scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF MATRIX TABLET TRAZODONE HYDROCHLORIDE USING NATURAL POLYMER

2021 ◽  
Vol 12 (8) ◽  
pp. 46-51
Author(s):  
Jeetendra Kushwaha ◽  
Dev Sharan Chaturvedi ◽  
Manisha Verma ◽  
Kuldeep Kumar Tiwari ◽  
Neelesh Anuragi

Increased complications and costs of marketing of innovative drugs focused greater attention to the development of sustained release (SR) or controlled release (CR) drug delivery systems. Trazodone Hydrochloride (TRZ) is a well-known chemical compound that is used as an antidepressant that belongs to a selective serotonin reuptake inhibitor (SARI). The objective of present work was to develop and evaluated oral sustained release matrix tablet of TRZ. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. No interactions were observed between TRZ and excipients from the Fourier transform infrared spectroscopy. The present research work was successful in improving the efficacy TRZ oral therapy as the drug release was extended for 12 hours thus reducing dosing frequency thereby improving patient compliance. The study also revealed the applicability of HPMC K-15, Gaur gum and PVP K30 as rate-controlling polymers in matrix tablets. The hydrophilic matrix of HPMC alone cannot control the release TRZ effective for 12 h while when combined with guar gum, may slow down the release of the drug and therefore, can be successfully employed for the formulation of matrix tablets SR. It may be concluded from the study that; the optimized formulation F-8 was shown maximum drug release 99.12 % in 12 h of dissolution. The release kinetic data of formulation F-8 shown first order release kinetics (R2 = 0.980).

2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.


2021 ◽  
Vol 11 (5) ◽  

The objective of this research work was to carry out design and evaluation of sustained release matrix tablets of Itopride by use of natural and synthetic polymers. Matrix tablets were prepared by wet granulation technique by using natural polymers like Carbopol 934, Tamarind poly saccharide, Locust bean gum, Ethyl cellulose, HPMC K 100 as matrix forming agent and excipients such as Lactose, Starch 1500, Magnesium stearate, MCC and talc were used. The dissolution medium consisted of 900 ml of 0.1 N HCl for first 2 hours and then 7.4 phosphate buffer for remaining 10 hours. The release of Itopride from matrix containing lactose, micro crystalline cellulose and starch 1500 as diluents. The drug release rate was found in order of lactose> micro crystalline cellulose>starch 1500. The formulation was optimized on the basis of acceptable tablet properties and in-vitro drug release. The release data were fit into different kinetic models (zero-order, first- order, Higuchi’s equation and Korsmeyer-Peppas equation). Optimized formulation was tested for their compatibility with Itopride by FT-IR studies, which revealed that there is no chemical interaction occurred with polymer and other excipients. The drug release profile of the best formulation was well controlled and uniform throughout the dissolution studies. Keywords: Matrix tablets, Itopride, Carbopol 934, HPMC K 100, Ethyl cellulose.


Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  

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.


Author(s):  
Ruchi Sunayana S ◽  
Gowda Dv ◽  
Vishal Gupta N ◽  
Praveen Sivadasu ◽  
Manjunath M

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.


1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)


2014 ◽  
Vol 2 (01) ◽  
pp. 68-75 ◽  
Author(s):  
Swapnil J. Kodalkar ◽  
Rohan A. Khutale ◽  
Sachin S. Salunkhe ◽  
Sachin S. Mali ◽  
Sameer J. Nadaf

In present study, the attempts have been made to formulate sustained release tablets of lornoxicam by direct compression method. Based on viscosity grades different proportions of hydrophilic polymers (HPMC K4M, HPMC K15M, HPMC K100M) are used for preparation of lornoxicam sustained release matrix tablet. The drug excipient mixtures were subjected to preformulation studies comprising of micromeritic properties. The tablets were subjected to various studies like as physicochemical studies, in vitro drug release, kinetic studies, etc. FTIR studies shown there was no interaction between drug and polymers. The physicochemical properties of tablets were found within the limits. Lornoxicam is a first generation analgesic, inflammatory and antipyretic agent used in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. From developed formulations batch F1 have shown zero order drug release behavior and prolong drug release over a period of 12 h which was deemed as suitable and optimum formulation for sustained drug delivery. Results of the present study indicated the suitability of the low viscous polymer in the proportion of (drug:polymer) 1:1 in the preparation of sustained release formulation of lornoxicam.


2021 ◽  
Vol 11 (5) ◽  

Methimazole is active pharmaceutical ingredient effectively utilized in hyperthyroidism. Methimazole inhibits peroxidase as well as iodine interactions with thyroglobulin to produce triiodothyronine with thyroxine. Methimazole shows very low protein binding (1-10%) bounds to plasma proteins and easily metabolized by liver. In this investigation, efforts given to develop a sustained release matrix tablet of Methimazole. Sustained release drug delivery systems are for a maximum of 24 hours clinical effectiveness. Such systems are primarily for the drugs of short elimination half-life. However, drugs with long half-life also qualify if a reduction in steady state fluctuation is desired. Matrix tablets of methimazole were prepared by utilizing direct compression method. HPMC along with Sodium carboxy methyl cellulose used to retard drug release from the dosage form. Matrix tablets of methimazole were evaluated for different quality control test to improve quality of the product. In vitro release study of methimazole matrix tablets shows that polymer percentage used in the formula is enough to extend the release of the drug for at least 12 hr. In dissolution study of matrix of methimazole formulation F2 shows maximum drug release 97.93 % at the end of 6 hours while F1 shows least 83.64 %. Keywords: Matrix tablet, Methimazole, Sustained Release


INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (04) ◽  
pp. 28-36
Author(s):  
R. R Karmarkar ◽  
◽  
M. P Wagh ◽  
S.R Baviskar ◽  
S.H Patil ◽  
...  

The aim of the present study was to evaluate carboxy methyl tamarind kernal powder as a novel drug release retarding agent. To evaluate the same, sustained release matrix tablets of stavudine were prepared by using HPMC K4M and carboxy methyl tamarind kernal powder, by using a direct compression technique. The formulations were prepared by using different drug: polymer ratios into formulations such as F1 to F9. The compressed tablets were evaluated for thickness, hardness, friability, drug content and in vitro dissolution rates. Formulation F6, having a hardness of 5.46 ± 0.25, showed the desired release profile for a period of 24 h in simulated intestinal fluids (pH 7.4). Kinetic data treatment indicated that the release of stavudine from the matrix tablet follows coupling of diffusion and erosion mechanisms. The study proves that the optimized sustained release tablet is capable of releasing the drug in a sustained manner for 24 h.


2015 ◽  
Vol 16 (2) ◽  
pp. 177-183
Author(s):  
Md Ziaur Rahman ◽  
Sayed Koushik Ahamed ◽  
Sujan Banik ◽  
Mohammad Salim Hossain

The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013


2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain

<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>


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