scholarly journals Development and Evaluation of Floating Sustained Release Bilayer Tablets Containing Dothiepin HCl

2021 ◽  
Vol 11 (4) ◽  
Keyword(s):  
Sustained Release ◽  
Xanthan Gum ◽  
Guar Gum ◽  
Release Kinetics ◽  
Immediate Release ◽  
Natural Polymers ◽  
Sustained Drug Release ◽  
Gum Karaya ◽  
Zero Order Kinetics ◽  
Karaya Gum

Bilayer floating tablets of Dothiepin HCL were developed by direct compression method. Immediate release layer contains 30 mg of drug and super disintegrant sodium starch glycolate, serves the purpose of loading dose. Sustained release layer contained HPMC K4M, natural polymers like xanthan gum, guar gum, karaya gum release the drug for 12 hours’ time. Sodium bicarbonate and citric acid are used to produce effervescence. Floating lag time of optimized tablet is 92 sec, whereas floating duration is more than 12 hours. FTIR results revealed that there was no interaction between drug and HPMC K4M / xanthan gum. The post compression parameters of developed tablets were found to be satisfactory. In this study, it was confirmed that the formulations containing HPMC K4M, have shown better floating properties and finally the formulation containing a combination of HPMC K4M and xanthan gum in 3:1 ratio, has exhibited decent sustained drug release properties. The release kinetics of optimized formulation prepared with the combination of HPMC K4M and xanthan gum followed zero order kinetics. Keywords: Floating Bilayer Tablet, Dothiepin HCL, HPMC K4M, Xanthan Gum, FTIR.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF BILAYER TABLET OF ATENOLOL FOR BIPHASIC DRUG RELEASE

2018 ◽  
Vol 11 (5) ◽  
pp. 114
Author(s):  
Tarun Parashar ◽  
Nardev Singh
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Regression Coefficient ◽  
Release Kinetics ◽  
Immediate Release ◽  
Drug Release Kinetics ◽  
Gum Acacia ◽  
Bilayer Tablet

Objective: In the present research work, the aim was to prepare the bilayer tablet of atenolol for biphasic drug release to improve its bioavailability and absorption in the lower gastrointestinal tract. Methods: In the formulation of immediate release crospovidone, croscarmellose sodium, and sodium starch glycolate was used as super disintegrate and was directly compressed. For a sustained release portion different grade hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M, gum tragacanth, gum acacia, guar gum, and ethyl cellulose. Preformulation studies were performed before compression. The compressed bilayer tablets were evaluated for weight variation, dimension, hardness, friability, drug content, disintegration time, and in vitro drug release using USP dissolution apparatus type 2 (paddle). Results: The formulation IR3 showed 95% drug release in 30 min, and regression coefficient value (r2) value was found to be 0.994 suggesting first-order drug release kinetics. The F9 formulation using HPMC K15M and gum acacia (1:1) showed 91.20% drug release at the end of 12 h, and regression coefficient value (r2) was 0.992 suggesting zero-order drug release kinetics. Formulation IR3F9 showed faster drug release for bilayer tablet containing 5%w/w crospovidone in immediate release layer and HPMC and guar gum (1:1) in sustained release. Formulation IR3F9 showed swelling index 206%, floating lag time was found to be 2 min and total floating time up to 12 h. Conclusion: The formulation IR3F9 showed a faster drug release profile among the others in the preparation of the atenolol bilayer tablet. Hence, it was considered as an optimized formulation.

scholarly journals Formulation Development and In Vitro Characterization of Zolmitriptan Controlled Release Drug Delivery Systems

2019 ◽  
Vol 2 (1) ◽  
Author(s):  
Shambhavi Pandala ◽  
Vasudha Bakshi ◽  
Rajendra Kumar Jadi
Keyword(s):  
Xanthan Gum ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Natural Polymers ◽  
Formulation Development ◽  
Gum Karaya ◽  
Weight Variation

