Buccal Tablets Research Articles

A REVIEW UPDATE ON DILLENIA INDICA F.ELONGATA (MIQ.)MIQ.

Dillenia indica f. elongata (Miq.) Miq. (Dilleniaceae) commonly known as Elephant apple. The vernacular names include Chalta, Chulta, Karambel, Bhavya and Ramphal.It is found in Bangladesh, Nepal, China, Indonesia and Assam, West Bengal, Orissa, Bihar, Myanmar regions of India. Dillenia indica f. elongata (Miq.) Miq. has been prevalently used in Indian traditional and ayurvedic medicine for curing plethora of ailments such as digestive, respiratory and central nervous systems. The information was put together, with the help of literature surveyed. Traditionally different parts of Dillenia indica f. elongata (Miq.) Miq. have been used for the relief of indigestion, asthma, influenza, dysentery,jaundice,promeho,weakness and rheumatic pain. Moreover, the extractives showed significant cytotoxic, CNS depressant and free radical scavenging activity. Wood obtained from the bark of the plant has been used for preparing rafters, tool-handles, cupboard and house pots. It is interesting to know that bark of Dillenia indica f. elongata (Miq.) Miq. is used for production of charcoal. Microspheres of metformin hydrochloride and novel mucoadhesive buccal tablets of oxytocin were also prepared from Dillenia indica f. elongata (Miq.) Miq. In vitro propagation is practised whereas micropropagation is considered at the time, when large scale plant multiplication is required. Phytochemical studies revealed substantial presence of polyphenols, tannins, alkaloids and flavanoids which are responsible for the various pharmacological activities. Major chemical constituents present in the plant are betulin (pentacyclic triterpenoid) and betulinic acid that show wide spectrum of pharmacological activities which include anti-HIV, anti-inflammatory, anti-cancer, anti-malarial etc. Furthermore, Dillenia indica f. elongata (Miq.) Miq. is found to possess analgesic, anti-diabetic, anti- microbial,anti-bacterial,anti-diabetic,anti-oxidant,anti-proliferation,anti-diarrhoeal, antiimplantation, cytotoxic, wound healing and hair waving activity. Keyword(s)- Dillenia indica f. elongata (Miq.) Miq . ; Phytochemical profile; Traditional uses; Pharmacological properties.

Biointerfacial phenomena of amlodipine buccomucosal tablets of HPMC matrix system containing polyacrylate polymer/β-cyclodextrin: Correlation of swelling and drug delivery performance

ABSTRACTObjectives: This study focuses on the development of amlodipine bilayer buccal tablets of hydroxypropyl methylcellulose (HPMC) matrix system containing polyacrylate polymer (Carbopol®)/β-cyclodextrin as the drug layer and ethylcellulose as the non-swellable backing layer, and their biointerfacial phenomena.Methods: Tablets were evaluated for swelling, erosion and mucoadhesion using buccal mucosal tissue ex vivo. In vitro drug release and ex vivo drug transport across mucosal tissue were also performed in phosphate buffer (pH 6.8). The relationship of swelling with buccoadhesion and buccal permeation of various bilayer tablet formulations containing HPMC alone and in combination with Carbopol or drug-β-cyclodextrin complex has been prepared.Results: Overall buccoadhesion of the tablet with combination of HPMC and Carbopol was increased significantly compared with that of HPMC alone. Presence of cyclodextrin did not change bioadhesion force and swelling behavior significantly. Ex vivo permeation was increased with the increase of HPMC proportion in other formulations as observed in in vitro dissolution.Conclusion: Drug–cyclodextrin complexes in the tablet improved permeation due to its improved dissolution at the site of biointerface of tablet and buccomucosa. Correlations of ex vivo and in vitro data have been established to predict the buccomucosal permeation from the swelling index or drug release alone.

