Development of Orally Dispersible Dosage Forms

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (20 May 2023) | Viewed by 37499

Special Issue Editors

Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Iuliu Haţieganu” University of Medicine and Pharmacy, 41 V. Babes Street, 400012 Cluj-Napoca, Romania
Interests: orodispersible dosage forms; pediatric dosage forms; freeze-drying; quality by design drug development; product/process optimization; design of experiments; texture analysis in pharmaceutical product characterization
Special Issues, Collections and Topics in MDPI journals
Department of Pharmaceutical Technology and Biopharmacy, University of Medicine and Pharmacy “Iuliu Hațieganu”, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania
Interests: innovative dosage forms; drug delivery systems; quality by design (QbD); process analytical technology (PAT); multivariate data analysis (MVDA); 3D printing in pharmaceutics; novel methods of drugs manufacturing; pharmaceutical process optimization
Special Issues, Collections and Topics in MDPI journals
Department of Dermopharmacy and Cosmetics, Faculty of Pharmacy, “Iuliu Haţieganu” University of Medicine and Pharmacy, 12 I. Creanga Street, 400010 Cluj-Napoca, Romania
Interests: development and characterization of solid and semisolid dosage forms; texture analysis; development and optimization of cosmetic products based on nanocarriers or herbal extracts
Special Issues, Collections and Topics in MDPI journals
Department of Pharmaceutical Technology and Biopharmaceutics, Iuliu Hațieganu University of Medicine and Pharmacy, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania
Interests: dosage form development; formulation and process optimization; process analytical technology; chemometrics; amorphous solid dispersions; tablets; dynamic compaction analysis

Special Issue Information

Dear Colleagues,

In recent years, orally dispersible dosage forms were regarded as high interest research topics and quickly reached the pharmaceutical market as novel patient-centered products. The wide variety of preparation technologies and types of products (i.e., orodispersible tablets/ granules, oral lyophilisates, orodispersible minitablets) led to a dynamic research field that aims to fulfill the administration needs of special groups of patients, such as paediatrics or geriatrics. As the pharmaceutical industry adopts these new products, there is a constant need for innovation in terms of appropriate excipients, product and process development, taste-masking methods, quality assessment methods, and data on end-user perception and acceptability.

This Special Issue wants to map the current research landscape of orally dispersible dosage forms and welcomes original and review papers on all aspects of their design, development, manufacturing, characterization, administration or use.

Dr. Sonia M. Iurian
Prof. Dr. Ioan Tomuta
Dr. Catalina Bogdan
Dr. Tibor Casian
Guest Editors

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Keywords

  • orally dispersible dosage forms
  • oral lyophilisates
  • thin films
  • orodispersible films
  • orodispersible minitablets

Published Papers (13 papers)

