scholarly journals Development of Duloxetine Hydrochloride Tablets for Delayed and Complete Release Using Eudragit L 100

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
M. Yasmin Begum ◽  
Ali Alqahtani ◽  
Mohammed Ghazwani ◽  
Noura Abdullah Alhamood ◽  
Umme Hani ◽  
...  
Keyword(s):  
Toxic Substance ◽  
Dip Coating ◽  
Gastric Fluid ◽  
Dissolution Profile ◽  
Enteric Coating ◽  
Compression Technique ◽  
Duloxetine Hydrochloride ◽  
Enteric Coated ◽  
The One

The purpose of the research was to optimize the preparation of duloxetine hydrochloride (duloxetine HCl) delayed release tablets. Duloxetine HCl produces a toxic substance called alpha-naphthol when duloxetine HCl is in contact with gastric fluid. Thus, duloxetine HCl when given orally needed a protective enteric coating that disable the delivery of duloxetine HCl in gastric fluid while enabling the drug delivery only in small intestine. Four different core tablets were prepared by direct compression technique, and the one which displayed quick disintegration and dissolution was chosen for enteric coating. The compressed tablets were enteric coated by dip coating technique. Since subcoating is required to safeguard the enteric coating, the core tablets were subcoated by using polymer HPMC K15M and then enteric coated with Eudragit L 100. The prepared tablets were assessed for the entire precompression and postcompression characteristics. FTIR study revealed the existence of all prominent peaks signifying its compatibility and authenticity. The in vitro studies showed that enteric-coated tablets were capable of restricting release in acidic media. The formulation F8 was optimised with 5% and 15% increase in weight of seal coat and enteric coat with good dissolution profile. Stability studies revealed that the optimized formulation was intact without any deterioration for 3 months. In conclusion, the optimized formulation could resist the drug release in acidic environment of gastrointestinal region and release the drug at a time once the tablet reaches the intestine.

scholarly journals Eight enteric-coated 50 mg diclofenac sodium tablet formulations marketed in Saudi Arabia: in vitro quality evaluation

2020 ◽  
Vol 13 (1) ◽  
Author(s):  
Muhammad M. Hammami ◽  
Rajaa F. Hussein ◽  
Reem AlSwayeh ◽  
Syed N. Alvi
Keyword(s):  
Quality Evaluation ◽  
Diclofenac Sodium ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
United States Pharmacopoeia ◽  
Weight Variation ◽  
Tablet Formulations ◽  
Enteric Coated

Abstract Objective To evaluate in vitro quality of enteric-coated 50 mg diclofenac sodium tablet formulations on Saudi market. Results A reference and seven generic (G1-7) formulations were commercially available in December 2019/January 2020 and were assessed within 25–75% of manufacture-expiration period. Weight variation (range as% difference from mean, n = 20), active substance content (ASC, mean (SD) as% difference from label, n = 20), hardness (mean (SD), n = 10), and friability (% weight loss, n = 20) were 97–103%, 102.0% (3.4%), 15.4 (1.1) kg, and 0.24%, respectively, for the reference. For G2-7, they were ≤ ±5%, 98.6% (4.0%) to 109.9% (1.8%), 11.9 (0.9) to 18.3 (0.8) kg, and ≤ 0.00 to 0.75%, respectively. G1 ASC, hardness, and friability were 111.3% (1.7%), 20.1 (1.7) kg, and 1.10%, respectively. Disintegration time (n = 6) and dissolution profile (n = 8) were also determined. No formulation disintegrated or released ˃ 0.1% of label ASC in 0.1 N HCl for 2 h. The reference disintegrated in 15:00 min:seconds and released a mean (range) of 100% (99–103%) of label ASC by 45 min in phosphate buffer (pH = 6.8). G1-7 disintegrated in 8:53 to 20:37 min:seconds and released 81% (69–90%) (G1) to 109%. Except for borderline performance of G1, all formulations passed in vitro quality tests according to United States Pharmacopoeia.

