scholarly journals Evaluation of the Release of Ascorbic Acid in Prolonged-Release Tablets by in vitro Dissolution Tests

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
E.Damasceno Junior ◽  
J. M. F. DE Almeida ◽  
I. N. Silva ◽  
M. S. B. Silva ◽  
N. S. Fernandes
Keyword(s):  
Ascorbic Acid ◽  
Absorption Spectroscopy ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Molecular Absorption ◽  
Dissolution Medium ◽  
Dissolution Tests ◽  
Molecular Absorption Spectroscopy

In vitro dissolution tests are an extremely important tool in the development and quality control of drugs, making it possible to evaluate the performance or efficiency of the pharmaceutical form in releasing the active substance through the amount dissolved in the dissolution medium when the product is subjected to specific equipment. In this sense, the main objective of the present study was to evaluate the release of ascorbic acid in prolonged release commercial vitamin C tablets by dissolution tests. Ascorbic acid and drugs of two different brands were characterized using the techniques of Molecular Absorption Spectroscopy in the Region of Infrared (IR), Thermogravimetry/Derived Thermogravimetry (TG/DTG) and Differential Scanning Calorimetry (DSC). The in vitro dissolution tests were performed in a dissolver with a paddle apparatus at a temperature of 37°C (± 0.5°C), employing 900 mL of ultrapure water as the dissolution medium and a stirring speed of 50 rpm. The ascorbic acid dissolved in the aliquots of dissolution media obtained during the tests were quantified using the UV-Vis Molecular Absorption Spectroscopy technique. From the dissolution profiles, it was observed that the formulations of both brands promoted a prolonged release of ascorbic acid. The brand drug A dissolved about 67% of the active principle in about 360 minutes. The brand drug B, however, dissolved about 72% at the same dissolution time. Release kinetics was evaluated using kinetic models such as order zero, first order and Higuchi. The model that best fit the experimental data was that of Higuchi.

scholarly journals In Vitro Dissolution Evidence for Sustained and Prolonged Release of Vitamin C in a Phosphatidyl Choline-Enriched Lipid Encapsulation

2021 ◽  
Vol 5 (Supplement_2) ◽  
pp. 1328-1328
Author(s):  
Mastaneh Sharafi ◽  
Tyler White ◽  
Kelli Fowler ◽  
Kevin Ewell ◽  
Noe Galvan ◽  
...  
Keyword(s):  
Ascorbic Acid ◽  
Los Angeles ◽  
Vitamin C ◽  
Phosphatidyl Choline ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Prolonged Release ◽  
Lauryl Sulfate

Abstract Objectives In vitro dissolution tests are valuable first-step tools in the development of bioavailable delivery systems, making it possible to assess the performance of novel technologies in releasing active ingredients through the amount dissolved in a dissolution medium. The objective of this study was to evaluate whether phosphatidyl choline-enriched lipid encapsulation releases the majority of vitamin C as ascorbic acid past the stomach in a standard in vitro dissolution procedure and to assess the release profile. Methods A novel phosphatidyl choline-enriched lipid encapsulation that is solid at room temperature was tested for dissolution in a standard dissolution apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. One serving (included 1000 mg ascorbic acid) was placed into vessels containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.8) for an additional 360 minutes. Aliquots were tested for ascorbic acid concentration at 8 time points by titration. The data was compared with 1000 mg of regular ascorbic acid in a capsule format. Results The phosphatidyl choline-enriched lipid encapsulation released 36% of the vitamin C at 2 hours in the acid phase and released 56% at 3 hours, 67% at 4 hours, 85% at 6 hours and 98% at 8 hours in the intestinal phase. Regular vitamin C filled capsules released 100% of the vitamin C at 30 minutes. Conclusions The dissolution results indicated that phosphatidyl choline-enriched lipid encapsulation can pass the stomach and release the majority of vitamin C in the small intestine. The encapsulation demonstrated a sustained and prolonged release of vitamin C over an 8 hour period. The release profile observed in this in vitro study suggests phosphatidyl choline-enriched lipid encapsulation may improve nutrient absorption and bioavailability which requires further testing including human clinical trials. Funding Sources This study was supported by Lonza (Greenwood, SC) and Ritual (Natals Inc, Los Angeles, CA).