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Research

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24 pages, 5651 KiB  
Article
In Vitro and In Vivo Evaluation of Composite Oral Fast Disintegrating Film: An Innovative Strategy for the Codelivery of Ranitidine HCl and Flurbiprofen
by Aisha Rashid, Syed Haroon Khalid, Muhammad Irfan, Sajid Asghar, Waleed Y. Rizg, Fahad Y. Sabei, Eman Alfayez, Hanaa Alkharobi, Awaji Y. Safhi, Khaled M. Hosny, Muhammad Sohail Arshad and Ikram Ullah Khan
Pharmaceutics 2023, 15(7), 1987; https://doi.org/10.3390/pharmaceutics15071987 - 20 Jul 2023
Cited by 1 | Viewed by 1509
Abstract
Here, we evaluate the feasibility of co-loading plain ranitidine hydrochloride (RHCl) and microencapsulated flurbiprofen (FBP) in a Lycoat® RS780-based oral fast disintegrating film (ODF). These films were developed by the solvent casting method to minimize the adverse effects of FBP and reduce [...] Read more.
Here, we evaluate the feasibility of co-loading plain ranitidine hydrochloride (RHCl) and microencapsulated flurbiprofen (FBP) in a Lycoat® RS780-based oral fast disintegrating film (ODF). These films were developed by the solvent casting method to minimize the adverse effects of FBP and reduce the dosage form burden on patients. Optimized FBP microparticles (M3) with an average size of 21.2 ± 9.2 µm were loaded alone (F1) and in combination with plain RHCl (F2) in the composite ODF. All films were evaluated physicomechanically and physicochemically. These films were resilient, flexible, and disintegrated within thirty seconds. SEM images showed intact FBP microparticles in both formulations and, moreover, did not observe an interaction between the drug and film components. Microencapsulated FBP was released in a controlled manner over 48 h from the proposed formulations, while RHCl was released within 5 min from F2. After in vitro evaluation, formulations were also tested for in vivo anti-inflammatory activity, cytokine (TNF-α and IL-6) levels, and gastroprotective effects in rats. The anti-inflammatory activity and gastroprotective effect of F2 were markedly higher than pure FBP and other synthesized formulations (M3 and F1). The average score of gastric lesions was in the order of pure FBP (15.5 ± 1.32) > M3 (8 ± 2) > F1 (1 ± 0.5) > F2 (0.5 ± 0) > control (0). Additionally, F2 showed a sustained anti-inflammatory effect up to 10 h in the rat paw edema model. Furthermore, F2 also markedly reduced TNF-α and IL-6 levels. Conclusively, the Lycoat® RS780-based composite film could be a promising carrier for the co-loading of microencapsulated FBP with RHCl. In the future, an optimized formulation (F2) could be capable of countering the issues related to multiple drug administration in geriatric patients and evading the gastric irritation associated with FBP. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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23 pages, 4907 KiB  
Article
Formulation and Characterisation of Carbamazepine Orodispersible 3D-Printed Mini-Tablets for Paediatric Use
by Jiayu Hu, Rawan Fitaihi, Shorooq Abukhamees and Hend E. Abdelhakim
Pharmaceutics 2023, 15(1), 250; https://doi.org/10.3390/pharmaceutics15010250 - 11 Jan 2023
Cited by 6 | Viewed by 3299
Abstract
One of the main challenges to paediatric drug administration is swallowing difficulties, hindering the acceptability of the medicine and hence clinical outcomes. This study aims at developing a child-appropriate dosage form, the orodispersible mini-tablet (ODMT), using the model drug carbamazepine (CBZ). This dosage [...] Read more.
One of the main challenges to paediatric drug administration is swallowing difficulties, hindering the acceptability of the medicine and hence clinical outcomes. This study aims at developing a child-appropriate dosage form, the orodispersible mini-tablet (ODMT), using the model drug carbamazepine (CBZ). This dosage form was prepared and 3D-printed via a semi-solid extrusion technique. Design of Experiment methods were applied for optimising the formulation. The formulation with 40% (w/w) of SSG (superdisintegrant) and 5% (w/w) of PVP K30 (binder) was selected and loaded with CBZ. The drug-loaded tablets were characterised by a mean hardness of 18.5 N and a disintegrating time of 84 s, along with acceptable friability. The mean drug loading ratio of the tablets was tested as 90.56%, and the drug release rate in 0.1 M HCl reached 68.3% at 45 min. Excipients showed proper compatibility with the drug in physical form analysis. Taste assessment via an E-tongue was also conducted, where the drug did not show bitter taste signals at a low concentration in the taste assessment, and the sweetener also blocked bitterness signals in the testing. To this end, ODMTs were found to be potential candidates for child-appropriate dosage forms delivering CBZ. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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22 pages, 4978 KiB  
Article
