scholarly journals Effect of nonionic surfactants on the release of paracetamol from suppositories

2015 ◽  
Vol 26 (1) ◽  
pp. 40-44
Keyword(s):  
Drug Release ◽  
Physical Properties ◽  
Phosphate Buffer ◽  
Nonionic Surfactants ◽  
Tween 80 ◽  
Content Uniformity ◽  
Fusion Method ◽  
Disintegration Time ◽  
Span 60

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.

scholarly journals Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Rajni Bala ◽  
Sushil Khanna ◽  
Pravin Pawar
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Content Uniformity ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
Significant Difference ◽  
Film Formulation ◽  
Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

scholarly journals In vitro Studies on Sustained Release Suppository Formulations of Tiaprofenic Acid with Sucrose Fattv Acid Ester

2003 ◽  
Vol 71 (4) ◽  
pp. 357-364
Author(s):  
Sevgi Gūngör ◽  
Mine Orlu ◽  
Yildiz Özsoy ◽  
Ahmet Araman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Tiaprofenic Acid ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Sugar Ester ◽  
Disintegration Time ◽  
Suppository Base ◽  
Vitro Release

The objective of this study was to evaluate the performance of Sucro Ester 7 (sucrose distearate) as additive for preparing sustained release suppositories of tiaprofenic acid. Suppocire AIM (semi-synthetic glycerides) was used as suppository base and formulations were prepared containing different ratios of sugar ester: Suppocire AIM. Content uniformity, disintegration time and in vitro release characteristics of suppositories were investigated. Significant decrease in the extent of drug release was observed with the increase in the content of sugar ester, which was due to the longer disintegration time of suppositories.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF FAST DISSOLVING TABLET OF VERAPAMIL HYDROCHLORIDE

2018 ◽  
Vol 10 (10) ◽  
pp. 93 ◽  
Author(s):  
Dattatraya M. Shinkar ◽  
Pooja S. Aher ◽  
Parag D. Kothawade ◽  
Avish D. Maru
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Research Work ◽  
Time Interval ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Verapamil Hydrochloride ◽  
Sodium Starch Glycolate ◽  
Croscarmellose Sodium

Objective: The main objective of this research work was to formulate and evaluate fast dissolving tablet of verapamil hydrochloride for the treatment of hypertension.Methods: In this study, fast dissolving tablet were prepared by wet granulation method by using croscarmellose sodium and sodium starch glycolate as superdisintegrants in the concentration of 2%, 4%, and 6%. Polyvinyl pyrollidone K30 is used as a binder. The designed tablets were subjected to various assessment parameters like friability test, hardness test, disintegration test, wetting time, in vitro drug release and drug content.Results: All the prepared formulations were subjected to various assessment parameters, and the findings obtain within the prescribed limit. The calibration curve of pure drug using various solvents like distilled water, phosphate buffer pH 6.8 was plotted. F1-F9 containing croscarmellose sodium and sodium starch glycolate in various concentration demonstrate the minimum disintegration time. Among all these formulations F8 shows disintegration time upto 19±0.06 seconds due to the high concentration of superdisintegrants. In vitro drug release was tested in phosphate buffer pH 6.8 at a time interval of 0, 1, 3,6,9,12,15 min. The F8 shows drug release 98.5±0.567%. Accelerated stability study of optimized formulation (F8) up to 2 mo showed there was no change in disintegration time and percentage drug release.Conclusion: The results obtained in the research work clearly showed a promising potential of fast dissolving tablets containing a specific ratio of crosscarmellose sodium and sodium starch glycolate as superdisintegrants for the effective treatment of hypertension. 

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF ORAL SWELLABLE RAPID RELEASE FILM WITH SUPERDISINTEGRANT-SURFACTANT

2021 ◽  
pp. 75-80
Author(s):  
NEHA IMTIAZ ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Diclofenac Sodium ◽  
Hydroxypropyl Methylcellulose ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Disintegration Time ◽  
Rapid Release ◽  
Oral Films