Maraviroc Oral Disintegration Tablet: Analytical Design of Experiments (DoE) for Assessment and Comparison of In-Vitro Dissolution Profiles

2021 ◽  
Vol 17 ◽  
Author(s):  
Akula Ramesh ◽  
Jagadish P C ◽  
Vinay Jhawar ◽  
Proneel Das ◽  
Prajakta Patil ◽  
...  
Keyword(s):  
Drug Product ◽  
Hplc Method ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Compression Technique ◽  
Disintegration Time ◽  
Reference Drug ◽  
Orally Disintegrating Tablet ◽  
Rp Hplc

Background: The bioavailability of a drug in a solid oral dose depends on its release from the drug product and its balance in dissolution. Compared with a reference drug, the newly developed formulation needs to establish bioequivalence by comparing the dissolution profile. Objective: To compare dissolution profiles of a newly developed maraviroc oral disintegration tablet and the reference Axentri® tablet. The current research was designed to establish and validate an integral analytical consistency by Quality by Design (QbD) approach to quantify maraviroc from dissolution samples using the RP-HPLC method. Methods: Maraviroc was formulated into an orally disintegrating tablet using a direct compression technique at different concentrations of sodium starch glycolate as super disintegrants and talc and magnesium stearate as glidants. The dissolution test in 0.1N HCl was performed according to standard procedures to predict bioequivalence. The results of dissolution tests were analyzed using the QbD Box Behnken Design multivariate RP-HPLC method. Results: The optimized formulation (F2) was selected as it showed 90% drug release in 5 min and a disintegration time of 22 sec with dissolution profiles to the marketed reference to meet the FDA requirements of f2 similarity factor statistics. The integrated analytical QbD method was statistically analyzed by ANOVA, counter-plot, and 3D response surface plots, which demonstrated that the model is statistically significant. The developed method was validated as per ICH guidelines Q2 (R1). Conclusion : In conclusion, maraviroc oral disintegrating tablets have been well prepared, and superior statement consistency is established by the implementation of the QbD analytical method for orally disintegrating tablet excellence and adoption.

scholarly journals Various approaches to enhance the dissolution of Lornoxicam fast dissolving tablets prepared by using different categories of superdisintegrants: A comparative study

2018 ◽  
Vol 4 (1) ◽  
pp. 86-102 ◽  
Author(s):  
A. Acharya ◽  
G.B.K. Kumar ◽  
P. Goudanavar ◽  
K. Dhakal
Keyword(s):  
Guar Gum ◽  
Rapid Onset ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Onset Of Action ◽  
Compression Technique ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Recent Developments

Background: Recent developments in fast dissolving tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets.The main objective of the present study is to formulate fast dissolving tablet of Lornoxicam by direct compression method.Methods: Guar gum and crospovidone were used as natural and synthetic superdisintegrants respectively. Fast dissolving tablet of Lornoxicam were prepared by direct compression technique using three different approaches; superdisintegrant addition, sublimation, and solid dispersion.Results: IR and DSC studies showed no interaction between the drug and the excipients. All formulation showed disintegration time ranging from 16.09-42.54 second. Wetting time and disintegration time decreased by increasing the super disintegrant concentration from 2.5% to 5% w/w. Formulae L16 gave the best in- vitro disintegration and dissolution results, which would be due to swelling effect of Gaur gum and amorphization of the drug during the solid dispersion preparation.The best formulation L16 was subjected to stability testing for 3 month and results showed no significant change in appearance, hardness, drug content and dissolution profile of the tablets, hence tablet is stable throughout its stability studies.Conclusion: It was concluded that fast dissolving tablets of Lornoxicam were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance.JMMIHS,2018;4(1):86-102

scholarly journals In Vitro Dissolution Profile of Dapagliflozin: Development, Method Validation, and Analysis of Commercial Tablets

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Rafaela Zielinski Cavalheiro de Meira ◽  
Aline Biggi Maciel ◽  
Fabio Seigi Murakami ◽  
Paulo Renato de Oliveira ◽  
Larissa Sakis Bernardi
Keyword(s):  
Quality Evaluation ◽  
Systematic Approach ◽  
Gastric Fluid ◽  
Scientific Basis ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Dissolution Profile ◽  
Sodium Glucose Cotransporter ◽  
Dissolution Efficiency