Mucoadhesive Buccal Tablets Based on Chitosan/Gelatin Microparticles for Delivery of Propranolol Hydrochloride

Propranolol administration through buccal route offers some distinct advantages thanks to the easy access to the oral mucosa, fast onset of action, and avoidance of hepatic and intestinal degradation mechanisms. To overcome the effective removal existing in the buccal cavity, mucoadhesive delivery systems are considered a promising approach as they facilitate a close contact with the buccal mucosa. The aim of this study was to prepare mucoadhesive tablets based on chitosan/gelatin microparticles for buccal delivery of propranolol hydrochloride. Spray-dried microparticles were prepared with different chitosan-gelatin weight ratios and characterized in terms of yield and morphology. Microparticles were subsequently compressed with the drug to obtain loaded buccal tablets. In vitro water uptake, mucoadhesion, release, and permeation tests were performed to investigate tablet ability to hydrate, to adhere to the mucosa, and to deliver drug through buccal mucosa. Microparticles showed a different morphology based on the different chitosan-gelatin weight ratios. Moreover, buccal tablets based on the prepared microparticles showed different technological and functional characteristics in virtue of their composition. In particular, tablets with an excess of chitosan showed the best mucoadhesive properties, allowed the permeation of the greatest drug amount among all formulations, and could be promising for buccal administration of propranolol hydrochloride.

Compliance and Patient Acceptability of Clonidine Mucoadhesive Buccal Tablet (Clonidine Lauriad) to Prevent Severe Radiomucositis in Head and Neck Cancer Patients

Compliance and Patient Acceptability of Clonidine Mucoadhesive Buccal Tablet (Clonidine Lauriad) to Prevent Severe Radiomucositis in Head and Neck Cancer Patients

G18 - Breakthrough pain in patients with head and neck cancer: efficacy and safety of buccal fentanyl citrate

Background: More than 50% of patients with cancer experience pain, which is often of moderate-to-severe intensity. In particular, the highest prevalence of pain is observed in head-neck tumours (70%). In patients with advanced disease, management of pain remains a particular challenge. The breakthrough cancer pain (BTcP) is a transient pain, a temporary exacerbation with variable frequency (1-6 times a day), which occurs in patients with chronic pain normally well controlled by basic analgesic therapy administered at fixed times (therapy around-the-clock).Material (patients) and methods: from January 2012 to March 2015 we collected data from 50 patients with histological diagnosis of squamous cell carcinoma of the head and neck treated for symptomatic BTcP with fentanyl citrate buccal tablets. Basic pain was treated with oxycodone/naloxone at doses from 10 mg bid to 80 mg bid. The patients were evaluated for BTcP onset and any associated precipitating was considered. Treatment for BTcP with fentanyl citrate buccal tablets has been proposed at a starting dose of 100 micrograms increased up to 800 micrograms and repeatable every 4 hours. During the observation period all patients were assessed weekly by clinical examination and pain was valued through NRS.Results: basic chronic pain was well controlled with oxycodone/naloxone demonstrated by a reduction in NRS (average score from 7 to 2). Of the 50 patients with carcinoma of the head and neck, 22 patients had BTcP episodes repeated daily related to swallowing and 14 patients had episodes triggered by medication of external lesions; none of these episodes was attributable to the end of basic opioid dose. The maximum number of daily episodes was 5 for the BTcP triggered by swallowing and 3 for the one triggered by medication (average NRS was 8). The average effective dose of fentanyl buccal tablets was 400 micrograms bid and all patients reported disappearance of BTcP episodes. About side effects mainly observed, nausea occurred in 4% of cases and only 2% presented pain and bleeding where the tablet was applied.Conclusions: over 70% of the patients analyzed in our study suffered of repeated episodes of BTcP reflecting literature data. NRS scale reduction for chronic pain and BTcP episodes disappearance demonstrated efficacy of the therapies. Safety was demonstrated by the minimal side effects so that switching to another formulation of rapid-onset opioids wasn't necessary. Background: More than 50% of patients with cancer experience pain, which is often of moderate-to-severe intensity. In particular, the highest prevalence of pain is observed in head-neck tumours (70%). In patients with advanced disease, management of pain remains a particular challenge. The breakthrough cancer pain (BTcP) is a transient pain, a temporary exacerbation with variable frequency (1-6 times a day), which occurs in patients with chronic pain normally well controlled by basic analgesic therapy administered at fixed times (therapy around-the-clock). Material (patients) and methods: from January 2012 to March 2015 we collected data from 50 patients with histological diagnosis of squamous cell carcinoma of the head and neck treated for symptomatic BTcP with fentanyl citrate buccal tablets. Basic pain was treated with oxycodone/naloxone at doses from 10 mg bid to 80 mg bid. The patients were evaluated for BTcP onset and any associated precipitating was considered. Treatment for BTcP with fentanyl citrate buccal tablets has been proposed at a starting dose of 100 micrograms increased up to 800 micrograms and repeatable every 4 hours. During the observation period all patients were assessed weekly by clinical examination and pain was valued through NRS. Results: basic chronic pain was well controlled with oxycodone/naloxone demonstrated by a reduction in NRS (average score from 7 to 2). Of the 50 patients with carcinoma of the head and neck, 22 patients had BTcP episodes repeated daily related to swallowing and 14 patients had episodes triggered by medication of external lesions; none of these episodes was attributable to the end of basic opioid dose. The maximum number of daily episodes was 5 for the BTcP triggered by swallowing and 3 for the one triggered by medication (average NRS was 8). The average effective dose of fentanyl buccal tablets was 400 micrograms bid and all patients reported disappearance of BTcP episodes. About side effects mainly observed, nausea occurred in 4% of cases and only 2% presented pain and bleeding where the tablet was applied. Conclusions: over 70% of the patients analyzed in our study suffered of repeated episodes of BTcP reflecting literature data. NRS scale reduction for chronic pain and BTcP episodes disappearance demonstrated efficacy of the therapies. Safety was demonstrated by the minimal side effects so that switching to another formulation of rapid-onset opioids wasn't necessary.

FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS OF CANDESARTAN

Candesartan is an angiotensin II receptor antagonist and is widely  used in the management of hypertension to reduce cardiovascular mortality in patients with left ventricular dysfunction following myocardial infarction, and in the management of heart failure. The Mucoadhesive buccal tablets were prepared by direct compression method using carbopol 934, HPMC K4M, sodium CMC as mucoadhesive polymer. The compatibility studies of drug and excipients were performed by FT-IR spectroscopy. After examining the flow properties of the powder blends the results are found to be within prescribed limits and indicated good flowing property, hence it was subjected to tablet compression. The tablets were evaluated for post-compression parameters like weight variation, hardness, thickness, friability, drug content uniformity, Surface pH, in-vitro studies like swelling, mucoadhesive strength and drug release. Formulation (F6) containing Carbopol-934 and Sodium CMC in the ratio of (2: 3) showed good mucoadhesive strength (36.14) and maximum drug release of 98.15% in 8 hrs. Swelling increases with increase in concentration of Sodium CMC in tablets. The drug content of shown highest of 99.15 %, Surface pH was found to be 6.42. All the evaluation parameters given the positive results and comply with the standards. Stability studies were carried out on the developed formulations indicated that the formulations were stable during the study period. The results indicate that the mucoadhesive buccal tablets of Candesartan may be good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability of candesartan through buccal mucosa. Key Words: Mucoadhesive buccal tablets, direct compression, Hypertension, Candesartan cilexetil,

Fentanyl Buccal Tablet vs. Oral Morphine in Doses Proportional to the Basal Opioid Regimen for the Management of Breakthrough Cancer Pain: A Randomized, Crossover, Comparison Study

ContextFentanyl products have shown superiority to oral opioids for the management of breakthrough cancer pain (BTcP). However, these studies did not use appropriate patient selection, and drugs have been compared by using different rationales. ObjectivesThe aim of this randomized, crossover, controlled study was to compare efficacy and safety of fentanyl buccal tablets (FBTs) and oral morphine (OM), given in doses proportional to opioid daily doses. MethodsCancer patients with pain receiving ≥60 mg or more of oral morphine equivalents per day and presenting with ≤3 episodes of BTcP per day were included. In a randomized, crossover manner, patients received FBT or OM at doses proportional to the daily opioid regimen in four consecutive episodes of BTcP. Pain intensity was measured before (T0) and 15 (T15) and 30 minutes (T30), after study drugs. ResultsIn total, 263 episodes of BTcP were treated. A statistical difference in changes in pain intensity—decrease of ≥33% and ≥50%—between the two groups was observed at T15 and T30 (P < 0.0005). No severe adverse effects after study drug administration were observed. ConclusionWhen used in doses proportional to the basal opioid regimen, FBT showed a clear superiority and was well tolerated when compared with OM during the first 30 minutes, which is the approximate target for a timely intervention required for a BTcP medication.

