scholarly journals Formulation Development of Mouth Dissolving Film of Etoricoxib for Pain Management

2015 ◽  
Vol 2015 ◽  
pp. 1-11 ◽  
Author(s):  
K. Senthilkumar ◽  
C. Vijaya
Keyword(s):  
Pain Management ◽  
Immediate Release ◽  
Rapid Onset ◽  
Ease Of Use ◽  
Taste Masking ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Onset Of Action

Etoricoxib is a potent, orally active, and highly selective COX-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. The present research was undertaken to develop mouth dissolving films of etoricoxib to have rapid onset of action. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use, and the consequent patient compliance. Solubility enhancement and taste masking of etoricoxib were the two challenges solved by formulating drug-inclusion complex with beta-cyclodextrin (BCD). MDF prepared by solvent casting etoricoxib-BCD complex along with HPMC as film forming polymer was found to possess desirable physicomechanical properties. In vitro release of etoricoxib from MDF in simulated salivary fluid and 0.1 N HCl was more than 95% within 2 minutes. Taste masking and in vivo disintegration were in acceptable range as assessed by human volunteers. Etoricoxib MDF was further characterized by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy. The index of analgesia shown by etoricoxib MDF was comparable to that of immediate release tablets (100% activity within 40 minutes) in animal studies. Conclusively, the present study documents the development of a commercially viable formula for an MDF of etoricoxib with rapidity in pain management.

scholarly journals Formulation Development of Mucoadhesive Microparticle-Laden Gels for Oral Mucositis: An In Vitro and In Vivo Study

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 603
Author(s):  
Hiroomi Sakurai ◽  
Yuri Ikeuchi-Takahashi ◽  
Ayaka Kobayashi ◽  
Nobuyoshi Yoshimura ◽  
Chizuko Ishihara ◽  
...  
Keyword(s):  
Oral Mucosa ◽  
Oral Mucositis ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
In Vivo Experiments ◽  
Drug Retention ◽  
Drug Concentrations ◽  
Diffraction Patterns

In order to relieve pain due to oral mucositis, we attempted to develop mucoadhesive microparticles containing indomethacin (IM) and gel preparations with IM microparticles that can be applied to the oral cavity. The mucoadhesive microparticles were prepared with a simple composition consisting of IM and polyvinyl alcohol (PVA). Two kinds of PVA with different block properties were used, and microparticles were prepared by heating-filtration and mixing-drying. From the X-ray powder diffraction patterns, differential scanning calorimetry thermograms, and morphological features of the IM microparticles, IM should exist as polymorphic forms in the microparticles. Rapid drug release properties were observed in the IM microparticles. Increased drug retention was observed in IM microparticles containing PVA, and the IM-NK(50) gel, using a common block character PVA and heating-filtration, showed good long-term drug retention properties. In vivo experiments showing significantly higher drug concentrations in the oral mucosa were observed with IM microparticles prepared by heating-filtration, and the IM-NK(50) gel maintained significantly higher drug concentrations in the oral mucosa. From these results, the IM-NK(50) gel may be useful as a preparation for relieving oral mucositis pain.

An Evaluation of Andursil – A New Antacid

1977 ◽  
Vol 5 (6) ◽  
pp. 99-104 ◽  
Author(s):  
G Beaumont ◽  
G I J Rigby ◽  
J Seldrup
Keyword(s):  
General Practitioner ◽  
Rapid Onset ◽  
Onset Of Action ◽  
Duration Of Effect ◽  
The Ideal

A number of characteristics of an ideal antacid are proposed. A new antacid formulation, Andursil, has been assessed both by in vitro and in vivo methods. Andursil has been found to compare favourably in its properties, with the profile of the ideal antacid. In a multicentre general practitioner trial it was found to be effective in relieving the symptoms of dyspepsia, to have a rapid onset of action and a satisfactory duration of effect, to be palatable and to be relatively free from undesirable effects.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISSOLVING FILMS OF EBASTINE

2020 ◽  
pp. 111-115
Author(s):  
TEJASVI TORGAL ◽  
SHWETA BORKAR ◽  
PRASHANT BHIDE ◽  
ASMITA ARONDEKAR
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Rapid Onset ◽  
Content Uniformity ◽  
Formulation Development ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
In Vitro Drug Release ◽  
First Order Kinetics ◽  
Percentage Release

