scholarly journals THE DEVELOPMENT AND CHARACTERISATION OF FAST DISSOLVING FILM OF POORLY WATERSOLUBLE DRUG LURASIDONE HYDROCHLORIDE

2021 ◽  
pp. 170-177
Author(s):  
ANAGHA PRABHU ◽  
ASMITA ARONDEKAR Arondeka ◽  
PRASHANT BHIDE ◽  
SHWETA BORKAR
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Onset Of Action ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Casting Technique ◽  
Drug Content ◽  
In Vitro Disintegration ◽  
Lurasidone Hydrochloride

Objective: The objective of the present work was to formulate and evaluate a fast-dissolving oral film of lurasidone hydrochlorideused as an atypical antipsychotic for the treatment of schizophrenia capable of providing faster onset of action. Methods: The fastdissolving films of lurasidone hydrochloride were prepared by the solvent casting technique using different compositions and combinations of hydroxypropyl methylcellulose E-3, E-5, E-15, and K4M as fast-dissolving polymer bases. A set of seven formulations were prepared and evaluated for parameters like physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance,tensile strength), surface pH, in vitro disintegration time, drug content, and an in vitro drug release. Results: The prepared films exhibited uniform and a smooth surface with uniform weight, thicknessand 89-90% mg drug content. The formulation F7 Showed excellent elasticity and disintegration within seconds. Lurasidone hydrochloride was rapidly released in vitro from all formulations. The release was found to be rapid and maximum of 41.5% in Phosphate buffer pH 6.8 and 58.6% in 0.1 N hydrochloric acid over a period of 30 min. The further optimized formulation F7Adepicted a faster and maximum release of 78% as compared to the marketed tablet 74%. Conclusion: The developed formulation is a better alternative to tablets by its ability to produce good drug release.

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.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF BROMOCRIPTINE MESYLATE AS FAST DISSOLVING ORAL FILM

2018 ◽  
Vol 10 (1) ◽  
pp. 7
Author(s):  
Manar Adnan Tamer ◽  
Shaimaa Nazar Abd-al Hammid ◽  
Balqis Ahmed
Keyword(s):  
Drug Release ◽  
Physical Characterization ◽  
Type Ii ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content ◽  
Folding Endurance ◽  
In Vitro Disintegration

Objective: The aim of this study was to formulate and in vitro evaluate fast dissolving oral film of practically insoluble bromocriptine mesylate to enhance its solubility and to improve its oral bioavailability by avoiding first pass effect as well as to produce an immediate release action of the drug from the film for an efficient management of diabetes mellitus type II in addition to an improvement of the patient compliance to this patient-friendly dosage form.Methods: The films were prepared by the solvent casting method using hydroxypropyl methylcellulose of grades (E3, E5, E15), polyvinyl alcohol (PVA), pectin and gelatin as film-forming polymers in addition to polyethene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer. Poloxamer 407 was used as a surfactant, sodium saccharin as a sweetening agent, citric acid as a saliva stimulating agent, vanilla as a flavouring agent and crospovidone as a super disintegrant. The prepared films then tested for physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance, tensile strength, percent elongation and Young's modulus), surface pH, in vitro disintegration time, drug content and an in vitro drug release.Results: Films were found to be satisfactory when evaluated for physical characterization, thickness, weight uniformity, mechanical tests, in vitro disintegration time, folding endurance, drug content and an in vitro drug release. The surface pH of all the films was found to be neutral or minor change. Films in vitro drug release studies were also done using USP dissolution apparatus type II (paddle type). The in vitro drug release profile in the optimized formulation F14 was gave 86.8 % of drug released at 2 min. The optimized formulation F14 was also showed satisfactory pH (6.2±0.2), drug content (99.2±0.5%), the disintegration time of 9.2±0.1 seconds and the time needed for 80% of medication to be released (T80 %) was 1.35 minute.Conclusion: The bromocriptine mesylate fast dissolving oral film was formulated. The given film disintegrates within nine seconds which release the drug rapidly and gives an action.