Evaluation of a Novel, Natural Locust Bean Gum as a Sustained Release and Mucoadhesive Component of Tizanidine Hcl Buccal Tablets

Evaluation of a Novel, Natural Locust Bean Gum as a Sustained Release and Mucoadhesive Component of Tizanidine Hcl Buccal Tablets

New Easily Swallowed Tablets with Slippery Coating for the Antihypertensive Drug Valsartan

Different tablet dosage forms were prepared to be administered for patients with dysphagia (swallowing difficulties) like buccal, sublingual and orodispersible tablets, however, they possesses certain constrains like taste masking difficulties, limitations in drug and dose selection and friability. Hence, in an attempt to overcome these constrains, a new easily swallowed immediate release tablets containing (160mg) Valsartan were prepared, and designed to be slippery upon contact with saliva giving an easy swallowing of the intact tablet (without water) with efficient taste masking effect, thus, they called Oroslippery tablets (OSTs). Core tablets were prepared by direct compression using different superdisintegrants, followed by dipping in special coating dispersion containing different proportion of kollicoat IR (film former) and xanthan gum (slipperiness inducer) at different coating levels. These OSTs were optimized for their physical properties, in-vitro disintegration and release in addition to in-vivo slipperiness and taste masking effect. It was found that F12 containing 6% crosscarmellose sodium double coated with 15% kollicoat IR and 0.3% xanthan gum possessed a good mechanical strength (hardness=5.69±0.58 Kg/cm2, friability=0.09%±0.79), suitable in-vivo slipperiness and taste masking times (8±1.45 and 58±2.18 seconds) respectively, with longer disintegration time (5.57±1.36 minutes) but similar release profile to the commercial conventional tablet Diovan® with similarity factor (f2= 68.4±1.07) and difference factor (f1= 1.39± 0.95). Therefore, this study developed a new easily swallowed tablet with an efficient taste masking property, high loading capacity and adequate mechanical strength that can be used as an alternative to buccal, sublingual and orodispersible tablets.

Enhanced Permeation of an Antiemetic Drug from Buccoadhesive Tablets by Using Bile Salts as Permeation Enhancers: Formulation Characterization, In Vitro, and Ex Vivo Studies.

Buccal bioadhesive bilayer tablets of prochlorperazine maleate were designed and formulated by using buccoadhesive polymers such as hydroxypropylmethyl cellulose, Carbopol 934P, and sodium alginate. Physicochemical characteristics like the uniformity of weight, hardness, thickness, surface pH, drug content, swelling index, microenvironment pH, in vitro drug release, and in vivo buccoadhesion time of the prepared tablets were found to be dependent on the type and composition of the buccoadhesive materials used. The effect of bile salts on the permeation was studied through porcine buccal mucosa and it was found that out of three bile salts incorporated (sodium glycholate, sodium taurocholate, and sodium deoxycholate), sodium glycholate enhanced the permeation rate of prochlorperazine maleate by an enhancement factor of 1.37.

Pictorial prescribing reduces fentanyl drug administration errors: a simulated controlled study

ObjectivesTransmucosal fentanyl is used to treat transient exacerbations of cancer pain. Several immediate release products are available, presented as intranasal sprays, sublingual and buccal tablets, or lozenges. These are not...

A review on fast dissolving tablet

These tablets are distinguished from conventional sublingual tablets, lozenges, and buccal tablets which require more than a minute to dissolve in the mouth. In the literature, ODTs also are called orally disintegrating, orodisperse, mouth-dissolving, quick-dissolve, fast-melt, and rapid-disintegrating tablets. Over the past three decades, orally disintegrating tablets (ODTs) have gained much attention as a preferred alternative to conventional oral dosage forms such as tablets and capsules. An ODT is a solid dosage form that disintegrates and dissolves in the mouth (either on or beneath the tongue or in the buccal cavity) without water within 60 seconds or less. The desire of improved palatability in orally administered products has prompted the development of numerous formulations with improved performance and acceptability, and the field has become a rapidly growing area in the pharmaceutical industry. The unique property of mouth dissolving tablet is that they are rapidly disintegrating and/or dissolving and release the drug as soon as they come in contact with saliva, thus obviate the requirement of water during administration. This article reviews the earlier applications and methodologies of taste masking and also emphasize on the recent developments and approaches of bitterness reduction for orally used pharmaceuticals. Apart from the conventional methods of fabrication, this review also provides the detailed concept of some unique patents; technologies developed and marketed formulations of Mouth Dissolving Tablets (MDTs).