Embedding of Poorly Water-Soluble Drugs in Orodispersible Films—Comparison of Five Formulation Strategies
by Denise Steiner, Marius Tidau and Jan Henrik Finke
Pharmaceutics 2023, 15(1), 17; https://doi.org/10.3390/pharmaceutics15010017 - 21 Dec 2022
Cited by 4 | Viewed by 1418
Abstract
The poor bioavailability of many newly developed active pharmaceutical ingredients (APIs) poses a major challenge in formulation development. To overcome this issue, strategies such as the preparation of amorphous solid dispersions (ASDs), and the application of the APIs in lipid nanocarriers or the [...] Read more.
The poor bioavailability of many newly developed active pharmaceutical ingredients (APIs) poses a major challenge in formulation development. To overcome this issue, strategies such as the preparation of amorphous solid dispersions (ASDs), and the application of the APIs in lipid nanocarriers or the wet-milling of the substances into nanoparticles have been introduced. In addition to an efficient formulation strategy, a dosage form that is accepted by all patients is also of great importance. To enable a simple application of the oral dosage form for all patients, orodispersible films (ODFs) are a very promising delivery platform for the APIs because the films directly disintegrate in the mouth. In this study, two poorly water-soluble APIs, fenofibrate and naproxen, were formulated using five different formulation strategies and then embedded in ODFs. It was found that the deliverable amount of API with one ODF highly depends on the formulation strategy as well as the physicochemical properties of the formulated API. The most promising film formulations were ASD-ODFs as well as films with API-loaded lipid nanoemulsions. Both showed a reduction of the dissolution time of the APIs from the ODF compared to an ODF with unformulated API micro particles. In addition, short disintegration times were achieved, although the mechanical film properties were slightly worse compared to the API-free film formulation. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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20 pages, 2091 KiB  
Article
Preparation and Evaluation of Directly Compressible Orally Disintegrating Tablets of Cannabidiol Formulated Using Liquisolid Technique
by Ekapol Limpongsa, Peera Tabboon, Thaned Pongjanyakul and Napaphak Jaipakdee
Pharmaceutics 2022, 14(11), 2407; https://doi.org/10.3390/pharmaceutics14112407 - 08 Nov 2022
Cited by 8 | Viewed by 2344
Abstract
This study demonstrated the implementation of a liquisolid technique to formulate directly compressible orally disintegrating tablets (ODTs). Cannabidiol (CBD), a hydrophobic cannabinoid, was prepared as a liquisolid powder using microcrystalline cellulose–colloidal silicon dioxide as a carrier–coating material. Different liquid vehicles differing in their [...] Read more.
This study demonstrated the implementation of a liquisolid technique to formulate directly compressible orally disintegrating tablets (ODTs). Cannabidiol (CBD), a hydrophobic cannabinoid, was prepared as a liquisolid powder using microcrystalline cellulose–colloidal silicon dioxide as a carrier–coating material. Different liquid vehicles differing in their volatility, hydrophilicity, and viscosity were investigated. Each of the CBD–ODTs comprised CBD liquisolid powder (10 mg CBD), superdisintegrant, flavors, lubricant, and filler. The physical mixture (PM) ODT was prepared as a control. Ethanol-based ODTs (CBD–EtOH–ODTs) had comparable tablet properties and stability to CBD–PM–ODTs. ODTs with nonvolatile-vehicle-based liquisolid powder had lower friability but longer disintegration times as compared with CBD–PM–ODTs and CBD–EtOH–ODTs. Compression pressure influenced the thickness, hardness, friability, and disintegration of the ODTs. With a suitable compression pressure to yield 31-N-hardness-ODTs and superdisintegrant (4–8%), CBD–ODTs passed the friability test and promptly disintegrated (≤25 s). Times to dissolve 50% of CBD–PM–ODTs, CBD–EtOH–ODTs, and nonvolatile-vehicle-based CBD–ODTs were 10.1 ± 0.7, 3.8 ± 0.2, and 4.2 ± 0.4–5.0 ± 0.1 min, respectively. CBD–EtOH–ODTs exhibited the highest dissolution efficiency of 93.5 ± 2.6%. Long-term and accelerated storage indicated excellent stability in terms of tablet properties and dissolution. Nonvolatile-vehicle-based CBD–ODTs exhibited a higher percentage of remaining CBD. This study provides useful basic information for the development of ODT formulations using a liquisolid technique application. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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12 pages, 1388 KiB  
Article
Evaluation of Newly Designed and Traditional Punches in Manufacturing of Scored ODTs
by Luca Palugan, Saliha Moutaharrik, Alessandra Maroni, Anastasia Anna Foppoli, Alice Melocchi, Carlo Vecchio, Andrea Gazzaniga and Matteo Cerea
Pharmaceutics 2022, 14(10), 2054; https://doi.org/10.3390/pharmaceutics14102054 - 27 Sep 2022
Viewed by 1352
Abstract
