scholarly journals Formulation and Invitro evaluation of immediate release tablets containing febuxostat

Author(s):  
Srikumar Billa ◽  
Saibabu Ch ◽  
Malyadri T

In the present research work, Febuxostat Immediate Release Tablet was prepared by direct compression method using varying concentrations of Lycoat, Crospovidone& Croscarmellose sodium as disintegrants. The formulations prepared were evaluated for precompression& post-compression parameters. From the drug excipient compatibility studies, we observe that there are no interactions between the pure drug (Febuxostat) and optimized formulation (Febuxostat+ excipients) which indicates there are no physical changes. Post compression parameters were found to be within the limits. Among the formulation prepared the tablet containing 12mg of CCS shows 98.13% of the drug release within 45 min & follows first-order kinetics.

Author(s):  
Pratiksha S. Deore ◽  
Yashpal M. More ◽  
Avish D. Maru

The aim of present work is to formulate and develop tablets of promethazine HCL.by using various superdisintegrating agent by direct compression method. The main objective of the study is to increase rapid onset of action of promethazine HCL in the treatment of nausea and vomiting. The orodispersible tablet of promethazine hcl is were prepared by direct compression method. Using different concentration of Crospovidone, croscarmellose sodium Mannitol, lactose, maltose, mg. stearate. The tablet was evaluated by various parameters and result are found to be satisfactory.


Author(s):  
Ashok Thulluru ◽  
Veeravalli Kumar Sai ◽  
Pavan Kumar M ◽  
Roshitha B

ABSTRACTObjective: The current research work is intended to formulate propranolol HCl (PLH) as orally disintegrating tablet (ODT). It is also intending to checkthe superiority in a combination of superdisintegrants and effervescent mixture than the use of superdisintegrants alone by a direct compressiontechnique. To fasten the onset of action and thereby enhancing the bioavailability of PLH in comparison to its conventional tablets.Methods: Standard calibration curve of PLH was obtained in pH 6.8 phosphate buffer by spectrophotometric method, drug-excipient compatibilitystudies were carried by Fourier transform infrared (FT-IR) studies. All the formulations were evaluated for pre and postcompression studies.Accelerated stability studies were carried out up to 6 months for the optimized formulation, EF3.Results and Discussion: Superdisintegrants used in the study are compatible with PLH. Pre- and post-compression parameters were within theacceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of PLH from ODT increases as the concentration ofsuperdisintegrants as well as the ratio of citric acid: NaHCO3 of effervescent mixture increases. Formulations with an effervescent mixture are havingrapid disintegration and dissolution rate when compared to the formulations with superdisintegrants alone. The order of superdisintegrants inenhancing the dissolution rate of PLH is crospovidone (CPV) > croscarmellose sodium (CCS) > sodium starch glycolate (SSG). Formulation, EF3 (10%CPV and 1:3, citric acid: NaHCO3 ratio, respectively) had the highest dissolution efficiency at 10 minutes (DE10=82.74%); the first order dissolutionrate constant (K1=0.141/minutes) with a regression coefficient (r2=0.974) and lesser time for 90% of drug release (t90=4 minutes), was considered asthe optimal ODT in this study. Formulation EF3, passed the test for stability.Conclusion: Hence, an effective PLH ODT was formulated by the direct compression technique with disintegration by combination of superdisintegrantsand effervescent mixture, will fasten the onset of action and enhances the bioavailability of PLH in comparison to its conventional tablets.Keywords: Propranolol HCl, Orally disintegrating tablet, Sodium starch glycolate, Croscarmellose sodium, Crospovidone, Direct compression, In vitrodissolution studies.


2018 ◽  
Vol 10 (1) ◽  
pp. 31-38 ◽  
Author(s):  
S. Karim ◽  
A. Biswas ◽  
A. Bosu ◽  
F. R. Laboni ◽  
A. S. Julie ◽  
...  

Present study aspires at the design of an immediate release formulation with prospective use of fexofenadine hydrochloride by exploring the effect of sodium starch glycolate as super disintegrant. Fexofenadine hydrochloride immediate release tablets (Formulations F-1, F-2, F-3, F-4 and F-5) using different ratios of sodium starch glycolate as a disintegrant were prepared by direct compression method. Standard physicochemical tests were performed for all the formulations. Dissolution studies of the formulations were done in phosphate buffer, pH 6.8 using USP apparatus II (paddle apparatus) at 50 rpm. Percent release of fexofenadine hydrochloride of formulations F-1, F-2, F-3, F-4 and F-5 were 89.98%, 90.98%, 92.95, 96.92% and 99.85%, respectively after 1 h and the release pattern followed the zero order kinetics. The release rate in the formulation F-5 was higher compared to other formulations and the studied market products. Sodium starch glycolate speed up the release of the drug from the core tablets, and the release of fexofenadine hydrochloride from tablets was directly proportional to the amount of sodium starch glycolate present in the formulations and there by produced immediate action.


