scholarly journals Development and Evaluation of Mouth Dissolving Films of Amlodipine Besylate for Enhanced Therapeutic Efficacy

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
K. M. Maheswari ◽  
Pavan Kumar Devineni ◽  
Sravanthi Deekonda ◽  
Salma Shaik ◽  
Naga Pravallika Uppala ◽  
...  
Keyword(s):  
Therapeutic Efficacy ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Vinyl Pyrrolidone ◽  
Release Mechanism ◽  
Amlodipine Besylate ◽  
Disintegration Time ◽  
Dissolution Properties ◽  
Pvp K30

The present investigation was undertaken with an objective of formulating mouth dissolving films (MDFs) of Amlodipine Besylate (AMLO) to enhance convenience and compliance of the elderly and pediatric patients for better therapeutic efficacy. Film formers like hydroxy propyl methyl cellulose (HPMC) and methyl cellulose (MC) along with film modifiers like poly vinyl pyrrolidone K30 (PVP K30), and sodium lauryl sulphate (SLS) as solubilizing agents were evaluated. The prepared MDFs were evaluated for in vitro dissolution characteristics, in vitro disintegration time, and their physicomechanical properties. All the prepared MDFs showed good mechanical properties like tensile strength, folding endurance, and % elongation. MDFs were evaluated by means of FTIR, SEM, and X-RD studies. MDFs with 7.5% (w/w) of HPMC E3 gave better dissolution properties when compared to HPMC E5, HPMC E15, and MC. MDFs with PVP K30 and SLS gave superior dissolution properties when compared to MDFs without PVP K30 and SLS. The dissolution properties of MDFs with PVP K30 were superior when compared to MDFs with SLS. In the case of F3 containing 7.5% of HPMC E3 and 0.04% of PVP K30, complete and faster release was observed within 60 sec when compared to other formulations. Release kinetics data reveals diffusion is the release mechanism.

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 The application of povidone in the preparation of modified release tablets

2016 ◽  
Vol 29 (2) ◽  
pp. 71-78 ◽  
Author(s):  
Regina Kasperek ◽  
Lukasz Zimmer ◽  
Maria Zun ◽  
Dorota Dwornicka ◽  
Katarzyna Wojciechowska ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Release Mechanism ◽  
Prolonged Release ◽  
Modified Release ◽  
Compression Technique ◽  
Disintegration Time ◽  
Polymer Relaxation ◽  
Model Substance ◽  
Different Types

Abstract The aim of the study was to investigate the modified release of a model substance, of tablets containing different types of Kollidon and particular additives. Additionally, the release kinetics and mechanism of prolonged release of certain tablet preparations were investigated. In this work, tablets containing different types of povidone (Kollidon CL, Kollidon 30, Kollidon SR and other excipients) were prepared by the direct compression technique. The results showed that tablets with fast disintegration and release should contain in their composition, Kollidon CL, lactose and Avicel, however, the use of β-CD instead of lactose or Avicel brings about a slight prolongation in the disintegration time of tablets and the release of an active substance. Furthermore, while other tablet compositions generated within this study must be considered as being prolonged release types, only two of these showed the best fitted mathematical models. The in vitro dissolution data reveal that the dissolution profiles of the two formulations, one containing Kollidon SR with the addition of Kollidon 30, and the second with HPMC K15M, Kollidon 30, Kollidon CL and lactose, best fitted the Higuchi model. Moreover, the release mechanism of these two formulations plotted well into Korsmeyer-Peppas, indicating a coupling of drug diffusion in the hydrated matrix, as well as polymer relaxation – the so-called anomalous transport (non-Fickian).

scholarly journals Release Kinetics Study of Azithromycin from Bi-layered Tablets

2017 ◽  
Vol 20 (1) ◽  
pp. 54-63
Author(s):  
FM Shah Noman Ul Bari ◽  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
Israt Jahan Ira
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Pharmaceutical Journal ◽  
High Viscosity ◽  
Release Mechanism ◽  
Low Viscosity ◽  
Release Studies ◽  
Vitro Release

