Buccal Tablets Research Articles

Development of Mucoadhesive Chitosan-Iodoacetamide Buccal Tablets for Local Delivery of Dextromethorphan

Abstract This study aimed to synthesize a chitosan (CHI) derivative, chitosan-iodoacetamide (CHI-IA), with enhanced mucoadhesive properties and develop buccal mucoadhesive tablets of CHI-IA for local delivery of dextromethorphan (DXT). Mucoadhesive CHI-IA was synthesized by a chemical reaction between CHI and iodoacetic acid (IA) in different weight ratios. The synthesized CHI-IA was characterized by Fourier-transformed infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR) to confirm the chemical structure and assure successful synthesis. DXT was selected as the model drug to be incorporated into the matrix tablet to develop mucoadhesive buccal cough relief tablets. The mucoadhesive strength of the CHI-IA tablets was determined by a texture analyzer. Moreover, the drug content and the release characteristics of DXT from the mucoadhesive tablets were evaluated. The FT-IR and NMR spectra of CHI-IA indicated the conjugation of IA on the structure of CHI. The CHI-IA tablets exhibited a 4-time increase in mucoadhesion force compared with that of unmodified CHI. Moreover, a gradual release of DXT from the tablets was observed, and the release kinetics best fit with the Higuchi model (R2 = 0.9912). Therefore, the CHI-IA could be applied as the mucoadhesive carrier system for drug delivery. Keywords: Chitosan, Iodoacetic acid, Mucoadhesive, Buccal tablets, Dextromethorphan

A Review on Mucoadhesive Buccal Drug Delivery

The discovery and development of medical formulations is presently concentrated on the improvement of therapeutic drugs to be aimed at the targeted location or place to reduce total dissemination in the host. The Mucoadhesive drug delivery system is most potential therapeutic agent. The buccal route is a best route from all dosages form. In this review we study about the Mucoadhesive buccal drug there advantages, characteristics, ideal properties. The various Mucoadhesive buccal formulations. The survey on the polymer used for Mucoadhesive buccal tablets.

Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin

The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. Based on the early testing, a 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The FTIR, DSC, and XRD investigations validated the Quercetin interaction with nanosponges. The medicine released from the nanosponges buccal tablets in-vitro at a rate of 99.75%, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27 ± 0.06 ng/mL was significantly higher (p

Fentanyl buccal tablets recall due to omission of safety updates in PI

Fentanyl buccal tablets recall due to omission of safety updates in PI

Medical opioid disposal in Fukuoka and Kumamoto cities.

Medical expenses are increasing year by year in Japan. However, the quantity of disposed medical opioids is not well known. In this study, we assessed disposed medical opioids in community pharmacies of Fukuoka city and in all of medical organizations of Kumamoto cities for 3 and 2 years, respectively. We collected official opioid disposal reports in Kumamoto city and Fukuoka City Pharmaceutical Association disposal information sheet in Fukuoka city. The total amount of disposed opioids was worth 7.1 million ¥ from 2017 to 2019 in Fukuoka city, and 8.9 million ¥ in for 2 years (2018 and 2019) in Kumamoto city. In Fukuoka city, the most disposed opioid was 20 mg Oxycontin®, worth approximately 940,000 ¥. In Kumamoto city we assessed data in different organizations. The most disposed opioid was 5 mg Oxinorm® at a cost of 600,000 ¥ at the medical institutions over the 2-year study period. The most disposed opioid was 40 mg Oxycontin®, at a cost of 640,000 ¥ in community pharmacies. Two hundred µg E-fen® buccal tablet was the most disposed of opioid, was amounting to 960,000 ¥ in wholesalers. On the whole in Kumamoto city, non-dispensing was the most common reason of disposal. These results indicate that the amount of disposed opioids is huge. Small package simulation studies suggest that smaller package units of MS-Contin®, Anpec® suppository, and Abstral® sublingual tablet may be able to reduce the amount of disposed opioids.

