scholarly journals Formulation development and Stability Studies of Meropenem Extended-Release matrix Tablets

2018 ◽  
pp. 1-12
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Methyl Cellulose ◽  
Film Coating ◽  
Matrix Tablets ◽  
Formulation Development ◽  
High Concentration ◽  
Drug Diffusion

The aim of this research was to develop a new hydrophilic matrix system containing meropenem (MEX). Extended-release tablets are usually intended for once-a-day administration with benefits to the patient and lower discontinuation of the therapy. Formulations were developed with hydroxyl propyl methyl cellulose or poly (ethylene oxide) as hydrophilic polymers, with different molecular weights (MWs) and concentrations (20 and 30%). The tablets were found to be stable (6 months at 40 ± 2°C and 75± 5% relative humidity), and the film-coating process is recommended to avoid MEX photo-degradation. The dissolution profiles demonstrated an extended-release of MEX for all developed formulations. Dissolution curves analyzed using the Korsmeyer exponential equation showed that drug release was controlled by both drug diffusion and polymer relaxation or erosion mechanisms. A more erosion controlled system was obtained for the formulations containing lower MW and amount of polymer. With the increase in both MW and amount of polymer in the formulation, the gel layer became stronger, and the dissolution was more drug-diffusion dependent. Formulations containing intermediate MW polymers or high concentration (30%) of low MW polymers demonstrated a combination of extended and complete in vitro drug release. This way, these formulations could provide an increased bioavailability in vivo.

scholarly journals Formulation Development and Stability Studies of Norfloxacin Extended-Release Matrix Tablets

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Paulo Renato Oliveira ◽  
Cassiana Mendes ◽  
Lilian Klein ◽  
Maximiliano da Silva Sangoi ◽  
Larissa Sakis Bernardi ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Film Coating ◽  
Matrix Tablets ◽  
Formulation Development ◽  
High Concentration ◽  
Drug Diffusion ◽  
Erosion Mechanisms

The aim of this research was to develop a new hydrophilic matrix system containing norfloxacin (NFX). Extended-release tablets are usually intended for once-a-day administration with benefits to the patient and lower discontinuation of the therapy. Formulations were developed with hydroxypropylmethylcellulose or poly(ethylene oxide) as hydrophilic polymers, with different molecular weights (MWs) and concentrations (20 and 30%). The tablets were found to be stable (6 months at40±2°C and75±5% relative humidity), and the film-coating process is recommended to avoid NFX photodegradation. The dissolution profiles demonstrated an extended-release of NFX for all developed formulations. Dissolution curves analyzed using the Korsmeyer exponential equation showed that drug release was controlled by both drug diffusion and polymer relaxation or erosion mechanisms. A more erosion controlled system was obtained for the formulations containing lower MW and amount of polymer. With the increase in both MW and amount of polymer in the formulation, the gel layer became stronger, and the dissolution was more drug-diffusion dependent. Formulations containing intermediate MW polymers or high concentration (30%) of low MW polymers demonstrated a combination of extended and complete in vitro drug release. This way, these formulations could provide an increased bioavailability in vivo.

scholarly journals Formulation, Development, and Optimization of Anti- Hypertensive Nisoldipine Extended-Release Tablet Formulation

2020 ◽  
Vol 5 (03) ◽  
pp. 37-44
Author(s):  
Kukkadapu Pavan Kumar ◽  
Katta Sunand ◽  
Nerella Mounika ◽  
Mohammed Abdul Samad ◽  
A. Madhu Babu ◽  
...  
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
Aqueous Solubility ◽  
Cellular Membrane ◽  
Tablet Formulation ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Formulation Development ◽  
Release Tablet

A drug molecule has to be water-soluble to be readily delivered to the cellular membrane. Many drugs are waterinsoluble, which creates numerous problems in the development of dosage forms. Controlled drug delivery formulation releases the drug with controlled kinetics for days and months, reducing the frequency of dosing, minimizing side effects, and improving patient compliance. Nisoldipine is a calcium channel antagonist that is indicated for the treatment of hypertension with very poor aqueous solubility. Thus, there is a need to improve the rate of drug release. Hence, the study was carried out to design, formulate and evaluate sustained-release tablet formulation of nisoldipine. Nisoldipine controlled release matrix tablets were prepared by roll compaction method. Preformulation studies have confirmed the purity and compatibility of drug with excipients used in the formulation. Pre-compression studies have confirmed the stability of formulation blends for compression. All the prepared formulations were evaluated for various physical and compression parameters such as bulk and tapped density, hardness, friability, and in vitro drug release studies. The results of drug release from prepared compressed nisoldipine extended-release tablets were found to be within the desired range.

