ml of distilled water under continuous stirring for one hour to form a uniform solution;
Adding glycerine as a plasticizer to improve flexibility and mouthfeel, followed by continuous stirring to obtain a homogeneous mixture;
Incorporating the standardized pineapple extract containing 10–100 mg of bromelain per unit dose, along with optional ingredients selected from sucralose, citric acid, antioxidants, vitamin C, and natural pineapple or other fruit flavors, and stirring on a magnetic stirrer for 30 minutes;
degassing the solution to remove air bubbles;
Pouring the degassed solution onto a flat, inert surface such as a Teflon-coated plate and Spreading it evenly to achieve uniform thickness using the solvent casting method;
Drying the film at a temperature between 40°C and 50°C for 12 to 24 hours;
Peeling off the dried film, cutting it into appropriate unit doses, and
Packaging the films in moisture-resistant blister packs or sealed polyethylene sachets to maintain stability and shelf life.
The pineapple extract is standardized to contain bromelain in an amount ranging from 10 mg to 100 mg per film, providing therapeutic benefits for conditions such as motion sickness, dysphagia, recurrent diarrhea, and mental irregularities.
Glycerine is used as the plasticizer to enhance film flexibility and improve mouthfeel, and sucralose is added to increase palatability and patient compliance.
Citric acid functions both as a saliva-stimulating agent to accelerate film dissolution and as an antioxidant and pH adjuster to stabilize the formulation.
The prepared film has the following characteristics:
Antioxidant capacity of 0.65 mg/ml,
Maximum moisture content of 2.88%,
Total phenolic content of 78.42 mg GAE,
Total flavonoid content of 2.8 mg QE/g,
Disintegration time of less than 30 seconds in the oral cavity,
And a texture profile with hardness of -1.153 × 10⁵ N/m², viscosity of 5.729 × 10² N/m², cohesiveness of 0.0738, springiness of 1.2017, gumminess of 8.516 × 10³ N/m², and chewiness of 1.023 × 10⁴ N/m², making it suitable for rapid oral delivery.
BRIEF DESCRIPTION OF THE DRAWINGS
The illustrated embodiments of the subject matter will be understood by reference to the drawings, wherein like parts are designated by like numerals throughout. The following description is intended only by way of example, and simply illustrates certain selected embodiments of devices, systems, and methods that are consistent with the subject matter as claimed herein, wherein:
Fig. 1 image of thin films
DETAILED DESCRIPTION OF THE INVENTION
The detailed description of various exemplary embodiments of the disclosure is described herein with reference to the accompanying drawings. It should be noted that the embodiments are described herein in such details as to clearly communicate the disclosure. However, the amount of details provided herein is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the scope of the present disclosure as defined by the appended claims.
It is also to be understood that various arrangements may be devised that, although not explicitly described or shown herein, embody the principles of the present disclosure. Moreover, all statements herein reciting principles, aspects, and embodiments of the present disclosure, as well as specific examples, are intended to encompass equivalents thereof.
The terminology used herein is for the purpose of describing particular embodiments only and is not intended to be limiting of example embodiments. As used herein, the singular forms “a",” “an” and “the” are intended to include the plural forms as well, unless the context clearly indicates otherwise. It will be further understood that the terms “comprises,” “comprising,” “includes” and/or “including,” when used herein, specify the presence of stated features, integers, steps, operations, elements and/or components, but do not preclude the presence or addition of one or more other features, integers, steps, operations, elements, components and/or groups thereof.
It should also be noted that in some alternative implementations, the functions/acts noted may occur out of the order noted in the figures. For example, two figures shown in succession may, in fact, be executed concurrently or may sometimes be executed in the reverse order, depending upon the functionality/acts involved.
In addition, the descriptions of "first", "second", “third”, and the like in the present invention are used for the purpose of description only, and are not to be construed as indicating or implying their relative importance or implicitly indicating the number of technical features indicated. Thus, features defining "first" and "second" may include at least one of the features, either explicitly or implicitly.
Unless otherwise defined, all terms (including technical and scientific terms) used herein have the same meaning as commonly understood by one of ordinary skill in the art to which example embodiments belong. It will be further understood that terms, e.g., those defined in commonly used dictionaries, should be interpreted as having a meaning that is consistent with their meaning in the context of the relevant art and will not be interpreted in an idealized or overly formal sense unless expressly so defined herein.