Mucoadhesive buccal tablet of leuprolide and its fatty acid conjugate: Design, in vitro evaluation and formulation strategies

This study aimed to design mucoadhesive buccal tablets of leuprolide (LEU) and to manufacture and evaluate the properties of buccal tablets containing LEU-oleic acid conjugate (LOC) and self-assembled LEU-oleic acid nanoparticles (LON), which were developed in a previous study. Hydroxypropyl methylcellulose (HPMC 4000) was used as the mucoadhesive polymer, and tablets were prepared by direct compression. The formulations were characterized by weight, content uniformity, thickness, hardness, swelling index, disintegration time, mucoadhesion time, and drug release. The chosen formulation maintained an adhesion time of up to 6.43 h and a disintegration time of 4.10 h. Drug stability in the mucoadhesive tablets was confirmed after 2 h of storage in human mimic saliva (Phosphate buffer solution pH 6.8). Furthermore, the designed LEU formulation and the LOC and LON developed in a previous study were prepared as buccal tablets and compared. In the dissolution and permeation studies, LON-loaded buccal tablets showed the highest permeation rate. This study suggests that mucoadhesive buccal tablets containing self-assembled LON may effectively increase the medication adherence for pediatric and geriatric patients by improving the bioavailability and permeation rate of LEU.

Designing and characterization of Yahom buccal mucoadhesive tablets for oral ulcer treatment

Oral ulcer is a common oral mucosal disease that affects about 5–20% of general population, particularly the elderly, and is characterized by recurrent, painful ulcerations and burning sensation. Various possible causes include local, systemic, immunologic, genetic, allergic and microorganisms. Yahom is a Thai traditional medicine that has long been used to treat nausea, vomiting, dizziness and weakness in elderly. Yahom is produced from a variety components of dried medicinal plant parts that are mostly ground into powder dosage form. Ingredients are composed of following crude drugs are common incorporated in Yahom preparations such as clove, terminalia gall, costus root and ceylon ironwood flower which practically and clearly exhibit the potent antioxidant and antimicrobial activities. Therefore, it is interesting to apply Yahom as active component for oral ulcer treatment using appropriate approach such as mucoadhesive tablet. The objective of this study is to develop buccal mucoadhesive tablet consisting of hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as mucoadhesive polymers in formulations. The impact of various ratios of Yahom: polymer and polymer mixtures were investigated on physicochemical properties of mucoadhesive tablets were investigated including physical properties, disintegration time, water sorption/erosion behaviors and ex-vivo mucoadhesion. In addition, the antimicrobial activities of formulations against two standard microbes were also evaluated using agar cup diffusion methods. Yahom mucoadhesive tablets were successfully fabricated using direct compression tableting technique with good appearance and acceptable physical properties. Different amounts of Yahom and polymer ratios apparently influenced on water sorption, erosion behaviors and hardness of mucoadhesive tablets, resulting in alteration of disintegration time and muco-adhesion properties. In addition, these prepared tablets exhibited the efficient antimicrobial activities against Staphylococcus aureus ATCC 6538 and C. albicans ATCC 10231. Therefore, the buccal mucoadhesive tablets containing Yahom are the potential herbal delivery system for oral ulcer treatment.

FORMULATION AND EVALUATION OF RISPERIDONE MUCOADHESIVE BUCCAL TABLETS

FORMULATION AND EVALUATION OF RISPERIDONE MUCOADHESIVE BUCCAL TABLETS

Incorporating sodium deoxycholate endorsed the buccal administration of avanafil to heighten the bioavailability and duration of action.