Dapagliflozin was the first of its class (inhibitors of sodium-glucose cotransporter) to be approved in Europe, USA, and Brazil. As the drug was recently approved, there is the need for research on analytical methods, including dissolution studies for the quality evaluation and assurance of tablets. The dissolution methodology was developed with apparatus II (paddle) in 900 mL of medium (simulated gastric fluid, pH 1.2), temperature set at 37±0.5°C, and stirring speed of 50 rpm. For the quantification, a spectrophotometric (λ=224 nm) method was developed and validated. In validation studies, the method proved to be specific and linear in the range from 0.5 to 15 μg·mL−1 (r2=0.998). The precision showed results with RSD values lower than 2%. The recovery of 80.72, 98.47, and 119.41% proved the accuracy of the method. Through a systematic approach by applying Factorial 23, the robustness of the method was confirmed (p>0.05). The studies of commercial tablets containing 5 or 10 mg demonstrated that they could be considered similar through f1, f2, and dissolution efficiency analyses. Also, the developed method can be used for the quality evaluation of dapagliflozin tablets and can be considered as a scientific basis for future official pharmacopoeial methods.

scholarly journals Formulation and Dissolution Study of Valsartan Immediate Release Tablets

2013 ◽  
Vol 1 (02) ◽  
pp. 01-08
Author(s):  
B. Brahmaiah ◽  
K. Sasikanth ◽  
Sreekanth Nama ◽  
P. Suresh ◽  
Patan Adam Khan
Keyword(s):  
Potato Starch ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Compression Technique ◽  
Dissolution Studies ◽  
Main Motive

In the present study, design of oral immediate release tablets of Valsartan by direct compression technique was carried out. The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S) in different ratios. The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate. To determine the best fit dissolution profile for the dosage forms. Valsartan tablets were formulated by using microcrystalline cellulose (diluents), potato starch, acacia (binder) and magnesium stearate (lubricant). The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. The In-vitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.

scholarly journals Design of Catalase Monolithic Tablets for Intestinal Targeted Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 69
Author(s):  
Mirna Alothman ◽  
Pompilia Ispas-Szabo ◽  
Mircea Alexandru Mateescu
Keyword(s):  
Targeted Delivery ◽  
Intestinal Inflammation ◽  
Gastric Fluid ◽  
Oral Dosage ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
Negative Effects ◽  
Simulated Intestinal Fluid

Several studies confirmed a correlation between elevated hydrogen peroxide (H2O2) levels in patients with intestinal bowel diseases (IBD) and the negative effects caused by its presence. The objective of this study was to explore the potential use of catalase (CAT) to diminish the level of H2O2 and its deleterious action on intestinal mucosa. Oral dosage forms of a CAT bioactive agent targeted to the intestines were designed and tested in various simulated gastric and intestinal media. Monolithic tablets (30% loading) were prepared using commercial CarboxyMethylCellulose (CMC) or synthesized CarboxyMethylStarch (CMS) and TriMethylAmineCarboxyMethylStarch (TMACMS) as matrix-forming excipients. For starch derivatives, the presence of the ionic groups (carboxymethyl and trimethylamine) was validated by spectral analysis. In vitro studies have shown that tablets formulated with TMACMS and 30% CAT resisted the acidity of the simulated gastric fluid and gradually released the enzyme into the simulated intestinal fluid. The investigation of the CAT release mechanism revealed the role of anionic and cationic groups of polymeric excipients and their involvement in the modulation of the CAT dissolution profile. The proposed drug delivery system can be considered an efficient solution to target CAT release in the intestine and contribute to the reduction of H2O2 associated with intestinal inflammation.

In-vitro Fundamental Assessment of Disintegration and Dissolution Profile of Enteric Coated Rabeprazole Tablet Commercially Accessible in Bangladesh

2015 ◽  
Vol 6 (6) ◽  
pp. 423-428
Author(s):  
Shaila Eamen ◽  
M. Islam ◽  
Safinaj Alam ◽  
M. Pk ◽  
M. Mucktady ◽  
...  
Keyword(s):  
Dissolution Profile ◽  
Enteric Coated

scholarly journals Formulation of enteric coated microspheres containing pantoprazole

2021 ◽  
Vol 63 (3) ◽  
pp. 56-62
Author(s):  
Xuan Truong Le ◽  
◽  
Hue Minh Nguyen ◽  
Ngoc Quynh Le ◽  
Thi Thu Loan Trinh ◽  
...  
Keyword(s):  
Gastric Acid ◽  
Morphological Characteristics ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
In Vitro Drug Release ◽  
Enteric Coated ◽  
Inhibitor Drug ◽  
Emulsification Solvent Evaporation ◽  
Average Size

