Swelling of Hydroxypropyl Methylcellulose Matrix Tablets. 2. Mechanistic Study of the Influence of Formulation Variables on Matrix Performance and Drug Release

Floating matrix tablets were designed and evaluated. Theophylline was used as a model drug. The system was prepared by mixing drug, matrix-forming polymer (hydroxypropyl methylcellulose, HPMC) and fillers together. The blended powder was compressed by hydraulic press. The effect of formulation variables such as type of matrix forming polymer (HPMC K100LV, HPMC K4M, HPMC K100M), amount of effervescent agent (0, 20, 30, 40% w/w) and compression force (0.5, 1 ton) on floating properties and drug release of floating matrix tablets were investigated. The results demonstrated that type of polymer affected floating properties of the floating matrix tablets. The floating matrix tablets prepared from lower viscosity HPMC (HPMC K100LV) showed faster drug release than those prepared from higher viscosity HPMC (HPMC K4M, HPMC K100M). Increasing amount of effervescent agent decreased time to float and increased drug release from the floating matrix tablets. Higher compression force did not affect time to float but decreased drug release from the floating matrix tablets. According to these results, floating properties and drug release of the floating matrix tablets could be modified by formulation variables. Some floating tablet formulations developed in this study showed good floating properties (time to float less than 15 minutes, floating time more than 8 hours) with sustained release as required. The system is promising as a carrier for gastroretentive drug delivery systems.

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

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v2i1.8840 ◽

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.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.1.8 ◽

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.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.5.6 ◽

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.

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Formulation and evaluation of effervescent floating tablets of tizanidine hydrochloride

Acta Pharmaceutica ◽

10.2478/v10007-011-0015-5 ◽

2011 ◽

Vol 61 (2) ◽

pp. 217-226 ◽

Cited By ~ 7

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.

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Response Surface Optimization of Sustained Release Metformin-Hydrochloride Matrix Tablets: Influence of Some Hydrophillic Polymers on the Release

ISRN Pharmaceutics ◽

10.5402/2012/364261 ◽

2012 ◽

Vol 2012 ◽

pp. 1-10 ◽

Cited By ~ 1

Author(s):

Amitava Roy ◽

Kalpana Roy ◽

Sarbani Roy ◽

Jyotirmoy Deb ◽

Amitava Ghosh ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Hydroxypropyl Methylcellulose ◽

Dissolution Kinetics ◽

Matrix Tablets ◽

Metformin Hydrochloride ◽

Wet Granulation ◽

Matrix Tablet ◽

Response Surface Optimization

The aim of the present work was designed to develop a model-sustained release matrix tablet formulation for Metformin hydrochloride using wet granulation technique. In the present study the formulation design was employed to statistically optimize different parameters of Metformin hydrochloride tablets at different drug-to-polymer ratios employing polymers Hydroxypropyl methylcellulose of two grades K4M and K100M as two independent variables whereas the dependent variables studied were X60, X120, T50, T90, n, and b values obtained from dissolution kinetics data. The in vitro drug release studies were carried out at simulated intestinal fluids, and the release showed a non-Fickian anomalous transport mechanism. The drug release was found to reveal zero order kinetics. The granules and the tablets were tested for their normal physical, morphological, and analytical parameters and were found to be within the satisfactory levels. There were no significant drug-polymer interactions as revealed by infrared spectra. It has been found out that on an optimum increased Hydroxypropyl methylcellulose K100M concentration and decreased Hydroxypropyl methylcellulose K4M concentration the formulations were elegant in terms of their release profiles and were found to be statistically significant and generable.

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FORMULATION AND EVALUATION OF FLOATING MATRIX TABLETS OF LEVOFLOXACIN HEMIHYDRATE USING HYDROXYPROPYL METHYLCELLULOSE K4M TO TREAT HELICOBACTER PYLORI INFECTION

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i6.20296 ◽

2018 ◽

Vol 11 (6) ◽

pp. 148

Author(s):

Srinivasa Rao Baratam ◽

Vijayaratna J

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Release Kinetics ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Linear Regression Method ◽