The objective of this study was to analysis in vitro release kinetics of Azithromycin from bi-layer tablets prepared by direct compression using high viscosity to low viscosity grades of hydroxypropyl methyl cellulose (HPMC K15M, HPMC K4M, HPMC 50 cps), Carbopol 934p and Carbopol 974p. In addition, it also includes evaluating the effect of formulation variables like polymer proportion and polymer viscosity on the release of Azithromycin. In vitro release studies were performed using USP Type-II (Rotating paddle method) at 100 rpm. The dissolution medium consisted of 0.1N HCl (900 ml) for the first 2 hr and the phosphate buffer (pH 6.0) from 3rd to 10th hour. From twenty five different formulations (F-1 to F-25) based on polymer variation, model-dependent and independent methods were used for data analysis and the best results were observed for HPMC 50cps in Korsmeyer- Peppas (R2=0.995 on F-23) kinetic model. The release mechanism of all formulations was Fickian.Bangladesh Pharmaceutical Journal 20(1): 54-63, 2017

scholarly journals Formulation and Evaluation of Chlorpheniramine Maleate Mouth Dissolving Films

2019 ◽  
Vol 9 (1-s) ◽  
pp. 244-251 ◽  
Author(s):  
D Teja ◽  
E Jasvanth ◽  
B Mounika ◽  
Buchi N Nalluri
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
The Elderly ◽  
Physicomechanical Properties ◽  
Vinyl Pyrrolidone ◽  
Release Mechanism ◽  
Chlorpheniramine Maleate ◽  
Poly Ethylene ◽  
Poly Vinyl Pyrrolidone

The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of an anti-histamine drug, Chlorpheniramine Maleate (CPM) to enhance convenience and compliance to the elderly and paediatric patients. The MDFs were prepared using wet film applicator and evaluated for physicochemical and physicomechanical properties. MDFs were prepared with 0.6% and 0.8% w/w CPM. The MDFs with 0.8% w/w drug load showed re-crystallisation within 10 days, while the MDFs with 0.6% w/w CPM load were transparent with no re-crystallization. The effect of film formers, film thickness, film modifiers, saliva stimulating and soothing agents on the physicomechanical properties and CPM release from MDFs were evaluated. MDFs casted at 30mil thickness containing poly ethylene glycol (PEG-400) as plasticizer showed superior CPM release rates along with good physicomechanical properties. MDFs with hydroxy propyl methyl cellulose (HPMC) E3 as film former gave superior CPM release rate when compared to E5 and E15 formulations. MDFs with poly vinyl pyrrolidone K30 (PVPK30) gave superior drug release properties when compared to MDFs without PVP K30. The MDFs with citric acid (CA) and xylitol gave superior CPM release than the other MDFs. Release kinetics data reveals diffusion as drug release mechanism.

scholarly journals In Vitro Drug Release, Permeability, and Structural Test of Ciprofloxacin-Loaded Nanofibers

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 556
Author(s):  
Luca Éva Uhljar ◽  
Sheng Yuan Kan ◽  
Norbert Radacsi ◽  
Vasileios Koutsos ◽  
Piroska Szabó-Révész ◽  
...  
Keyword(s):  
Amorphous State ◽  
Physical Mixture ◽  
Water Soluble ◽  
Vinyl Pyrrolidone ◽  
Amorphous Solid Dispersion ◽  
Release Mechanism ◽  
Dissolution Studies ◽  
In Vitro Diffusion ◽  
Poly Vinyl Pyrrolidone