Objective: Oral disintegrating films consisting of hydrophilic polymer are designed to be quickly hydrated by saliva, adhere to the mucosa and disintegrate rapidly to release the drug. The aim of the present study was to prepare stable, flexible swellable rapid release oral films with hydroxypropyl methylcellulose E15 LV (HPMC) and polyvinyl alcohol (PVA) in different ratios. Guar gum was incorporated as the mucoadhesive agent. In order to achieve rapid disintegration of the film cross carmellose sodium (superdisintegrant) and surfactant like Tween 80 were added. The model drug used in the study was diclofenac sodium. Methods: Films were developed using HPMC E15 LV and PVA by solvent casting method and characterized for thickness, swelling index, disintegration time, folding endurance, drug content, and in vitro drug release pattern and kinetics. Results: The prepared swellable rapid release oral films were quite flexible and transparent with a smooth texture. The swelling index study confirmed that the films possessed the desired swelling property. Fastest disintegration was observed with the oral film containing HPMC: PVA in the ratio of 2:1, guar gum at 120 mg, 20% w/w crosscarmellose sodium and 4%w/w Tween 80. The swellable rapid release oral films were found to follow either Higuchi or Korsmeyer-Peppas model with drug release following either Fickian or non-Fickian diffusion. Maximum drug release of around 70% was observed from the above-mentioned film in 1hr in simulated salivary fluid. Conclusion: Therefore, swellable rapid release oral films with HPMC E15 LV: PVA, guar gum, croscarmellose sodium and Tween 80 demonstrated satisfactory swelling, rapid disintegration and improved drug release for oromucosal absorption.

scholarly journals Development and optimization of a sublingual tablet formulation for physostigmine salicylate

2009 ◽  
Vol 59 (3) ◽  
pp. 301-312 ◽  
Author(s):  
Noushin Bolourchian ◽  
Naghmeh Hadidi ◽  
Seyed Foroutan ◽  
Bijan Shafaghi
Keyword(s):  
Physical Properties ◽  
Tablet Formulation ◽  
Drug Dissolution ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Sublingual Tablet ◽  
Gas Poisoning ◽  
Cubic Model ◽  
Predicted Values ◽  
Tablet Hardness

Development and optimization of a sublingual tablet formulation for physostigmine salicylateThis study is aimed to design and optimize a sublingual tablet formulation of physostigmine salicylate, an effective drug in Alzheimer's disease and nerve gas poisoning, by means of the D-optimal experimental design methodology. Polyvinyl pyrrolidone, lactose, starch 1500 and sodium starch glycolate were used in the formulations as independent variables. Tablets were prepared by the direct compression method and evaluated for their physical properties (tablet hardness, disintegration time and friability), which were regarded as responses in a D-optimal design. Due to the significance of the special cubic model for data fitted, compared to other models, it was used to examine the obtained results. Response surface plots were plotted to study the tablet properties and the optimized overlay plot was generated based on the results and targets considered for the responses. After verification of the optimum checkpoint formulations, an optimized formulation was chosen due to its desirable physical properties and closely observed and predicted values. Drug assay, content uniformity of the dosage unit, drug dissolution and accelerated stability studies were done on the optimum formulation as further experiments. All the obtained results complied with the requirements of a sublingual tablet formulation.

scholarly journals Disintegrant Properties of Microcrystalline Cellulose isolated from Rami (Boehmeria nivea L. Gaud) in Dimenhydrinate tablets by Wet Granulation and Direct compression

2021 ◽  
Vol 2 (3) ◽  
Author(s):  
Nagina Gulab Belali ◽  
Anis Y. Chaerunisaa ◽  
Taofik Rusdiana
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Physical Properties ◽  
Process Parameters ◽  
Microcrystalline Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Disintegration Time ◽  
Boehmeria Nivea ◽  
Significant Difference

Microcrystalline cellulose was isolated from rami (Boehmeria Nivea L. Gaud), and applied as disintegrant in tablets of dimenhydrinate, made by direct compression and wet granulation. The aim of this study is to produce dimenhydrinate tablets with Microcrystalline Cellulose Rami (MCC Rami) isolated from Rami (Boehmeria Nivea L. Gaud), as a disintegrant and assess the effect of MCC Rami and Granulation technique on physical properties of drug such as, disintegration time, drug release and dissolution. Formulations of dimenhydrinate 100mg tablets were prepared with a combination of mannitol and lactose as a filler and MCC Rami as disintegrant in a concentration of 10-20%. The formulas were directly compressed or were compressed into tablets after wet granulation. The mechanical properties, drug release, physical properties and effects of process parameters, methods of applying disintegrant in tablet formulas were examined. A significant difference in disintegration time of tablets that were produced by direct compression and wet granulation was seen, that can be attributed to the porous structure of granules that enhanced fast disintegration, which had eventually improved dissolution and drug release. F1 and F2 with MCC Rami and physical mixture of MCC Rami with crosspovidone as a disintegrant that were directly compressed disintegrated in 79 and 72 seconds respectively thats not a significant difference, however when MCC was applied in an intragranular way its disintegration time is 67 seconds. The results showed that the method of disintegrant application and press of tableting has a significant effect on drug release and dissolution.Keywords : Microcrystalline Cellulose, wet granulation, disintegrant, Boehmeria Nivea L. Gaud.

