Achieving a robust drug release from extended release tablets using an integrated continuous mixing and direct compression line

2016 ◽  
Vol 511 (1) ◽  
pp. 659-668 ◽  
Author(s):  
Satu Lakio ◽  
Pirjo Tajarobi ◽  
Håkan Wikström ◽  
Magnus Fransson ◽  
Johan Arnehed ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Direct Compression ◽  
Continuous Mixing ◽  
Compression Line

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

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

scholarly journals Development of extended-release formulation of domperidone using a blend of Raphia hookeri gum and hydroxypropyl methylcellulose as tablet matrix

2017 ◽  
Vol 16 (10) ◽  
pp. 2341-2347
Author(s):  
Emmanuel O. Olorunsola ◽  
Stephen O. Majekodunmi
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Extended Release ◽  
Hydroxypropyl Methylcellulose ◽  
Direct Compression ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
Raphia Hookeri ◽  
The Matrix ◽  
The Individual

Purpose: To develop an extended-release formulation of domperidone using a blend of Raphia hookeri gum and hydroxypropyl methylcellulose as tablet matrix.Methods: Tablets (400 mg) containing 30 mg domperidone (DPD) were formulated using binary mixtures of hydroxypropyl methylcellulose (HPMC) and Raphia hookeri gum (RHG) as matrix former; and microcrystalline cellulose (MCC) as direct compression excipient. The proportions of the matrix formers (40 % of tablet weight) was varied as 100:0, 75:25, 50:50, 25:75 and 0:100. The composition of the matrix former was also kept constant (50:50) while MCC was varied as 40, 30, 20 and 10 %. The tablets were evaluated for compact density, tensile strength, friability and drug release over 24 h.Results: The tensile strength of tablets decreased while their friability increased with increase in the proportion of RHG. A similar trend was observed with decrease in the concentration of MCC. Tablets containing RHG alone as matrix former and 40 % MCC as direct compression excipient had tensile strength of 0.95 MNm-2, friability of 1.07 % and cumulative drug release of 83.2 % over a period of 24 h. Tablets containing equal proportions of HPMC and RHG as matrix former had the best release properties of 95.0 % over a period of 24 h.Conclusion: RHG is comparable with HPMC in terms of extending the release of  domperidone for a once daily administration. A suitable combination of the two  polymers for use as a matrix former is superior to either of the individual polymers.Keywords: Domperidone, Extended drug release, Hydroxypropyl methylcellulose, Raphia hookeri gum, Tablet properties

Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and Cassia fistula Seed Gum by QbD Approach

2020 ◽  
Vol 17 (5) ◽  
pp. 422-437
Author(s):  
Dixita Jain ◽  
Akshay Sodani ◽  
Swapnanil Ray ◽  
Pranab Ghosh ◽  
Gouranga Nandi
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Extended Release ◽  
Polymer Concentration ◽  
Green Manufacturing ◽  
Full Factorial Design ◽  
Cassia Fistula ◽  
Negative Environmental Impact ◽  
Seed Gum ◽  
Full Factorial

Aim: This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. Background: The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been reported as a solution to this problem. But most of them are found to be composed of synthetic, semi-synthetic or their combination having physiological toxicity as well as negative environmental impact. Therefore, fabrication and formulation of multi-unit extended-release peroral preparations with natural, non-toxic, biodegradable polymers employing green manufacturing processes are being appreciated worldwide. Objective: Lamotrigine-loaded extended-release multi-unit beads have been fabricated with the incorporation of a natural polysaccharide Cassia fistula seed gum in calcium-cross-linked alginate matrix employing a simple green process and 23 full factorial design. Methods: The total polymer concentration, polymer ratio and [CaCl2] were considered as independent formulation variables with two different levels of each for the experiment-design. The extended-release beads were then prepared by the ionotropic gelation method using calcium chloride as the crosslinkerions provider. The beads were then evaluated for drug encapsulation efficiency and drug release. ANOVA of all the dependent variables such as DEE, cumulative % drug release at 2h, 5h, 12h, rate constant and dissolution similarity factor (f2) was done by 23 full factorial design using Design-Expert software along with numerical optimization of the independent variables in order to meet USP-reference release profile. Results: The optimized batch showed excellent outcomes with DEE of 84.7 ± 2.7 (%), CPR2h of 8.41± 2.96 (%), CPR5h of 36.8± 4.7 (%), CPR12h of 87.3 ± 3.64 (%) and f2 of 65.9. Conclusion: This approach of the development of multi-unit oral devices utilizing natural polysaccharides might be inspiring towards the world-wide effort for green manufacturing of sustained-release drug products by the QbD route.

scholarly journals Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technology

2009 ◽  
Vol 59 (1) ◽  
pp. 15-30 ◽  
Author(s):  
Pramod Kumar ◽  
Sanjay Singh ◽  
Brahmeshwar Mishra
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Relative Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Healthy Human ◽  
Tramadol Hydrochloride ◽  
Release Formulation ◽  
Extended Release Formulation

Development and biopharmaceutical evaluation of extended release formulation of tramadol hydrochloride based on osmotic technologyExtended release formulation of tramadol hydrochloride (TRH) based on osmotic technology was developed and evaluated. Target release profile was selected and different variables were optimized to achieve it. Formulation variables such as the level of swellable polymer, plasticizer and the coat thickness of semipermeable membrane (SPM) were found to markedly affect drug release. TRH release was directly proportional to the levels of plasticizer but inversely proportional to the levels of swellable polymer and coat thickness of SPM. Drug release from developed formulations was independent of pH and agitation intensity but dependent on osmotic pressure of the release media.In vivostudy was also performed on six healthy human volunteers and various pharmacokinetic parameters (cmax,tmax,AUC0-24,MRT) and relative bioavailability were calculated. Thein vitroandin vivoresults were compared with the performance of two commercial TRH tablets. The developed formulation provided more prolonged and controlled TRH release compared to the marketed formulation.In vitro-in vivocorrelation (IVIVC) was analyzed according to the Wagner-Nelson method. The optimized formulation (batch IVB) exhibited good IVIV correlation (R= 0.9750). The manufacturing procedure was found to be reproducible and formulations were stable over 6 months of accelerated stability testing.

In vitro and in vivo release of dinalbuphine sebacate extended release formulation: Effect of the oil ratio on drug release

2017 ◽  
Vol 531 (1) ◽  
pp. 306-312 ◽  
Author(s):  
Chan-Jung Li ◽  
Mei-Yun Ku ◽  
Chia-Yin Lu ◽  
Yu-En Tien ◽  
Wendy H. Chern ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Release Formulation ◽  
Extended Release Formulation ◽  
In Vivo Release

scholarly journals FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Rapid Release ◽  
Weight Variation ◽  
Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

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