Fentanyl Buccal Tablet: A New Breakthrough Pain Medication in Early Management of Severe Vaso-Occlusive Crisis in Sickle Cell Disease.

Sickle cell disease (SCD) is a worldwide distributed hereditary red cell disorder. The principal clinical manifestations of SCD are the chronic hemolytic anemia and the acute vaso-occlusive crisis (VOCs), which are mainly characterized by ischemic/reperfusion tissue injury. Pain is the main symptom of VOCs, and its management is still a challenge for hematologists, requiring a multidisciplinary approach. We carried out a crossover study on adult SCD patients, who received two different types of multimodal analgesia during two separate severe VOCs with time interval between VOCs of at least 6months. The first VOC episode was treated with ketorolac (0.86mg/kg/day) and tramadol (7.2mg/kg/day) (TK treatment). In the second VOC episode, fentanyl buccal tablet (FBT; 100μg) was introduced in a single dose after three hours from the beginning of TK analgesia (TKF treatment). We focused on the first 24hours of acute pain management. The primary efficacy measure was the time-weighted-sum of pain intensity differences (SPID24). The secondary efficacy measures included the pain intensity difference (PID), the total pain relief (TOTPAR), and the time-wighted sum of anxiety (SAID24). SPID24 was significantly higher in TKF than in TK treatment. All the secondary measures were significantly ameliorated in TKF compared to TK treatment, without major opioid side effects. Patients satisfaction was higher with TKF treatment than with TK one. We propose that VOCs might require breakthrough pain drug strategy as vaso-occlusive phenomena and enhanced vasoconstriction promoting acute ischemic pain component exacerbate the continuous pain of VOCs. FBT might be a powerful and feasible tool in early management of acute pain during VOCs in emergency departments.

Manejo de opioides para el dolor basal e irruptivo oncológico

Cancer-related pain is experienced by 90% of patients with cancer. The mainstays of treatment are opioids and the World Health Organization's analgesic ladder. Breakthrough cancer pain (BCP) is a form of cancer-related pain that is particularly difficult to manage with classical opioids. In this review, we discuss titration and opioid rotation in both background and breakthrough pain. We also review the contribution of fast-acting fentanyl preparations for the treatment of BCP and its indications and dose titration. The first drugs developed specifically for the treatment of BCP were oral transmucosal fentanyl citrate (CFOT) and fentanyl buccal tablets. Because oral fentanyl administration is not an option in many cancer patients, the development of a fentanyl nasal spray (FNS) has emerged as a more effective method of administration.

Gasto económico del tratamiento del dolor irruptivo

This article presents two pharmacoeconomic studies comparing the compressedfentanyl lozengewith an integral oromucosalapplicator (Actiq®); fentanyl sublingual tablets(Abstral®); effervescent fentanyl buccal tablets(Effentora®) and nasal fentanyl with two technologies: a formulation that contains pectin in a gel-based nasal spray (PecFent®) and another formulation in an aqueous solution without pectin (Instanyl®). The first of these studies aimed to analyze the potential savings due to the progressive introduction of fentanyl pectin nasal spray for the treatment of adult patients with breakthrough cancer pain. The second study aimed to determine the effectiveness and efficiency of fentanyl pectin nasal spray compared with the other tansmucosal treatments currently on the market. The first study showed a reduction in healthcare costs with the progressive introduction of fentanyl pectin nasal spray for the treatment of breakthrough pain in the publicly-funded health system in Spain. The second study showed that the most efficient option (greatest effectiveness and lowest cost) in all the cases analyzed was the fentanyl-pectin nasal spray.

