Formulation development and in-vitro/ex-vivo evaluation for a polysaccharide-based colon targeted matrix tablet

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohsina Shaikh ◽  
Neha Desai ◽  
Munira Momin ◽  
Lokesh Kumar Bhatt
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
Metoprolol Succinate ◽  
Gum Ghatti

Objective: The objective of this study was to develop and optimize a microflora-triggered colon targeted sustained-release dosage form using gum ghatti (GG) and hydroxypropyl methylcellulose (HPMC K100). Methods: GG and HPMC K100 were used to prepare microflora triggered colon targeted sustained-release dosage form. For evaluation, two different tablets comprising metoprolol succinate and mesalamine as an active ingredient were used with the objective of developing a platform technology for various categories of drugs. The tablets were coated with Eudragit® L100 and Eudragit® S100 to provide enteric coating and evaluated for hardness, thickness, friability, weight variation, disintegration, and drug content. In vitro release studies for the prepared tablets were carried out mimicking the physiological transit time. Further, the effects of microflora were evaluated using rat cecal content. Results: The in vitro dissolution profile of coated matrix tablets showed that 86.03±0.43% of metoprolol succinate and 80.26±0.67% of mesalamine were released at the end of 12 h. The ex vivo dissolution profile of coated matrix tablets showed that 96.50±0.27% of metoprolol succinate and 92.58±0.39% of mesalamine were released at the end of 12 h in the presence of rat ceacal content. The developed formulation was stable when subjected to the standard ICH stability study conditions. Conclusion: The result of this study showed that gum ghatti together with hydroxypropyl methylcellulose could be successfully used for the preparation of microflora triggered colon targeted matrix tablets.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

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

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
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.

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF ALMOND GUM BASED SUSTAINED RELEASE MATRIX TABLET OF INDOMETHACIN

2018 ◽  
Vol 11 (12) ◽  
pp. 166
Author(s):  
Ruchi Sunayana S ◽  
Gowda Dv ◽  
Vishal Gupta N ◽  
Praveen Sivadasu ◽  
Manjunath M
Keyword(s):  
Sustained Release ◽  
Research Work ◽  
Morphological Characteristics ◽  
Polymeric Matrix ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
Formulation Development

Objective: The aspiration of the current research involves employing various concentrations of polymer and filler to develop indomethacin sustained release (SR) matrix tablets. The objective of this research work is to reduce dosing frequency thereby increasing patients compliance and enhanced therapeutic activity.Methods: Polymers such as Almond gum (AG), polyvinylpyrrolidone (PVP), and starch at different concentrations were used for formulating SR polymeric matrix tablets. Evaluation of pre-compression and post-compression parameters was done for both granules and formulated tablets.Results: Results obtained from pre-compression parameters and post-compression parameters suggested that all the parameters are within the prescribed limits, demonstrating that formulated granules had shown better flow properties. The morphological characteristics of the developed tablet were observed by employing scanning electron microscope where the surface of the tablet was found to be smooth from the in vitro dissolution study, combination of AG (30 mg) with PVP (30 mg), and starch used as a filler has sustained the release of drug up to 10 h.Conclusion: Therefore, developed polymeric matrix tablet exhibited enhanced potency over a conventional tablet by exhibiting an excellent dissolution profile for a period of 10 h.

scholarly journals Formulation and In vitro Release Behavior of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Containing Poorly Soluble Fenofibrate

2020 ◽  
Vol 23 (1) ◽  
pp. 10-16
Author(s):  
Ramesh Kandel ◽  
Tushar Saha ◽  
Zia Uddin Masum ◽  
Jakir Ahmed Chowdhury
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
The Matrix

Fenofibrate, a water insoluble drug was used to prepare matrix tablet with four different viscosity grades of Hydroxypropyl Methylcellulose (HPMC) which were Methocel K4M CR, Methocel K15M CR, Methocel K100M CR and Methocel K100LV CR. The concentration of those excipients was 5, 10, 20, and 40% (w/w), respectively. The content of drug in a fixed quantity of powder in every formulation was ranged between 96.47 to 104.78 %. The dissolution study was done by using USP dissolution apparatus II. The kinetics of release was analyzed by using zero-order, first order, Korsmeyer-Peppas, Higuchi and Hixon-crowell equations to explain the drug release mechanism from the matrix tablets. In-vitro dissolution profile of matrix tablets were dependent upon the HPMC concentration and dissolution was rapid for tablets containing lower polymer proportion i.e. 5,10, and 20% Percentage (w/w) HPMC than those containing 40% (w/w) HPMC. Bangladesh Pharmaceutical Journal 23(1): 10-16, 2020

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Matrix Tablets of Venlafaxine

2017 ◽  
Vol II (I) ◽  
pp. 10-24
Author(s):  
Zubair Anwar ◽  
Tanveer Ahmed Khan ◽  
Muhammad Farhan Sohail ◽  
Maryam Anwar
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Sustained Effect ◽  
Release Data ◽  
Drug Studies