Objective: To overcome the limitations of fast dissolving tablets, a novel fast dissolving film of ebastine was formulated for attaining quick onset of action, aiding in the enhancement of bioavailability favorable in severe conditions of allergies. Methods: Films of ebastine were prepared by the solvent casting method using hydroxypropyl methylcellulose E-15, hydroxypropyl methylcellulose K-4 as a film base with different concentrations of crospovidone as superdisintegrant and polyethylene glycol-400 as a plasticizer. Further physical characteristics such as uniformity of weight, thickness, and drug content uniformity, tensile strength, folding endurance, percentage elongation, surface pH, disintegration and in vitro drug release were evaluated. Results: The optimized formulations with film base hydroxypropyl methylcellulose E-15 and hydroxypropyl methylcellulose K-4 containing 8% crospovidone showed 99.34 % and 97.42 % of maximum cumulative percentage release respectively exhibiting first order kinetics. However, no significant change was observed in stability studies. Conclusion: The concept of formulating fast dissolving films of ebastine offers a suitable approach in exhibiting rapid onset of action with improved delivery.

scholarly journals Deimmunized Lysostaphin Synergizes with Small-molecule Chemotherapies and Re-sensitizes MRSA to β-Lactam Antibiotics

2020 ◽  
pp. AAC.01707-20
Author(s):  
Yongliang Fang ◽  
Jack R. Kirsch ◽  
Liang Li ◽  
Seth A. Brooks ◽  
Spencer Heim ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Standard Of Care ◽  
Rapid Onset ◽  
Multidrug Resistant ◽  
Genetically Engineered ◽  
High Potency ◽  
Onset Of Action ◽  
New Antibiotics

There is an urgent need for novel agents to treat drug-resistant bacterial infections, such as multidrug-resistant Staphylococcus aureus (MRSA). Desirable properties for new antibiotics include high potency, narrow species selectivity, low propensity to elicit new resistance phenotypes, and synergy with standard of care (SOC) chemotherapies. Here, we describe analysis of the anti-MRSA potential exhibited by F12, an innovative anti-MRSA lysin that has been genetically engineered to evade detrimental antidrug immune responses in human patients. F12 possesses high potency and rapid onset of action, it has narrow selectivity against pathogenic Staphylococci, and it manifests synergy with numerous SOC antibiotics. Additionally, resistance to F12 and β-lactam antibiotics appears mutually exclusive, and importantly we provide evidence that F12 re-sensitizes normally resistant MRSA strains to β-lactams both in vitro and in vivo. These results suggest that combinations of F12 and SOC antibiotics could be a promising new approach to treating refractory S. aureus infections.

scholarly journals In Vitro Dissolution and in Silico Modeling Shortcuts in Bioequivalence Testing

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 45 ◽  
Author(s):  
Moawia M. Al-Tabakha ◽  
Muaed J. Alomar
Keyword(s):  
Computer Simulation ◽  
In Silico ◽  
Immediate Release ◽  
Pbpk Modeling ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Drug Formulations ◽  
Drug Modeling

Purpose: To review in vitro testing and simulation platforms that are in current use to predict in vivo performances of generic products as well as other situations to provide evidence for biowaiver and support drug formulations development. Methods: Pubmed and Google Scholar databases were used to review published literature over the past 10 years. The terms used were “simulation AND bioequivalence” and “modeling AND bioequivalence” in the title field of databases, followed by screening, and then reviewing. Results: A total of 22 research papers were reviewed. Computer simulation using software such as GastroPlus™, PK-Sim® and SimCyp® find applications in drug modeling. Considering the wide use of optimization for in silico predictions to fit observed data, a careful review of publications is required to validate the reliability of these platforms. For immediate release (IR) drug products belonging to the Biopharmaceutics Classification System (BCS) classes I and III, difference factor (ƒ1) and similarity factor (ƒ2) are calculated from the in vitro dissolution data of drug formulations to support biowaiver; however, this method can be more discriminatory and may not be useful for all dissolution profiles. Conclusions: Computer simulation platforms need to improve their mechanistic physiologically based pharmacokinetic (PBPK) modeling, and if prospectively validated within a small percentage of error from the observed clinical data, they can be valuable tools in bioequivalence (BE) testing and formulation development.

scholarly journals SOLUBILITY ENHANCEMENT OF GLIBENCLAMIDE USING MESOPOROUS SILICA

