scholarly journals Design and Development of Bi-layered Sustained Release Azithromycin Tablets

2017 ◽  
Vol 15 (2) ◽  
pp. 227-234
Author(s):  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
FM Shah Noman Ul Bari ◽  
Elias Al Mamun
Keyword(s):  
Spectral Analysis ◽  
Drug Release ◽  
Sustained Release ◽  
Direct Compression ◽  
Design And Development ◽  
Bilayer Tablet ◽  
Formulation Variables

The objective of the current study was to develop a bilayer tablet of Azithromycin containing both immediate and sustained layer and evaluate the effect of formulation variables on drug release. Thirty different formulations (F-1 to F-30) were prepared by direct compression. When the fraction of polymer was increased from 5.55% to 10%, the rate of drug release was found to be slower. Maximum release of Azithromycin was from F-11 (within 8 hours), which contained 50 mg (5.55%) of HPMC 50 cps. Slowest release was observed from F-30 containing 90 mg (10%) of Carbopol 974 P. The IR spectral analysis revealed that all rate regarding agents and excipients used in this study are compatible with the active Azithromycin.Dhaka Univ. J. Pharm. Sci. 15(2): 227-234, 2016 (December)

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 Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Log P ◽  
Physical Parameters ◽  
Direct Compression ◽  
Formulation Development ◽  
Compression Technique

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF BILAYER TABLET OF ATENOLOL FOR BIPHASIC DRUG RELEASE

2018 ◽  
Vol 11 (5) ◽  
pp. 114
Author(s):  
Tarun Parashar ◽  
Nardev Singh
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Regression Coefficient ◽  
Release Kinetics ◽  
Immediate Release ◽  
Drug Release Kinetics ◽  
Gum Acacia ◽  
Bilayer Tablet

Objective: In the present research work, the aim was to prepare the bilayer tablet of atenolol for biphasic drug release to improve its bioavailability and absorption in the lower gastrointestinal tract. Methods: In the formulation of immediate release crospovidone, croscarmellose sodium, and sodium starch glycolate was used as super disintegrate and was directly compressed. For a sustained release portion different grade hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M, gum tragacanth, gum acacia, guar gum, and ethyl cellulose. Preformulation studies were performed before compression. The compressed bilayer tablets were evaluated for weight variation, dimension, hardness, friability, drug content, disintegration time, and in vitro drug release using USP dissolution apparatus type 2 (paddle). Results: The formulation IR3 showed 95% drug release in 30 min, and regression coefficient value (r2) value was found to be 0.994 suggesting first-order drug release kinetics. The F9 formulation using HPMC K15M and gum acacia (1:1) showed 91.20% drug release at the end of 12 h, and regression coefficient value (r2) was 0.992 suggesting zero-order drug release kinetics. Formulation IR3F9 showed faster drug release for bilayer tablet containing 5%w/w crospovidone in immediate release layer and HPMC and guar gum (1:1) in sustained release. Formulation IR3F9 showed swelling index 206%, floating lag time was found to be 2 min and total floating time up to 12 h. Conclusion: The formulation IR3F9 showed a faster drug release profile among the others in the preparation of the atenolol bilayer tablet. Hence, it was considered as an optimized formulation.

scholarly journals Formulation Development and In Vitro Evaluation of Metformin Hydrochloride Matrix Tablets Based on Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 1 (1) ◽  
pp. 51-56 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Tasbira Jeseem ◽  
Rumana Jahangir ◽  
DM Mizanur Rahman ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Bulk Density ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Metformin Hydrochloride ◽  
Direct Compression ◽  
Drug Content