The highly effective phosphodiesterase type 5 inhibitor (avanafil; AVA) is routinely prescribed to treat erectile dysfunction. The drug has poor oral bioavailability and undergoes a significant first-pass metabolism. Therefore, altering AVA's solubility and choosing a different delivery method may boost its effectiveness. Nine different solid dispersion formulations utilizing polyvinylpyrrolidone (PVP) at three different ratios were prepared and characterized. The Box-Behnken design was employed to optimize AVA-buccal tablets. The pre-compression and post-compression characteristics of the tablets were assessed. The mucoadhesion strength of the optimized tablet was investigated using cow buccal mucosal tissue. In vivo performance of the optimized tablets was examined on human volunteers compared to the commercial tablets. PVP K90 at 2:1 drug to polymer ratio showed the highest solubilization capacity. The mucoadhesive polymer type and percentage and the mucopenetration enhancer percentage were significantly affect the mucoadhesion strength, tablet hardness, and the initial and cumulative AVA released from the prepared tablets. The optimized AVA-buccal tablet showed 4.96 folds increase in the mean residence time, higher plasma exposure, and an improvement in the relative bioavailability of AVA by 1076.27% compared with the commercial tablet. Therefore, a successful approach to deal with AVA first-pass metabolism and low bioavailability could be to employ buccal tablets containing a solubility-enhanced form of AVA.

Formulation and Evaluation of Mucoadhesive Buccal tablets using Nimodipine Solid Lipid Nanoparticles

This study aimed to create and describe mucoadhesive nimodipine solid lipid nanoparticles as buccal tablets by altering the amounts of three polymers: Carbopol 934, Hydroxypropyl methylcellulose and Hydroxyethyl cellulose. The Nimodipine-loaded solid lipid nanoparticles (SLN) were formulated by high shear homogenization and ultrasonication process using palmitic and stearic acid as the lipid matrix and Tween-80 as the surfactant. The swelling properties of all formulations were investigated, and it was discovered that all formulations have a good swelling index at 6 hours. The surface pH of each batch varied between 5.6 and 6.1. The mucoadhesive strengths (15.3-29.5 g) varied with polymer concentrations, particularly Carbopol 934. All batches had considerably different dissolution profiles, ranging from a maximum release of 89.08% (at 8h in batch NT3) to a minimum release of 80.32% (at 8h in batch NT2). SLN formulations had the best results in both Entrapment efficiency and In-vitro drug release, showing that SLN may be a promising delivery strategy for improving Nimodipine release.

Predicting tolerability of high-dose fentanyl buccal tablets in cancer patients.

Fentanyl buccal tablets (FBTs) are a rapid-onset opioid indicated for breakthrough cancer pain (BTcP) and FBT titration is needed to optimize BTcP management. We aimed to predict which patients could tolerate a high dose of FBT (400 μg or more at a time). A retrospective analysis was performed to assess the final FBT dose. The final FBT doses were compared according to the clinical features. The prediction accuracy of patients tolerant of 400 μg or higher FBT was compared using the area under the receiver operating characteristic (ROC) curves. A risk scoring model based on the odds ratio (OR) was developed from the final multivariable model, and patients were assigned into two groups: low tolerance (0-1 point) and high tolerance (2-3 points). Among 131 patients, the most frequently effective dose of FBT was 200 μg (54%), followed by 100 μg (30%). The median value of morphine equivalent daily doses (MEDD) was 60 mg/day, and the most common daily use was 3-4 times/day. In multivariable analysis, male sex, younger age, and use of FBTs three or more times per day were independently associated with high-dose FBT. According to the risk scoring model, the patients with a final FBT of 400 μg or higher were significantly more in the high tolerance group (17%) compared to the low tolerance group (3%; p = 0.023). According to the dose relationship between the final FBT dose and the clinical features, three factors (sex, age, daily use of FBT) were independently associated with the final dose of FBT. Our risk score model could help predict tolerance to high-dose FBT and guide the titration plan for BTcP.

