Pharmacokinetics and relative bioavailability study of multiple oral doses of pyridostigmine bromide sustained-release tablets in rabbits

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.

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

Current Pharmaceutical Analysis ◽

10.2174/1573412915666190328234326 ◽

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.

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

Drug Delivery Letters ◽

10.2174/2210303108666180227140554 ◽

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

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Formulation and characterization of ibuprofen sustained release tablets by solid dispersion technique

International Journal of Pharma and Bio Sciences ◽

10.22376/ijpbs.2019.10.4.p64-75 ◽

2019 ◽

Vol 10 (4) ◽

Author(s):

MANJU S. ◽

C.RUBINA REICHAL Dr.

Keyword(s):

Sustained Release ◽

Solid Dispersion ◽

Sustained Release Tablets ◽

Dispersion Technique

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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 ◽

10.3390/pharmaceutics13060804 ◽

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.

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Benznidazole Extended-Release Tablets for Improved Treatment of Chagas Disease: Preclinical Pharmacokinetic Study

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.02506-15 ◽

2016 ◽

Vol 60 (4) ◽

pp. 2492-2498 ◽

Cited By ~ 8

Author(s):

Marcelo Gomes Davanço ◽

Michel Leandro Campos ◽

Talita Atanazio Rosa ◽

Elias Carvalho Padilha ◽

Alejandro Henao Alzate ◽

...

Keyword(s):

Chagas Disease ◽

Extended Release ◽

Hydroxypropyl Methylcellulose ◽

Immediate Release ◽

Relative Bioavailability ◽

Pharmacokinetic Parameters ◽

Therapeutic Success ◽

Preclinical Pharmacokinetics ◽

Bioavailability Study

ABSTRACTBenznidazole (BNZ) is the first-line drug for the treatment of Chagas disease. The drug is available in the form of immediate-release tablets for 100-mg (adult) and 12.5-mg (pediatric) doses. The drug is administered two or three times daily for 60 days. The high frequency of daily administrations and the long period of treatment are factors that significantly contribute to the abandonment of therapy, affecting therapeutic success. Accordingly, this study aimed to evaluate the preclinical pharmacokinetics of BNZ administered as extended-release tablets (200-mg dose) formulated with different types of polymers (hydroxypropyl methylcellulose K4M and K100M), compared to the tablets currently available. The studies were conducted with rabbits, and BNZ quantification was performed in plasma and urine by ultraperformance liquid chromatography methods previously validated. The bioavailability of BNZ was adequate in the administration of extended-release tablets; however, with the administration of the pediatric tablet, the bioavailability was lower than with other tablets, which showed that the clinical use of this formulation should be monitored. The pharmacokinetic parameters demonstrated that the extended-release tablets prolonged drug release from the pharmaceutical matrix and provided an increase in the maintenance of the drug concentrationin vivo, which would allow the frequency of administration to be reduced. Thus, a relative bioavailability study in humans will be planned for implementation of a new product for the treatment of Chagas disease.

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