An attempt was to formulate the oral sustained release Metformin hydrochloride matrix tablets by using hydroxyl methyl cellulose polymer (HPMC) as rate controlling factor and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct compression method. The granules were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity, drug content etc. and showed satisfactory results. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 8 hours using United States Pharmacopoeia USP 2 (paddle-type dissolution apparatus) in phosphate buffer (pH 7.4) as dissolution media. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The results indicated that a decrease in release kinetics of the drug was observed by increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion mechanism in all cases. Besides, this study explored both of the optimum concentration and the effect of polymer on drug release pattern from the tablet matrix for 8 hours period. Key Words: Metformin HCl, Sustained release, Hydrophilic matrix, HPMC, Direct compression   doi:10.3329/sjps.v1i1.1808 S. J. Pharm. Sci. 1(1&2): 51-56

Effects of Formulation Variables and Post-compression Curing on Drug Release from a New Sustained-Release Matrix Material: Polyvinylacetate-Povidone

2001 ◽  
Vol 6 (2) ◽  
pp. 247-254 ◽  
Author(s):  
Zezhi J. Shao ◽  
Mohammad I. Farooqi ◽  
Steven Diaz ◽  
Aravind K. Krishna ◽  
Nouman A. Muhammad
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Material ◽  
Formulation Variables

Influence of Hydroxypropyl Methylcellulose on Flowing and Swelling Parameters in Biomucoadhesive Tablets with Miconazole Nitrate

2017 ◽  
Vol 68 (10) ◽  
pp. 2346-2349
Author(s):  
Magdalena Birsan ◽  
Nela Bibire ◽  
Madalina Vieriu ◽  
Alina Diana Panainte ◽  
Ileana Cojocaru
Keyword(s):  
Friction Coefficient ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Pharmaceutical Formulations ◽  
Direct Compression ◽  
Miconazole Nitrate ◽  
Proportionality Relationship ◽  
Formulation Variables

Original pharmaceutical formulations have been produced as oral biomucoadhesive tablets for antifungal medication. They have been obtained through direct compression using as matrix forming polymers various sorts of hydroxypropyl methylcellulose. The main goal of the study was determining the swelling index of the new mucobioadhesive formulations with miconazole nitrate in order to correctly evaluate the time of contact with mucosa, and the prolongation of drug release. For each formulation, the flowing parameters have been determined: flowing time, friction coefficient, repose angle, Haussner ratio, Carr index, and the swelling index for 6 formulations containing various sorts of hydroxypropyl methylcellulose as matrix molders, while the formulation variables studied were time and association ratio between those polymers. Though results analysis, we noticed that the values of the swelling index depended on the type and quantity of polymer, results that could also be explained by the proportionality relationship to flowing and compressibility parameters.

scholarly journals FORMULATION AND EVALUATION OF BILAYER TABLET CONTAINING DICLOFENAC SODIUM AS SUSTAINED RELEASE AND ALOE VERA GEL POWDER AS IMMEDIATE RELEASE

2019 ◽  
pp. 70-78
Author(s):  
HARSHAD PADEKAR ◽  
OMKAR LOHOTE
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sustained Release ◽  
Diclofenac Sodium ◽  
Aloe Vera ◽  
Immediate Release ◽  
Angle Of Repose ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablet ◽  
Aloe Vera Gel

Objective: The objective of the present investigation is to design formulate and characterized the bilayer tablet containing Diclofenac sodium and Aloe Vera gel powder. In which diclofenac sodium is sustained release and Aloe Vera gel powder is immediate release. In order to produce a single dosage form containing two different classes, drug are widely prescribed by the physician to have better patient compliance. Methods: Bilayer tablet was prepared by direct compression, The immediate release layer of Aloe Vera gel powder was prepared by using different excipients such as starch, sodium starch glycolate, lactose, talc etc. sustained release layer of diclofenac sodium was prepared by using HPMC K4M, lactose, Talc Magnesium stearate, talc etc. for preparation of bilayer tablet sodium starch glycolate are use as super disintegrants in immediate release tablet and HPMC K4M are use as controlled release polymer. Various Preformulation parameter i.e. Identification, melting point, compatibility study, solubility are checked. Micromeritics properties of powder blend such as bulk density, tapped density, hausner’s ratio, Carr’s index, angle of repose are performed. Post-compression parameter was done such as hardness, friability, weight variation, drug content uniformity, thickness, in vitro drug release. Results: Result was found within the limit of the standard of optimized formulation. The drug release of the tablet was in the range of 82 to 92%in 8 h. Conclusion: Bilayer tablet was prepared by optimized batches of both layers. The prepared tablets showed satisfactory results for various evaluation parameters. The optimized formulation based on all the parameter A1 (Sodium starch glycolate) is selected for the immediate release layer and D3 (HPMC K4M) was selected for the controlled release layer. The drug release mechanism was found to be zero order release depends upon diffusion.