2019 ◽  
pp. 302-314
Author(s):  
Swati Mittal ◽  
AKSHAY SONAWANE ◽  
MANGESH KHUNE
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Drug Loading ◽  
Immediate Release ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Precipitation ◽  
Poorly Soluble

Glibenclamide is a BCS Class II drug and poses a major problem during formulation development. In the present study, adsorption onto various carriers was used to enhance the solubility of glibenclamide. It was observed that solubility of glibenclamide was greatly enhanced by adsorbing onto mesoporous silica. The increase in solubility of poorly soluble drugs is often associated with the generation of supersaturation, which results in the risk of drug precipitation. HPMC E5 was used as precipitation inhibitor to maintain sink condition for a longer duration. A 32 full factorial design was adopted to optimize the ratio of glibenclamide (X1) and mesoporous silica as a carrier (X2) and the effect of different ratios was studied on percent yield, percent drug loading, and percent drug release. X-ray powder diffraction (XRPD) and Differential scanning calorimetry studies were performed to investigate any possible interaction in between glibenclamide and mesoporous silica. An optimum batch of drug adsorbate was used to prepare immediate-release tablets. The tablets prepared were evaluated for thickness, uniformity of weight, hardness, friability, in-vitro disintegration time, and in vitro drug release study.

scholarly journals Segmental-Dependent Solubility and Permeability as Key Factors Guiding Controlled Release Drug Product Development

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 295 ◽  
Author(s):  
Milica Markovic ◽  
Moran Zur ◽  
Noa Fine-Shamir ◽  
Ester Haimov ◽  
Isabel González-Álvarez ◽  
...  
Keyword(s):  
Controlled Release ◽  
Product Development ◽  
Drug Product ◽  
Immediate Release ◽  
Class Ii ◽  
Distribution Coefficients ◽  
Analysis Model ◽  
Formulation Development

The main factors influencing the absorption of orally administered drugs are solubility and permeability, which are location-dependent and may vary along the gastrointestinal tract (GIT). The purpose of this work was to investigate segmental-dependent intestinal absorption and its role in controlled-release (CR) drug product development. The solubility/dissolution and permeability of carvedilol (vs. metoprolol) were thoroughly studied, in vitro/in vivo (Octanol-buffer distribution coefficients (Log D), parallel artificial membrane permeability assay (PAMPA), rat intestinal perfusion), focusing on location-dependent effects. Carvedilol exhibits changing solubility in different conditions throughout the GIT, attributable to its zwitterionic nature. A biorelevant pH-dilution dissolution study for carvedilol immediate release (IR) vs. CR scenario elucidates that while the IR dose (25 mg) may dissolve in the GIT luminal conditions, higher doses used in CR products would precipitate if administered at once, highlighting the advantage of CR from the solubility/dissolution point of view. Likewise, segmental-dependent permeability was evident, with higher permeability of carvedilol vs. the low/high Peff marker metoprolol throughout the GIT, confirming it as a biopharmaceutical classification system (BCS) class II drug. Theoretical analysis of relevant physicochemical properties confirmed these results as well. A CR product may shift the carvedilol’s solubility behavior from class II to I since only a small dose portion needs to be solubilized at a given time point. The permeability of carvedilol surpasses the threshold of metoprolol jejunal permeability throughout the entire GIT, including the colon, establishing it as a suitable candidate for CR product development. Altogether, this work may serve as an analysis model in the decision process of CR formulation development and may increase our biopharmaceutical understanding of a successful CR drug product.

scholarly journals DESIGN AND FORMULATION DEVELOPMENT OF FAST-DISSOLVING TABLETS OF IBUPROFEN USING NOVEL NATURAL SUPERDISINTEGRANT

2019 ◽  
pp. 34-41
Author(s):  
CHANDRA SEKHAR NAIK D ◽  
BHARATHI A ◽  
BASAVESWARA RAO MV
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
The Fourier Transform ◽  
Dissolution Efficiency

