Design and Evaluation of Sustained-Release Tablets of Lithium in a Fat Matrix and Its Bioavailability in Humans

1991 ◽  
Vol 80 (11) ◽  
pp. 1012-1016 ◽  
Author(s):  
M. Llabrés ◽  
J.B. Fariña
Keyword(s):  
Sustained Release ◽  
Sustained Release Tablets

Formulation and Evaluation of Sustained Release Dosage Forms of Norfloxacin

2018 ◽  
Vol 11 (6) ◽  
pp. 4331-4337
Author(s):  
C Suja ◽  
Sismy C
Keyword(s):  
Sustained Release ◽  
Guar Gum ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Prolonged Release ◽  
Weight Variation ◽  
Sustained Release Tablets ◽  
Release Study ◽  
Vitro Release

The goal of this study was to formulate and evaluate norfloxacin sustained release tablets. Norfloxacin sustained release tablets were prepared by wet granulation method using two polymers such as HPMC K 100 M (hydrophilic polymer) and guar gum (natural polymer) and with three polymer ratios (0.5, 1.0 and 1.5). The prepared granules were evaluated to preformulation studies such as angle of repose, bulk density, tapped density, bulkiness, compressibility index and Hauser’s ratio. All the parameters shows that the granules having good flow properties. Then the formulated tablets were taken to evaluation studies such as hardness, weight variation, friability, drug content and thickness. All the parameters were within the acceptable limits. IR spectral analysis showed that there was no interaction between the drug and polymers. The in vitro release study was performed in phosphate buffer pH 7.4 at 293 nm. The in vitro release study showed that if the polymer ratio is increased, then the release of the drug is prolonged. HPMC K 100M shows a prolonged release when compared to guar gum.

Crystal Transition and Drug-excipient Compatibility of Clarithromycin in Sustained Release Tablets

2020 ◽  
Vol 16 (7) ◽  
pp. 950-959
Author(s):  
Yu Li ◽  
Xiangwen Kong ◽  
Fan Hu
Keyword(s):  
Sustained Release ◽  
Powder Diffraction ◽  
Magnesium Stearate ◽  
Influential Factor ◽  
High Concentration ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Sustained Release Tablets ◽  
Crystal Transition ◽  
Excipient Compatibility

Background: Clarithromycin is widely used for infections of helicobacter pylori. Clarithromycin belongs to polymorphic drug. Crystalline state changes of clarithromycin in sustained release tablets were found. Objective: The aim of this study was to find the influential factor of the crystal transition of clarithromycin in preparation process of sustained-release tablets and to investigate the possible interactions between the clarithromycin and pharmaceutical excipients. Methods and Results: The crystal transition of active pharmaceuticals ingredients from form II to form I in portion in clarithromycin sustained release tablets were confirmed by x-ray powder diffraction. The techniques including differential scanning calorimetry and infrared spectroscopy, x-ray powder diffraction were used for assessing the compatibility between clarithromycin and several excipients as magnesium stearate, lactose, sodium carboxymethyl cellulose, polyvinyl-pyrrolidone K-30 and microcrystalline cellulose. All of these methods showed compatibilities between clarithromycin and the selected excipients. Alcohol prescription simulation was also done, which showed incompatibility between clarithromycin and concentration alcohol. Conclusion: It was confirmed that the reason for the incompatibility of clarithromycin with high concentration of alcohol was crystal transition.

Matrix Based Sustained Release Tablets of Carvedilol: Formulation and In-vitro Characterization

2018 ◽  
Vol 8 (2) ◽  
pp. 153-158
Author(s):  
Praveen Radhakrishnan ◽  
Shinu Chacko ◽  
Raman Saraswathi ◽  
Palamadai Neelakantam Krishnan
Keyword(s):  
Sustained Release ◽  
In Vitro Characterization ◽  
Sustained Release Tablets

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 Development of sustained release tablets containing solid dispersions of baclofen

2015 ◽  
Vol 5 (2) ◽  
pp. 220
Author(s):  
KH Janardhana ◽  
R Deveswaran ◽  
S Bharath ◽  
BV Basavaraj ◽  
V Madhavan
Keyword(s):  
Sustained Release ◽  
Solid Dispersions ◽  
Sustained Release Tablets

scholarly journals Study on Sustained-Release Tablets of Tramadol Hydrochloride

2014 ◽  
Vol 26 (15) ◽  
pp. 4723-4727
Author(s):  
Qing Huo ◽  
Chenyang Guo ◽  
Tianhao Gu ◽  
Wanying Liu
Keyword(s):  
Sustained Release ◽  
Tramadol Hydrochloride ◽  
Sustained Release Tablets

scholarly journals Investigation of the sustained-release mechanism of hydroxypropyl methyl cellulose skeleton type Acipimox tablets

2018 ◽  
Vol 16 (1) ◽  
pp. 333-339
Author(s):  
Wanying Liu ◽  
Qing Huo ◽  
Yue Wang ◽  
Na Yu ◽  
Rongjian Shi
Keyword(s):  
Sustained Release ◽  
Diffusion Mechanism ◽  
Methyl Cellulose ◽  
Magnesium Stearate ◽  
Test Method ◽  
Release Mechanism ◽  
Hydroxypropyl Methyl Cellulose ◽  
Hypolipidemic Agents ◽  
Sustained Release Tablets ◽  
The Difference

AbstractIn this study, we investigate the production of hypolipidemic agents in the form of Acipimox sustained-release tablets, using a wet pelleting process. The purpose of this research is to reduce the total intake time for patients and to lower the initial dose in such that the adverse reactions could be reduced. This study adopts the single-factor method and orthogonal experiments by using hydroxypropyl methyl cellulose (HPMC K15M) as the main sustained-release prescription composition. The final prescription is Acipimox 20%, HPMC K15M 26.67%, sodium carboxymethyl cellulose 30%, polyethylene glycol (PEG 6000) 1%, ethyl cellulose 16.6%, lactose 4.67% and magnesium stearate 1%. The dissolution of tablets reached 85.88% in 8 h. The difference in the weight, hardness and friability of the tables met the requirements in the Chinese Pharmacopoeia; to test the stability, a temperature and illumination accelerated test method was used, the results indicate that the Acipimox sustained-release tablets should be sealed and stored in a dark, cool area. A preliminary study on the tablets’ releasing mechanism showed that their release curve fitted the Higuchi model (the formula is Mt/M∞ = 31.137 t1/2–3.605 (R2 = 0.9903)). The Acipimox tablets’ release principle is dominated by the diffusion mechanism.

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