Formulation and evaluation of Buccal mucoadhesive tablets of diclofenac sodium using 23 factorial designs

Diclofenac sodium is an NSAID (Non-Steroidal anti-inflammatory widely used in the treatment of pain, migraine, and inflammation). It has been observed that Diclofenac undergoes extensive first-pass metabolism when administered using conventional dosage forms through the oral route. The aim of this study is to formulate and evaluate pre-compression, post-compression factors and release kinetics of buccal mucoadhesive tablets formulated by a 23 factorial method that can prevent the first-pass metabolism of the drug thereby increasing its bioavailability. This formulation increases patient compliance by reducing its dosing frequency. In these formulations, two polymers polyvinyl pyrrolidine (PVP K30) and Chitosan are used in varying proportions. Eight different formulations were prepared by varying concentrations of the polymers. The buccal mucoadhesive tablets formulated have been evaluated for their general appearance, thickness, hardness, weight variation, friability and other in vitro tests such as swelling and dissolution studies. The evaluation studies demonstrated that formulation F8 showed better properties as a buccal mucoadhesive formulation compared to other formulations.

PP067 Predicting tolerability of high-dose fentanyl buccal tablets in cancer patients

PP067 Predicting tolerability of high-dose fentanyl buccal tablets in cancer patients

Buccal films: A review of therapeutic opportunities, formulations & relevant evaluation approaches.

The potential of the mucoadhesive film technology is hard to ignore, owing to perceived superior patient acceptability versus buccal tablets, and significant therapeutic opportunities compared to conventional oral drug delivery systems, especially for those who suffer from dysphagia. In spite of this, current translation from published literature into the commercial marketplace is virtually non-existent, with no authorised mucoadhesive buccal films available in the UK and very few available in the USA. This review seeks to provide an overview of the mucoadhesive buccal film technology and identify key areas upon which to focus scientific efforts to facilitate the wider adoption of this patient-centric dosage form. Several indications and opportunities for development were identified, while discussing the patient-related factors influencing the use of these dosage forms. In addition, an overview of the technologies behind the manufacturing of these films was provided, highlighting manufacturing methods like solvent casting, hot melt extrusion, inkjet printing and three-dimensional printing. Over thirty mucoadhesive polymers were identified as being used in film formulations, with details surrounding their mucoadhesive capabilities as well as their inclusion alongside other key formulation constituents provided. Lastly, the importance of physiologically relevant in vitro evaluation methodologies was emphasised, which seek to improve in vivo correlations, potentially leading to better translation of mucoadhesive buccal films from the literature into the commercial marketplac.

Oromucosal delivery of macromolecules: Challenges and recent developments to improve bioavailability.

Owing to their biological diversity, high potency, good tolerability, low immunogenicity, site-specific activity, and great efficacy, macromolecular drugs (i.e., proteins and peptides, antibodies, hormones, nucleic acids, vaccines, etc.) are extensively used as diagnostics, prophylactics, and therapeutics in various diseases. To overcome drawbacks associated with parenteral (invasive) delivery of macromolecules as well as to preserve their therapeutic integrity, oromucosal route (sublingual and buccal) has been proven efficient alternate port of delivery. This review aims to summarize challenges associated with oromucosal route and overtime developments in conventional delivery systems with special emphasis on most recent delivery strategies. Over the past few decades, significant efforts have been made for improving the oromucosal absorption of macromolecules by employing chemical penetration enhancers (CPE), enzyme inhibitors, chemical modification of drug structure (i.e., lipidation, PEGylation, etc.), and mucoadhesive materials in the form of buccal tablets, films (or patches), sprays, fast disintegrating tablets, and microneedles. Adaptation of adjunct strategies (e.g., iontophoresis in conjunction with CPE) has shown significant improvement in oromucosal absorption of macromolecules; however, these approaches were also associated with many drawbacks. To overcome these shortcomings and to further improve therapeutic outcomes, specialized delivery devices called "hybrid nanosystems" have been designed in recent times. This newer intervention showed promising potential for promoting oromucosal absorption and absolute bioavailability of macromolecules along with improved thermostability (cold chain free storage), enabling self-administration, site-specific activity, improving therapeutic efficacy and patient compliance. We anticipate that tailoring of hybrid nanosystems to clinical trials as well as establishing their short- and long-term safety profile would substantiate their therapeutic value as pharmaceutical devices for oromucosal delivery of macromolecules.

