scholarly journals DoE-Based Design of a Simple but Efficient Preparation Method for a Non-Effervescent Gastro-Retentive Floating Tablet Containing Metformin HCl

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1225
Author(s):  
Byungsuk Kim ◽  
Youngjoo Byun ◽  
Eun Hee Lee
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Cetyl Alcohol ◽  
Metformin Hydrochloride ◽  
High Dose ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Bootstrap Analysis ◽  
Similarity Factor ◽  
Gastro Retentive

A sustained-release non-effervescent floating matrix tablet was prepared using a simple and efficient direct compression of spray-dried granules containing metformin hydrochloride and cetyl alcohol with hydroxypropyl methylcellulose K15M (HPMC K15M). The design of experiments was employed to explore the optimal composition of the tablet. The similarity factor was employed to evaluate the equivalence in dissolution profiles between the test tablets and Glucophage XR as a reference. Bootstrap analysis was used to eliminate the formulations for which the dissolution profile was potentially inequivalent to that of the reference. The optimized tablet consisting of 150 mg of cetyl alcohol and 17% HPMC K15M showed a dissolution profile comparable with that of the reference with a similarity factor of 52.41, exhibited a floating lag time of less than 3 s in buffer media, remained floating for 24 h, and reduced the tablet weight by about 20% compared to that of the reference. The current study sheds light on the potential use of non-effervescent gastro-retentive extended-release tablets for high-dose drugs using a simple and efficient direct compression method, and as a potential alternative treatment for Glucophage XR. This study also highlights the importance of a systematic approach to formulation optimization and the evaluation of the dissolution profile.

scholarly journals Formulation and In-vitro evaluation of sustained release matrix tablet of Metformin hydrochloride

2019 ◽  
Vol 9 (3) ◽  
pp. 95-98
Author(s):  
Ravi U Gaware ◽  
Gayatri R Waykar ◽  
Madhuri K Yewale ◽  
Rutuja B Mhaske ◽  
Poonam S Mhaske
Keyword(s):  
Sustained Release ◽  
Ethyl Cellulose ◽  
Metformin Hydrochloride ◽  
High Dose ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Hydrophilic Matrix ◽  
Compaction Behavior

The low bioavailability and short half-life of Metformin hydrochloride (MH) make the development of sustained-release forms desirable. Present work involves preparation and optimization of sustained release matrix tablet of MH by direct compression method using HPMC K 100 and ethyl cellulose as a matrix forming polymer. Avicel was added as a direct compaction vehicle to improve the compaction behavior of Metformin which otherwise exhibits poor compaction behavior which again is further increased by its relatively high dose. Hydrophilic matrix of HPMC alone resulted in initial burst of Metformin release, however when combined with ethyl cellulose drug release was slowed down and thereafter it became optimal at particular concentration of polymers. Keywords:  Metformin, HPMC, Ethyl cellulose, sustained release, matrix, tablet.

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 AND EVALUATION OF EFFERVESCENT GASTRO-RETENTIVE FLOATING TABLETS FOR CONTROLLED RELEASE OF AN ANTI-ULCER COMPOUND

2013 ◽  
Vol 3 (1) ◽  
pp. 23-30
Author(s):  
Aleksandar Aleksovski ◽  
◽  
Emina Zahirović ◽  
Amra Demirović ◽  
Emilija Spaseska Aleksovska ◽  
...  
Keyword(s):  
Small Intestine ◽  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Different Types ◽  
Model Drug ◽  
Absorption Window ◽  
Pharmacopoeial Requirements ◽  
Gastro Retentive

Effervescent floating gastro-retentive matrix tablets present novel and promising approach towards targeted and controlled drug delivery in the stomach and in the upper part of the small intestine. This kind of dosage form could be obtained by combining in a suitable ratio effervescent compounds and hydrophilic/hydrophobic polymer/s. The aim of our investigation was to develop controlled release effervescent matrix tablet which will float over the gastric media for longer than 8 hours and will release the active compound in a continuous manner over 8 hours period. We used ranitidine HCl as a model drug which has narrow absorption window in the upper small intestine, and is a good candidate for this type of dosage forms. We employed sodium bicarbonate and citric acid as effervescent compounds and two different types of hydroxypropyl methylcellulose (HPMC K4M and HPMC K15M) as a controlled release hydrophilic polymer. Three batches of tablets were produced (one containing HPMC K4M, other containing HPMC K15M, and the third containing 1:1 mixture of these two polymers) and every batch was compressed with two different forces 5.5 kN and 4.7 kN, so completely six probes of tablets were made. All six probes complied the pharmacopoeial requirements concerning mass uniformity, content, friability and hardness. All six probes tended to float fast to the surface of the medium and tend to hydrate and swell fast enough which actions provided controlled release of the compound over period of 8 hours. No significant differences in the dissolution profiles of all six probes were noticed during the investigation.

