scholarly journals Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets

2015 ◽  
Vol 18 (2) ◽  
pp. 157-162
Author(s):  
Samira Karim ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Sohel Rana

This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015

2017 ◽  
Vol 4 (1) ◽  
pp. 14
Author(s):  
Hitesh Jain ◽  
Kinjal Patel ◽  
Neha Savant ◽  
Umesh Upadhyay

Objective: The aim of the present study was to formulate the floating bilayer tablets of Ketorolac tromethamine, first immediate release layer and second sustained release floating layer which would provide initial loading dose of drug and remain in stomach and upper part of GIT for prolonged period of time in a view to maximize solubility of drug which is necessary for its absorption.Methods: The floating bilayered tablets of Ketorolac tromethamine were prepared by using 32 factorial designs by direct compression method. For this, polymers like sodium starch glycolate and polyox WSR 303 were used in various concentrations. Sodium bicarbonate was used as a floating effervescent agent. The formulations were evaluated for hardness, friability, weight variation, swelling index, floating lag time, floating time, % CDR etcResults: From the result obtained, S3 having 23% Polyox WSR 303 and 12% sodium bicarbonate showed better results.Conclusions: The results showed that Polyox WSR is promising tool to designing of sustained release formulation.


2013 ◽  
Vol 16 (1) ◽  
pp. 1-9
Author(s):  
Shahriar Ahmed ◽  
Mehrina Nazmi ◽  
Ikramul Hasan ◽  
Sabiha Sultana ◽  
Shimul Haldar ◽  
...  

Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37°C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14483 Bangladesh Pharmaceutical Journal 16(1): 1-9, 2013


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.


2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.


2011 ◽  
Vol 311-313 ◽  
pp. 1751-1754
Author(s):  
Gui Yu Li ◽  
Xi Hong Lu ◽  
Xue Hu Li ◽  
Lei Tao ◽  
Jian Ping Liang

Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.


2011 ◽  
Vol 58 (12) ◽  
pp. 647-652
Author(s):  
Amparo Araíco ◽  
Francisca Torres-Molina ◽  
Anas Saadeddin ◽  
Jaime Cárcel-Trullols ◽  
Josefa Alvarez-Fuentes ◽  
...  

2020 ◽  
Vol 19 (1) ◽  
pp. 65-76
Author(s):  
Tushar Saha ◽  
Nusrat Ahmed ◽  
Ikramul Hasan ◽  
Md Selim Reza

In pharmaceutical industry, statistically valid experimental design can be utilized to optimize data in order to provide an economic and effective formulation, which could overcome several product and process development problems. Domperidone is a BCS Class II drug and has wide range of use, but has very poor bioavailability when administered orally because of degradation in intestinal fluid. The present study was focused on formulation, evaluation and optimization of mucoadhesive tablets of domperidone using a four-factor, three-level Box-Behnken design (BBD) so as to retain the prepared optimized formulation in gastric fluid for a prolong period of time in order to have better bioavailability and to get a sustained action. Physicochemical properties of the prepared formulations were determined according to the USP pharmacopeia official method and found satisfactory, except friability which was optimized to get the acceptable value. In-vitro dissolution study was performed for 8 hours for all the prepared formulations using USP II (paddle type) dissolution tester having 0.1N HCl (pH 1.2) as dissolution medium. Obtained data was further analyzed by means of quadratic response surface models so as to find out an optimize formulation in terms of desirable condition of dissolution rate after 1 hour, after 8 hours, total mucoadhesion time and tablet friability. Optimized formulation was further evaluated and it was found that, it was almost similar to the proposed optimized data. The formulation can provide a high degree of patient compliance, as sustained release formulation reduces the side effects and the cost of the formulation will be minimal as lesser amount of effort will be needed employing statistical model instead of conventional trial and error method. Dhaka Univ. J. Pharm. Sci. 19(1): 65-76, 2020 (June)


2016 ◽  
Vol 12 (25) ◽  
pp. 5679-5699
Author(s):  
K.Sathish Kumar ◽  
C. Kumaresan ◽  
R. Anantharaj

The present work was designed to develop and compare orally inhalable sustained release formulation for salbutamol sulphate (SS), ambroxol hydrochloride (AH) and montelukast sodium (MS).The emulsion solvent evaporation method was used to prepare microparticles with the polymers. The prepared polymer encapsulated microparticles were blended with carrier inhalable lactose and filled in size 3 hard empty gelatin capsule. Formulations T1-T9 were prepared with 1:1 ratio of PLGA (50:50), PLGA (75:25) and Eudragit RS100. The formulation T1 prepared with SS:PLGA (50:50) produces best result when compared with other formulations T2-T9. Formulation T1 gives in vitro release 91.23% at 12 h and having particle size of microparticles (D0.5 µm) 1.94±0.6 and respiratory fraction 34.9± 2.59 %.


2019 ◽  
Vol 10 (3) ◽  
pp. 1602-1607
Author(s):  
Harish Choodappa ◽  
Subramanian Somaskandan

In this study, we aimed to prepare bilayer tablets of Glimepiride in floating drug delivery and Metformin in sustained release formulation. Glimepiride is chosen in floating drug delivery to overcome the gastric irritation and gastric emptying time. Glimepiride was prepared by different polymers such as guar gum, xanthan gum, carbopol and sodium bicarbonate act as effervescent agent, and other excipients were mixed and compressed by direct compression as the first layer.  Metformin was chosen in sustained release to reduce dose frequency using different polymer HPMC K100M, methylcellulose, PVP K30 in different ratio and other excipients were mixed and compressed as the second layer. The first layer and second layer are combined as a bilayer tablet. Tablets were evaluated for hardness, friability, thickness, weight variation; the In vitro studies were done for all formulation. Among all formulation, F2 was selected as best formulation and release kinetics studies were evaluated for formulation F2.


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