To overcome difficulties in splitting, uneven breaking and inconsistent dosing frequently reported with scored tablets, a novel punch was proposed for the manufacturing of easy breakable tablets (EBTs). In this work, the performance of the EBT punch was investigated vs. a ridged one [...] Read more.
To overcome difficulties in splitting, uneven breaking and inconsistent dosing frequently reported with scored tablets, a novel punch was proposed for the manufacturing of easy breakable tablets (EBTs). In this work, the performance of the EBT punch was investigated vs. a ridged one for traditional breakable tablets (TBTs) using a furosemide powder formulation for orally disintegrating tablets (ODTs). A Face Centered Central Composite Design was applied to investigate the influence of punch type, compaction force, tablet weight and press rotation speed on the mechanical properties of ODTs, their behavior in aqueous fluids and aptitude for splitting. Mass uniformity and adequate crushing strength, friability, water uptake, disintegration and wetting times were obtained from both TBTs and EBTs. Interestingly, more favorable splitting behavior was shown by tablets manufactured by the novel punch, in view of lower mass loss and portion mass variability after breaking. The ease of breaking, accuracy of subdivision and mass loss of ODTs were also evaluated by a volunteer (n = 20) panel test. Less difficulty was found in splitting EBTs than TBTs (p < 0.05), and a larger number of tablets were properly broken into four parts. Thus, this study proved the usefulness of the EBT punch in overcoming drawbacks associated with divisible tablets. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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15 pages, 2803 KiB  
Article
Stability, Permeability and Cytotoxicity of Buccal Films in Allergy Treatment
by Krisztián Pamlényi, Géza Regdon, Jr., Dániel Nemes, Ferenc Fenyvesi, Ildikó Bácskay and Katalin Kristó
Pharmaceutics 2022, 14(8), 1633; https://doi.org/10.3390/pharmaceutics14081633 - 05 Aug 2022
Cited by 4 | Viewed by 1934
Abstract
Oral mucoadhesive systems, such as polymer films, are among innovative pharmaceutical products. These systems can be applied in swallowing problems and can also be used in geriatrics and paediatrics. In our earlier work, we successfully formulated buccal mucoadhesive polymer films, which contained cetirizine-hydrochloride [...] Read more.
Oral mucoadhesive systems, such as polymer films, are among innovative pharmaceutical products. These systems can be applied in swallowing problems and can also be used in geriatrics and paediatrics. In our earlier work, we successfully formulated buccal mucoadhesive polymer films, which contained cetirizine-hydrochloride (CTZ) as the API. The present study focused on investigating the stability and permeability of the prepared films. The stability of the films was studied with an accelerated stability test. During the stability test, thickness, breaking hardness and in vitro mucoadhesivity were analysed. Furthermore, the interactions were studied with FT-IR spectroscopy, and the changes in the amount of the API were also monitored. Cytotoxicity and cell line permeability studies were carried out on TR 146 buccal cells. Compositions that can preserve more than 85% of the API after 6 months were found. Most of the compositions had a high cell viability of more than 50%. Citric acid (CA) decreased the stability and reduced every physical parameter of the films. However, cell line studies showed that the permeability of the films was enhanced. In our work, we successfully formulated CTZ-containing buccal films with adequate stability, high cell viability and appropriate absorption properties. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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24 pages, 19659 KiB  
Article
Comparison of Nozzle-Based and Nozzle-Free Electrospinning for Preparation of Fast-Dissolving Nanofibers Loaded with Ciprofloxacin
by Luca Éva Uhljar, Areen Alshweiat, Gábor Katona, Michael Chung, Norbert Radacsi, Dávid Kókai, Katalin Burián and Rita Ambrus
Pharmaceutics 2022, 14(8), 1559; https://doi.org/10.3390/pharmaceutics14081559 - 27 Jul 2022
Cited by 3 | Viewed by 1974
Abstract
The study aimed to prepare ciprofloxacin-loaded polyvinylpyrrolidone electrospun nanofibers for oral drug delivery, using a conventional nozzle-based and a lab-built nozzle-free electrospinning equipment. To produce nanofibers, electrospinning is the process most often used. However, from the industry’s point of view, conventional electrospinning does [...] Read more.
