FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILMS OF PROCHLORPERAZINE MALEATE

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (12) ◽  
pp. 23-33
Author(s):  
R. Kanekar ◽  
◽  
P. M. Dandagi ◽  
A. P. Gadad
Keyword(s):  
Ex Vivo ◽  
Rapid Onset ◽  
Drug Release Profile ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Physico Chemical ◽  
Film Forming ◽  
Oral Films ◽  
Ex Vivo Study

The objective of the present study was to prepare and evaluate fast-dissolving oral films of prochlorperazine maleate (PCM), in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The solubility of the drug was increased by preparing inclusion complex with 2-hydroxypropyl-β-cyclodextrin (2HPβCD) and then incorporating it into the fast dissolving films. The fast-dissolving films of PCM were prepared by solvent casting method using different film forming polymers such as HPMC E15 and HPMC E5, either as single polymer or combination of the two. The film formulations were evaluated for various physico-chemical parameters. All formulations released more than 85% of the drug within 15 minutes. Formulation F4 showed best in vitro drug release profile. From the ex vivo study it was found that 94.79% of drug permeated through the porcine oral mucosa from the optimized formulation F4 within 60 mins.

scholarly journals Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1883
Author(s):  
Patrícia Varga ◽  
Rita Ambrus ◽  
Piroska Szabó-Révész ◽  
Dávid Kókai ◽  
Katalin Burián ◽  
...  
Keyword(s):  
Spray Drying ◽  
Ex Vivo ◽  
Average Particle Size ◽  
Rapid Onset ◽  
Average Particle ◽  
Nasal Drug Delivery ◽  
Onset Of Action ◽  
Physico Chemical

Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The application of mucoadhesive polymers can increase the contact time with the nasal mucosa, and permeation enhancers can enhance the absorption of the drug. We aimed to produce nanoparticles containing meloxicam potassium (MEL-P) by spray drying intended for nasal application. Various cyclodextrins (hydroxypropyl-β-cyclodextrin, α-cyclodextrin) and biocompatible polymers (hyaluronic acid, poly(vinylalcohol)) were used as excipients to increase the permeation of the drug and to prepare mucoadhesive products. Physico-chemical, in vitro and ex vivo biopharmaceutical characterization of the formulations were performed. As a result of spray drying, mucoadhesive nanospheres (average particle size <1 µm) were prepared which contained amorphous MEL-P. Cyclodextrin-MEL-P complexes were formed and the applied excipients increased the in vitro and ex vivo permeability of MEL-P. The highest amount of MEL-P permeated from the α-cyclodextrin-based poly(vinylalcohol)-containing samples in vitro (209 μg/cm2) and ex vivo (1.47 μg/mm2) as well. After further optimization, the resulting formulations may be promising for eliciting a rapid analgesic effect through the nasal route.

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.

DESIGN DEVELOPMENT AND EVALUATION OF FAST DISSOLVING ORAL FILMS OF RANITIDINE HYDROCHLORIDE

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 27-36
Author(s):  
B.V. Ramana ◽  
◽  
C Triveni ◽  
G Nagarajan ◽  
T.E.G.K. Murthy
Keyword(s):  
Polyvinyl Alcohol ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Design Development ◽  
Drug Release Profile ◽  
Film Forming ◽  
Film Formulation ◽  
Oral Films

The aim of this study was to develop an innovative fast dissolving oral film of Ranitidine HCl based on polymers such as Hydroxy Propyl Methyl Cellulose-E6, Hypromellose-E3 LV, and Polyvinyl alcohol. Trials on various concentrations of polymers were conducted in order to optimize polymer concentration and develop the films with best suitability and acceptability. The various concentrations of super disintegrating agents like Crospovidone, Croscarmellose sodium and Sodium Starch Glycolate were evaluated. The fast dissolving oral films were characterized for weight, thickness, folding endurance, disintegration and dissolution using in vitro experimentations. The effect of super disintegrating agents on drug release profile and film forming properties was investigated. The prepared films exhibited satisfactory physicochemical characteristics. Finally, it is concluded that Ranitidine can be formulated with Hydroxy Propyl Methyl Cellulose-E6, Hypromellose-E3 LV, and Polyvinyl Alcohol polymers to achieve oral film formulation by using solvent casting method.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Design, Optimization and Evaluation of Fast-Dissolving Oral Films of Ropinirole