Development of Bilayer Tablet Containing Saxagliptin Immediate Release and Metformin Sustained Release using Quality by Design Approach

2021 ◽  
Vol 16 ◽  
Author(s):  
Amit Kaushal ◽  
Sandeep Arora ◽  
Neelam Sharma ◽  
Sukhbir Singh
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Patient Compliance ◽  
Numerical Optimization ◽  
Quality By Design ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Fixed Dose ◽  
Bilayer Tablet ◽  
Independent Parameters

Objective: Adequate glycemic control in diabetes patients requires oral combination therapy. Saxagliptin is a dipeptidyl peptidase-4 inhibitor having less adverse effects and metformin is a first line medicine for diabetes treatment. The aim of this research work is to develop a bilayer tablet of saxagliptin and metformin in fixed dose combination (FDC) using quality by design (QbD) to acquire immediate release of saxagliptin and sustained release of metformin from bilayer tablet to ultimately achieve superior patient compliance. Methods: The development of the bilayer tablet was done in four stages using QbD. In first step, quality target product profile (QTPP) of bilayer tablet was defined and critical quality attributes (CQAs) were identified by risk estimation matrix and taguchi design, an immediate release saxagliptin layer was optimized in second step, optimization of sustained release metformin layer was carried out in third step and in final step bilayer tablet was prepared and characterized. The effect of independent parameters i.e. magnesium stearate level (X1), kneading time (X2) and lubrication time (X3) on Carr’s Index (Y1), percentage relative standard deviation of content uniformity (Y2) and drug release at 30 minute (Y3) were estimated for optimization of immediate release saxagliptin layer using Box-Behnken design (BBD). The effect of independent parameters i.e. hydroxypropyl methyl cellulose level (X4), compritol level (X5) and magnesium stearate level (X6) on Carr’s Index (Y4), drug release at 2 h (Y5), drug release at 5 h (Y6) and drug release at 10 h (Y7) were estimated for optimization of sustained release metformin layer using BBD. Results: The optimized composition of immediate release saxagliptin layer estimated using numerical optimization by Design expert was 0.88% (X1), 15 minutes (X2) and 3.85 minutes (X3) with predicted variables i.e. 10.59% (Y1), 3.16% (Y2) and 85% (Y3). The optimized composition of sustained release saxagliptin layer predicted through numerical optimization was 30% (X4), 3.36% (X5) and 0.9% (X6) having 10.89 % (Y4), 43.44 % (Y5), 60% (Y6) and 85.14% (Y7). In-vitro dissolution study of bilayer tablet showed immediate release of Saxagliptin (approximately 85% in 30 minute) and sustained release of metformin illustrating 43.21±1.21, 60.86±2.96 and 86.26±1.38% drug release at 2, 5 and 10 h, respectively. The release exponent for Korsmeyer-Peppas model for Saxagliptin and metformin was 0.237 (<0.45) and 1.536 (n>0.85) indicating Fickian and super case II transport drug release behavior, respectively. Conclusion: By QbD approach, bilayer tablet containing saxagliptin and metformin was successfully developed and influence of various formulation parameters on CQAs of drug products was understood with fewer experiments. This leads to conclusion that cost can be reduced using QbD in development of FDC for improving patient compliance.

Sign in / Sign up

Export Citation Format

Share Document