scholarly journals FORMULATION, DEVELOPMENT AND EVALUATION OF FAST DISSOLVING DRUG. LEVOSALBUTAMOL TABLETS

2020 ◽  
Vol 9 (4) ◽  
Author(s):  
Aditya Duby ◽  
Md Shamimuddin ◽  
Mukesh Sharma
Keyword(s):  
Release Kinetics ◽  
Bronchial Hyperresponsiveness ◽  
Noncommunicable Disease ◽  
Effect Of Temperature ◽  
Anticholinergic Agent ◽  
Formulation Development ◽  
Visual Appearance ◽  
Acute Exacerbations ◽  
Acute Asthma Exacerbations

Asthma symptoms are the result of bronchial hyperresponsiveness, bronchospasm, and chronic airway inflammation. Short-acting, inhaled beta2 agonists; oxygen; intravenous fluids; and corticosteroids are the mainstays of treatment for acute exacerbations. The R-enantiomer of albuterol is responsible for bronchodilation. The S-enantiomer exhibits broncho-constricting activity in vitro, which may be mediated by muscarinic receptors and may be opposed by adding the anticholinergic agent ipratropium bromide. Levalbuterol improves pulmonary function to a greater extent than racemic albuterol and reduces the need for costly hospitalizations in patients with acute asthma exacerbations. It was estimated that more than 339 million people suffer from asthma. Asthma is the most common noncommunicable disease among children. Most deaths occur in older adults. Under Preformulation study, the physicochemical properties were complied with the IP and USP specification. Physical properties such as appearance, melting point, effect of temperature and humidity in different conditions were more in Levosabutamol raw powder.  Parameters evaluated were within the USP limit. The compatibility evaluations were performed by FTIR spectroscopy. The observation implies that the drug and polymers were compatible with each other.  There were no interaction found between polymers and drug. The formulations were evaluated on the basis of Pharmacopoeial specification visual appearance, pH, drug content, Hardness, Friability, Disintegration test, assessment of drug release,  release kinetics were carried out as per specifications and results were found to be complied with the Pharmacopoeial specification.

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

scholarly journals Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kenneth Chibuzor Ofokansi ◽  
Franklin Chimaobi Kenechukwu
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Local Treatment ◽  
Wet Granulation ◽  
Formulation Development ◽  
Swelling Properties ◽  
Interpolyelectrolyte Complexes ◽  
Bowel Diseases

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

scholarly journals Formulation development and in-vitro/ex-vivo evaluation of novel buccoadhesive films of metoprolol tartrate using 23 factorial design techniques

2015 ◽  
Vol 49 (3) ◽  
pp. 165-172
Author(s):  
T Ayyappan ◽  
D Bharathiraja ◽  
T Vetrichelvan
Keyword(s):  
Drug Delivery ◽  
Factorial Design ◽  
Buccal Mucosa ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Metoprolol Tartrate ◽  
Formulation Development ◽  
Independent Variables ◽  
Software Analysis

The aim of present investigation was to develop an optimized buccoadhesive film of metoprolol tartrate, a BCS class I drug, to provide unidirectional sustained drug delivery to the buccal mucosa that has potential to enhance the bioavailability. The films were prepared using HPMC K4M as film former, carbopol 934 P as buccoadhesive polymer and dimethyl sulfoxide as penetration enhancer, by solvent casting technique. The films were characterized for various pharmacotechnical parameters and 23 full factorial design was employed to study the effect of independent variables. The design was validated by extra design checkpoint formulation (BF9). The response of design was employed to study the effect of independent variables. The responses of design were analyzed using Design Expert 8.0.7.1 and the analytical tools of software were used to draw pareto charts. On the basis of software analysis, formulation BF4 with desirability factor of 0.698 was selected as optimized formulation and was evaluated for independent parameters. Optimized formulation showed 12.05 hr, ex-vivo residence time, and good permeation (42.68%) through goat buccal mucosa and 82.19% drug release after 8th hour. The release kinetics of optimized formulation best fitted the higuchi model. Histopathological studies revealed no buccal mucosal damage. Hence BF4 formulation can be concluded as promising drug delivery system to enhance the permeability limited absorption of metoprolol tartrate. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22130 Bangladesh J. Sci. Ind. Res. 49(3), 165-172, 2014

scholarly journals Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Gustavo H. Rodrigues da Silva ◽  
Gabriela Geronimo ◽  
Juan P. García-López ◽  
Lígia N. M. Ribeiro ◽  
Ludmilla D. de Moura ◽  
...  
Keyword(s):  
Release Kinetics ◽  
In Vitro Release ◽  
Tween 80 ◽  
Inflammatory Activity ◽  
Formulation Development ◽  
Anesthetic Effect ◽  
Copaiba Oil ◽  
Anti Inflammatory