Background: Zolmitriptan is an artificial tryptamine, employed for the acute cure of migraine attack with or exclusive of aura and cluster headaches. Objective: It is an attempt to develop the extended release (ER) of Zolmitriptan matrix (ZMT) tablets to treat migraine safely and effectively. Methods: All formulations were prepared with natural polymers or gums like guar gum, xanthan gum, karaya gum through direct compression method using 6mm punch. Results: Powder blend of all formulations (F1 - F12) using different ratios of the above mentioned gums (5%, 10%, 15% and 20%) were characterized with pre-compression parameters (angle of repose, bulk density, tapped density, compressibility index, hausner ratio, compatibility studies) and post-compression parameters (weight variation, thickness, friability, hardness, assay, in vitro dissolution studies). F1 - F4 formulations were prepared with gum karaya and compared with remaining gums; gum karaya shows more retardance capacity. F9 - F12 (with guar gum) formulations were unable to produce the desired release, whereas F5 - F8 formulations containing with xanthan gum exhibited more retarding effect with increasing concentration of polymer. Conclusion: All prepared formulations (F1 - F12) were characterized and F3 formulation was optimized (97.3% drug released in 8 hours). All prepared formulations (F1 - F12) showed good flow properties and release patterns. Hence, formulations of ZMT matrix tablets have a promising delivery system which will enhance bio-availability and achieve greater therapeutic efficacy.

scholarly journals Formulation, Development and Evaluation of Gastroretentive Sustained Release Tablets of Lansoprazole Using Natural Polymer

2021 ◽  
Vol 11 (5-S) ◽  
pp. 108-112
Author(s):  
, Sonam ◽  
Nilesh Jain ◽  
Jitendra Banveer
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Acid Secretion ◽  
Release Kinetics ◽  
Natural Polymers ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Multiple Dosing ◽  
Long Acting

The goal of this study is to develop a long-acting Lansoprazole delivery system. Lansoprazole belongs to a class of antisecretory drugs known as substituted benzimidazoles, which decrease gastric acid secretion by inhibiting the (H+,K+)-ATPase enzyme system at the secretory membrane of the stomach parietal cell. Due to its mechanism of action, despite its short half-life of 1-5 hours, it can effectively block acid secretion for 24 hours. However, as his plasma concentration falls, the effect will diminish. Lansoprazole will be given as a sustained release tablet to avoid multiple dosing or to reduce the frequency of dose. Lansoprazole was produced and analysed utilizing natural and synthetic polymers such as Xanthan gum, Gellan gum, Carbopol 940 P, and Chitosan. Based on the findings of this experiment, it was determined that formulation F7 demonstrated sustained drug release for up to 12 hours in all developed formulations. Formulation (F1, F2, F3, F4, F5, and F6) were tested in vitro for drug release. For the improved formulation F7, the formulation and release kinetics were estimated. When the regression coefficient values of were evaluated, it was found that Peppas had the highest ‘r2' value, 0.952, indicating that drug release from formulations followed Peppas release kinetics. Key words: Lansoprazole, Sustain release tablets, Synthetic and Natural Polymers, formulation, evaluation

Formulation and Evaluation of Metoprolol Tartrate Sustained Release Matrix Tablets

2019 ◽  
Vol 12 (5) ◽  
pp. 4865-4671
Author(s):  
Shravan Kumar Y ◽  
Shireesha G ◽  
Harika S
Keyword(s):  
Sustained Release ◽  
Xanthan Gum ◽  
Guar Gum ◽  
Chemical Interaction ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Metoprolol Tartrate ◽  
Gum Kondagogu