The study aimed to prepare ciprofloxacin-loaded polyvinylpyrrolidone electrospun nanofibers for oral drug delivery, using a conventional nozzle-based and a lab-built nozzle-free electrospinning equipment. To produce nanofibers, electrospinning is the process most often used. However, from the industry’s point of view, conventional electrospinning does not have sufficiently high productivity. By omitting the nozzle, productivity can be increased, and so the development of nozzle-free processes is worthwhile. In this study, a solution of ciprofloxacin and polyvinylpyrrolidone was electrospun under similar conditions, using both single-nozzle and nozzle-free methods. The two electrospinning methods were compared by investigating the morphological and physicochemical properties, homogeneity, in vitro drug release, and cytotoxicity. The stability of the nanofibers was monitored from different aspects in a 26 month stability study. The results showed that the use of the nozzle-free electrospinning was preferable due to a higher throughput, improved homogeneity, and the enhanced stability of nanofiber mats, compared to the nozzle-based method. Nevertheless, fast dissolving nanofibers loaded with poorly water-soluble ciprofloxacin were produced by both electrospinning methods. The beneficial properties of these nanofibers can be exploited in innovative drug development; e.g., nanofibers can be formulated into orodispersible films or per os tablets. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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17 pages, 2212 KiB  
Article
Development and Evaluation of Cannabidiol Orodispersible Tablets Using a 23-Factorial Design
by Robert-Alexandru Vlad, Paula Antonoaea, Nicoleta Todoran, Emöke-Margit Rédai, Magdalena Bîrsan, Daniela-Lucia Muntean, Silvia Imre, Gabriel Hancu, Lénárd Farczádi and Adriana Ciurba
Pharmaceutics 2022, 14(7), 1467; https://doi.org/10.3390/pharmaceutics14071467 - 14 Jul 2022
Cited by 6 | Viewed by 1899
Abstract
Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from [...] Read more.
Orodispersible tablets (ODTs) are pharmaceutical formulations used to obtain fast therapeutic effects, usually recommended for geriatric and pediatric patients due to their improved compliance, bioavailability, ease of administration, and good palatability. This study aimed to develop ODTs with cannabidiol (CBD) phytocannabinoid extracted from Cannabis sativa used in the treatment of Lennox–Gastaut and Dravet syndromes. The tablets were obtained using an eccentric tableting machine and 9 mm punches. To develop CBD ODTs, the following parameters were varied: the Poloxamer 407 concentration (0 and 10%), the type of co-processed excipient (Prosolv® ODT G2—PODTG2 and Prosolv® EasyTab sp—PETsp), and the type of superdisintegrant (Croscarmellose—CCS, and Soy Polysaccharides—Emcosoy®—EMCS), resulting in eleven formulations (O1–O11). The following dependent parameters were evaluated: friability, disintegration time, crushing strength, and the CBD dissolution at 1, 3, 5, 10, 15, and 30 min. The dependent parameters were verified according to European Pharmacopoeia (Ph. Eur.) requirements. All the tablets obtained were in accordance with quality requirements in terms of friability (less than 1%), and disintegration time (less than 180 s). The crushing strength was between 19 N and 80 N. Regarding the dissolution test, only four formulations exhibited an amount of CBD released higher than 80% at 30 min. Taking into consideration the results obtained and using the Modde 13.1 software, an optimal formulation was developed (O12), which respected the quality criteria chosen (friability 0.23%, crushing strength of 37 N, a disintegration time of 27 s, and the target amount of CBD released in 30 min of 99.3 ± 6%). Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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20 pages, 4284 KiB  
Article
Milk Oral Lyophilizates with Loratadine: Screening for New Excipients for Pediatric Use
by Sonia Iurian, Cătălina Bogdan, Ștefana Suciu, Dana-Maria Muntean, Lucia Rus, Mihaela Berindeie, Szidonia Bodi, Rita Ambrus and Ioan Tomuță
Pharmaceutics 2022, 14(7), 1342; https://doi.org/10.3390/pharmaceutics14071342 - 24 Jun 2022
Cited by 3 | Viewed by 1700
Abstract
The development of suitable formulations for the pediatric population remains a challenging field with great advances reported every year in terms of excipients and technology. When developing pediatric formulations, the acceptability of medicines represents a key element to consider. For this reason, milk [...] Read more.
The development of suitable formulations for the pediatric population remains a challenging field with great advances reported every year in terms of excipients and technology. When developing pediatric formulations, the acceptability of medicines represents a key element to consider. For this reason, milk can be a widely accepted excipient with taste-masking properties and supplementary advantages for drug solubility. In recent years, the orodispersible dosage forms have come onto the market as child-friendly formulations. The current study aimed to develop freeze-dried orodispersible dosage forms containing bovine milk or infant formulae as the main component. In the first stage, an exploratory study evaluated the mechanical properties of placebo milk formulations and the suitability of milk as a matrix-forming agent. As the appropriate mechanical strength to withstand manipulation was demonstrated, milk oral lyophilizates were loaded with a poorly soluble model API, loratadine. Hence, a D-optimal design was conducted to prepare milk lyophilizates with loratadine and to evaluate the effects of three factors (dose of loratadine, the lyophilizate size, and the type of milk) and their interactions. Finally, three formulations were prepared to confront the predictions of the DoE and further studied to thoroughly understand the observed effects. The experimental results showed the potential of milk in the development of oral lyophilizates loaded with different doses of suspended API. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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23 pages, 4903 KiB  