scholarly journals Dissolution Test for Mianserin Hydrochloride in Tablets

2019 ◽  
Vol 3 (2) ◽  
pp. 18-22
Author(s):  
Letícia Lenz Sfair ◽  
Caren Gobetti ◽  
Martin Steppe ◽  
Elfrides Schapoval
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Drug Release Profile ◽  
Dissolution Tests ◽  
Usp Apparatus ◽  
Usp Apparatus 2

A dissolution test for mianserin hydrochloride in coated tablets containing 30 mg was developed and validated using a fast ultraviolet spectrophotometric method. The appropriate conditions were determinate after testing sink conditions, agitation spped and dissolution medium. The sink conditions tested showed that mianserin hydrochloride was soluble in 0.01 and 0.1 M hydrochloric acid (HCl), acetate buffer pH 4.1 and 5.0 and phosphate buffer pH 6.8. Then, dissolution tests were performed to investigate the drug release in each medium. Optimal conditions to carry out the dissolution test were 900 mL 0.1 M HCl and USP apparatus 2 (paddle) at 50 rpm stirring speed. The quantification method was also adapted and validated. The UV method showed specificity, linearity, precision and accuracy. The in vitro dissolution test can be used to evaluate the drug release profile and the data was used as an aid to establish a possible correlation with in vivo data.

Study on the Formulation and Pharmacotechnical Characterization of Hydrophilic Matrix Tables with Amiodarone Chlorhydrate

2019 ◽  
Vol 70 (1) ◽  
pp. 1-5
Author(s):  
Andreea Creteanu ◽  
Alina Stefanache ◽  
Madalina Vieriu ◽  
Gladiola Tantaru ◽  
Lacramioara Ochiuz
Keyword(s):  
In Vitro Release ◽  
Pharmaceutical Product ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Class Iii ◽  
Dose Uniformity ◽  
Dissolution Tests

The study is based on new oral matrix tablets based on Kollidon®SR and chitosan, formulated in order to optimize the low oral bioavailability of amiodarone, a class III antiarrhythmic drug. Pharmacotechnical characterization included the analysis of flowability and compressibility properties (flow time, friction coefficient, angle of repose, Hausner ratio, Carr Index), and of pharmaco-chemical characteristics (mass and dose uniformity, thickness, diameter, mechanical strength, friability, degree of softening, in vitro release profile) of the tablets obtained using direct compression method. The results obtained have shown that both Kollidon®SR and chitosan may be used as matrix forming agents when combined with amiodarone. In vitro dissolution tests revealed that the nine formulations studied provided a prolonged release of amiodarone when compared to an industrial pharmaceutical product formulated as conventional release tablets.

scholarly journals Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug labetalol

2018 ◽  
Vol 8 (6-s) ◽  
pp. 187-191 ◽  
Author(s):  
Surendranath Betala ◽  
M. Mohan Varma ◽  
K. Abbulu
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Spherical Geometry ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Dissolution Medium

Labetalol is an adrenergic receptor blocking agent used in the treatment of hypertension and characterized by high solubility and high permeability which corresponds to BCS class I drug. Plasma half life ranges from 6 & bioavailability is 25%. Ethyl cellulose was used as a rate controlling polymer. Effects of addition of ethyl cellulose on in vitro dissolution were studied. Nanoparticles were formulated using different polymer ratios. In vitro drug release was carried out by using USP Type II at 50 rpm in 900 ml of acidic dissolution medium (pH 1.2) for 2 hours, followed by 900 ml alkaline dissolution medium (pH7.4) for 12 hours. Mean dissolution time is used to characterize drug release rate from a dosage form. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Excipients are selected by FTIR studies. Finally the nanoparticles were evaluated for various characteristics like encapsulation efficiency, percentage yield, partial size and the In vitro release for 12 hrs.  The nanoparticles were found to be discrete, spherical, and free-flowing.  The nanoparticles were uniform in size, and the microencapsulation efficiency was in the range of 52.5-81.7%. The surface morphology of prepared Labetalol nanoparticles was observed under scanning electron Microscopy. Nanoparticles had good spherical geometry. The stability study was performed at 40ºC ± 2ºC and 75 ± 5% RH for 6 months. Keywords: Nanoparticles; Labetalol, Hypertension, Ethyl Cellulose, Dissolution, entrapment efficiency.