Formulation and Evaluation of Mucoadhesive Bilayered Buccal Tablet of Ziprasidone Hydrochloride

The present project was carried out to formulate and evaluate the mucoadhesive bilayered buccal tablet of Ziprasidone Hcl. Ziprasidone HCl is an antipsychotic agent with half-life of about 2hrs and shows extensive metabolism i.e the drug concentration is < 5% after elimination in the body. The formulations (F1 to F6) were developed which comprises of polymers such as Hydroxypropyl methyl cellulose (HPMC K-15), Polyvinyl pyrollidine (PVP K-30) in various concentrations along with carbopol to achieve the desired characteristics. Mucoadhesive bilayered buccal tablets were fabricated with the aid of direct compression technique and the prepared formulation was evaluated for its physicochemical parameters along with evalauation test. The results from different evaluation test demonstrated that the formulation F1 containing HPMC (25 mg) and CP (10 mg) was selected as optimised formulation and result values of precompression parameters were within the limits and post compression results showed the mucoadhesive strength of F1 formulation was 25.27gm, the drug release at 8th hr was 85.7 % and the formulation was stable throughout the stability studies. Hence mucoadhesive bilayered buccal tablets of Ziprasidone HCl can be prepared. Based on the above results it can be stated that mucoadhesive bilayered buccal tablets can be successfully developed. Formulation described that the nature of tablet depends not only on the se lected polymer excipient but also on the concentration of polymers selected. 
 Keywords: Ziprasidone HCl, Bilayered Buccal Tablet, Mucoadhesion.

Near-Infrared data classification at phone terminal based on the combination of PCA and CS-RBFSVC algorithms

Near-infrared (NIR) spectroscopy is a non-destructive, efficient and convenient detection technology, with the emergence of portable NIR spectrometers, NIR mobile applications (APPs) come into being. The popularity of intelligent mobile phones provides an impetus to the research and development of NIR APPs, however, the primary functions such as operating the NIR spectrometers and collecting data cannot satisfy NIR users in the field of data processing. Herein, we propose an APP processing NIR data locally at the mobile terminal, by the comprehensive utilization of Principal Component Analysis (PCA) and Cuckoo Search algorithm optimized Support Vector Classifier with radial basis function (RBFSVC) kernel (CS-RBFSVC). 738 NIR samples of four drugs (Cydiodine Buccal Tablets, Sulfasalazine Enteric-coated Tablets, Dexamethasone Acetate Tablets, Vecuronium Bromide for Injection) were used as the validation objects to train and test the data classification model. Firstly, the original data were subjected to dimensional reduction through PCA for the purpose of compressing calculation amount. Secondly, the CS-RBFSVC model was utilized to classify the types of drugs and their manufacturers, moreover, the improved accuracy and efficiency by introducing Cuckoo Search (CS) algorithm into RBFSVC were proven in comparison with the conventional grid optimized RBFSVC (Grid-RBFSVC) and Linear Support Vector Classifier (Linear-SVC). Last but not least, an APP based on the proposed PCA and CS-RBFSVC model is developed and demonstrated to be able to classify the type of drugs with an accuracy of 100%, the accuracies of classifying the drugs’ manufacturers were 100%, 100%, 98.3% and 90.7%, respectively. Conclusively, the proposed PCA and CS-RBFSVC based model can provide a low-consumption, high accuracy and quick strategy for NIR data classification and overcome the limitations of internal storage and operating speed at phone terminals, in conjunction with the portable NIR spectrometer, it is believed to push forward NIR technology into the instant detection and on-site inspection.

An Individualized Approach to Managing Testosterone Therapy in the Primary Care Setting.