The objective of the present work was to develop sustained release matrix tablets of Metoprolol tartrate using different polymers viz. Guar gum, Xanthan gum, Kondagogu gum and HPMC K100M. The release rates were modulated by combination of two different rates controlling material and triple mixture of two different rate controlling materials. After evaluation of physical properties of tablet, the in-vitro release study was performed in phosphate buffer pH 6.8 up to 12 hrs. Dissolution data was analyzed for release kinetics. It was observed that matrix tablets contained polymer Xanthan gum was successfully sustained the release of drug up to 12 hrs. Among all the formulations, F6 which contains 45 % of Xanthan gum, release of drug which follows zero order kinetics via, swelling, diffusion and the release profile of formulation F6 was compared with marketed product. The FTIR study revealed that there was no chemical interaction between drug and excipient.

scholarly journals Development and evaluation of sustained release matrix tablets of losartan potassium

2016 ◽  
Vol 1 (04) ◽  
pp. 127-132
Author(s):  
V. Viswanath ◽  
U. Chandrasekhar ◽  
B. Narasimha Rao ◽  
K. Gnana Prakash
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Wet Granulation ◽  
Natural Polymers ◽  
Hypertensive Drug

The objective of the present study was to develop a sustained release matrix tablets of Losartan potassium, an anti hypertensive drug. The sustained release tablets were prepared by wet granulation and formulated using different drug and polymer ratios. Hydrophilic natural polymers like xanthan Gum (XG), guar gum and cellulose were used. Compatibility of the drug with various excipients was studied. The compressed tablets were evaluated and showed compliance with Pharmacopoeial limits. Formulation was optimized (F2) on the basis of acceptable tablet properties and in vitro drug release. The resulting formulation produced matrix tablets with optimum hardness, consistent weight uniformity and friability. All tablets but one exhibited gradual and near completion sustained release for losartan potassium and 90.88% released at the end of 12h. The results of dissolution studies indicated that formulation F2 (drug to polymer 1:2) is the most successful of the study and exhibited drug release pattern very close to theoretical release profile. A decrease in release kinetics of the drug was observed on increasing polymer ratio. Applying exponential equation, all the formulation tablets (except F2) showed diffusion-dominated drug release. The mechanism of drug release from F2 was diffusion coupled with erosion.

scholarly journals Formulation and Evaluation of Sustained Release Verapamil Hydrochloride Using Natural Polymers

2016 ◽  
Vol 1 (02) ◽  
pp. 76-87
Author(s):  
B. Ramu ◽  
S. Ullas Kumar ◽  
G. Srikanth ◽  
Bigala Rajkamal
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Natural Polymers ◽  
Release Formulation ◽  
Verapamil Hydrochloride ◽  
Sustained Release Formulation ◽  
Release Pattern ◽  
Zero Order Release

The aim of the present study was to develop sustained release formulation of Verapamil Hydrochloride to maintain constant therapeutic levels of the drug for over 12 hrs. Various grades of HPMC polymers, Guar gum, and Xanthum gum were employed as polymers. Verapamil Hydrochloride dose was fixed as 120 mg. Total weight of the tablet was considered as 400 mg. Polymers were used in the concentration of 60, 120 and 180 mg concentration. All the formulations were passed various physicochemical evaluation parameters and they were found to be within limits. Whereas from the dissolution studies it was evident that the formulation (F6) showed better and desired drug release pattern i.e.,96.10 % in 12 hours containing Guar gum polymer in the concentration of 180mg. It followed zero order release kinetics. For the optimized formulation alcohol effect has been studied by using various concentrations of alcohol in dissolution medium. As the concentration of alcohol increased the sustained action of polymer was decreased. Hence it was concluded that alcohol has significant effect on drug release pattern.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

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
Keyword(s):  
Sustained Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Zero Order Kinetics ◽  
Weight Variation ◽  
Sustained Release Tablets

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

scholarly journals Formulation and Evaluation of Fixed-Dose Combination of Bilayer Gastroretentive Matrix Tablet Containing Atorvastatin as Fast-Release and Atenolol as Sustained-Release