scholarly journals Plasticiser-Free 3D Printed Hydrophilic Matrices: Quantitative 3D Surface Texture, Mechanical, Swelling, Erosion, Drug Release and Pharmacokinetic Studies

Polymers ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 1095 ◽  
Author(s):  
Zara Khizer ◽  
Muhammad R. Akram ◽  
Rai M. Sarfraz ◽  
Jorabar Singh Nirwan ◽  
Samia Farhaj ◽  
...  
Keyword(s):  
Drug Release ◽  
Surface Texture ◽  
Drug Absorption ◽  
Extended Release ◽  
Matrix Tablets ◽  
Hydrophilic Matrices ◽  
3D Printed ◽  
3D Surface Texture

Hydroxypropyl methyl cellulose, HPMC, a hydrophilic polymer, is widely used for the development of extended release hydrophilic matrices and it is also considered as a good contender for the fabrication of 3D printing of matrix tablets. It is often combined with plasticisers to enable extrusion. The aim of the current project was to develop plasticizer-free 3D printed hydrophilic matrices using drug loaded filaments prepared via HME to achieve an in vitro (swelling, erosion and drug release) and in vivo (drug absorption) performance which is analogous to hydrophilic matrix tablets developed through conventional approaches. Additionally, the morphology of the printed tablets was studied using quantitative 3D surface texture studies and the porosity calculated. Filaments were produced successfully and used to produce matrix tablets with acceptable drug loading (95–105%), mechanical and surface texture properties regardless of the employed HPMC grade. The viscosity of HPMC had a discernible impact on the swelling, erosion, HPMC dissolution, drug release and pharmacokinetic findings. The highest viscosity grade (K100M) results in higher degree of swelling, decreased HPMC dissolution, low matrix erosion, decreased drug release and extended drug absorption profile. Overall, this study demonstrated that the drug loaded (glipizide) filaments and matrix tablets of medium to high viscosity grades of HPMC, without the aid of plasticisers, can be successfully prepared. Furthermore, the in vitro and in vivo studies have revealed the successful fabrication of extended release matrices.

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

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 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.

scholarly journals Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

2011 ◽  
Vol 61 (2) ◽  
pp. 217-226 ◽  
Author(s):  
Komuravelly Someshwar ◽  
Kalyani Chithaluru ◽  
Tadikonda Ramarao ◽  
K. Kumar
Keyword(s):  
Drug Release ◽  
Residence Time ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Gastric Residence Time

Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility through-out the length of the gastrointestinal tract. The objective of the present investigation was to develop effervescent floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34-40 %) and short biological half life (4.2 h). Tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropyl methylcellulose (HPMC K4M, K15M and K100M). Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in vitro drug release characteristics in 12 hours. Drug release from effervescent floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there is no drug excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. Optimized formulation (F9) was selected based on the similarity factor (f2) (74.2), dissolution efficiency at 2, 6 and 8 h, and t50 (5.4 h) and was used in radiographic studies by incorporating BaSO4. In vivo X-ray studies in human volunteers showed that the mean gastric residence time was 6.2 ± 0.2 h.

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

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 DESIGN AND IN VITRO/IN VIVO EVALUATION OF EXTENDED RELEASE MATRIX TABLETS OF NATEGLINIDE

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Mohini Sihare ◽  
Rajendra Chouksey
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vivo Studies ◽  
Release Mechanism ◽  
In Vivo Evaluation

Aim: Nateglinide is a quick acting anti-diabetic medication whose potent activity lasts for a short duration. One of the dangerous side effects of nateglinide administration is rapid hypoglycemia, a condition that needs to be monitored carefully to prevent unnecessary fatalities. The aim of the study was to develop a longer lasting and slower releasing formulation of nateglinide that could be administered just once daily. Methods: Matrix tablets of nateglinide were prepared in combination with the polymers hydroxypropylmethylcellulose (HPMC), eudragits, ethyl cellulose and polyethylene oxide and the formulated drug release patterns were evaluated using in vitro and in vivo studies. Conclusion: Of the seventeen formulated matrix tablets tested, only one formulation labelled HA-2 that contained 15% HPMC K4M demonstrated release profile we had aimed for. Further, swelling studies and scanning electron microscopic analysis confirmed the drug release mechanism of HA-2. The optimized formulation HA-2 was found to be stable at accelerated storage conditions for 3 months with respect to drug content and physical appearance. Mathematical analysis of the release kinetics of HA-2 indicated a coupling of diffusion and erosion mechanisms. In-vitro release studies and pharmacokinetic in vivo studies of HA-2 in rabbits confirmed the sustained drug release profile we had aimed for. Keywords: Hydroxypropylmethylcellulose, Matrix tablets, Nateglinide, Sustained release

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