A New Approach to the Dissolution Tests Management to Obtain Kinetic and Thermodynamic Data: Release of a Model Drug from Glyceryl Behenate Matrix Tablets

2021 ◽  
pp. 2000235
Author(s):  
Barbora Slezáková ◽  
Kevin Matzick ◽  
Alena Komersová ◽  
Václav Lochař ◽  
Martin Bartoš ◽  
...  
Keyword(s):  
Thermodynamic Data ◽  
Matrix Tablets ◽  
New Approach ◽  
Dissolution Tests ◽  
Glyceryl Behenate ◽  
Data Release ◽  
Model Drug

Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma
Keyword(s):  
Phosphate Buffer ◽  
Guar Gum ◽  
Oral Route ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Caecal Content ◽  
Model Drug

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.

scholarly journals Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 804
Author(s):  
Ewelina Juszczyk ◽  
Kamil Kisło ◽  
Paweł Żero ◽  
Ewa Tratkiewicz ◽  
Maciej Wieczorek ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Sustained Release ◽  
Development Strategy ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Mechanical Agitation ◽  
Development Cycle ◽  
Dissolution Tests ◽  
Sustained Release Tablets ◽  
Biopharmaceutical Properties

Sustained-release (SR) formulations may appear advantageous in first-in-human (FIH) study of innovative medicines. The newly developed SR matrix tablets require prolonged maintenance of API concentration in plasma and should be reliably assessed for the risk of uncontrolled release of the drug. In the present study, we describe the development of a robust SR matrix tablet with a novel G-protein-coupled receptor 40 (GPR40) agonist for first-in-human studies and introduce a general workflow for the successful development of SR formulations for innovative APIs. The hydrophilic matrix tablets containing the labeled API dose of 5, 30, or 120 mg were evaluated with several methods: standard USP II dissolution, bio-predictive dissolution tests, and the texture and matrix formation analysis. The standard dissolution tests allowed preselection of the prototypes with the targeted dissolution rate, while the subsequent studies in physiologically relevant conditions revealed unwanted and potentially harmful effects, such as dose dumping under an increased mechanical agitation. The developed formulations were exceptionally robust toward the mechanical and physicochemical conditions of the bio-predictive tests and assured a comparable drug delivery rate regardless of the prandial state and dose labeled. In conclusion, the introduced development strategy, when implemented into the development cycle of SR formulations with innovative APIs, may allow not only to reduce the risk of formulation-related failure of phase I clinical trial but also effectively and timely provide safe and reliable medicines for patients in the trial and their further therapy.

scholarly journals Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 174
Author(s):  
Rebeca Simancas-Herbada ◽  
Ana Fernández-Carballido ◽  
Juan Aparicio-Blanco ◽  
Karla Slowing ◽  
Jorge Rubio-Retama ◽  
...  
Keyword(s):  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Metformin Hydrochloride ◽  
Oral Toxicity ◽  
Crosslinking Degree ◽  
Polymer Swelling ◽  
Hydrophilic Drugs ◽  
Swelling Capacity ◽  
The Matrix ◽  
Model Drug

The potential of a new poly(magnesium acrylate) hydrogel (PAMgA) as a pharmaceutical excipient for the elaboration of matrix tablets for the extended release of highly hydrophilic drugs was evaluated. The polymer was synthetized with two different crosslinking degrees that were characterized by FTIR and DSC. Their acute oral toxicity was determined in a mouse model, showing no toxicity at doses up to 10 g/kg. Matrix tablets were prepared using metformin hydrochloride as a model drug and the mechanisms involved in drug release (swelling and/or erosion) were investigated using biorrelevant media. This new hydrogel effectively controlled the release of small and highly hydrophilic molecules as metformin, when formulated in matrix tablets for oral administration. The rate of metformin release from PAMgA matrices was mainly controlled by its diffusion through the gel layer (Fickian diffusion). The swelling capacity and the erosion of the matrix tablets influenced the metformin release rate, that was slower at pH 6.8, where polymer swelling is more intensive, than in gastric medium, where matrix erosion is slightly more rapid. The crosslinking degree of the polymer significantly influenced its swelling capacity in acid pH, where swelling is moderate, but not in intestinal fluid, where swelling is more intense.

