scholarly journals INTEND, DEPICTION IN VITRO AND IN VIVO APPRAISAL OF GLIPIZIDE FLOATING MICROSPHERES USING ETHYL CELLLULOSE AND HYDROXYL PROPYL METHYL CELLULOSE AS POLYMER BY SUBSTANTIALLY MODIFIED METHOD

2016 ◽  
Vol 9 (5) ◽  
pp. 112
Author(s):  
Rishikesh Gupta ◽  
Sk Prajapati ◽  
Snigdha Pattnaik ◽  
Peeyush Bhardwaj
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Size Analysis ◽  
Release Study ◽  
Tapped Density ◽  
Vitro Release

ABSTRACTObjective: The purpose of this research was to formulate and evaluate floating microsphere of glipizide.Methods: Glipizide microsphere containing ethyl cellulose (EC) and hydroxyl propyl methyl cellulose (HPMC) were prepared by solvent evaporationmethod. Polymer to drug ratio affected characteristics of microspheres. Microspheres were discrete, spherical, and perforated form. The microspheresexhibited good floating property and achieved good gastric retention.Result: In vitro performance was evaluated by the usual pharmacopoeial and other tests such as drug polymer compatibility (Fourier transforminfrared scan), yield (%), micrometric properties such as tapped density (%). Compressibility particle size analysis (by optical microscopy), drugentrapment efficiency, surface topography (scanning electron microscope), and in vitro release study. On the basis of results, increasing the polymerratio increased the particle size (195.6±20.24 to 200.89±16.61), increased tapped density (maximum 0.29.60±0.00037 HGF4, batch), and decreased% compressibility (2.13±0.188). Drug loaded floating microspheres were found to be float more than 12 hrs on simulated gastric fluid (pH-1.2).Maximum drug entrapment was found in batch HGF3 (Drug:HPMC:EC) (1:1:3). Electron microscopy showed its perforated surface with hollowness.After 10 hrs, maximum release was found to be 78.0% (batch-GF1).Conclusion: The release study was performed in simulated gastric fluid with 0.02% tween80. The best release result was obtained at the ratio ofdrug: polymer (1:1).Keywords: Floating microspheres, Glipizide, Gastrorentensive system, In vitro release.

scholarly journals IN VITRO RELEASE STUDIES OF CARBAMAZEPINE TABLETS AND BENZOYL METRONIDAZOLE SUSPENSIONS USING THE FLOW-THROUGH CELL APPARATUS AND SIMULATED GASTROINTESTINAL FLUIDS

2017 ◽  
Vol 9 (4) ◽  
pp. 54 ◽  
Author(s):  
Jose Raul Medina ◽  
Jonathan Hernandez ◽  
Marcela Hurtado
Keyword(s):  
In Vitro Release ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Dissolution Time ◽  
Intestinal Fluid ◽  
Simulated Intestinal Fluid ◽  
Release Studies ◽  
Flow Through ◽  
Vitro Release

Objective: To characterize the in vitro release of carbamazepine tablets and benzoyl metronidazole suspensions using the flow-through cell apparatus and simulated gastrointestinal fluids.Methods: Tegretol® tablets, Flagyl® suspension, and generic formulations of each were tested. Release studies were performed using an automated flow-through cell apparatus. Simulated gastric fluid (with and without pepsin) and simulated intestinal fluid (without pancreatin) at 16 ml/min and fasted state simulated intestinal fluid at 8 ml/min, all at 37.0±0.5 °C, were used as dissolution media. The quantity of dissolved carbamazepine and benzoyl metronidazole was determined at 5-min intervals until 60 min at 285 and 278 nm, respectively. Percentage dissolved at 60 min, mean dissolution time, dissolution efficiency values, and t10%, t25%, t50% and t63.2% were calculated. Mean values for all parameters were compared between the reference and generic formulations using Studentʼs t-test. Dissolution data were fitted to different kinetic models.Results: Simulated gastric fluid without pepsin showed no discriminative capability for carbamazepine tablets. Significant differences were observed between the reference and generic formulations for almost all parameters (*P<0.05). In some cases, the logistic model best described the in vitro release of both drugs.Conclusion: Using an apparatus and media that best simulates the gastrointestinal environment, we identified differences in the rate and extent of dissolution of both drugs that could help to optimise the design of interchangeable formulations. Based on the physicochemical characteristics of carbamazepine and benzoyl metronidazole and the conditions in which the formulations were tested, these differences could be of clinical relevance. 