Gastroretentive System of Fluvastatin Sodium by Using Natural Mucilage and Synthetic Polymer

2014 ◽  
Vol 4 (2) ◽  
Author(s):  
Umamaheswara G. ◽  
Anudeep D.
Keyword(s):  
Half Life ◽  
Release Kinetics ◽  
Kinetic Studies ◽  
Diffusion Path ◽  
Synthetic Polymer ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Drug Content ◽  
Biological Half Life

Fluvastatin sodium is a novel compound used as cholesterol lowering agent which acts through the inhibition of 3- hydroxyl-3- methyl glutaryl- coenzyme A (HMG-Co A) reductase. It has short biological half life (1-3h) in humans required a dosing frequency of 20 to 40mg twice a day. Due to its short variable biological half life it has been developed to a sustained gastroretentive system with a natural and synthetic polymer and to study how far the natural mucilage improves the sustained activity. Floating tablets were prepared by direct compression method using in combination of natural mucilage and synthetic polymer. Prior to the preparation of tablets the physical mixtures were subjected to FT IR studies and pre compression parameters. After preparation of tablets they were subjected to various tests like swollen index, drug content, In vitro dissolution and release kinetics with pcp disso software etc. The tablets prepared by direct compression shown good in thickness, hardness and uniformity in drug content, the prepared tablets floated more than 12h except FS1 and FS2 shows 9 and 11h. Swollen index studies shows with increase in concentration of polymer the swelling increases the diffusion path length by which the drug molecule may have to travel and cause lag time. In vitro results shows that on increasing the amount of hibiscus polymer the sustain activity is increased because of its integrity and forms a thick swollen mass and reduces the erosion property of the HypromelloseK100M, kinetic studies shows that FS 1, FS2, FS3 followed the Korsmeyer peppas model and the rest FS 4, FS 5, FS6 follows the zero order respectively. Based on n value indicating that the drug release followed super case II transport mechanism due to the erosion of the polymer.

scholarly journals Design and characterization of 3D printed, neomycin-eluting poly-L-lactide mats for wound-healing applications

2021 ◽  
Vol 32 (4) ◽  
Author(s):  
Mahima Singh ◽  
Sriramakamal Jonnalagadda
Keyword(s):  
Release Kinetics ◽  
Biological Properties ◽  
In Vitro Dissolution ◽  
3D Printer ◽  
Topical Antibiotic ◽  
Young’S Moduli ◽  
Base Polymer ◽  
Potential Applications ◽  
3D Printed

AbstractThis study evaluates the suitability of 3D printed biodegradable mats to load and deliver the topical antibiotic, neomycin, for up to 3 weeks in vitro. A 3D printer equipped with a hot melt extruder was used to print bandage-like wound coverings with porous sizes appropriate for cellular attachment and viability. The semicrystalline polyester, poly-l-lactic acid (PLLA) was used as the base polymer, coated (post-printing) with polyethylene glycols (PEGs) of MWs 400 Da, 6 kDa, or 20 kDa to enable manipulation of physicochemical and biological properties to suit intended applications. The mats were further loaded with a topical antibiotic (neomycin sulfate), and cumulative drug-release monitored for 3 weeks in vitro. Microscopic imaging as well as Scanning Electron Microscopy (SEM) studies showed pore dimensions of 100 × 400 µm. These pore dimensions were achieved without compromising mechanical strength; because of the “tough” individual fibers constituting the mat (Young’s Moduli of 50 ± 20 MPa and Elastic Elongation of 10 ± 5%). The in vitro dissolution study showed first-order release kinetics for neomycin during the first 20 h, followed by diffusion-controlled (Fickian) release for the remaining duration of the study. The release of neomycin suggested that the ability to load neomycin on to PLLA mats increases threefold, as the MW of the applied PEG coating is lowered from 20 kDa to 400 Da. Overall, this study demonstrates a successful approach to using a 3D printer to prepare porous degradable mats for antibiotic delivery with potential applications to dermal regeneration and tissue engineering.

scholarly journals Automation of dissolution tests

2003 ◽  
Vol 25 (1) ◽  
pp. 7-15 ◽  
Author(s):  
Rolf Rolli
Keyword(s):  
Quality Control ◽  
In Vitro Dissolution ◽  
Pharmaceutical Companies ◽  
Dissolution Testing ◽  
Simultaneous Operation ◽  
Task Forces ◽  
The Core ◽  
Dissolution Tests ◽  
The 1960S

