Formulation and Evaluation of Levetiracetam Extended Release Tablets

2013 ◽  
Vol 6 (1) ◽  
pp. 1958-1965
Author(s):  
Sudarshan Singh ◽  
Shankar Bhavesh ◽  
Sanjaykumar Nayak ◽  
Sunil Bothara
Keyword(s):  
Data Analysis ◽  
Drug Release ◽  
Extended Release ◽  
Zero Order ◽  
Release Profile ◽  
Matrix Tablet ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Mechanism

Extended release formulation of levetiracetam is approved by the food and drug administration as an add-on to other antiepileptic drugs for adults with partial onset seizures. The main objective of present study was to developed and evaluate matrix tablet of levetiracetam by using various grade of hydroxypropylmethylcellulose (HPMC) polymer. Various trials were taken by using HPMC K4M, K15M, and K100M.  Different parameters like Physical properties, FTIR, DSC, in vitro drug release profile and swelling index were determined. In vitro drug release was performed in phosphate buffer pH 6.8. The in vitro release profile was compared with model independent method. Stability studies were performed as per ICH guidelines for 1 month at (40 °C ± 2 °C/75 % ± 5 % RH).Data analysis was performed for determination of drug mechanism and order of drug release. The in vitro drug release profile of optimized formulation was compared with marketed formulation LEVERAXR. The regression value for zero order, first order, Higuchi and Korsmeyer Peppas was found to be 0.9604, 0.9245, 0.9889 and 0.9729, respectively. Similarity factor (f2) and dissimilarity factor (f1) was found to be 88.61 and 1.82, respectively. The FTIR and DSC study shows that there is no chemical interaction between levetiracetam and excipients. From the data analysis, it was concluded that optimized formulation follow Higuchi model having diffusion mechanism. The order of drug release was considered zero  order release. Stability study shows that there was no remarkable change in drug release after 1 month. It is concluded that the formulation is stable at accelerated conditions.

scholarly journals DESIGN AND IN VITRO EVALUATION OF EXTENDED RELEASE TABLET OF NATEGLINIDE

2018 ◽  
Vol 8 (5-s) ◽  
pp. 235-239
Author(s):  
NILESH M MAHAJAN ◽  
Kalyanee Wanaskar ◽  
Yogesh Bhutada ◽  
Raju Thenge ◽  
Vaibhav Adhao
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Tablet Properties ◽  
Vitro Release

The aim of present study is to formulate and evaluate extended release matrix tablet of Nateglinide by direct compression method using different polymer like HPMC K4 and HPMC K15. Matrix tablet of nateglidine were prepared in combination with the polymer HPMC K4, HPMC K15, along with the excipients and the formulations were evaluated for tablet properties and in vitro drug release studies. Nateglinide matrix tablet prepared by using polymer such as HPMC K4 and HPMC K15,  it was found that HPMC K15 having higher viscosity as compare to HPMC K4 therefore different concentration of polymer were studied to extend the drug release up to 12 h. The tablets of Nateglinide prepared by direct compression had acceptable physical characteristics and satisfactory drug release. The study demonstrated that as far as the formulations were concerned, the selected polymers proved to have an acceptable flexibility in terms of in-vitro release profile. In present the study the percent drug release for optimize batch was found to 94.62%.  Hence it can be conclude that Nateglinide extended release matrix tablet can prepared by using HPMC. The swollen tablet also maintains its physical integrity during the drug release study Keywords: Tablet, in-vitro drug release, Nateglinide, HPMC

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE PATCHES OF NICERGOLINE FOR BUCCAL DRUG DELIVERY BY USING FACTORIAL DESIGN OF EXPERIMENT (DOE)

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (07) ◽  
pp. 52-57
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Design Of Experiment ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Drug Content ◽  
Release Study

The aim of this research was to develop mucoadhesive buccal patches of nicergoline by using Factorial Design of Experiment, in order to provide a sustained release of drug into the systemic circulation. A 33 factorial experimental design was employed for optimization and to study the effect of formulation variables on responses R1 (% swelling index), R2 (% drug content), R3 (mucoadhesion time) and R4 (mucoadhesion strength). In vitro drug release study was performed on the optimized formulations. All the prepared formulations had good mechanical strength, mucoadhesion strength, neutral surface pH and drug content up to 98.17%. In vitro drug release study revealed that F-5 formulation showed promising sustained drug release profile (98.21%) for over 8 h and could be a potential substitute for marketed conventional formulations. The developed formulation (F5) was found to be optimized with considerably good stability and extended drug release profile.

scholarly journals Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs

2021 ◽  
Vol 11 (5-S) ◽  
pp. 100-107
Author(s):  
M. Pradeep Kumar ◽  
Goparaju Suryanarayana Murthy ◽  
Annamdasu Lakshmi Poojitha ◽  
P. Sindhuri ◽  
A Sreekanth ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Similarity Factor ◽  
Time Required ◽  
Full Factorial

The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).  

scholarly journals Release Behaviour of Single Pellets and Internal Fine 3D Structural Features Co-define the In Vitro Drug Release Profile