Objective: The objective of the study was to evaluate Ocimum gratissimum mucilage as a novel superdisintegrant in the formulation of fast-dissolving tablets (FDT) of Biopharmaceutical Classification System-II drug (Ibuprofen) employing a 23 factorial design. Methods: O. gratissimum mucilage was extracted by seeds and it was subjected to physical, chemical, and micrometric studies were evaluated. To establish FDT of ibuprofen with O. gratissimum mucilage as a superdisintegrants in different ratios using direct compression method employing 23 factorial design. All the formulation tablets were evaluated pre-compression and post-compression parameters like dissolution efficiency (DE%) percent of drug dissolved at 5 min. Results: The mucilage was to be found fine, free-flowing crystalline powder, and excellent swelling nature in all suitable solvents and buffers. The Fourier transform infrared and differential scanning calorimetry studies were indicated to no interactions between ibuprofen and O. gratissimum mucilage. All the FDT formulated employing novel mucilage shows good quality with regard drug content (98.05±0.31–99.39±0.54), hardness (3.6– 4 kg/sq. cm), and friability (0.12–0.15%). The optimized formulation batch shows less disintegrant time (30±0.06). In vitro wetting time was less (i.e., 90 s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of 99±0.56. The cumulative drug dissolved in the optimized formulation F2 was found to be 99% in 10 min. Conclusion: O. gratissimum mucilage was found to be a novel superdisintegrant which enhanced the DE when combined with crospovidone and croscarmellose sodium; hence, it could be used in the formulation of FDT to provide immediate release of the contained drug within 5 min.

Morphological effects and tegumental alterations induced by mefloquine on schistosomula and adult flukes ofSchistosoma mansoni

Parasitology ◽  
2009 ◽  
Vol 137 (1) ◽  
pp. 85-98 ◽  
Author(s):  
T. MANNECK ◽  
Y. HAGGENMÜLLER ◽  
J. KEISER
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Rapid Onset ◽  
Current Treatment ◽  
Current Evidence ◽  
Onset Of Action ◽  
Tegumental Surface ◽  
Scanning Electron

SUMMARYThere is a pressing need to develop novel anti-schistosomal drugs, as current treatment relies largely on praziquantel (PZQ). To further strengthen current evidence of the anti-schistosomal properties of mefloquine (MQ), we studied the temporal effect of this compoundin vitroandin vivo, and examined alterations on the tegumental surface of schistosomula and adults ofS. mansoniby means of scanning electron microscopy (SEM). Schistosomula and adults were each incubatedin vitrousing MQ over a wide concentration range (1–100 μg/ml). In addition, mice infected with adultS. mansoniwere treated with a single oral dose of 400 mg/kg MQ, and worms were recovered 24, 48, 72, 96 and 120 h following treatment. MQ showed a rapid onset of action on schistosomulain vitro; 100 and 75 μg/ml of MQ killed schistosomula immediately; the minimal lethal and effective concentrations of MQ on schistosomula after 1 h were 25 and 5 μg/ml, respectively. Adult worms incubated with 100 and 10 μg/ml of MQ were dead after 1 h and 24 h of incubation, respectively. A hepatic shift of adult schistosomes was observed in mice already 24 h after treatment, and 120 h following treatment >98% of all worms had translocated to the liver. SEM observations revealed extensive tegumental destruction, including blebbing, shrinking and sloughing, particularly followingin vitroincubation and on the tegument of female worms.

Tobramycin Collagen Fast Dissolving Ocular Films for Corneal Tissue Engineering of Keratoconus

2019 ◽  
Vol 9 (6) ◽  
pp. 804-809
Author(s):  
Jing Qin ◽  
Ni Yin
Keyword(s):  
Pharmaceutical Research ◽  
Immediate Release ◽  
Ease Of Use ◽  
Corneal Tissue ◽  
Disintegration Time ◽  
Weight Variation ◽  
Orally Disintegrating Tablets ◽  
Drug Polymer Interaction

Fast dissolving films are a one of novel dosage form in pharmaceutical research. They have convenience and ease of use over other dosage forms such as orally disintegrating tablets and immediate release tablets. In the present research, rapidly dissolving films of Tobramycin were developed using Polyvinyl acetate (PVA) and polyvinyl pyrollidone (PVP) as film forming polymers by solvent casting method. The prepared films were evaluated for drug content, weight variation, thickness and in vitro in vivo disintegration time. The in vitroand in vivodissolving time of the optimized formulation was found to be below 15–40 seconds respectively. The prepared films exhibited good integrity and thickness. In vitro dissolution studies were performed as per the FDA dissolution guidelines for about 3 minutes, the optimum formulation released complete drug within 3 minutes. Statistical analysis showed no drug polymer interaction.

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