Dissolution testing of drug formulations was introduced in the 1960s and accepted by health regulatory authorities in the 1970s. Since then, the importance of dissolution has grown rapidly as have the number of tests and demands in quality-control laboratories. Recent research works lead to the development of in-vitro dissolution tests as replacements for human and animal bioequivalence studies. For many years, a lot of time and effort has been invested in automation of dissolution tests. There have been a number of in-house solutions from pharmaceutical companies and many have created task forces or even departments to develop automation. Robotic solutions with sequential operation were introduced as well as the simultaneous operation concept developed by SOTAX. Today, pharmaceutical companies focus their resources mainly on the core business and in-house engineering solutions that are very difficult to justify. Therefore, it is important to know the basic considerations in order to plan an automation concept and implement it together with a vendor.

scholarly journals In vitro Release Kinetics Study of Ambroxol Hydrochloride Pellets Developed by Extrusion Spheronization Technique Followed by Acrylic Polymer Coating

1970 ◽  
Vol 7 (1) ◽  
pp. 75-81 ◽  
Author(s):  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Golam Kibria ◽  
Muhammad Rashedul Islam ◽  
Reza-ul Jalil
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Acrylic Polymer ◽  
Eudragit Rs ◽  
Methacrylate Copolymer ◽  
Ambroxol Hydrochloride ◽  
Eudragit Rl ◽  
Extrusion Spheronization

The aim of the present study was to investigate the effect of Ammonio Methacrylate Copolymer Dispersion Type A (Eudragit RL 30 D) and Ammonio Methacrylate Copolymer Dispersion Type B (Eudragit RS 30 D) combination in different weight ratios on the release kinetics of Ambroxol Hydrochloride from coated pellets. Microcrystalline cellulose, lactose, maize starch, hydroxypropyl methylcellulose and the drug was incorporated in the nuclei prepared by Extrusion-Spheronization technique which was coated with Eudragit RL 30D and Eudragit RS 30D in 1:1,1:1.5,1:2,1:2.5 and 1:3 ratios. The in vitro dissolution studies were carried out in 0.1N HCl for 1 hour followed by phosphate buffer (pH 6.8) for 11 h with USP dissolution apparatus Type-II. Drug release decreased with increasing amount of Eudragit RS 30 D in all cases. The drug release followed first order and Higuchi release kinetics. The Korsmeyer plot revealed n=0.50-0.61 or non-Fickian transport mechanism for drug release. From one way ANOVA it was found that the ratio of binary polymer mixer had significant (p < 0.05) effect on drug release. Key words: Aqueous coating, Eudragit, release kinetics, pellet, extrusion-spheronization  DOI = 10.3329/dujps.v7i1.1222 Dhaka Univ. J. Pharm. Sci. 7(1): 75-81, 2008 (June)

scholarly journals Development of a reservoir type prolonged release system with felodipine via simplex methodology

2015 ◽  
Vol 89 (1) ◽  
pp. 128-136
Author(s):  
Rareș Iuliu Iovanov ◽  
Ioan Tomuță ◽  
Sorin Emilian Leucuța
Keyword(s):  
Simplex Method ◽  
Release Kinetics ◽  
Prolonged Release ◽  
Lauryl Sulfate ◽  
Pore Former ◽  
Release System ◽  
Reservoir Type ◽  
Model Drug ◽  
Kinetics Of

Background and aims. Felodipine is a dihydropyridine calcium antagonist that presents good characteristics to be formulated as prolonged release preparations. The aim of the study was the formulation and in vitro characterization of a reservoir type prolonged release system with felodipine, over a 12 hours period using the Simplex method.Methods. The first step of the Simplex method was to study the influence of the granules coating method on the felodipine release. Furthermore the influence of the coating polymer type, the percent of the coating polymer and the percent of pore forming agent in the coating on the felodipine release were studied. Afterwards these two steps of the experimental design the percent of Surelease applied on the felodipine loaded granules and the percent of pore former in the polymeric coating formulation variables were studied. The in vitro dissolution of model drug was performed in phosphate buffer solution (pH 6.5) with 1% sodium lauryl sulfate. The released drug quantification was done using an HPLC method. The release kinetics of felodipine from the final granules was assessed using different mathematical models.Results. A 12 hours release was achieved using granules with the size between 315 – 500 µm coated with 45% Surelease with different pore former ratios in the coating via the top-spray method.Conclusion. We have prepared prolonged release coated granules with felodipine using a fluid bed system based on the Simplex method. The API from the studied final formulations was released over a 12 hours period and the release kinetics of the model drug substance from the optimized preparations fitted best the Higuchi and Peppas kinetic models. 

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

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