scholarly journals Application of Central Composite Design for Citalopram Hydrogen bromide Mouth Dissolving Films

2020 ◽  
pp. 360-367
Author(s):  
Shimmula Rohini Reddy ◽  
Bomma Ramesh
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Central Composite Design ◽  
Hydrogen Bromide ◽  
Drug Dissolution ◽  
Effective Dosage ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Central Composite

Citalopram is an antidepressant used for treating major depressive disorder. In the current work Citalopram HBr is formulated as mouth dissolving film with enhanced drug dissolution. The Central Composite Design (CCD), employed to examine the effects of amount of HPMC E50 (A), amount of maltodextrin (B) and amount of glycerol (C) on response variables tensile strength, disintegration time and cumulative % drug release. 27 formulations prepared according to CCD and evaluated for physicochemical parameters and in vitro dissolution studies. Citalopram HBr mouth dissolving films formulated by employing solvent-casting method using HPMC E50, maltodextrin and glycerol, optimized for the effective dosage of superdisintegrants.  The formulation CF21 with maximum tensile strength of 67.21±1.31 gm, least disintegration time of 9±1.60 sec and highest drug release of 98.41±1.81% is chosen optimal formulation with maximum content uniformity and folding endurance. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, quick onset of action as well as improve patient compliance in the effective management of depression.

scholarly journals Production of Itraconazole Nanocrystal-Based Polymeric Film Formulations for Immediate Drug Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 960
Author(s):  
Anna Karagianni ◽  
Leena Peltonen
Keyword(s):  
Drug Release ◽  
Physicochemical Characterization ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Polymeric Film ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming

In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.

scholarly journals Formulation and Evaluation of Clopidogrel Bisulfate Liquisolid Compact

2018 ◽  
pp. 135-149
Author(s):  
Amina Moustafa Mohammed ◽  
Entidhar Jasim Mohammed
Keyword(s):  
Dissolution Rate ◽  
Vascular Diseases ◽  
Tween 80 ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Clopidogrel Bisulfate ◽  
Weight Variation ◽  
Poorly Soluble ◽  
Low Solubility

Liquisolid compact is the most promising technique for increasing dissolution rate and bioavailability of poorly soluble drugs.Clopidogrel bisulfate is an oral antiplatelets used for treatment and prophylaxis of cardiovacular and peripheral vascular diseases related to platelets aggreagation.Clopidogrel has low solubility at high pH media of intestine and low bioavailability of a bout 50% after oral doses.The purpose of this work was to enhance dissolution pattern of clopidogrel through its formulation into liquisolid tablets.A mathematical model was used to calculate the optimum quantities of tween 80 , carrier (Avicel PH 102) and coating material (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures.The liquisolid tablets were evaluated for hardness, percent friability, weight variation, content uniformity , disintegration time and in vitro drug release profile.DSC , FTIR , XRD and SEM were used for assessment of physicochemical properties of drug and compatibility with excipients in the liquisolid compacts.The selected formulation (F2) released 92.2% of its content during first 10 min. compared to 13.6% of directly compressed tablet and 24.2% of marketed tablet. In conclusion the dissolution rate and bioavailability of clopidogrel can be enhanced to a great extent by liquisolid technique.

scholarly journals FORMULATION OPTIMIZATION AND EVALUATION OF MOUTH DISSOLVING FILM OF RAMOSETRON HYDROCHLORIDE

2020 ◽  
pp. 99-106
Author(s):  
ZANKAHANA PATEL ◽  
RAHIL BHURA ◽  
SAMIR SHAH
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Methyl Cellulose ◽  
Taste Masking ◽  
Content Uniformity ◽  
Solvent Casting ◽  
Disintegration Time ◽  
Duration Of Action ◽  
In Vitro Drug Release

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis. Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 32 full factorial design was applied considering the concentration of HPMC E5 (X1) and concentration of PEG400 (X2) as independent variables and % cumulative drug release (Y1) (CDR), disintegration time (Y2) (DT) and tensile strength (Y3) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X1 and X2 were found to be having a positive effect on DT and TS and negative effects on CDR. Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm2 tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness. Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.

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