scholarly journals FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

2020 ◽  
pp. 34-41
Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
Bioavailability Enhancement ◽  
Disintegration Time ◽  
Peg 400 ◽  
Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

scholarly journals ENHANCEMENT OF SOLUBILITY AND OPTIMIZATION OF ORALLY DISINTEGRATING FILMS OF ACYCLOVIR

2018 ◽  
Vol 11 (9) ◽  
pp. 280 ◽  
Author(s):  
Bikash Pandey ◽  
Arshad Bashir Khan
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antiviral Agent ◽  
Disintegration Time ◽  
Casting Technique ◽  
Accelerated Stability ◽  
Full Factorial

Objective: The objective of this work was to prepare and optimize orally disintegrating films of acyclovir (ACV), which is a known antiviral agent. To enhance the solubility of ACV, solid dispersions of ACV were made.Methods: The films were prepared using a solvent casting technique. Full factorial design was utilized for the optimization of the effect of independent variables such as the amount of hydroxypropyl methylcellulose 5 cps, sodium starch glycolate, and propylene glycol on the disintegration time. Other evaluation tests such as drug release, drug content, thickness, and folding endurance of film were also conducted.Results: Compatibility studies by Fourier transform infrared showed that there was no significant interaction between the drug and excipients used. Disintegration time was found to be 43 s for the optimized batch. The in vitro release profile of formulation response disintegrating time in phosphate buffer pH 6.8 revealed that there was a significant increment in drug release of the optimized batch in comparison to the screening batches. Further, short-term accelerated stability studies carried out for 4 weeks for the optimized formulation which proved that the formulated films were stable at the accelerated conditions of temperature and humidity (40±2°C/75±5% RH).Conclusions: It was concluded that such ACV solid dispersion films could be beneficial in enhancement of dissolution and consequently the oral bioavailability of ACV.

scholarly journals FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

2019 ◽  
pp. 124-129
Author(s):  
Jasvanth E ◽  
Teja D ◽  
Mounika B ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Release Mechanism ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Preparation And Evaluation ◽  
Pvp K30

Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy.

scholarly journals PREPARATION, CHARACTERIZATION AND EVALUATION OF FLOATING MICROPARTICLES OF CIPROFLOXACIN

2016 ◽  
Vol 9 (1) ◽  
pp. 1 ◽  
Author(s):  
Sumit Durgapal ◽  
Sayantan Mukhopadhyay ◽  
Laxmi Goswami
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Evaluation Parameters

Objective: The main purpose of this study is to prepare a floating micro articulated drug delivery system of ciprofloxacin by using non-aqueous solvent evaporation technique to increase the bioavailability and therapeutic effectiveness of the drug by prolonging its gastric residence time.Methods: Floating microparticles were prepared by using different low-density polymers such as ethyl cellulose and hydroxypropyl methylcellulose either alone or in combination with the aid of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as percentage yield, drug content, drug entrapment, rheological studies, floating characteristics and in vitro drug release studies.Results: Drug-excipient compatibility studies performed with the help of FTIR instrument indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique is a suitable technique for the preparation of floating microspheres as most of the formulations were discrete and spherical in shape with a good yield of 65% to 85% and 15 to 22 h of floating duration with 90% of maximum percentage floating capacity shown by formulation FM9. Though, different drug-polymer ratios, as well as a combination of polymers, play a significant role in the variation of overall characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, drug content, drug entrapment, rheological studies and in vitro drug release characteristics formulation FM9 was found to fulfil the criteria of ideal floating drug delivery system.Conclusion: Floating microparticles were successfully prepared, and from this study, it can be concluded that the developed floating microspheres of ciprofloxacin can be used for prolonged drug release in the stomach to improve the bioavailability and patient compliance.

scholarly journals Formulation design, optimization & in vitro evaluation of novel orodissolving tablets of efavirenz for hiv infections

2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Wetting Time

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014

scholarly journals The Effects of Lubricants on the Disintegration and Dissolution Profile of Metronidazole Tablets Formulated Using Sida acuta Gum as a Binder

2021 ◽  
pp. 350-362
Author(s):  
Sinodukoo Eziuzo Okafo ◽  
Avbunudiogba John Afokoghene ◽  
Christian Areruruoghene Alalor ◽  
Deborah Ufuoma Igbinake
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Sodium Lauryl Sulphate ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Sida Acuta ◽  
Drug Content

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder. Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release. Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35% Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.