Sustained release matrix tablets of venlafaxine were formulated using synthetic polymers (ethylcellulose & hydroxypropyl methylcellulose). Six (06) different batches of matrix tablets of venlafaxine (dose 75 mg) were prepared by the wet granulation method. Polymers were used alone or in combination. The physical properties of compressed tablets were evaluated. In vitro release drug studies were performed in phosphate buffer at pH 6.8 over 24 hours. The drug release data fitted well to the First-order (R2 = 0.9725 � 0.9900). The n value obtained for most batches ranged from 0.523 to 0.946 indicates that the drug is released through an anomalous or non�Fickian transport. Results revealed that the combination of ethyl cellulose (EC) and hydroxypropyl methylcellulose produced a sustained effect compared to hydroxypropyl methylcellulose alone. Formulation F6 containing single polymer (EC) showed the highest control over initial burst release, and extended-release of the drug continued up to 16 hours.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals DESIGN AND IN VITRO CHARACTERIZATION OF FLOATING TABLETS OF METRONIDAZOLE

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.

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals Gastro-retentive floating beads of curcumin β-cyclodextrin complex to treat stomach tumors

2011 ◽  
Vol 1 (1) ◽  
pp. 12 ◽  
Author(s):  
Shishu Goindi ◽  
Kamalpreet Mann ◽  
Nidhi Aggarwal
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Solubility ◽  
Pharmacokinetic Studies ◽  
Cyclodextrin Complex ◽  
Enhanced Solubility ◽  
Tumor Studies ◽  
Gastro Retentive

The aim of present study was to develop a multi-unit gastro-retentive floating dosage form of curcumin with targeted and sustained release characteristics. Although, protective effect of curcumin against inflammation and cancer is well documented, the clinical potential is underutilized owing to the physicochemical properties of the molecule which lead to poor oral bioavailability. Aqueous solubility of curcumin was enhanced by complex formation with β-cyclodextrin (β-CD). This complex with enhanced solubility profile was further used to prepare multiple unit floating beads. Floating beads of curcumin β-cyclodextrin complex (FBCC) were prepared by dripping a mixture of sodium alginate and hydroxypropyl methylcellulose solution into calcium chloride solution acidified with acetic acid. FBCC were evaluated for percent drug entrapment, diameter, surface topography, buoyancy,<em> in vitro</em> release and pharmacodynamic activity against Benzo(a) pyrene [B(a)P] induced forestomach papillomas in albino female mice (Balb/C strain). The investigation revealed that floating beads possessed optimum formulation characteristics. The drug release from FBCC was fickian and sufficiently sustained for 12 h. Results of antitumor studies against B(a)P induced neoplasia of forestomach suggests that the tumor incidence significantly reduced (50%) using FBCC where as pure curcumin resulted in only 25% reduction. A multi-unit floating dosage form of curcumin β-CD complex possessing sustained release characteristics was developed for targeting gastric tumors. Results of i<em>n vitro</em> studies and anti-tumor studies in animals suggest that FBCC can be safely and effectively used to treat neoplasia of stomach. However, these preliminary investigations warrant further pharmacokinetic studies and clinical evaluation in humans

scholarly journals Formulation of Once a Day Controlled Release Tablet of Indomethacin Based on HPMC-Mannitol

1970 ◽  
Vol 4 (1) ◽  
pp. 55-67 ◽  
Author(s):  
Roshan Pradhan ◽  
Uttam Budhathoki ◽  
Panna Thapa
Keyword(s):  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Reference Sample ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Dissolution Profile ◽  
Key Words Indomethacin ◽  
Viscosity Grade

p>A hydroxypropyl methylcellulose (HPMC K4M, HPMC K15M, and HPMC K100M) matrix tablet containing Indomethacin along with mannitol was formulated as a function of HPMC viscosity, and was compared with the commercial products. The release characteristics of the matrix tablet were investigated in the intestinal fluid, 6.8 pH phosphate buffer for 12 hours. The formulated products and two marketed products as reference sample were studied for its different physicochemical parameters and in vitro dissolution studies. It was found that the drug release profile decreases with increase in viscosity of polymer and, with increase polymer level in the formulations. Matrix tablets formulated employing Drug:HPMC K15M:mannitol::1:0.25:1 and Drug:HPMC K15M:mannitol::1:0.25:2 gave slow release of indomethacin spread over 12 hours and their dissolution profiles were compared with the Indian marketed product. The dissolution profiles of both the formulations were similar to the dissolution profile of the marketed product, the similarity factor being 74.59 and 68.04 respectively. The dissolution profiles of formulations containing same viscosity grade of HPMC in remarkably different concentrations and different viscosity grade of HPMC in same concentrations were different. Key words: Indomethacin; Controlled release; Hydroxypropyl methyl cellulose; Mannitol; Dissolution. DOI: 10.3126/kuset.v4i1.2884 Kathmandu University Journal of Science, Engineering and Technology Vol.4, No.1, September 2008, pp 55-67

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