scholarly journals A A COMPARATIVE STUDY OF QUALITY CONTROL TESTING ON CANDESARTAN CILEXETIL CONVENTIONAL TABLETS IN IRAQ

2020 ◽  
pp. 103-108
Author(s):  
KARRAR TALIB KHUDHAIR ALBO HAMRAH ◽  
ABULFADHEL JABER NEAMAH AL-SHAIBANI ◽  
SARMAD SABAH AL-EDRESI ◽  
KARRAR MOHAMMED HASAN AL-GBURI
Keyword(s):  
Quality Control ◽  
Candesartan Cilexetil ◽  
In Vitro Release ◽  
Simulated Gastric Fluid ◽  
Control Analysis ◽  
Disintegration Time ◽  
Drug Content ◽  
Release Study ◽  
Vitro Release

Objective: The present study was performed to compare the quality of conventional tablets loaded with candesartan cilexetil. The selected candesartan cilexetil tablets were commercialized in the Iraq market and produced by different companies.  Methods: Different batches of candesartan cilexetil oral tablets (the concentration of candesartan was 8 mg) were subjected to quality control tests. Tests included weight variation, friability, hardness, drug content, disintegration time and in vitro release study. The protocols of these tests were performed according to USP pharmacopeia. Results: The results, in this study, revealed that all the used batches of candesartan cilexetil oral tablets complied with the specification of USP pharmacopeia for weight uniformity, friability value (% loss) was<1. Hardness results of the tablets were 4.9-6.6 Kg/cm2, which was within the required limits (i.e. 4-8 Kg/cm2). Disintegration time was<15 min in both Simulated Gastric Fluid (SGF) and Simulated Intestinal Fluid (SIF). The percentage of drug content in all marketed tablets was found between 96.2 % and 99.8 %, reflecting compliance with the pharmacopeia limits (i.e. 85-115 %). An in vitro release study indicated that the release of all marketed tablets exceeds 80 % within 15 min. Conclusion: All the studied tablets, loaded with candesartan cilexetil, were produced within the standard criteria of tablet production. The quality control analysis of the selected tablets, in this study, revealed satisfactory pharmaceutical properties (including safety and effectiveness) that comply within the limits of USP pharmacopeia.

An Innovative Approach for Development and Evaluation of Nanosized Lamotrigine Loaded Bionanoparticles Using Biopolymer from Fragaria × ananassa Fruit

2020 ◽  
Vol 13 (4) ◽  
pp. 4990-4999
Author(s):  
Sushant Kumar ◽  
Satheesh Madhav N V ◽  
Anurag Verma ◽  
Kamla Pathak
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Kinetic Study ◽  
In Vitro Release ◽  
Release Kinetic ◽  
Fruit Pulp ◽  
Fragaria Ananassa ◽  
Release Study ◽  
Vitro Release

The purpose of this research was to isolate the smart biopolymer from the fruit pulp of Fragaria × ananassa (garden strawberry). We isolated natural fruit pulp to evaluate the potentiality of biopolymer in delivery of nanosized lamotrigine as an antiepileptic drug. Lamotrigine was nanosized by screening its nano-size particle by UV method. The nanosized lamotrigine was used for preparation of bionanoparticles (LF1-LF8) by sonication method. The isolated biopolymer was characterized for DSC, FTIR, NMR, Mass and Zeta particle size analysis. The obtained results confirm its polymeric nature in different analysis. The prepared bionanoparticles showed the release of lamotrigine in sustained manner over 36 hours. The release kinetic study was done by using the BIT-SOFT 1.12 software and T50% and T80%, r2 were calculated. All the formulation showed more than 99.78% drug release. The In-vitro release study of different formulations showed the % drug release from 90.92% to 99.78%. The different formulations were evaluated for the In-vitro release study and release kinetic was studied. The formulation LF5 was found to be the best formulation having T50% of 17 hours and T80% of 29 hours with r2 value of 0.9925. The best formulation LF5 showed up to 90.925% drug release over 36 hours. According to the release kinetic study, the best-fit model was found to be Koresmayer-Peppas and the mechanism of drug release was found to be anomalous transport. The results obtained from different evaluations like percentage entrapment efficiency, particle size, release study, kinetic studies and stability study revealed that isolated biopolymer has good potentiality to form bionanoparticles and it can be safely used as an alternative to synthetic and semisynthetic polymers for the preparation of lamotrigine loaded stable bionanoparticles