In Vitro Drug Release ◽

Sustained Drug Delivery

Objective: The aim of the study was to develop a floating drug delivery system of levofloxacin (LVF) hemihydrate for sustained drug delivery to improve the extended retention in the stomach, oral bioavailability, and local site-specific action in the stomach. Methods: Preparation of LVF tablets using melt granulation method using hydroxypropyl methylcellulose (HPMC) K4M with sodium bicarbonate as gas generating agent. From LFTA1 to LFTA5, formulations were developed and evaluated for floating properties for swelling characteristics and in vitro drug release studies. In vitro dissolution was carried out using USP II paddle method using 0.1N HCI pH buffer at 50 rpm and samples were measured at 294 nm using ultraviolet-visible spectroscopy. Results: Obtained Fourier-transform infrared charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. In vitro drug release was performed and drug release kinetics were evaluated using the linear regression method and were found to be followed the zero-order release by diffusion controlled release. Optimized formula was found to be LFTA4 with 20% of a polymer with 99.03% of drug release with 12 h of floating time and 32 s floating lag time. Conclusion: Matrix tablets (LFTA4) formulated employing 20% HPMC K4M are best suited to be used for gastroretentive dosage form of LVF.

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DESIGN AND IN VITRO CHARACTERIZATION OF FLOATING TABLETS OF METRONIDAZOLE

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2019.v12i3.31018 ◽

2019 ◽

pp. 539-544

Author(s):

CHINNA ESWARAIAH M ◽

JAYA S

Keyword(s):

Drug Release ◽

Xanthan Gum ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Release Mechanism ◽

Content Uniformity ◽

Matrix Tablet ◽

N Value

Objective: The objective of the present study was to formulate the effervescent floating matrix tablet of metronidazole and to evaluate the effect of varying concentrations of hydrophilic polymers on drug release. Methods: Drug excipients interaction was studied by Fourier transform infrared spectrophotometer. The effervescent floating matrix tablets were prepared by direct compression technique using hydroxypropyl methylcellulose (HPMCK4) and xanthan gum alone and in combination as release retardants. Microcrystalline cellulose was used as diluent. Sodium bicarbonate was used as effervescent agent. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity, buoyancy time, and in vitro dissolution. Results: Micromeritic properties and post-compression parameters were evaluated and all the parameters were found within the acceptable limit. The drug release data were subjected to different models to evaluate release kinetics and mechanism of drug release. The matrix tablets prepared with xanthan gum and a mixture of xanthan gum and HPMCK4 were retarded the drug release up to 12 h. The release mechanism of metronidazole was evaluated on the basis of release exponent n value in Peppas model. The n value of the formulations ranged from 0.46 to 0.89 which indicated Case II transport and zero-order release. Conclusion: Floating matrix tablet is the simple, efficient, and economic method to sustain the release of metronidazole to eradicate Helicobacter pylori in peptic ulcer disease.

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Development and evaluation of gastroretentive norfloxacin floating tablets

Acta Pharmaceutica ◽

10.2478/v10007-009-0019-6 ◽

2009 ◽

Vol 59 (2) ◽

pp. 211-221 ◽

Cited By ~ 14

Author(s):

Ramesh Bomma ◽

Rongala Swamy Naidu ◽

Madhusudan Yamsani ◽

Kishan Veerabrahma

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

Fickian Diffusion ◽

Release Mechanism ◽

Wet Granulation ◽

Drug Bioavailability ◽

Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

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In Vitro Evaluation of Sustained Released Matrix Tablet Formulations of Clarithromvcin

Scientia Pharmaceutica ◽

10.3797/scipharm.aut-05-05 ◽

2005 ◽

Vol 73 (1) ◽

pp. 59-74

Author(s):

Lütfi Genç ◽

A. Kıran

Keyword(s):

Drug Release ◽

Hydroxypropyl Methylcellulose ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Assay Method ◽

Content Uniformity ◽

Matrix Tablet ◽

Compression Technique ◽

23 Factorial Design

Sustained release matrix tablets of clarithromycin were prepared using different polymers as Hydroxypropyl methylcellulose (H PMC), Carbopol 934 and Eudragit RL/PO by direct compression technique. For the quality control of these formulations, weight deviation, hardness, friability, diameter-height ratio, content uniformity of the active substance and in vitro dissolution technique were performed. HPLC was used for the assay of clarithromycin and the assay method was validated. Dissolution profiles of the tablets were plotted and evaluated kinetically. The effects on drug release of polymer type and concentrations were investigated by 23 factorial design. The tablets containing HPMC, Carbopol 934 and Eudragit RLIPO were found suitably to sustain drug release

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