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Sanjay Dey ◽  
Sankha Chattopadhyay ◽  
Bhaskar Mazumder
Keyword(s):  
Sustained Release ◽  
Xanthan Gum ◽  
Guar Gum ◽  
Molar Ratio ◽  
Fixed Dose ◽  
Matrix Tablet ◽  
Bilayer Tablets ◽  
Fast Absorption ◽  
Dose Combination ◽  
Fast Release

The objective of the present study was to develop bilayer tablets of atorvastatin and atenolol that are characterized by initial fast-release of atorvastatin in the stomach and comply with the release requirements of sustained-release of atenolol. An amorphous, solvent evaporation inclusion complex of atorvastatin withβ-cyclodextrin, present in 1 : 3 (drug/cyclodextrin) molar ratio, was employed in the fast-release layer to enhance the dissolution of atorvastatin. Xanthan gum and guar gum were integrated in the sustained-release layer. Bilayer tablets composed of sustained-release layer (10% w/w of xanthan gum and guar gum) and fast-release layer [1 : 3 (drug/cyclodextrin)] showed the desired release profile. The atorvastatin contained in the fast-release layer showed an initial fast-release of more than 60% of its drug content within 2 h, followed by sustained release of the atenolol for a period of 12 h. The pharmacokinetic study illustrated that the fast absorption and increased oral bioavailability of atorvastatin as well as therapeutic concentration of atenolol in blood were made available through adoption of formulation strategy of bilayer tablets. It can be concluded that the bilayer tablets of atorvastatin and atenolol can be successfully employed for the treatment of hypertension and hypercholesterolemia together through oral administration of single tablet.

scholarly journals FORMULATION AND INVESTIGATION OF POLYMERIC MULTIPLE UNIT PELLET SYSTEMS CONSISTING OF SUSTAINED RELEASE GLIMEPIRIDE AND IMMEDIATE RELEASE ATORVASTATIN CALCIUM

2019 ◽  
pp. 142-150
Author(s):  
BHARAT BIJAPUR ◽  
GOWDA DV ◽  
VISHAL GUPTA N ◽  
SHAILESH THIRUMALESHWAR ◽  
PRAVEEN SIVADASU ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Sustained Release ◽  
Immediate Release ◽  
Fixed Dose ◽  
Locust Bean Gum ◽  
Natural Polymers ◽  
Atorvastatin Calcium ◽  
Gum Ghatti ◽  
Multiple Unit ◽  
Locust Bean

Objective: The objective of the present work was to develop novel fixed-dose combinations (FDCs) for improvement of glucose tolerance in type II diabetes mellitus patients associated with dyslipidemia. Methods: Multiple unit pellet systems (MUPSs) consisting of sustained release (SR) glimepiride and immediate release atorvastatin calcium pellets were formulated. The SR glimepiride pellets were prepared using a combination of locust bean gum and gum ghatti/guar gum. Similarly, the immediate release of atorvastatin calcium pellets was prepared using locust bean gum suspension as a binder. Results: The formulated pellets were characterized using Fourier transform infrared spectroscopy (FTIR) and Differential scanning calorimetry (DSC). Further, surface morphology of the formulated pellets was done by scanning electron microscopy (SEM). FT-IR and DSC studies suggested that there were no chemical interactions between the drug and natural polymers. SEM studies revealed that formulated pellets were in spherical shape. Based on in vitro evaluation, the SR glimepiride formulation developed using a combination of 2% locust bean gum and 2.5% gum ghatti polymers sustained the release of the drug up to 12 h. Similarly, the immediate release atorvastatin calcium formulation containing 1% w/w locust bean gum suspension as a binder and 7% croscarmellose sodium showed fast disintegration of pellets. The in vivo studies in albino Wistar rat revealed that there was an improvement in bioavailability of the drugs. Stability studies showed that there were no significant changes in the drug content and physical appearance of the prepared SR glimepiride and immediate release atorvastatin pellet formulations. Conclusion: Thus, the formulated FDC as MUPS can be used as an alternative approach for treating diabetes mellitus-induced dyslipidemia.

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