2018 ◽  
Vol 11 (1) ◽  
pp. 3958-3967
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas A
Keyword(s):  
Parkinson’S Disease ◽  
Parkinson's Disease ◽  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 4000 ◽  
Oral Films

The main objective of this study was to develop fast dissolving oral films of ropinirole HCl to attain quick onset of action for the better management of Parkinson’s disease. Twenty-seven formulations (F1-F27) of ropinirole oral dissolving films by solvent-casting method using 33 response surface method by using HPMC E15, Maltodextrin PEG 4000 by using Design of experiment software. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F4 showed minimum disintegration time 11 sec, maximum drug was released i.e. 99.68 ± 1.52% of drug within 10 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions takes place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 92.77 ± 1.52 after 50 min. Therefore, it can be a good alternative to conventional ropinirole for immediate action. In vitro evaluation of the ropinirole fast dissolving films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of ropinirole. The oral dissolving film is considered to be potentially useful for the treatment of Parkinson’s disease where quick onset of action is desired

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

Aryl Maleimides as Apoptosis Inducers on L5178-Y Murine Leukemia Cells (in silico, in vitro and ex vivo Study)

2016 ◽  
Vol 16 (12) ◽  
pp. 1615-1621 ◽  
Author(s):  
Erik Andrade-Jorge ◽  
Marycarmen Godínez-Victoria ◽  
Luvia Enid Sánchez-Torres ◽  
Luis Humberto Fabila-Castillo ◽  
José G. Trujillo-Ferrara
Keyword(s):  
In Silico ◽  
Ex Vivo ◽  
Leukemia Cells ◽  
Ex Vivo Study ◽  
Murine Leukemia

scholarly journals 64Cu-ATSM/64Cu-Cl2 and their relationship to hypoxia in glioblastoma: a preclinical study

2019 ◽  
Vol 9 (1) ◽  
Author(s):  
Elodie A. Pérès ◽  
Jérôme Toutain ◽  
Louis-Paul Paty ◽  
Didier Divoux ◽  
Méziane Ibazizène ◽  
...  
Keyword(s):  
Ex Vivo ◽  
In Vitro Study ◽  
Tumor Location ◽  
Preclinical Study ◽  
Significant Rise ◽  
Lower Oxygen ◽  
Cu Complexes ◽  
Ex Vivo Study

Abstract Background Diacetyl-bis(N4-methylthiosemicarbazone), labeled with 64Cu (64Cu-ATSM) has been suggested as a promising tracer for imaging hypoxia. However, various controversial studies highlighted potential pitfalls that may disable its use as a selective hypoxic marker. They also highlighted that the results may be tumor location dependent. Here, we first analyzed uptake of Cu-ATSM and its less lipophilic counterpart Cu-Cl2 in the tumor over time in an orthotopic glioblastoma model. An in vitro study was also conducted to investigate the hypoxia-dependent copper uptake in tumor cells. We then further performed a comprehensive ex vivo study to compare 64Cu uptake to hypoxic markers, specific cellular reactions, and also transporter expression. Methods μPET was performed 14 days (18F-FMISO), 15 days (64Cu-ATSM and 64Cu-Cl2), and 16 days (64Cu-ATSM and 64Cu-Cl2) after C6 cell inoculation. Thereafter, the brains were withdrawn for further autoradiography and immunohistochemistry. C6 cells were also grown in hypoxic workstation to analyze cellular uptake of Cu complexes in different oxygen levels. Results In vivo results showed that Cu-ASTM and Cu-Cl2 accumulated in hypoxic areas of the tumors. Cu-ATSM also stained, to a lesser extent, non-hypoxic regions, such as regions of astrogliosis, with high expression of copper transporters and in particular DMT-1 and CTR1, and also characterized by the expression of elevated astrogliosis. In vitro results show that 64Cu-ATSM showed an increase in the uptake only in severe hypoxia at 0.5 and 0.2% of oxygen while for 64Cu-Cl2, the cell retention was significantly increased at 5% and 1% of oxygen with no significant rise at lower oxygen percentages. Conclusion In the present study, we show that Cu-complexes undoubtedly accumulate in hypoxic areas of the tumors. This uptake may be the reflection of a direct dependency to a redox metabolism and also a reflection of hypoxic-induced overexpression of transporters. We also show that Cu-ATSM also stained non-hypoxic regions such as astrogliosis.

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