Article
Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology
by Mahmoud M. A. Elsayed, Moustafa O. Aboelez, Bakheet E. M. Elsadek, Hatem A. Sarhan, Khaled Ali Khaled, Amany Belal, Ahmed Khames, Yasser A. Hassan, Amany A. Abdel-Rheem, Eslam B. Elkaeed, Mohamed Raafat and Mahmoud Elkot Mostafa Elsadek
Pharmaceutics 2022, 14(4), 880; https://doi.org/10.3390/pharmaceutics14040880 - 18 Apr 2022
Cited by 20 | Viewed by 3335
Abstract
Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms have a [...] Read more.
Tolmetin sodium (TLM) is a non-steroidal anti-inflammatory drug (NSAIDs). TLM is used to treat inflammation, skeletal muscle injuries, and discomfort associated with bone disorders. Because of the delayed absorption from the gastro intestinal tract (GIT), the currently available TLM dosage forms have a rather protracted start to the effect, according to pharmacokinetic studies. The aim of this study was to create a combination for TLM fast dissolving tablets (TLM-FDT) that would boost the drug’s bioavailability by increasing pre-gastric absorption. The TLM-FDTs were developed using a Box-Behnken experimental design with varied doses of crospovidone (CP), croscarmellose sodium (CCS) as super-disintegrants, and camphor as a sublimating agent. In addition, the current study used response surface approach to explore the influence of various formulation and process factors on tablet qualities in order to verify an optimized TLM-FDTs formulation. The optimized TLM-FDTs formula was subsequently evaluated for its in vivo anti-inflammatory activity. TLM-FDTs have good friability, disintegration time, drug release, and wetting time, as well as fast disintegration and dissolution behavior. Significant increase in drug bioavailability and reliable anti-inflammatory efficacy were also observed, as evidenced by considerable reductions in paw thickness in rats following carrageenan-induced rat paw edema. For optimizing and analyzing the effect of super-disintegrants and sublimating agents in the TLM-FDTs formula, the three-factor, three-level full factorial design is a suitable tool. TLM-FDTs are a possible drug delivery system for enhancing TLM bioavailability and could be used to treat rheumatoid arthritis. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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24 pages, 3394 KiB  
Article
Mucoadhesive Buccal Film of Estradiol for Hormonal Replacement Therapy: Development and In-Vivo Performance Prediction
by Sadikalmahdi Abdella, Franklin Afinjuomo, Yunmei Song, Richard Upton and Sanjay Garg
Pharmaceutics 2022, 14(3), 542; https://doi.org/10.3390/pharmaceutics14030542 - 28 Feb 2022
Cited by 9 | Viewed by 3805
Abstract
The age-related loss of circulating estrogen that occurs during the menopausal transition manifests itself through a variety of symptoms including vasomotor (hot flushes and night sweats), genito-urinary syndrome (vaginal dryness and urinary symptoms), sexual dysfunction, mood, and sleep disturbance that often last longer [...] Read more.
The age-related loss of circulating estrogen that occurs during the menopausal transition manifests itself through a variety of symptoms including vasomotor (hot flushes and night sweats), genito-urinary syndrome (vaginal dryness and urinary symptoms), sexual dysfunction, mood, and sleep disturbance that often last longer than a decade. Furthermore, reductions in estrogen level increase the risks of chronic complications such as osteoporosis, cardiovascular disease, and cognitive decline among others, thereby affecting the quality of life of women. Although oral estrogens are the most widely used therapy for menopausal symptoms, they suffer from poor bioavailability, and there are concerns over their safety, creating a significant concern to consumers. Mucoadhesive buccal films are an innovative dosage form that offers several advantages including avoidance of the first-pass metabolism, fast onset of action, and importantly, improved patient acceptance. In the current work, we developed mucoadhesive estradiol film for hormonal replacement therapy using film-forming polymers. Two approaches, namely, co-solvency and nano-emulsion were evaluated to increase solubility and hence incorporate estradiol, a poorly water-soluble