Pantoprazole is a first-line proton pump inhibitor drug for the treatment of gastric acid secretion disorders that is known to have minimal side effects and drug interactions. To improve its stability in gastric acid, delayed-release microspheres containing pantoprazole was prepared by emulsification-solvent evaporation using a polymer-containing mixture of hydroxypropyl cellulose (HPC) and ethyl cellulose (EC), which was then coated by alginate and EudragitL100. The morphological characteristics of the microspheres were examined by SEM, the particle size distribution inferred by laser diffraction, and the physical state of drug substance was measured by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and in vitro drug release. The three formulations of microspheres chosen for this study had an average size of 100 μm. The dissolution profile showed less than 10% of the drug was released after 120 min in 0.1-M HCl and more than 75% of drug was released after 45 min in a phosphate buffer with a pH of 6.8.

scholarly journals In Vitro Biological and Antimicrobial Properties of Chitosan-based Bioceramic Coatings on Zirconium

2021 ◽  
Author(s):  
Salim Levent Aktug ◽  
Salih Durdu ◽  
Selin Kalkan ◽  
Kultigin Cavusoglu ◽  
Metin Usta
Keyword(s):  
Antimicrobial Properties ◽  
Dip Coating ◽  
Thermal Cracks ◽  
Coating Method ◽  
Micro Arc Oxidation ◽  
Edx Analyses ◽  
Dip Coating Method ◽  
The One ◽  
Bioceramic Coatings

Abstract Ca-based porous and rough bioceramic surfaces were coated on zirconium by micro arc oxidation (MAO). Subsequently, an antibacterial chitosan layer was covered on the MAO-coated zirconium surfaces by dip coating method to develop an antibacterial, bioactive and biocompatible composite biopolymer and bioceramic layer for implant applications. The cubic-ZrO2, meta-stable Ca0.15Zr0.85O1.85, and Ca3(PO4)2 were detected on the MAO surface by powder-XRD. The existence of chitosan on the MAO-coated Zr surfaces was verified by FTIR. The micro-pores and thermal cracks on the bioceramic MAO surface were sealed by chitosan coating, while the MAO surface is porous and rough. All elements such as Zr, O, Ca, P and C were homogenously distributed through both surfaces. Moreover, both surfaces indicated hydrophobic properties. However, the contact angle value of the MAO surface was lower than the one of chitosan-based MAO surface. In vitro bioactivity on both surfaces was investigated by XRD, SEM and EDX analyses at post-immersion in simulated body fluid (SBF) up to 14 days. In vitro bioactivity was significantly enhanced on the chitosan-based MAO surface with respect to the MAO surface. In vitro bacterial adhesions on the chitosan-based MAO surfaces were lower compared to the MAO surfaces for Staphylococcus aureus and Escherichia coli.

scholarly journals Factors Contributing to Drug Release From Enteric-Coated Omeprazole Capsules: An In Vitro and In Vivo Pharmacokinetic Study and IVIVC Evaluation in Beagle Dogs

Dose-Response ◽  
2020 ◽  
Vol 18 (1) ◽  
pp. 155932582090898
Author(s):  
Cheng Cui ◽  
Jiabei Sun ◽  
Xueqing Wang ◽  
Zhenxi Yu ◽  
Yaqin Shi
Keyword(s):  
Drug Release ◽  
Critical Factor ◽  
Pharmacokinetic Studies ◽  
Beagle Dogs ◽  
Enteric Coating ◽  
Coating Materials ◽  
Enteric Coated ◽  
Release Profiles

This study was performed to explore factors influencing the release of the proton pump inhibitor omeprazole from enteric-coated capsules in vitro and absorption in vivo in beagle dogs. Enteric-coated pellets with different enteric coating materials and coating levels were designed and prepared. All self-prepared formulations were characterized in vitro as well as in vivo and compared to the brand and generic commercial products. Evaluation of the corresponding release profiles suggested that coating material was the most critical factor. Enteric coating level determined the lag time before initiation of drug release, and subcoating level affected the drug release rate. Pharmacokinetic studies were performed in beagle dogs to further confirm the influence of formulation factors on drug absorption. Medium at pH 6.8 was a more biorelevant condition for in vitro drug release tests, although medium at pH 6.0 was better for discriminating release profiles of different formulations. A multiple level C in vitro/in vivo correlation was preliminarily established by which Tmax and Cmax of omeprazole formulations could be predicted with release parameters such as Tlag and T25. These results may facilitate quality evaluation and potentially improve the clinical efficacy of generic omeprazole products.

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