scholarly journals In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

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)


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


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.


2017 ◽  
Vol 20 (1) ◽  
pp. 54-63
Author(s):  
FM Shah Noman Ul Bari ◽  
Muhammad Rashedul Islam ◽  
Md Mizanur Rahman Moghal ◽  
Israt Jahan Ira

The objective of this study was to analysis in vitro release kinetics of Azithromycin from bi-layer tablets prepared by direct compression using high viscosity to low viscosity grades of hydroxypropyl methyl cellulose (HPMC K15M, HPMC K4M, HPMC 50 cps), Carbopol 934p and Carbopol 974p. In addition, it also includes evaluating the effect of formulation variables like polymer proportion and polymer viscosity on the release of Azithromycin. In vitro release studies were performed using USP Type-II (Rotating paddle method) at 100 rpm. The dissolution medium consisted of 0.1N HCl (900 ml) for the first 2 hr and the phosphate buffer (pH 6.0) from 3rd to 10th hour. From twenty five different formulations (F-1 to F-25) based on polymer variation, model-dependent and independent methods were used for data analysis and the best results were observed for HPMC 50cps in Korsmeyer- Peppas (R2=0.995 on F-23) kinetic model. The release mechanism of all formulations was Fickian.Bangladesh Pharmaceutical Journal 20(1): 54-63, 2017


2020 ◽  
Vol 13 (3) ◽  
pp. 172-179
Author(s):  
Dharmendra Solanki ◽  
Mohit Motiwale ◽  
Sujata Mahapatra

Sustained-release (SR) matrix tablets of Acyclovir and polysaccharide isolated from corms of Colocasia esculenta, at different drug to polymer ratios, were prepared by using wet granulation method. The formulated tablets were also characterized by physical and chemical parameters and results were found in acceptable limits. The investigation focuses on the influence of the proportion of the matrix material on the mechanism and the release rate of the drug from the tablets. In vitro drug release appears to occur both by diffusion and a swelling-controlled mechanism, indicates the drug release from the tablet was non-Fickian super case II transport. The drug release data fit well to the Zero-order drug release Model and the Korsmeyer equation.


Author(s):  
Suriyaprakash T N K ◽  
S. Lakshmana Prabu ◽  
Arumugarajan A ◽  
Sumathi A

The objective of the present study was to develop clarithromycin tablets from polymeric hydrophilic matrices using methocel and characterization for its physic-chemical properties and in vitro release studies to optimize its release profile with the standard marketed product. Matrix tablets were prepared by wet granulation method using PVP and ethyl cellulose as binding agents. The matrix tablets were evaluated for its thickness, hardness, friability, weight variation, drug content and in vitro release studies. The drug delivery was analyzed using the paddle method in phosphate buffer pH 6.0 (dissolution medium I) and phosphate buffer pH 6.8 containing 0.5% sodium lauryl sulfate (dissolution medium II) and compared with USP dissolution limits. The dissolution release profile of formulation F9 was comparable with the market formulation and the difference factor and similarity factor f1 and f2 was found to be 2.44 and 83.18 in dissolution medium I; 1.44 and 89.71 in dissolution medium II. Stability studies were carried out as per ICH guidelines and tested for its physicochemical properties and in vitro studies. The study shows that the matrix method can be employed for preparing clarithromycin sustained release formulation using combination of hydrophilic polymers like Methocels and sodium carboxy methyl cellulose.


2020 ◽  
Vol 13 (3) ◽  
pp. 166-173
Author(s):  
Dharmendra Solanki ◽  
Mohit Motiwale

Sustained-release (SR) matrix tablets of Isoniazid and polysaccharide isolated from tubers of Dioscorea alata, at different drug to polymer ratios, were prepared by using wet granulation method. The formulated tablets were also characterized by physical and chemical parameters and results were found in acceptable limits. The investigation focuses on the influence of the proportion of the matrix material on the mechanism and the release rate of the drug from the tablets. In vitro drug release appears to occur both by diffusion and a swellingcontrolled mechanism, indicates the drug release from the tablet was non-Fickian super case II transport. The drug release data fit well to the Korsmeyer equation.


2018 ◽  
Vol 21 (1) ◽  
pp. 24-34
Author(s):  
K Latha ◽  
T Chinni Kranthi ◽  
Naseeb Basha Shaik

The present study is based on preparation of sustained release matrix tablets of tolterodine tartrate (for overactive bladder treatment) using guggul resin. Tolterodine tartrate is a highly soluble drug, to increase the duration of action the release of the drug has to be sustained. Natural resin is used as a polymer to sustain the release of drug, which was isolated from guggul gum by petroleum ether. Natural polymers are economical, biodegradable and can be chemically modified. Different ratios of drug and guggul resin were tried in the formulation of sustained release matrix tablets of tolterodine tartrate. Wet granulation technique was adopted for preparation of tolterodine tartrate granules, showed good flow properties and compressibility. The fabricated tablets were evaluated for various physicochemical characteristics and in vitro release studies like hardness, thickness, weight variation, friability, drug content and content uniformity were found to be within the limits. The drug release of optimized formulation (F6) was fitted to various kinetic models and the R2 value is 0.988 and the n value of drug release is 0.787. Therefore, the drug release follows zero order with non-fickian diffusion. The mechanism of drug release involves erosion and diffusion. Stability studies were performed for the optimized formulation as per ICH guidelines climatic zone III and were found to be stable with insignificant changes in physicochemical characteristics and in vitro release studies.Bangladesh Pharmaceutical Journal 21(1): 24-34, 2018


2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.


2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.


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