Insights into the mechanisms of chitosan–anionic polymers-based matrix tablets for extended drug release

2014 ◽  
Vol 476 (1-2) ◽  
pp. 253-265 ◽  
Author(s):  
Liang Li ◽  
Linlin Wang ◽  
Jinfeng Li ◽  
Shan Jiang ◽  
Yitong Wang ◽  
...  
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Anionic Polymers

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

Influence of Formulation Variables and Processing Techniques on Drug Release from Carbopol-971 based Matrix Tablets of Cinnarizine and Nimodipine.

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Weight Variation ◽  
Diffusion Controlled ◽  
The Matrix ◽  
Processing Techniques ◽  
Formulation Variables

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.

Colon targeting oral matrix tablets of mesalamine: Design, development and invitro evaluation

2020 ◽  
Vol 10 (1) ◽  
pp. 18-27
Author(s):  
Audinarayana N ◽  
Anala Srinivasulu ◽  
Vellore Sruthikumari ◽  
Likitha ◽  
Ananda Deepak V
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Stability Study ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Matrix Tablet ◽  
Cellulose Acetate Phthalate ◽  
Design Development ◽  
Release Pattern ◽  
The Matrix

The principle in this present research is to formulate Mesalamine containing colon targeted tablets by using different polymers and evaluate the effect of different polymers in drug release pattern. The matrix tablets of Mesalamine are formulated by polysaccharides based polymers like Cellulose acetate phthalate (CAP), Ethyl cellulose (EC), Guar gum (GG) and Xanthan gum (XG) which protects the drug to release in Stomach and Small Intestine. The invitro drug dissolution investigation of F2 (GG and XG) Matrix tablet was controlled by swelling into a viscous gel in colonic pH, which have been accomplished as the best tablet. The optimized tablet F2 was found to be stable in stability study (short term) with reproducible evaluation data, which also shows the highest swelling index, increased viscosity in colonic pH. The drug release pattern from the F2 formulation follows swelling and erosion behavior. From the data it show that F2 tablets suitable for providing colon targeted drug delivery.

A Comparative Study of Matrix Tablets Designed by Different Methods

2017 ◽  
Vol 10 (2) ◽  
pp. 3645-3652
Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Once Daily ◽  
Gum Acacia ◽  
Weight Variation ◽  
Evaluation Parameters

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  

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.   

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

2018 ◽  
Vol 11 (5) ◽  
pp. 4259-4268
Author(s):  
Nirmala Rangu ◽  
Gande Suresh
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Magnesium Stearate ◽  
Zero Order ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Dissolution Profile ◽  
Release Formulation

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

Evaluation of swelling properties and drug release from mechanochemical pre-gelatinized glutinous rice starch matrix tablets by near infrared spectroscopy

2021 ◽  
pp. 096703352098235
Author(s):  
Tomomi Takaku ◽  
Yusuke Hattori ◽  
Tetsuo Sasaki ◽  
Tomoaki Sakamoto ◽  
Makoto Otsuka
Keyword(s):  
Drug Release ◽  
Near Infrared ◽  
Nir Spectroscopy ◽  
Matrix Tablets ◽  
Rice Starch ◽  
Release Time ◽  
Swelling Properties ◽  
X Ray ◽  
Glutinous Rice ◽  
Pharmaceutical Properties

The effect of grinding on the pharmaceutical properties of matrix tablets consisting of ground glutinous rice starch (GRS) and theophylline (TH) was predicted by near infrared (NIR) spectroscopy. Ground GRS samples were prepared by grinding GRS in a planetary ball mill for 0-120 min, measured by X-ray diffractometry (XRD) and NIR, and then evaluated for crystallinity (%XRD) based on XRD profiles. Tablets containing TH (5 w/w%), ground GRS (94 w/w%), and magnesium stearate (1 w/w%) were formed by compression. Gel-forming and drug-release processes of the tablets were measured using a dissolution instrument with X-ray computed tomography (XCT). Swelling ratio (SWE) and mean drug-release time (MDT) were evaluated based on XCT and drug-release profiles, respectively. Calibration models for predicting percent %XRD, MDT, and SWE were constructed based on the NIR of ground GRS using partial least-squares. The results indicated the possibility of controlling the pharmaceutical properties of matrix tablets by altering the pre-gelatinization of GRS based on changes in their NIR spectra during the milling process.

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