Author(s):  
Naveen Goyal ◽  
Anil Kumar

Objective: The main objective of this research work was to design, prepare and evaluate extended release (ER) tablets of anti-asthmatic drugs (salbutamol sulphate and theophylline) by direct compression method using diverse ratios of hydroxypropyl methylcellulose (HPMC K100M) and ethyl cellulose (EC) along with some other excipients.Methods: Extended-release matrix tablets of salbutamol sulphate and theophylline were successfully fabricated by direct compression method and coded the formulations as F1 to F7 depending on the ratios of modified polymers. The core tablets composed of hydrophilic polymers of various ratios that allow the discharge of drugs at a controlled rate after coming in contact with the aqueous medium. The designed tablets were subjected to various assessment parameters i.e. friability test, hardness test, drug content consistency and In vitro dissolution tests.Results: Prepared formulations were subjected to various assessment parameters and the findings obtained were within the prescribed limit. To perform the in vitro drug dissolution tests of fabricated tablets, the calibration plots of pure drugs using various solvents i.e. 0.1N HCl, phosphate buffer (pH 6.8) and distilled water were plotted. Dosage forms F1-F7 containing ethyl cellulose and HPMC K100M in various concentration demonstrates the prolonged medications discharge for up to 8 h, among these formulations, F6 shows 95.32±0.24 % for salbutamol sulphate and 94.19±0.39 % for theophylline release at the end of 8 h. This finding reveals that a particular window of concentrations of ethylcellulose and HPMC K100M was capable of providing prolonged drugs discharge.Conclusion: The results obtained in this research work clearly showed a promising potential of extended-release tablets containing a specific ratio of HPMC K100M and ethylcellulose as a release rate controlling polymers for effective treatment of asthma and chronic obstructive pulmonary diseases (COPD).


Author(s):  
PRADIP KUMAR CHAUDHARY ◽  
ABDUL RAHEEM T. ◽  
MANJUNATH U MACHALE ◽  
VASIA ◽  
SHAIK SADIK

Objective: The aim of the present study was to prepare and optimize levamisole chewable tablets by using various super disintegrants, namely; sodium starch glycolate, DRC Indion 204, and DRC Indion 234. Methods: Drug excipient compatibility study was carried out by FTIR spectroscopy to verify the compatibility of levamisole with the excipients. Nine batches of levamisole chewable tablets were prepared according to 32 factorial designs using a direct compression method by optimizing the super disintegrant concentration. The powder blend was exposed to pre-compression studies of the powder blend followed by post-compression studies of the formulated tablets. Results: FTIR study revealed that the excipients used in the formulations were compatible with the drug. The pre-compression and post-compression parameters were found within the IP limits. Form the dissolution studies, it was evident that the formulation prepared with DRC Indion 234 (50 mg) showed maximum percentage drug release in 45 min (97.13%) hence it is considered as optimized formulation. When compared to all other formulation, the batches with DRC Indion 234 (F7-F9) showed a better release of the drug (90 % drug release within 45 min). Conclusion: Nine batches of levamisole chewable tablets were successfully formulated by optimizing the concentration of super disintegrants such as sodium starch glycolate, DRC Indion 204, and DRC Indion 234. It was concluded from the dissolution studies that the DRC Indion 234 is the best super disintegrant irrespective of their concentration for the formulation of levamisole chewable tablets when compared to sodium starch Glycolate and DRC Indion 204.


Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design. Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min. Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.