Effect of Compression Force and Concentration of Superdisintigrant on Directly Compressed Tablets of Metformin HCl

2014 ◽  
Vol 7 (4) ◽  
pp. 2677-2684
Author(s):  
Suryakanta Swain ◽  
Chinam Niranjan Patra ◽  
Kahnu Charan Panigrahi ◽  
Muddana Eswara Bhanoji Rao ◽  
Rashmita Patro
Keyword(s):  
Drug Release ◽  
Diffusion Mechanism ◽  
Compression Force ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Powder Mixtures ◽  
Drug Content ◽  
Croscarmellose Sodium ◽  
Metformin Hcl

The present research work was to evaluate the effect of compression force and concentration of superdisintigrant on tableting properties of metformin HCl. Initially powder mixtures of drug, croscarmellose sodium (0.62% to 10% w/w) and microcrystalline cellulose PH-200 sufficient quantity were prepared and evaluate their pre-compression parameters of different formulation batches such as angle of repose, bulk density, tapped density, Hausner’s ratio and compressibility index. The prepared powder mixtures of different batches were compressed into tablet using hydraulic pellet press machine at two optimized compression forces (77 MPa and 154 MPa). The post compression parameters such as thickness, diameter, weight variation, hardness, friability, drug content, disintegration time and in-vitro drug release study of the prepared tablets were evaluated. FT-IR and DSC studies showed that no incompatibility of the selected drug with the selected excipients. At selected compression force (77 MPa) and increased concentration of superdisintigration (0.62% to 10% w/w) of formulations F1 to F5 indicated that, disintegration time were periodically decreased up to F3 (1.25% w/w croscarmellose sodium). When the concen-tration of superdisintigrant increased up to 10% showed that disintegration time were periodically increased. Similarly, at compression force 154 MPa there is increased in tablet hardness but this effect was less significant when the superdisintegrant concentration more than 1.25% w/w. The hardness and drug content of all the formulations were found to be 3.59 ± 0.23 to 4.85 ± 0.01 kg/cm2 and 97.89 ± 0.10% to 99.42 ± 0.03% respectively. The in-vitro drug release data suggested that drug release of all the formulations followed Higuchi’s kinetic (R> = 0.998). The release rate exponent values (n) suggested the mechanism of drug release followed Quasi-Fickian diffusion mechanism at compression force 77 MPa and anomalous diffusion mechanism at compression force 154 MPa, respectively.

scholarly journals OPTIMIZATION AND EVALUATION OF CHLORPHENIRAMINE MALEATE ORAL STRIP FOR PEDIATRIC USE

2018 ◽  
Vol 11 (12) ◽  
pp. 548 ◽  
Author(s):  
Sura Zuhair Mahmood ◽  
Hiba Sabah Sabry ◽  
Nora Zawar Yousif ◽  
Zeina D Salman
Keyword(s):  
Pediatric Population ◽  
Hydroxypropyl Methylcellulose ◽  
Chlorpheniramine Maleate ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Casting Technique ◽  
Fast Onset ◽  
Pediatric Use

Objective: The goal of performing this study is to prepare an oral strip, especially designed for pediatric use that provides fast onset of action with ease of swallowing particularly for young individuals who suffer from difficulty of swallowing, in addition provides maximum therapeutic effectiveness by reducing the first pass effect.Materials and Methods: The oral strip was prepared by solvent casting technique through using different sole polymers (hydroxypropyl methylcellulose [HPMC] 15cp, HPMC 50cp, polyvinyl alcohol, and sodium carboxymethyl cellulose). Maltodextrin (MD) was added as the secondary polymer in different ratios to optimize the release parameters, and disintegration time (DT), three different plasticizers were employed (propylene glycol, dibutyl phthalate, and glycerin) to boost the film forming polymer characteristics.Results: From this study, it is obvious that F10 which composed of HPMC as a main polymer and MD as a secondary polymer in ratio 2:1, respectively, provides adequate physicochemical characteristics, in vivo/in vitro DT (40/36 s), respectively, nevertheless a satisfactory release parameters as (59.9%) released at 2 min and 80% of drug released at 14.8 min.Conclusion: The optimized formula is pretty encouraging to originate an oral strip that provides ease of administration, fast onset of action with wide acceptance for the pediatric population.

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