In some embodiments of the present invention, the formulation and development of an oral disintegrating film (ODF) utilizing pineapple (Ananas comosus) waste as a natural source of bromelain and bioactive compounds.
In some embodiments of the present invention, the invention addresses the challenges faced by patients who experience difficulty in swallowing conventional solid dosage forms, such as tablets and capsules, particularly children, elderly individuals, and patients with dysphagia, motion sickness, recurrent diarrhea, and mental health irregularities.
In some embodiments of the present invention, the oral disintegrating film is formulated using pullulan and hydroxypropyl methylcellulose (HPMC) as film-forming polymers, glycerine as a plasticizer to improve flexibility and mouthfeel, sucralose as a sweetener to enhance palatability, natural pineapple flavor or other fruit essences to improve taste, and citric acid as a saliva-stimulating agent and antioxidant.
In some embodiments of the present invention, the formulation process involves solvent casting, where the polymers are dissolved in distilled water and stirred continuously, followed by the incorporation of plasticizer, standardized pineapple extract, and optional ingredients to form a homogeneous mixture.
In some embodiments of the present invention, the solution is de-gassed to remove air bubbles, spread evenly on a Teflon-coated plate, and dried at 40–50°C for 12–24 hours. Once dried, the film is carefully peeled off and cut into unit doses containing 10–100 mg of bromelain per film.
Herein enclosed a method for preparing an oral disintegrating film utilizing pineapple (Ananas comosus) waste extract comprising the steps of:
Collecting pineapple juice and vacuum drying it at 40°C for three days to obtain a concentrated extract;
Grinding the dried extract into a fine powder;
Dissolving a film-forming polymer selected from the group consisting of Pullulan and Hydroxypropyl Methylcellulose (HPMC) in 100 ml of distilled water under continuous stirring for one hour to form a uniform solution;
Adding glycerine as a plasticizer to improve flexibility and mouthfeel, followed by continuous stirring to obtain a homogeneous mixture;
Incorporating the standardized pineapple extract containing 10–100 mg of bromelain per unit dose, along with optional ingredients selected from sucralose, citric acid, antioxidants, vitamin C, and natural pineapple or other fruit flavors, and stirring on a magnetic stirrer for 30 minutes;
degassing the solution to remove air bubbles;
Pouring the degassed solution onto a flat, inert surface such as a Teflon-coated plate and Spreading it evenly to achieve uniform thickness using the solvent casting method;
Drying the film at a temperature between 40°C and 50°C for 12 to 24 hours;
Peeling off the dried film, cutting it into appropriate unit doses, and
Packaging the films in moisture-resistant blister packs or sealed polyethylene sachets to maintain stability and shelf life.
The pineapple extract is standardized to contain bromelain in an amount ranging from 10 mg to 100 mg per film, providing therapeutic benefits for conditions such as motion sickness, dysphagia, recurrent diarrhea, and mental irregularities.
Glycerine is used as the plasticizer to enhance film flexibility and improve mouthfeel, and sucralose is added to increase palatability and patient compliance.
Citric acid functions both as a saliva-stimulating agent to accelerate film dissolution and as an antioxidant and pH adjuster to stabilize the formulation.
The prepared film has the following characteristics:
Antioxidant capacity of 0.65 mg/ml,
Maximum moisture content of 2.88%,
Total phenolic content of 78.42 mg GAE,
Total flavonoid content of 2.8 mg QE/g,
Disintegration time of less than 30 seconds in the oral cavity,
And a texture profile with hardness of -1.153 × 10⁵ N/m², viscosity of 5.729 × 10² N/m², cohesiveness of 0.0738, springiness of 1.2017, gumminess of 8.516 × 10³ N/m², and chewiness of 1.023 × 10⁴ N/m², making it suitable for rapid oral delivery.
EXAMPLE 1
BEST METHOD
A pineapple extract that has been standardized to have a specific amount of bromelain (10–100 mg per film) and may be enhanced with antioxidants and vitamin C. chosen from the group that included Pullulan and Hydroxypropyl Methyl Methylcellulose (HPMC). Glycerine is used to improve the mouthfeel and flexibility of films. Sucralose to increase patient compliance and taste. To improve palatability, use natural pineapple taste or other fruit essences. Citric acid is a significant saliva-stimulating agent and an antioxidant and pH adjuster. By Solvent casting technique film is made by constant stirring, dissolving the film-forming polymer in distilled water 100ml. To create a homogeneous solution, adding the plasticizer into it and stirring on the magnetic stirrer. Addition of the pineapple extract is done along with any additional optional ingredients. In order to eliminate air bubbles, degas the solution. Spread the solution to a consistent thickness on a level, inert surface (such as a plate covered with Teflon). Dry for 12 to 24 hours at 40 to 50°C. Cut into the appropriate unit doses after peeling. Present in blister packets or sachets that can withstand dampness.
Preparation of pineapple extracts oral dissolving film:
Extract of pineapple (after collecting juice)