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

DEVELOPMENT OF FLOATING GASTRORETENTIVE DRUG DELIVERY SYSTEM BASED ON A NOVEL EXCIPIENT FOR METFORMIN HYDROCHLORIDE USING MIXTURE DESIGN

2020 ◽  
pp. 62-71
Author(s):  
R. PAWAR ◽  
S. JAGDALE ◽  
D. RANDIVE
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Mixture Design ◽  
Release Profile ◽  
Metformin Hydrochloride ◽  
Matrix Tablet ◽  
Vitro Release

Objective: The present study aimed to develop a new SR metformin hydrochloride (MH) gastroretentive formulation with novel excipient (NE), which has better floatation and can be prepared with more simple pharmaceutical techniques for the treatment of diabetes Mellitus. Methods: A gastro-retentive floating matrix tablet (GFT) formulation of MH was prepared using various concentrations of PEO (Polyox WSR-303) and hydroxypropyl methylcellulose K100M (HPMC K100 M) and Floating agent (novel excipient) to achieve desirable TFT, FLT and drug release. The wet granulation method was selected using isopropyl alcohol as a binder for the preparation of tablets. D-optimal non-simplex mixture design was used for the selection of suitable polymer concentrations and floating agents. Release kinetics was used to determine the mechanism of drug release. Results: It was observed that GFT with optimum quantities of PEO, HPMC K100M, and the floating agent showed 100 % of drug release in 24h with FT up to 24h and minimum FLT of less than 2 min. Formulation with an in vitro release profile slower to the marketed sample was prepared. Conclusion: A sustained-release (GFT) of MH tablets using PEO-, HPMC K100M, and an effervescent system was successfully prepared. AGFT formulation with an in vitro release profile slower to the marketed sample that releases MH for 24h may suitable for once-daily dosing can be prepared.

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 In Vitro Release Kinetic Study of Ciprofloxacin HCl from Methocel K15M CR, Methocel K4M CR and Methocel K4M Premium Matrix Tablets

1970 ◽  
Vol 2 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Muhammad Shahidul Islam ◽  
Tasnuva Haque ◽  
Rumana Jahangir ◽  
Kanij Fatema ◽  
Mynol Islam Vhuiyan ◽  
...  
Keyword(s):  
Release Rate ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Release Kinetic ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Kinetic Order ◽  
Kinetics Of

In the present study Ciprofloxacin HCl sustained release matrix tablet was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K4M CR, Methocel K4M Premium & Methocel K15M CR by direct compression method. Different amount of Methocel K15M CR was used to develop matrix builder in the three proposed formulations (F1-F3) for the study of release rate retardant effect at 5%, 6%, and 7% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M CR based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for 8 hours using USP dissolution apparatus II. Similarly Methocel K4M premium was used to develop matrix builder in another three proposed formulations (F4-F6). It was found that formulations F-4 (15%), F-5 (17%) and F-6 (18.3%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-4, F-5 and F-6 followed Higuchi kinetic order. Again Methocel K4M premium was used for another three proposed formulations (F7-F9). It was found that formulations F-7 (6.7%), F-8 (12.3%) and F-9 (15.6%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-7, F-8 and F-9 followed Higuchi kinetic order. Among these three polymers, Methocel K4M Premium showed better release retardant effect than Methocel K4M CR and Methocel K15M CR. Key Words: Ciprofloxacin HCl; Direct compression; Controlled release; Methocel K15M CR; Methocel K4M CR; Methocel K4M premium.DOI: 10.3329/sjps.v2i1.5814Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 37-43

scholarly journals CONTROLLED-RELEASE EFFERVESCENT FLOATING MATRIX TABLETS OF METFORMIN USING COMBINATION OF POLYMERS

2016 ◽  
Vol 8 (11) ◽  
pp. 114
Author(s):  
Meenakshi Bhavesh Patel ◽  
Farhatjahan Shaikh ◽  
Vandana Patel ◽  
Naazneen Imtiaz Surti
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
Statistical Design ◽  
Matrix Tablets ◽  
High Dose ◽  
Direct Compression ◽  
Compression Method ◽  
Sustained Drug Release ◽  
Kappa Carrageenan ◽  
Gastro Retentive

Objective: It is always challenging to prepare the floating gastro retentive formulation of the high dose drug. The present research was aimed to prepare gastro retentive controlled release, matrix tablets of metformin, using the combination of different ionic, anionic and polyanionic polymers with HPMC.Methods: Formulations were prepared using sodium alginate, pullulan, kappa carrageenan, xanthan gum, poloxamer 68 in combination with HPMC K15M. All matrix tablets were prepared by direct compression method and evaluated for swelling, floating adhesive period and drug release.Results: All the tablets showed acceptable physicochemical properties. Statistical analyses of data revealed that tablets prepared using HPMC K15M and kappa carrageenan, formulation F2, is best in terms of showing excellent floating properties, extended adhesion periods and sustained drug release characteristics with similarity factor as 92 on comparison with the theoretical release of the drug.Conclusion: The combination of HPMC K15M and kappa carrageenan can be further optimized by applying the appropriate statistical design.

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.

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