Formulation and Evaluation of Mucoadhesive Buccal Tablets of Repaglinide

Objective: Delivery of the desired drug as mucoadhesive drug delivery systems has been subject of interest since 1980s. The various advantages associated with these systems made the buccal drug delivery as a novel route of drug administration. Buccal region offers an attractive route for the administration of systemic drug delivery. The objective of the study was to develop mucoadhesive buccal tablets of repaglinide. Methodology: The tablets were prepared by wet granulation method using a combination of mucoadhesive polymers like chitosan, hydroxyethyl cellulose, guar gum and carbopol 934P in different ratios. Results: Buccal tablets were evaluated by different methods for parameters such as thickness, hardness, weight uniformity, drug content uniformity, surface pH, ex vivo mucoadhesive strength, ex vivo residence time, in vitro drug release, ex vivo drug permeation. The tablets were evaluated for in vitro release in phosphate buffer of pH 6.8 for 12 h. In order to determine the mode of release, the data was subjected to zero order, first order, Higuchi and Korsmeyer-Peppas model. The mucoadhesive strength was evaluated by measuring the force required to detach the tablets from sheep buccal mucosal membrane. Carbopol 934P showed maximum mucoadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. DSC and XRD study of the pure drug indicated that the drug is in the crystalline form. But in the formulations, peaks indicated that the drug is in the amorphous form. FTIR spectroscopic studies indicated that there is no drug-excipient interaction. Conclusion: The prepared formulations showed good mucoadhesive strength and ability to sustain the drug release over 12 h; hence, these are the versatile drug delivery systems for repaglinide.

Effect of Sodium Taurocholate on Omeprazole Buccal Adhesive Tablet: Physicochemical Characterization and Pharmacokinetics in Hamster

To formulate an omeprazole buccal adhesive tablet with improved bioavailability using sodium taurocholate, omeprazole buccal adhesive tablets were prepared with sodium alginate, HPMC, magnesium oxide and different quantities of sodium taurocholate. Their physicochemical properties, such as the mucoadhesive force, stability in human saliva and release, were examined. Moreover, the absolute bioavailability was assessed by comparing the buccal administration to an omeprazole solution given intravenously to hamsters. Sodium taurocholate barely influenced the mucoadhesive force of the tablets; however, it affected the drug stability in human saliva. It positively influenced the fast drug release, but did not affect the release mechanism. In particular, omeprazole buccal adhesive tablets [omeprazole/ sodium alginate/HPMC/magnesium oxide/sodium taurocholate (20/24/6/50/10 mg/tab)] showed an absolute bioavailability of about 30% in hamsters. They remained attached to the cheeks without disintegration. Moreover, they were stable in human saliva for at least 4 h. Thus, it was concluded that this omeprazole buccal adhesive tablet could be a useful possible commercial pharmaceutical product. Keywords: Absolute bioavailability, enhancer, mucoadhesive force, omeprazole buccal adhesive tablet, sodium taurocholate, stability in human saliva.

Fentanyl buccal tablet versus oral oxycodone for Emergency Department treatment of musculoskeletal pain

Background:Emergency Department (ED) analgesia can potentially be delivered quickly using transbuccal administration. A previous study identified time-of-onset advantage of a 100 mcg fentanyl buccal tablet (FBT) as compared to a dose of 5 mg oxycodone with 325 mg acetaminophen. The current study reports comparison of higher-dose (200 mcg) FBT as compared to a more commonly used oxycodone dose of 10 mg with 650 mg acetaminophen.Methods:Time frame: Patients were enrolled between October 2012 and October 2014.Setting: The study was conducted in an urban teaching ED with annual census of 55,000.Patients: The 50 convenience-sampled cases met eligibility criteria of age 18-60, with isolated orthopedic complaints; subjects required X-ray to rule-out fracture, and to have pain sufficient to warrant opioids.Interventions: In this double-blind placebo-controlled analgesia trial, patients were randomized to one of two study groups. OXY subjects received two orally ingested tablets, each containing 5 mg oxycodone and 325 mg acetaminophen, and a transbuccal inactive comparator. FBT subjects received two placebo oral tablets and a 200 mcg FBT.Data:The main study endpoint was achievement of at least two points' reduction in numeric pain rating scale (NPRS) within ten minutes of study drug administration. NPRS was assessed at the time of study entry and every five minutes' post-drug administration for an hour. Secondary endpoints included assessment of side effects and subjects' desire to have the same medication for future similar pain.Analysis: Categorical data were assessed with binomial exact 95% confidence intervals (CIs). Continuous data, after being demonstrated as non-normal with skewness-kurtosis testing, were analyzed with Kruskal-Wallis testing. Multivariate Cox proportional hazards analysis was performed to assess whether, after adjustment for potential confounders, there was a difference between FBT and OXY groups with respect to time to achieving significant analgesia.Results:Study groups were similar with respect to age (medians: OXY 34, FBT 38, p = 0.47), initial pain score (median 8 in each group), sex (proportion of males: OXY 64%, FBT 48%, p = 0.25), and ethnicity (proportion of whites: OXY 68%, FBT 56%, p = 0.38). The same proportion (52%) of OXY and FBT cases achieved significant reduction in pain within 15 minutes. Multivariate Cox regression adjusting for potential confounders confirmed (p = 0.28) no difference in rates of pain reduction between OXY and FBT. There were no major complications in either group. The majority of subjects in each group (80% in FBT group versus 76% in OXY group, p = 0.73) expressed high satisfaction and preference to receive the same regimen in future.Conclusion:This study's results suggest approximate equivalence between 200 mcg FBT and 10 mg oxycodone with 650 mg acetaminophen, with respect to time-to-analgesia, analgesic efficacy, side effects, and patient satisfaction.