Author(s):  
SHWETHA MARGRET JL ◽  
MADHAVI BLR

Objective: Direct compression method is preferable for tablet manufacture. The direct compression method is followed for many formulations but the relevant study is not reported. The present work aims to study the suitability of the direct compression process to prepare tablets of quinapril hydrochloride (QHCl), a low dose drug with a starting dose of 5 mg, indicated in the treatment of hypertension, congestive heart failure, and other conditions. Methods: QHCl is reported to be unstable in the presence of moisture, heat, and some excipients. The direct compression method was tried instead of a wet granulation technique to prepare the tablets. Initially, drug-excipient compatibility study was carried out. For selected excipients and QHCl preformulation tests were conducted. The stabilizer was employed. Three formulations were tried. The blends were prepared by tumbling and trituration methods. Blend uniformity and precompression parameters were determined. Tablets were directly compressed and evaluated. Results: Drug-excipient compatibility was studied at 60°C and 40°C with an Relative humidity (RH) of 75% for 4 weeks. It showed discoloration of the pure drug and most of the drug excipient mixtures. Three formulations Q1, Q2, and Q3 were prepared using magnesium oxide (light), magnesium carbonate (light), and Aerosil as stabilizers. Blending was done by trituration and tumbling method for 10 min and 15 min duration for the given batch size. Blend uniformity was determined. Tumbling method for 15 min showed good blending as evident from the percentage coefficient of variation values. The blends had a good flow. Tablet evaluation showed hardness in the range of 2.5–3 kg/cm2 and disintegration time of 1–2 min. Q1 and Q2 passed the friability test. The content uniformity criterion was achieved with an acceptance value <20. In vitro dissolution, Q1 and Q2 were 100% and 98.8%, respectively, in 30 min and followed first-order kinetics. The stability study of Q1 indicated a single peak in the chromatogram corresponding to the drug. Q2 showed spotted discoloration. Conclusion: The direct compression technique could be employed for the preparation of QHCl tablets. Q1 showed better stability and release characteristics. Q2 and Q3 are considered for further study.


Author(s):  
A. HARI OM PRAKASH RAO ◽  
SANTOSH KUMAR RADA ◽  
SHAMBHAVI KANDUKURI

Objective: To synthesize, characterize and evaluate starch crotonate as a superdisintegrant in the formulation of Piroxicam fast dissolving tablets by employing 23 factorial design. Methods: Starch crotonate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Piroxicam were prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. Results: The starch chrotonate prepared was found to be fine, free flowing and amorphous. Starch crotonate exhibited good swelling in water with swelling index (50%). The study of starch crotonate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (<0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch crotonate. The disintegration time of all the formulated tablets was found to be in the range of 18±03 to 66±03 sec. The optimized formulation F8 had the least disintegration time i.e., 18±03 sec. The wetting time of the tablets was found to be in the range of 49.92±0.11 to 140±0.18s. The In vitro wetting time was less (i.e., 74±0.37s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 27.58±0.01 to 123.07±0.33%. The percent drug dissolved in the optimized formulation F8 was found to be 99.83% in 10 min. Conclusion: Starch crotonate, when combined with sodium starch glycolate, croscarmellose sodium, with Piroxicam was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 10 min.


Author(s):  
NATALIA DARZULI ◽  
LILIIA BUDNIAK ◽  
TARAS HROSHOVYI

Objective: The aim of the present study was to select excipients in an oral solid dosage form with a dry extract of round-leaved wintergreen (Pyrola rotundifolia L.) by using asymmetric, rotatable composite plan of the second-order (uniform plan No. 17). Methods: The tablets were prepared by using a direct compression method. The most important pharmaceutical factors selected were considered in more details at developing the optimal composition and technology of the studied tablets of the round-leaved wintergreen extract. Each one was studied at five levels using asymmetric, rotatable composite plan of the second order. Results: Increasing amounts of PROSOLV® EASYtab SP and croscarmellose sodium in the powder mass, its flowability decreases, and increasing amounts of Tablettose® 80 improves flowability. Increasing the amount of Tablettose® 80 in the tablets composition leads to improved uniformity. The strength of the tablets increased with increasing amounts of Neusilin® US 2 at different combinations of levels of the other three factors. When studying the effect of the amounts of croscarmellose sodium on the disintegration of tablets, it was found that the best disintegration values were obtained in the study of croscarmellose sodium at the upper level. Conclusion: Oral solid dosage form with dry extract of round-leaved wintergreen was successfully prepared by the direct compression method. The optimal composition of tablets was determined by the regression analysis.


2014 ◽  
Vol 50 (4) ◽  
pp. 943-953 ◽  
Author(s):  
Fozia Israr ◽  
Zafar Alam Mahmood ◽  
Fouzia Hassan ◽  
Syed Muhammad Farid Hasan ◽  
Sabahat Jabeen ◽  
...  

Cefuroxime axetil immediate release tablets were formulated by direct compression method with different percentages of sodium lauryl sulphate (SLS) such as 0.5, 1.0, 1.5 and also without SLS. Resulting batches of tablets were evaluated by both pharmacopeial and non-pharmacopeial methods to ascertain the physico-mechanical properties. Dissolution test were carried out in different medium like 0.07 M HCl, distilled water, 0.1M HCl of pH 1.2 and phosphate buffers at pH 4.5 and 6.8 to observe the drug release against the respective concentration of SLS used. Later, test formulations were compared by f1(dissimilarity) and f2(similarity) factors using a reference brand of cefuroxime axetil. Significant differences (p<0.05) in dissolution rate were recorded with the change in concentration of SLS in different media. Test formulation T3 containing 1% SLS was found to be best optimized formulation based on assay, disintegration, dissolution and similarity and dissimilarity factors.


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