Synthesis and Characterization of Alginate-Based Hydrogel Microbeads for Magnesium Release

2016 ◽  
Author(s):  
Shalil Khanal ◽  
Udhab Adhikari ◽  
Nava P. Rijal ◽  
Devdas Pai ◽  
Jagannathan Sankar ◽  
...  
Keyword(s):  
Particle Size ◽  
Tissue Injury ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Synthesis And Characterization ◽  
Average Particle ◽  
Release Study ◽  
Vitro Release

Magnesium injection is a suitable approach for replenishment of its ions (Mg++) during neural or tissue injury and stroke to avoids risks associated with abnormally low level of Mg++ in blood. In this study, alginate encapsulated magnesium sulfate microbeads were fabricated by the electrospraying technique for Mg++ delivery. Microbeads were evaluated for particle size and surface morphology using inverted optical microscopy and scanning electron microscopy (SEM) respectively. Average particle size of 200–500 μm for hydrated and 50–200 μm for dry beads were observed. An in vitro release study of Mg++ was performed; revealing a cumulative release of ∼50% within first 24 h. This strategy can potentially be useful for the targeted local delivery of magnesium at required concentrations and subsequently enhance the therapeutic efficacy of magnesium in treating tissue injury or stroke.

scholarly journals QUALITY CONTROL TESTING OF CONVENTIONAL CLOPIDOGREL BISULFATE TABLETS MARKETED IN IRAQ

2022 ◽  
pp. 221-225
Author(s):  
MAZIN THAMIR ABDUL-HASAN ◽  
ABULFADHEL JABER NEAMAH Al-SHAIBANI ◽  
ALI N. WANNAS ◽  
KARRAR MOHAMMED HASAN AL-GBURI
Keyword(s):  
Quality Control ◽  
In Vitro Release ◽  
Gastric Fluid ◽  
Disintegration Time ◽  
Drug Content ◽  
Clopidogrel Bisulfate ◽  
Weight Variation ◽  
Release Study ◽  
Vitro Release

Objective: This study was employed to evaluate the quality of marketed oral tablets containing clopidogrel bisulfate. Tablets produced by various companies and commercialized in the Iraq market were used in the study. Methods: Batches of clopidogrel bisulfate conventional tablets (containing 75 mg of drug) were exposed to the quality control tests. These tests involved friability, weight variation, hardness, drug content, disintegration time, and in vitro release study; these tests were conducted depending on USP pharmacopeia. Results: The data indicate that all batches of clopidogrel bisulfate complied with the limitations of USP pharmacopeia for variation of weight, results of the hardness of tablets were 7.2-9.6 Kg/cm2. Friability value (% loss) was less than one, which was within the required limits. The time of disintegration was less than 25 min in both artificial gastric fluid (AGF) and artificial intestinal fluid (AIF). Drug content was observed between 97.1 % and 99.8 %, indicating compliance with the limits of pharmacopeia (85-115 %). An in vitro release study of batches was greater than 80 % within 25 min. Conclusion: All batches of clopidogrel bisulfate were manufactured within the criteria of tablet manufacturing. The quality control tests of tablets showed acceptable pharmaceutical properties (effectiveness and safety) that lie within the limits of USP pharmacopeia.