AbstractAnesthetic failure is common in dental inflammation processes, even when modern agents, such as articaine, are used. Nanostructured lipid carriers (NLC) are systems with the potential to improve anesthetic efficacy, in which active excipients can provide desirable properties, such as anti-inflammatory. Coupling factorial design (FD) for in vitro formulation development with in vivo zebrafish tests, six different NLC formulations, composed of synthetic (cetyl palmitate/triglycerides) or natural (avocado butter/olive oil/copaiba oil) lipids were evaluated for loading articaine. The formulations selected by FD were physicochemically characterized, tested for shelf stability and in vitro release kinetics and had their in vivo effect (anti-inflammatory and anesthetic effect) screened in zebrafish. The optimized NLC formulation composed of avocado butter, copaiba oil, Tween 80 and 2% articaine showed adequate physicochemical properties (size = 217.7 ± 0.8 nm, PDI = 0.174 ± 0.004, zeta potential = − 40.2 ± 1.1 mV, %EE = 70.6 ± 1.8) and exhibited anti-inflammatory activity. The anesthetic effect on touch reaction and heart rate of zebrafish was improved to 100 and 60%, respectively, in comparison to free articaine. The combined FD/zebrafish approach was very effective to reveal the best articaine-in-NLC formulation, aiming the control of pain at inflamed tissues.

scholarly journals STAT6 siRNA Matrix-Loaded Gelatin Nanocarriers: Formulation, Characterization, andEx VivoProof of Concept Using Adenocarcinoma Cells

2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Susanne R. Youngren ◽  
Rakesh K. Tekade ◽  
Brianne Gustilo ◽  
Peter R. Hoffmann ◽  
Mahavir B. Chougule
Keyword(s):  
Release Kinetics ◽  
Average Particle Size ◽  
A549 Cells ◽  
Average Particle ◽  
Formulation Development ◽  
Nonspecific Effects ◽  
Adenocarcinoma Cells ◽  
Sirna Therapy ◽  
The Stability

The clinical utility of siRNA therapy has been hampered due to poor cell penetration, nonspecific effects, rapid degradation, and short half-life. We herewith proposed the formulation development of STAT6 siRNA (S6S) nanotherapeutic agent by encapsulating them within gelatin nanocarriers (GNC). The prepared nanoformulation was characterized for size, charge, loading efficiency, release kinetics, stability, cytotoxicity, and gene silencing assay. The stability of S6S-GNC was also assessed under conditions of varying pH, serum level, and using electrophoretic assays.In vitrocytotoxicity performance was evaluated in human adenocarcinoma A549 cells following MTT assay. The developed formulation resulted in an average particle size, surface charge, and encapsulation efficiency as70±6.5 nm,+10±1.5 mV, and85±4.0%, respectively. S6S-GNC showed an insignificant (P<0.05) change in the size and charge in the presence of buffer solutions (pH 6.4 to 8.4) and FBS (10% v/v). A549 cells were treated with native S6S, S6S-lipofectamine, placebo-GNC, and S6S-GNC using untreated cells as a control. It was observed that cell viability was decreased significantly with S6S-GNC by55±4.1%(P<0.001) compared to native S6S (2.0±0.55%) and S6S-lipofectamine complex (40±3.1%). This investigation infers that gelatin polymer-based nanocarriers are a robust, stable, and biocompatible strategy for the delivery of siRNA.

Formulation development of Temozolomide liposomal formulation in the treatment of Glioma

2021 ◽  
pp. 203-206
Author(s):  
Swapna Velivela ◽  
Nikunja B Pati ◽  
B. Ravindra Babu
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Physicochemical Characteristics ◽  
Liposomal Formulation ◽  
Cancer Drug ◽  
Formulation Development ◽  
In Vitro Drug Release

Temozolomide is an anti-cancer drug; it was encapsulated in liposomal intravenous application. To avoid the side effects and to target the drug to the specific site, we have formulated liposomal formulation of Temozolomide. The liposomal were prepared by dried thin film hydration technique using rotary evaporator with drug and Soya phosphatidyl choline as carrier. The prepared liposomes were characterized for size, shape, % entrapment efficiency, in-vitro drug release and physical stability. The evaluated batches showed good physicochemical characteristics. The maximum encapsulation efficiency of Temozolomide was achieved with formulation TMZ 6 with 40.19% and the in-vitro drug release is 64.94%. Based on the results it can be concluded that TMZ 6 was selected as optimized formulation and the optimized formulation Optimized formulation follows zero order release kinetics and follow super case II transport when it applied to Korsmeyer-Pepps model for mechanism of drug release.

scholarly journals Formulation Development and Evaluation of Floating Microsphere of Famotidine for the Treatment of Peptic Ulcer