Fabrication of Shellac-Based Effervescent Floating Matrix Tablet as a Novel Carrier for Controlling of Drug Release

2013 ◽  
Vol 747 ◽  
pp. 135-138 ◽  
Author(s):  
Noppadol Chongcherdsak ◽  
Direk Aekthammarat ◽  
Chutima Limmatvapirat ◽  
Sontaya Limmatvapirat
Keyword(s):  
Drug Release ◽  
Equation Model ◽  
Matrix Tablets ◽  
Basic Knowledge ◽  
Matrix Tablet ◽  
Sustained Drug Release ◽  
Factors Affecting ◽  
Model Drug ◽  
High Level ◽  
Power Law Equation

The aim of this research was to elucidate the factors affecting drug release and buoyancy properties of effervescent shellac based matrix tablet. Theophylline was selected as a model drug and sodium bicarbonate was used as a gas forming agent. To fabricate floating matrix tablets, the model drug, gas forming agent and other excipients were blended, compressed and then annealed at 80C for 24 h. The factors affecting floating and drug release, including amount of SHL and gas forming agent were investigated. The result demonstrated that the hardness of all formulations before annealing was within the range of 60+10 N. After annealing process, the hardness was significantly increased especially for formulation containing high level of SHL. The hardness of tablets containing 55% w/w or more of SHL was more than 200 N. As increasing amount of SHL (> 35% w/w), the more sustained drug release was also observed. The results were agreed well with the increased hardness. In addition, the tablets containing 20% w/w or more of gas forming agent were floated in 0.1 N HCl for more than 10 h, suggesting the good buoyancy characteristic. The kinetics of drug release in 0.1N HCl for all formulations were both fitted with Higuchi model and power law equation model, suggesting that the main mechanism of drug release in 0.1N HCl was obeyed the diffusion process. The result from this research could provide the basic knowledge for fabricating of SHL-based floating matrix tablet through varying amount of SHL and gastric forming agent.

A New Approach to Galaxy Morphology. I. Analysis of the Sloan Digital Sky Survey Early Data Release

2003 ◽  
Vol 588 (1) ◽  
pp. 218-229 ◽  
Author(s):  
Roberto G. Abraham ◽  
Sidney van den Bergh ◽  
Preethi Nair
Keyword(s):  
Sloan Digital Sky Survey ◽  
Early Data ◽  
New Approach ◽  
Sky Survey ◽  
Data Release ◽  
Galaxy Morphology

scholarly journals FORMULATION AND EVALUATION OF EFFERVESCENT GASTRO-RETENTIVE FLOATING TABLETS FOR CONTROLLED RELEASE OF AN ANTI-ULCER COMPOUND

2013 ◽  
Vol 3 (1) ◽  
pp. 23-30
Author(s):  
Aleksandar Aleksovski ◽  
◽  
Emina Zahirović ◽  
Amra Demirović ◽  
Emilija Spaseska Aleksovska ◽  
...  
Keyword(s):  
Small Intestine ◽  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Different Types ◽  
Model Drug ◽  
Absorption Window ◽  
Pharmacopoeial Requirements ◽  
Gastro Retentive

Effervescent floating gastro-retentive matrix tablets present novel and promising approach towards targeted and controlled drug delivery in the stomach and in the upper part of the small intestine. This kind of dosage form could be obtained by combining in a suitable ratio effervescent compounds and hydrophilic/hydrophobic polymer/s. The aim of our investigation was to develop controlled release effervescent matrix tablet which will float over the gastric media for longer than 8 hours and will release the active compound in a continuous manner over 8 hours period. We used ranitidine HCl as a model drug which has narrow absorption window in the upper small intestine, and is a good candidate for this type of dosage forms. We employed sodium bicarbonate and citric acid as effervescent compounds and two different types of hydroxypropyl methylcellulose (HPMC K4M and HPMC K15M) as a controlled release hydrophilic polymer. Three batches of tablets were produced (one containing HPMC K4M, other containing HPMC K15M, and the third containing 1:1 mixture of these two polymers) and every batch was compressed with two different forces 5.5 kN and 4.7 kN, so completely six probes of tablets were made. All six probes complied the pharmacopoeial requirements concerning mass uniformity, content, friability and hardness. All six probes tended to float fast to the surface of the medium and tend to hydrate and swell fast enough which actions provided controlled release of the compound over period of 8 hours. No significant differences in the dissolution profiles of all six probes were noticed during the investigation.