scholarly journals ORAL GENTAMICIN PREPARATION USING SOLIDIFIED LIPID PARTICULATE DELIVERY SYSTEM

2017 ◽  
Vol 9 (9) ◽  
pp. 22
Author(s):  
Musiliu Adedokun ◽  
Tenderwealth Jackson ◽  
Kelechi Uchegbu ◽  
Anthony Attama
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Delivery System ◽  
In Vitro Release ◽  
Zero Order ◽  
Lipid Matrix ◽  
Mean Particle Size ◽  
Release Study ◽  
Vitro Release

Objective: Despite the broad pharmacological activity of gentamicin against a number of bacteria, it's very inadequate oral bioavailability due to poor intestinal membrane permeability has limited its formulation into oral dosage delivery system. This work was thus aimed at formulation and evaluation of gentamicin-loaded microemulsions based on preparation of lipid matrix for sustained release delivery.Methods: Oral gentamicin suspensions were prepared by emulsification method using Tween 80 as a mobile surfactant in the lipid matrix dispersion. The resultant oral suspensions were evaluated for mean particle size and morphology using a photomicrograph, encapsulation efficiency/entrapment, EE (%), dispersibility, pH and absolute drug content. Release study as a function of inhibition zone diameter (IZD) and in vitro release study was also carried out. The in vitro release study was performed in both simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) respectively. The release data were analyzed mathematically according to zero order, first order and Higuchi equations.Results: The prepared suspensions were cream-white in colour, easily dispersed and well homogenized. Batch D, which had least amount of excipients incorporated into the lipid matrix showed clumped irregular-shaped and less free-flowing particles. The particle size was significantly influenced by lipid matrix combination ratio in the presence of a surfactant (p<0.05). The mean particle size diameters of the samples were 15.44 mm, 10.64 mm, 4.12 mm, and 2.70 mm for batches A, B, C and D respectively. The values of EE obtained varied between 47% and 59% with Batch B exhibiting the highest value. The Higuchi model gave the best release kinetics result followed by zero order kinetics.Conclusion: Oral gentamicin prepared exhibited antibacterial properties against Klebsiella spp., Escherchia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa. The results suggest that a lipid matrix system could be useful as a sustained release oral delivery system of a poorly absorbable drug such as gentamicin.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Development, in vitro and in vivo Evaluations of Solid-Lipid Microparticles based on Solidified Micellar Carrier System for Oral Delivery of Cefepime

2017 ◽  
Vol 10 (1) ◽  
pp. 3582-3593
Author(s):  
Chukwuebuka Umeyor ◽  
Uchechukwu Nnadozie ◽  
Anthony Attama
Keyword(s):  
Oral Delivery ◽  
In Vitro Release ◽  
Carrier System ◽  
Solid Lipid ◽  
Solid Lipid Microparticles ◽  
Release Study ◽  
Lipid Microparticles ◽  
Vitro Release

This study seeks to formulate and evaluate a solid lipid nanoparticle-based, solidified micellar carrier system for oral delivery of cefepime. Cefepime has enjoyed a lot of therapeutic usage in the treatment of susceptible bacterial infections; however, its use is limited due to its administration as an injection only with poor patient compliance. Since oral drug administration encourage high patient compliance with resultant effect in improved therapy, cefepime was formulated as solid lipid microparticles for oral delivery using the concept of solidified micellar carrier system. The carrier system was evaluated based on particle yield, particle size and morphology, encapsulation efficiency (EE %), and thermal analysis using differential scanning calorimeter (DSC). Preliminary microbiological studies were done using gram positive and negative bacteria. In vitro release study was performed using biorelevant media, while in vivo release study was performed in white albino rats. The yield of solid lipid microparticles (SLM) ranged from 84.2 – 98.0 %. The SLM were spherical with size ranges of 3.8 ± 1.2 to 42.0 ± 1.4 µm. The EE % calculated ranged from 83.6 – 94.8 %. Thermal analysis showed that SLM was less crystalline with high potential for drug entrapment. Microbial studies showed that cefepime retained its broad spectrum anti-bacterial activity. In vitro release showed sustained release of cefepime from SLM, and in vivo release study showed high concentration of cefepime released in the plasma of study rats. The study showed that smart engineering of solidified micellar carrier system could be used to improve oral delivery of cefepime.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

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