Vacuum dry at 40*C for 3 days

Powder form (Through Grinding)

Dissolve the film-forming polymer in distilled water under continuous stirring for 1hr

Add the plasticizer and mix until a homogenous solution is obtained.

Incorporate the pineapple extract and other optional ingredients; stir it on magnetic stirrer for 30 min

Pour the solution onto a flat, inert surface (e.g., Teflon-coated plate) and spread to uniform thickness (Solvent casting method)

Dry at 40–50°C for 12–24 hours.

Pack the film into the sealed polyethene material leading to stable and more shelf life.
EXAMPLE 2
Antioxidant Capacity: The antioxidant value measured was 0.65mg/ml.
Textural Profile:
• Hardness: -1.153*10⁵ N/m²
• Fracture ability: - 0.000 N/m²
• Viscosity: - 5.729*10² N/m²
• Cohesiveness: - 0.0738
• Springiness: - 1.2017
• Gumminess: - 8.516*10³ N/m²
• Chewiness: - 1.023*10⁴ N/m²
• Probe Diameter: - 20.000 mm
Moisture Content: Maximum moisture percent was recorded in the sample was 2.88%.
Total Phenolic content: the phenolic content measured was 78.42mgGAE.
Total Flavonoids Content: The flavonoids content was 2.8mgQE/g.
Disintegration Time: The disintegration time was noted as the film dissolve within 30 sec in mouth.
ADVANTAGES OF THE INVENTION:
1. Oral strip technology gives medications with first-pass metabolism a different route.
2. Due to their inability to swallow large amounts of water, patients with motion sickness, dysphagia, repetitive emesis, and mental abnormalities are better suited for this dosage form.
3. Thin film drug delivery technology presents additional business opportunities from a commercial standpoint, including life cycle management, patent extensions, product differentiation, and product promotion.
4. The availability of a larger surface area allows for rapid disintegration and dissolving in the oral cavity, improving the medication's start of action, lowering dosage, and improving its efficacy and safety profile.
5. OTFs have been welcomed by both pharmaceutical firms and customers as a viable and well-received substitute for conventional over-the-counter medication forms like liquids, tablets, and capsules. OTFs provide quick, precise dosage in a portable, convenient, safe, and effective manner without the need for measuring tools or water.
, Claims:1. A method for preparing an oral disintegrating film utilizing pineapple (Ananas comosus) waste extract comprising the steps of:
a) collecting pineapple juice and vacuum drying it at 40°C for three days to obtain a concentrated extract;
b) grinding the dried extract into a fine powder;
c) dissolving a film-forming polymer selected from the group consisting of Pullulan and Hydroxypropyl Methylcellulose (HPMC) in 100 ml of distilled water under continuous stirring for one hour to form a uniform solution;
d) adding glycerine as a plasticizer to improve flexibility and mouthfeel, followed by continuous stirring to obtain a homogeneous mixture;
e) incorporating the standardized pineapple extract containing 10–100 mg of bromelain per unit dose, along with optional ingredients selected from sucralose, citric acid, antioxidants, vitamin C, and natural pineapple or other fruit flavors, and stirring on a magnetic stirrer for 30 minutes;
f) degassing the solution to remove air bubbles;
g) pouring the degassed solution onto a flat, inert surface such as a Teflon-coated plate and spreading it evenly to achieve uniform thickness using the solvent casting method;
h) drying the film at a temperature between 40°C and 50°C for 12 to 24 hours;
i) peeling off the dried film, cutting it into appropriate unit doses, and
j) packaging the films in moisture-resistant blister packs or sealed polyethylene sachets to maintain stability and shelf life.
2. The method as claimed in claim 1, wherein the pineapple extract is standardized to contain bromelain in an amount ranging from 10 mg to 100 mg per film, providing therapeutic benefits for conditions such as motion sickness, dysphagia, recurrent diarrhea, and mental irregularities.
3. The method as claimed in claim 1, wherein glycerine is used as the plasticizer to enhance film flexibility and improve mouthfeel, and sucralose is added to increase palatability and patient compliance.
4. The method as claimed in claim 1, wherein citric acid functions both as a saliva-stimulating agent to accelerate film dissolution and as an antioxidant and pH adjuster to stabilize the formulation.
5. The method as claimed in claim 1, wherein the prepared film has the following characteristics:
• Antioxidant capacity of 0.65 mg/ml,
• Maximum moisture content of 2.88%,
• Total phenolic content of 78.42 mg GAE,
• Total flavonoid content of 2.8 mg QE/g,
• Disintegration time of less than 30 seconds in the oral cavity,
• And a texture profile with hardness of -1.153 × 10⁵ N/m², viscosity of 5.729 × 10² N/m², cohesiveness of 0.0738, springiness of 1.2017, gumminess of 8.516 × 10³ N/m², and chewiness of 1.023 × 10⁴ N/m², making it suitable for rapid oral delivery.