scholarly journals Gellan gum and polyvinylpyrrolidone (PVP) as binding agents in extrusion/spheronization pellet formulations

2019 ◽  
Vol 69 (1) ◽  
pp. 99-109 ◽  
Author(s):  
Eduardo José Barbosa ◽  
Humberto Gomes Ferraz
Keyword(s):  
Aspect Ratio ◽  
Immediate Release ◽  
Gellan Gum ◽  
Pellet Size ◽  
Dissolution Tests ◽  
Binding Agents ◽  
Physical Tests ◽  
Model Drug ◽  
Different Response ◽  
Extrusion Spheronization

Abstract The aim of this work was to evaluate gellan gum as binder in pellet formulations, with theophylline as the model drug, in comparison with polyvinylpyrrolidone (PVP). A full 32 factorial design was realized, with binder and diluent factors at three levels each. Pellets were produced by the extrusion/spheronization technique, and dried in a fluid-ized bed. Physical tests and dissolution tests were conducted. The results showed that the binder factor was not significant for pellet size and granulometry distribution. Rather, trends of a different response of gellan gum were identified, in comparison with PVP, in aspect ratio and dissolution tests: more round pellets were obtained in formulations with gellan gum, and more variable dissolution resulted when this polysaccharide was present. Therefore, if the usage of this compound in immediate release pellet formulations is verified, this justifies the interest in the development of sustained release systems using gellan gum.

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug

2020 ◽  
Vol 17 ◽  
Author(s):  
Wasfy M. Obeidat ◽  
Shadi F. Gharaibeh ◽  
Abdolelah A. Jaradat ◽  
Osama Abualsuod
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Sustained Drug Release ◽  
Basic Drug ◽  
Basic Model ◽  
Polymeric Compositions ◽  
Model Drug

Objective: The objective of this study was to evaluate the suitability of ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Methods: Matrix tablets formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8 and 6.8). Tablets made of low to intermediate proportions of sodium alginate and an approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have significant modification of drug release rates. Result: Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Conclusion: Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of weakly basic drug.

Ultrasound Effect on Swelling Properties and Drug Release Behaviors of Spray-Dried Tapioca Starch Tablets

2013 ◽  
Vol 747 ◽  
pp. 131-134
Author(s):  
Somkamon Manchun ◽  
Sontaya Limmatvapirat ◽  
Pornsak Sriamornsak
Keyword(s):  
Drug Release ◽  
Controlled Drug Release ◽  
Matrix Tablets ◽  
Swelling Properties ◽  
Tapioca Starch ◽  
Control Drug ◽  
Model Drug ◽  
New Processing ◽  
Modified Tapioca Starch

Modified starches have been widely used as an excipient in matrix tablets to control drug release. A new processing method for the production of modified starch, high power ultrasonic treatment (400 W), was applied to native tapioca starch. The spray drying technique was used after modification (i.e., by ultrasonic or heat treatment). Matrix tablets were then prepared by direct compression using theophylline as a model drug. The effect of starch modification on swelling, erosion and in vitro drug release behaviors of compressed matrices was investigated in 0.1 N HCl or phosphate buffer (pH 6.8). The matrix tablets of modified tapioca starch formed a continuous gel layer while in contact with the aqueous medium undergoing a combination of swelling and erosion. The ultrasound-treated starch swelled and eroded less than the native starch and heat-treated starch, thus the drug release from matrix tablets using ultrasound-treated starch was slower. For these results, it can be concluded that the ultrasound-treated starch was a promising excipient for controlled drug release.

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