drug, into a formulation made from the hydrophilic polymer/s. The films were characterised for their mechanical and physicochemical properties. In-vitro release study showed that about 80% of the drug was released within 6 min from films prepared by the nano-emulsion approach, whereas it took about 10.5 min to get similar drug release from films prepared by the co-solvency approach. The ex-vivo permeation result indicates that about 15% of the drug permeated across the porcine buccal mucosa in the first 10 h from films prepared by the nano-emulsion approach, while permeation across porcine buccal mucosa was only observed at around 24 h from films prepared by the co-solvency method. The nano-emulsion films were evaluated for in vivo performance using a convolution technique using R software. The predicted Cmax and Tmax were found to be 740.74 ng mL−1 and 7 min, respectively, which were higher than previously reported in vivo concentration from oral tablets. The results demonstrated that mucoadhesive film of estradiol based on the nano-emulsion approach could be a promising platform for the delivery of estradiol through the buccal mucosa for the treatment of menopausal symptoms. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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17 pages, 1247 KiB  
Review
Orodispersible Film (ODF) Platform Based on Maltodextrin for Therapeutical Applications
by Irma E. Cupone, Andrea Sansone, Fabio Marra, Andrea M. Giori and Emmanuele A. Jannini
Pharmaceutics 2022, 14(10), 2011; https://doi.org/10.3390/pharmaceutics14102011 - 22 Sep 2022
Cited by 8 | Viewed by 4867
Abstract
Orodispersible film (ODF) is a new dosage form that disperses rapidly in the mouth without water or swallowing. The main ingredient of an ODF is a polymer that can be both of natural or synthetic origin. Maltodextrin is a natural polymer, mainly used [...] Read more.
Orodispersible film (ODF) is a new dosage form that disperses rapidly in the mouth without water or swallowing. The main ingredient of an ODF is a polymer that can be both of natural or synthetic origin. Maltodextrin is a natural polymer, mainly used in pharmaceutical and nutraceutical fields. This review aims to examine the literature regarding ODFs based on maltodextrin as the platform for developing new products for therapeutical application. ODFs based on maltodextrin contain plasticizers that enhance their flexibility and reduce their brittleness. Surfactants; fillers, such as homopolymer and copolymer of vinylacetate; flavour and sweetener were introduced to improve ODF characteristics. Both water-soluble and insoluble APIs were introduced up to 100 mg per dosage unit. The solvent casting method and hot-melt extrusion are the most useful techniques for preparing ODFs. In particular, the solvent casting method allows manufacturing processes to be developed from a lab scale to an industrial scale. ODFs based on maltodextrin are characterized in terms of mechanical properties, dissolution rate, taste and stability. ODFs made of maltodextrin, developed by IBSA, were tested in vivo to evaluate their bioequivalence and efficacy and were demonstrated to be a valid alternative to the marketed oral dosage forms. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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28 pages, 1147 KiB  
Review
Orally Dispersible Dosage Forms for Paediatric Use: Current Knowledge and Development of Nanostructure-Based Formulations
by Andreea Cornilă, Sonia Iurian, Ioan Tomuță and Alina Porfire
Pharmaceutics 2022, 14(8), 1621; https://doi.org/10.3390/pharmaceutics14081621 - 03 Aug 2022
Cited by 10 | Viewed by 6431
Abstract
The paediatric population has always suffered from a lack of medicines tailored to their needs, especially in terms of accurate dosage, stability and acceptability. Orodispersible dosage forms have gone through a resurrection as an alternative to liquid formulations or fractioned solid formulations, although [...] Read more.
The paediatric population has always suffered from a lack of medicines tailored to their needs, especially in terms of accurate dosage, stability and acceptability. Orodispersible dosage forms have gone through a resurrection as an alternative to liquid formulations or fractioned solid formulations, although they are still subject to several inconveniences, among which the unpleasant taste and the low oral bioavailability of the API are the most significant hurdles in the way of achieving an optimal drug product. Nanostructures can address these inconveniences through their size and variety, owing to the plethora of materials that can be used in their manufacturing. Through the formation and functionalisation of nanostructures, followed by their inclusion in orodispersible dosage forms, safe, stable and acceptable medicines intended for paediatric use can be developed. Full article
(This article belongs to the Special Issue Development of Orally Dispersible Dosage Forms)
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