The incidence of testosterone deficiency and the use of testosterone therapy have increased in recent years, and currently the majority of testosterone prescriptions in the United States and Canada are written by primary care physicians. Meanwhile, the range of available testosterone therapy formulations has widened to include buccal tablets, intramuscular injections, transdermal gels, intranasal gel, subcutaneous injections, oral capsules, and subdermal pellets, each with unique pharmacokinetic and clinical characteristics. Despite the growing use of testosterone therapy and its overall efficacy and safety as demonstrated in clinical trials, concerns exist about the potential impact of testosterone therapy on spermatogenesis and fertility, development of prostate cancer, and risk of polycythemia and cardiovascular events. In addition, ongoing research aims to better characterize the effects of testosterone therapy in specific populations, such as patients aged 65 years and older, patients with obesity and type 2 diabetes, and transgender patients. The range of treatment options and the diversity of patients’ goals, preferences, comorbidities, and risk factors necessitate an individualized approach to testosterone therapy that considers each patient’s clinical needs alongside the distinct features of different testosterone formulations.

Formulation Development and Evaluation of Mucoadhesive Buccal Tablets of Acebutolol Hydrochloride

A mucoadhesive drug delivery system is an oral dosage form, where the tablet, gel, or patch is attached to the buccal region for direct absorption of the drug into blood circulation. This dosage form has been employed to improve the bioavailability of drugs that undergoes significant hepatic first-pass metabolism. Acebutolol is a beta sympatholytic agent used to treat high blood pressure and irregular heartbeat (arrhythmia). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. In present investigation, mucoadhesive buccal tablets of acebutolol HCl were prepared using carbopol 940 in varying concentrations with secondary polymer xanthan gum by direct compression method. Nine batches were prepared as per 32 factorial designs, to investigate the combined effects of independent variables namely carbopol 940 and xanthan gum on dependant variables namely swelling index, mucoadhesion strength and in-vitro drug release using design expert software version 8.0.7.1. Preformulation studies confirmed the identity and purity of the drug by means of UV spectroscopy, IR spectroscopy, DSC analysis, and melting point determination. The tablets were evaluated for hardness, thickness, weight variation, friability, and drug content concluded that all these parameters were in an acceptable range of pharmacopoeial specification. The buccal tablets were studied for surface pH, swelling index, in vitro drug release study, adhesion force, in vitro mucoadhesive strength, stability, and compatibility study to optimise the formula. Amongst all factorial batches (F1 to F9), batch F5 (30 mg carbopol 940 and 30 mg xanthan gum) showed maximum drug release of 99.96 % after 12 hr of study and also showed better contact with biological membrane. The drug release kinetics of batch F5 was found to be best fitted to zero order kinetic model and exhibited anomalous diffusion release mechanism. The formulation F5 exhibited good correlation (R2=0.992) for in-vitro drug release. All the evaluation parameters give positive results and comply with the standards. Stability studies were carried out on the developed formulations indicating that the formulations were stable during the period of 6 months. In conclusion, the formulation F5 is stable and effective for quick action and seems to be alternative to the conventional tablet.

Bimodal Release Two-In-One Clonazepam Matrix Lozenge Tablets for Managing Anxiety-Related Disorders: Formulation, Optimization and In Vivo Evaluation

Clonazepam (CLZ), an antipsychotic drug reported for its efficiency in managing anxiety-related disorders, is being marketed only as conventional tablets. Some patients have abstention to swallow the conventional tablets; therefore, the proposed study was aimed at developing a buccal lozenge tablet by direct compression of two types of optimized granules. Conazepam’s water solubility was first enhanced by a solid dispersion technique for a fast and better dissolution of type 1 granules, while the impact of gelling polymers was investigated on controlled-release type 2 granules. The optimized formulae met the acceptable pharmacopeial limits for tablets’ evaluation. A differential scanning calorimetry study revealed the compatibility between the drug and used excipients. All formulae gave a burst release of CLZ in the first hour of investigation, followed by a sustained release over 24 h. The formula that showed the highest prolonged in vitro release (99.0 + 0.1%), following the Higuchi diffusion model (R2 = 0.99), was then selected for further study. The formula succeeded in controlling the induced stress in a rat model with a significant impact on the behavioral tests throughout the experiment. The results were further confirmed by a pharmacokinetic study that showed a significant increase in Cmax, Tmax, and AUC (1.5, 2, and 3.9 folds), respectively, compared to oral suspension. The newly proposed delivery system has proven a better efficacy with a reduced dosing frequency.