2019 ◽  
Vol 9 (4-s) ◽  
pp. 426-431
Author(s):  
Dharmendra Rai ◽  
Durga Pandey ◽  
Nishi Prakash Jain ◽  
Surendra Kumar Jain
Keyword(s):  
Ethyl Cellulose ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Extended Period ◽  
Prolonged Release ◽  
Formulation Development ◽  
Evaporation Method ◽  
Solvent Diffusion

The purpose of this research was to prepare a floating drug delivery system of famotidine. The floating microspheres can be prepared for the improvement of absorption and bioavailability of famotidine by retaining the system in the stomach for prolonged period of time. Floating microspheres of famotidine were prepared using different polymers like ethyl cellulose, hydroxy propyl methyl cellulose by solvent diffusion-evaporation method. The microspheres had smooth surfaces with free-flowing and good-packing properties. The yield of the microspheres was up to 73.32±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in 331.6 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to 73.25±0.23. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to stability studies and In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of famotidine offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved. Keywords: Famotidine, Solvent diffusion evaporation method, Ethyl cellulose, Hydroxyl propyl methyl cellulose

scholarly journals Formulation Development, Characterization and In-vitro Evaluation of Tamoxifen Loaded Liposomes

2020 ◽  
pp. 64-82
Author(s):  
Md. Mazed Hasan ◽  
Md. Hamiduzzaman ◽  
Ishrat Jahan ◽  
A. H. M. Nazmul Hasan ◽  
Md. Asaduzzaman
Keyword(s):  
Drug Delivery ◽  
Controlled Release ◽  
Side Effects ◽  
Cancer Treatment ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Formulation Development

Background: The study was aimed to prepare and evaluate tamoxifen loaded controlled release liposomes to reduce the side effects of tamoxifen during cancer treatment.  Methods: Different tamoxifen loaded liposomes were prepared by modified ether injection (MEIM) and thin film hydration method (TFHM) under prescribed conditions. The prepared liposomes were characterized by using optical microscopy, evaluating encapsulation efficiency, in-vitro and ex-vivo diffusion studies by using dialysis membrane and chicken intestinal sac respectively. Results: The data revealed that all of the liposomes were spherical in shape and stable under three physical conditions i.e. 4, 25 and 37 ± 2°C temperatures and 60 ±5% relative humidity. Additionally most of the liposomes followed zero order and class II release kinetics. It was also observed that with the increase of phospholipids and cholesterol, entrapment efficiency of liposome vesicles increased thus giving a controlled release drug delivery system but further increase reduced this efficiency at a certain level. Conclusion: The formulated control release liposomes might be a good drug delivery system for target oriented drug delivery with minimum side effects of tamoxifen during cancer treatment.

scholarly journals Formulation, Development and Evaluation of Gastroretentive Sustained Release Tablets of Lansoprazole Using Natural Polymer

2021 ◽  
Vol 11 (5-S) ◽  
pp. 108-112
Author(s):  
, Sonam ◽  
Nilesh Jain ◽  
Jitendra Banveer
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Acid Secretion ◽  
Release Kinetics ◽  
Natural Polymers ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Multiple Dosing ◽  
Long Acting

The goal of this study is to develop a long-acting Lansoprazole delivery system. Lansoprazole belongs to a class of antisecretory drugs known as substituted benzimidazoles, which decrease gastric acid secretion by inhibiting the (H+,K+)-ATPase enzyme system at the secretory membrane of the stomach parietal cell. Due to its mechanism of action, despite its short half-life of 1-5 hours, it can effectively block acid secretion for 24 hours. However, as his plasma concentration falls, the effect will diminish. Lansoprazole will be given as a sustained release tablet to avoid multiple dosing or to reduce the frequency of dose. Lansoprazole was produced and analysed utilizing natural and synthetic polymers such as Xanthan gum, Gellan gum, Carbopol 940 P, and Chitosan. Based on the findings of this experiment, it was determined that formulation F7 demonstrated sustained drug release for up to 12 hours in all developed formulations. Formulation (F1, F2, F3, F4, F5, and F6) were tested in vitro for drug release. For the improved formulation F7, the formulation and release kinetics were estimated. When the regression coefficient values of were evaluated, it was found that Peppas had the highest ‘r2' value, 0.952, indicating that drug release from formulations followed Peppas release kinetics. Key words: Lansoprazole, Sustain release tablets, Synthetic and Natural Polymers, formulation, evaluation

scholarly journals Design and characterization of metoprolol floating matrix tablet

2017 ◽  
Vol 4 (2) ◽  
pp. 118
Author(s):  
Vasudha Bakshi ◽  
Swapna S. ◽  
Deepa Kumari Choudhary ◽  
Ch. Revanth ◽  
B. Sai KumarCh. Praveen ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Gastric Residence Time

Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract.Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction.Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR).Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.

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