Formulation, Development and Evaluation of Sustained Release Gastroretentive Floating Tablets of Antidiabetic Drug using Natural Polymers

2020 ◽  
Vol 9 (4) ◽  
pp. 87-96
Author(s):  
Aksah Chandak ◽  
Sunil Kumar Shah ◽  
Prabhakar Budholiya ◽  
C. K. Tyagi
Author(s):  
Gururaj S Kulkarni ◽  
Prabhansh P Chaudhary ◽  
Shivakumar Swamy

The aim of the present study was to develop and evaluate sustained release floating tablets of Diltiazem hydro-chloride, an antihypertensive agent. The sustained release floating tablets were prepared by direct compression method and formulated using different polymer combinations, formulations such as F1 to F9. Natural polymer Sodium alginate and synthetic polymer HPMC K4M were used. Developed formulations were evaluated for the pre compression parameters i.e., drug- excipients compatibility by FTIR, bulk density, compressibility, and angle of repose etc. Post compression parameters i.e. weight variation; full factorial design was applied to optimize the developed formulation. SA and HPMC K4M were selected as independent variable at three different concentrations. The in-vitro drug release study revealed that formulation F8 combination of both synthetic (HPMC) and natural polymers (sodium alginate) was the most successful formulation of the study, all tablets but one exhibited gradual and near complete sustained release for diltiazem HCl (90-100%) that extended the drug release up to 8 hours, with satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile.  Model equations of zero and first order, Higuchi, Hixson-Crowell and Peppas, intended to elucidate the drug release mechanism, and were fitted to the release data. Mathematical modelling of in-vitro dissolution data indicated the best-fit release kinetics was achieved with Higuchi model with r2 vales of 0.994 in its semi log plot. The ‘n’ value in Higuchi model was >0.89 which indicated, Super Case-II transport of drug from polymer sustained, i.e., diffusion with relaxation of polymeric chain. In conclusion, the results indicated that the prepared sustained-release tablets of Diltiazem hydrochloride could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.     


2021 ◽  
Vol 11 (5-S) ◽  
pp. 108-112
Author(s):  
, Sonam ◽  
Nilesh Jain ◽  
Jitendra Banveer

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


Author(s):  
Pawan Avhad ◽  
Revathi Gupta

The sustained-release dosage form is a well-characterized and reproducible dosage form that is designed to control drug release profile at a certain rate to reach desired drug concentration in blood plasma or at the target site. There is immense demand in the market for new sustained-release formulations used for new drug molecules which release the drug at a sustained rate. Doxofylline is one of the widely useful drugs in the market and needs to be given in a single dose for a long duration of time. For the same, we have prepared a sustained released Doxofylline tablet. Aim: This research was done to design, formulate and evaluate Doxofylline sustained-release tablets by using different concentrations of Chitosan and Guar Gum.  Methods: The factorial design was used to prepare Doxofylline sustained-release tablet. Doxofylline sustained-release tablets were prepared to employ different concentrations of Chitosan, Guar Gum, Lactose, and Magnesium Stearate in different combinations by wet granulation technique. Total 9 formulations were designed, formulated, and evaluated for the hardness, thickness, friability, % drug content, and in-vitro drug release. Results: A study of the release of drug by in-vitro found that F8 is to be the best efficient formulation which consists of both Chitosan and Guar Gum helped in delayed the release of drug up to 24 hours and performs excellent release of drug in starting hours of drug release in the body. The drug released from the F8 formulation indicates the kinetic model of First Order, by anomalous diffusion. The formulation F8 shows optimum thickness, hardness and at 40ºC±2 99.35% drug release after 24 hours shows optimum formulation.  Conclusion: This study concludes that better drug release was observed by using natural polymers.  Doxofylline with natural polymer shows good release and better dissolution rate as compared with a single synthetic polymer. Synthetic drug with natural polymer shows more future scope and this work will help the researcher in the future.


2017 ◽  
Vol 5 (2) ◽  
pp. 26-44
Author(s):  
Vageesh N.M ◽  
◽  
Sri Sura Ramya ◽  
Begum K Gulijar ◽  
Swathi B ◽  
...  

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.


2020 ◽  
Vol 13 (12) ◽  
pp. 5909-5913
Author(s):  
Mohammad Akthar Sulthana ◽  
Mangulal Kethavath ◽  
Fazil Ahmad ◽  
Abeer Mohammed Al-Subaie

2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.


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