2014 ◽  
Vol 16 (4) ◽  
pp. 860-871 ◽  
Author(s):  
Shuo Yang ◽  
Xianzhen Yin ◽  
Caifen Wang ◽  
Haiyan Li ◽  
You He ◽  
...  
Keyword(s):  
Drug Release ◽  
Structural Features ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release

scholarly journals Optimizing similarity factor of in vitro drug release profile for development of early stage formulation of drug using linear regression model

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tulsi Sagar Sheth ◽  
Falguni Acharya
Keyword(s):  
Linear Regression ◽  
Drug Release ◽  
Regression Model ◽  
Linear Regression Model ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Similarity Factor ◽  
Release Profiles

AbstractThe objective of this article is to optimize the similarity factor within immediate release (IR) and modified release (MR) of in vitro drug release profiles. The least square method is used to minimize the difference between empirical and regression curve fitting data of in vitro IR/MR drug release profiles. An estimation of percentage drug release at intermediate timepoints has been done to improve the similarity factor $f_{2}$ f 2 using linear curve fit method. In this study linear regression model is used to analyze the similarity factor $f_{2}$ f 2 for Nitrofurantoin MR Capsules, Venlafaxine HCl MR Tablets and Lurasidone IR Tablets in order to exhibit the significance as well as similarity owing to the consideration of extra intervening timepoints. This linear regression model may help pharmaceutical industries to examine the inside comparison of IR/MR in vitro drug release profile with few modifications in timepoint selection to improve similarity factor $f_{2}$ f 2 .

scholarly journals Development and Characterization of a Theranostic Micelles System using TPGS with Docetaxel and Coumarin-6: A Dual Polymeric Nanocarrier System

2018 ◽  
Vol 5 (1) ◽  
pp. 99-108
Author(s):  
L.H. Ching ◽  
S. Mahmood ◽  
R. Edros ◽  
R.V. Kutty
Keyword(s):  
Drug Release ◽  
Early Stage ◽  
Drug Loading ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Dual Modality ◽  
Coumarin 6 ◽  
Polymeric Nanocarrier

Theranostic micelles and polymeric nanocarrier-based drug delivery system are well known techniques that involve a diagnostic agent in polymeric micelles for a combination of therapy by using a co-delivery approach which can help in detection of a cancer cell in an early stage, increase killing effect and suppress multi-drug resistance (MDS) for better therapeutic effectiveness. The aim of this study is to develop a dual modality micellar system using D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) as a nanocarrier for co-delivery of docetaxel as a model chemotherapeutic drug and coumarin-6 as a model fluorescence imaging agent for simultaneous cancer imaging and therapy in an early stage. The theranostic micelles were prepared by a solvent casting method and characterized by their particle size, drug loading, drug encapsulation efficiency (EE) and in-vitro drug release profile. These dual modality micellar system TPDC6 micelles were successfully developed with average particle size of 79.59±0.57 nm in diameter and drug loading up to 15.46±1.02 % (EE of 78.99±1.26%) and 9.83±0.76 % (EE of 36.20±0.89%) for docetaxel and coumarin-6 respectively. Besides, the in-vitro drug release profile of the micelles revealed a desired sustained and controlled drug release manner for both docetaxel (21.62±0.36%) and coumarin-6 (10.70±0.46%). In conclusion, the micelles size obtained is in the favourable range for passive targeting through enhanced permeability and retention (EPR) effect and the drug loading and encapsulation efficiency attained are adequate for therapy and diagnosis purposes on cancer cells. This dual modality system is taking great advantages for tumour imaging and inhibition of tumour growth which is very important for early cancer detection.

scholarly journals Design and characterization of metoprolol floating matrix tablet

2017 ◽  
Vol 4 (2) ◽  
pp. 118
Author(s):  
Vasudha Bakshi ◽  
Swapna S. ◽  
Deepa Kumari Choudhary ◽  
Ch. Revanth ◽  
B. Sai KumarCh. Praveen ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Gastric Residence Time

Objective: The objective of the present research was to develop a matrix embedded floating tablet of Metoprolol for the sustained activity and prolongation of gastric residence time to improve the bioavailability of the drug. Metoprolol was chosen as a model drug because it is better absorbed in the stomach than the lower gastro intestinal tract.Methods: The experimental work was divided into pre-formulation studies, formulation development, and evaluation. Standardization of drug and excipients confirmed the authentication of the samples. Floating test were conducted for all formulations, In vitro dissolution studies were carried out in a dissolution testing apparatus-II, FTIR study was performed to interpret the drug ,excipient interaction.Results: Floating tests were also performed for 15 formulations and among them five formulations have passed the floating tests (F1, F3, F5, F7, and F14). The In-vitro release kinetics study of this tablet indicated sustained release for Metoprolol and followed zero order release and 95% drug in 8 h in vitro. The drug release profile of formulated product was compared with marketed product Metolar. The floating tablets extended the drug release up to 8 hours. The drug-polymer interaction was evaluated by fourier transform infrared spectroscopy (FTIR).Conclusions: F3 formulation showed the best floating results. The comparative study between F3 and Metolar (Marketed Product) showed the similar in vitro drug release profile. Thus, the optimzed formulation F-3 can be successfully used for the management of hypertension.

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