Layered nanoemulsions as mucoadhesive buccal systems for controlled delivery of oral cancer therapeutics.

Oral cavity and oropharyngeal cancers are considered the eighth most common cancer worldwide, with relatively poor prognosis (62% of patients surviving 5 years, after diagnosis). The aim of this study was to develop a proof-of-concept mucoadhesive lozenge/buccal tablet, as a potential platform for direct sustained delivery of therapeutic antimitotic nanomedicines. Our system would serve as an adjuvant therapy for oral cancer patients undergoing full-scale diagnostic and operative treatment plans. We utilized lipid-based nanocarriers, namely nanoemulsions (NEs), containing mixed-polyethoxylated emulsifiers and a tocopheryl moiety–enriched oil phase. Prototype NEs, loaded with the proapoptotic lipophilic drug genistein (Gen), were further processed into buccal tablet formulations. The chitosan polyelectrolyte solution overcoat rendered NE droplets cationic, by acting as a mucoadhesive interfacial NE layer. With approximate size of 110 nm, the positively charged chitosan-layered NE (+25 mV) vs negatively charged chitosan-free/primary aqueous NE (−28 mV) exhibited a controlled-release profile and effective mucoadhesion for liquid oral spray prototypes. When punch-pressed, porous NE-based buccal tablets were physically evaluated for hardness, friability, and swelling in addition to ex vivo tissue mucoadhesion force and retention time measurements. Chitosan-containing NE tablets were found equivalent to primary NE and placebo tablets in compression tests, yet significantly superior in all ex vivo adhesion and in vitro release assays (P≤0.05). Following biocompatibility screening of prototype chitosan-layered NEs, substantial anticancer activity of selected cationic Gen-loaded NE formulations, against two oropahryngeal carcinomas, was observed. The data strongly indicate the potential of such nanomucoadhesive systems as maintenance therapy for oral cancer patients awaiting surgical removal, or postresection of identified cancerous lesions.

Micelle-enhanced spectrofluorimetric determination of amlexanox in bioadhesive buccal tablets: application to content uniformity testing.

A highly sensitive, simple and rapid spectrofluorimetric method was developed for the determination of Amlexanox (AMX) in its bioadhesive buccal tablets. The proposed method is based on measuring the native fluorescence of the methanolic solution of AMX at 400 nm after excitation at 242 nm in 0.2 M borate buffer (pH 10) and 0.5% w/v sodium dodecyl sulfate (SDS) solution. The interaction of AMX with SDS was studied, and the enhanced fluorescence intensity was exploited to develop an assay method for the determination of AMX. The relative fluorescence intensity-concentration plot was rectilinear over the range 5.0-80.0 ng/mL, with a lower detection limit of 0.57 ng/mL and a lower quantification limit of 1.74 ng/mL. The proposed method was successfully applied to the analysis of AMX in its commercial tablets. Moreover, content uniformity testing was conducted by applying official USP guidelines. Statistical evaluation and comparison of the data obtained using the proposed and comparison methods revealed good accuracy and precision for the proposed method.