scholarly journals Development of the "Dissolution" Test Method for Tablets of Sodium 4,4'-(propanediamido)dibenzoate with Sustained Release

2021 ◽  
Vol 10 (4) ◽  
pp. 146-154
Author(s):  
E. V. Flisyuk ◽  
Ju. M. Kotsur ◽  
I. A. Narkevich ◽  
I. E. Smekhova ◽  
D. Yu. Ivkin

Introduction. Non-alcoholic fatty liver disease is one of the most common chronic diseases of this parenchymal organ among the adult population. The search and creation of supporting drugs is an urgent task of modern pharmacy. The malonic acid derivative, sodium 4,4'-(propanediamido) dibenzoate, synthesized by the employees of the Department of Organic Chemistry of the SPСPU, has antisteatous activity, is a potential agent for the treatment of liver diseases. Sustained release tablets were prepared based on sodium 4,4'-(propanediamido)dibenzoate. An integral part of the pharmaceutical development of a medicinal product is the development of a method for conducting the Dissolution test and the selection of optimal conditions, which became the purpose of this study.Aim. To develop the "Dissolution" test method for the sustained-release tablets based on sodium 4,4'-(propanediamido)dibenzoate.Materials and methods. The objects of research are the active pharmaceutical ingredient sodium 4,4'-(propanediamido)dibenzoate, as well as sustained-release tablets based on this substance. Equilibrium biopharmaceutical solubility was determined by UV-spectrophotometry. To establish the conditions for the "Dissolution" test, an ERWEKA DT-620 dissolution tester (ERWEKA GmbH, Germany) was used.Results and discussion. The suitability of the UV-spectrophotometry method for the quantitative determination of sodium 4,4'-(propanediamido) dibenzoate in solutions was determined. The established high biopharmaceutical solubility of sodium 4,4'-(propanediamido)dibenzoate in a buffer solution with a pH of 6,8, as well as in a 0,01 M solution of hydrochloric acid with a pH of 2,6, determined the choice of these media for the "Dissolution" test of the dosage form. The apparatus "Rotating basket" (rotation speed of 100 rpm in a dissolution medium with a volume of 1000 ml) was reasonably chosen for the test on the basis of the obtained linear dependence of the rate of release of the substance on time, as well as the best test results by the end of the experiment.Conclusion. A study of the biopharmaceutical properties of the original substance with antisteatous activity has been carried out. High biopharmaceutical solubility was established in media with pH 2,6 and pH 6,8. The conditions of the "Dissolution" test for sustained-release tablets based on the original sodium 4,4'-(propanediamido)dibenzoate were experimentally substantiated.

2018 ◽  
Vol 16 (1) ◽  
pp. 333-339
Author(s):  
Wanying Liu ◽  
Qing Huo ◽  
Yue Wang ◽  
Na Yu ◽  
Rongjian Shi

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.


2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169


2020 ◽  
Vol 13 (2) ◽  
pp. 79-86
Author(s):  
Alexandra Pali ◽  
◽  
Georgiana Cristina Ordean ◽  
Greta Maria Pomian ◽  
Luca Liviu Rus ◽  
...  

Author(s):  
Alhumaidi Alsubaie ◽  
Saeed Mohammad ◽  
Abdulkarim Alqarni ◽  
Abdulkareem Alosaimi ◽  
Mutaz Alenizi ◽  
...  

2019 ◽  
Vol 24 (3) ◽  
pp. 196-202 ◽  
Author(s):  
S. A. Abdurakhmanova ◽  
G. S. Runova ◽  
M. S. Podporin ◽  
E. V. Tsareva ◽  
E. V. Ippolitov ◽  
...  

Relevance: Inflammatory-destructive periodontal diseases are the most complicated and became the main cause of tooth loss in adult population. Herbal medicines have a variety of pharmacological properties, so the development and introduction of new forms for the treatment of inflammatory periodontal diseases is an urgent task today.Purpose – experimental evaluation of effectiveness of the use of herbal medicines “Tonzinal” and “CM-1” in relation to the priority periodontal pathogenes.Materials and methods: in experimental studies, the basis for the experiment was the system for the cultivation of microorganisms in real time – the Revers-Spinner RTS-1 bioreactor. With the priority strains of periodontitis pathogens, the study of the growth dynamics of the culture was carried out in several parallels.Results: herbal medicines “CM-1” and “Tonsinal” has a multilateral therapeutic effect, exerting a diverse influence on the key stages of development of such bacterial populations as Aggregatibacter actinomycetemcomitans, Streptococcus constellatus, Candida albicans.Conclusion: tan integrated approach in the treatment of patients with inflammatory periodontal diseases is promising and will contribute to a more prolonged remission and increase the effectiveness of treatment. 


Author(s):  
C Suja ◽  
Sismy C

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.


2020 ◽  
Vol 16 (7) ◽  
pp. 950-959
Author(s):  
Yu Li ◽  
Xiangwen Kong ◽  
Fan Hu

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.


2018 ◽  
Vol 8 (2) ◽  
pp. 153-158
Author(s):  
Praveen Radhakrishnan ◽  
Shinu Chacko ◽  
Raman Saraswathi ◽  
Palamadai Neelakantam Krishnan

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