Nanofibers of the poorly water-soluble antibiotic ciprofloxacin (CIP) were fabricated in the form of an amorphous solid dispersion by using poly(vinyl pyrrolidone) as a polymer matrix, by the low-cost electrospinning method. The solubility of the nanofibers as well as their in vitro diffusion were remarkably higher than those of the CIP powder or the physical mixture of the two components. The fiber size and morphology were optimized, and it was found that the addition of the CIP to the electrospinning solution decreased the nanofiber diameter, leading to an increased specific surface area. Structural characterization confirmed the interactions between the drug and the polymer and the amorphous state of CIP inside the nanofibers. Since the solubility of CIP is pH-dependent, the in vitro solubility and dissolution studies were executed at different pH levels. The nanofiber sample with the finest morphology demonstrated a significant increase in solubility both in water and pH 7.4 buffer. Single medium and two-stage biorelevant dissolution studies were performed, and the release mechanism was described by mathematical models. Besides, in vitro diffusion from pH 6.8 to pH 7.4 notably increased when compared with the pure drug and physical mixture. Ciprofloxacin-loaded poly(vinyl pyrrolidone) (PVP) nanofibers can be considered as fast-dissolving formulations with improved physicochemical properties.

SYNTHESIS AND CHARACTERIZATION OF THIOLATED GUM KONDAGOGU AND EVALUATION AS MUCOADHESIVE POLYMER

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (01) ◽  
pp. 37-43
Author(s):  
Ashwin A. Patil ◽  
Ketan B. Patil ◽  
Laxmikant R. Zawar
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Matrix Tablet ◽  
Disintegration Time ◽  
Weight Variation ◽  
Zero Order Release ◽  
Gum Kondagogu ◽  
Ellman’S Method

Present work focused on thiolation for enhancing the mucoadhesive potential of Gum kondagogu (GK). Thiolation of GK was done by esterification process with 80 % thioglycolic acid in presence of 7N HCl. Thiolated Gum kondagogu (ThioGK) was determined to possess 1.59 ±0.04 mmol of thiol groups/g of the polymer by Ellman’s method. ThioGK was characterized by FTIR, NMR, DSC, XRD, and FE-SEM. The tablets were prepared by direct compression using 75 mg of ThioGK and GK. Tablets containing ThioGK (F1) and GK (F2) were subjected to evaluation of weight variation, hardness and friability and show enhanced disintegration time, swelling behavior, drug release and mucoadhesion. In vitro drug release of batch F1 exhibits complete release of drug in 24 hr with zero order release kinetics. Comparative mucoadhesive strength was studied using chicken ileum by texture analyzer and revealed higher mucoadhesion of tablet containing ThioGK. From the above study, ThioGK was suitability exploited as mucoadhesive sustained release matrix tablet.

Formulation and evaluation of proniosome loaded sertaconazole nitrate for topical application

2021 ◽  
Vol 1 (2) ◽  
pp. 023-037
Author(s):  
Shailaja D ◽  
Latha K ◽  
Manasa D ◽  
Shirisha A ◽  
Padmavathi R ◽  
...  
Keyword(s):  
Ex Vivo ◽  
Release Kinetics ◽  
Skin Irritation ◽  
Water Soluble ◽  
Ionic Surfactants ◽  
Release Mechanism ◽  
Stability Studies ◽  
Zero Order Release ◽  
Poorly Soluble

Proniosomal technology is a novel solution for poorly soluble drugs. Proniosomes are water-soluble carrier particles which are coated with non-ionic surfactants. Proniosomal gels were prepared by coacervation phase separation method using non-ionic surfactants, lipid carriers and cholesterol as a membrane stabilizer. FTIR compatibility studies revealed that the drug and excipients were compatible. All formulations were evaluated for pH, drug content, extrudability, spreadability, viscosity, in-vitro, ex-vivo, skin irritation and stability studies. Among formulations prepared, F80H1 has shown higher % EE (83.02) and least diffusion through dialysis membrane i.e., 17.68%. With ex-vivo studies, F80H1 formulation has shown highest skin deposition and lower flux of sertaconazole nitrate through the rat skin. F80H1 was selected as final optimized formulation. F80H1 exhibited good stability and SEM studies revealed that the vesicles were spherical in shape. The optimized formulation was found to follow zero order release kinetics and korsmeyer-peppas release mechanism. F80H1 found to be non-irritant and stable from skin irritation and stability studies.

Preparation and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

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