scholarly journals FORMULATION AND IN VITRO EVALUATION OF SALBUTAMOL SULPHATE AND THEOPHYLLINE EXTENDED-RELEASE TABLETS USING MODIFIED POLYMERS

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).

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  


Author(s):  
Sanket Jain ◽  
Sujit Pillai ◽  
Rampal Singh Mandloi ◽  
Nikhlesh Birla

Ondansetron is an anti-emetic drug which is insoluble in water. The present study was aimed to formulate and evaluate oral fast dissolving tablet of Ondansetron by Utilizing Liquisolid Compact Technique. The tablets were prepared by direct compression method and characterized by UV, FTIR studies. Six formulations (F1-F6) of ondansetron were prepared and tablets were evaluated for weight variations, hardness, thickness, friability, disintegration time, drug content and In-vitro dissolution studies gave satisfactory result. TF6 was found to be the best and acceptable formulation whose drug content was about 99.17±0.05 and percentage (%) drug release 97.49±2.03 in 10 min, high as compare to other formulation and has low disintegration time 17±0.01 as compare to other formulation which indicates that drug is rapidly dissolved and available at the site of action.


2020 ◽  
Vol 10 (5) ◽  
pp. 240-250
Author(s):  
Vinay Pandit ◽  
Dipanker Kashive ◽  
Tarun Kumar Sharma

Objectives: Diabetes is a chronic disease and is a group of metabolic disorders characterized by high levels of sugar in blood (hyperglycemia). Hypertension is a major modifiable risk factor for cardiovascular morbidity and mortality in patients with diabetes. The objective of this research is to formulate Fast dissolving tablets of Pioglitazone and Cilnidipine for the effective treatment of diabetes induced hypertension. Methods: Six formulations were prepared by direct compression technique by using Opuntia ficus-indica as an innate superdisintegrant. Result and Discussion: All the formulations were subjected for precomprression, post compression parameters and shows all the data within the specific limits. F5 formulation with the mixture of polymers viz. Opuntia ficus indica, SSG, croscarmellose sodium, magnesium stearate, DiCOM showed comparatively fast disintegration and best release of drug than that of all other formulation. The tablets of F5 formulation disintegrated within 18.53 seconds can provide fast relief in the body. The in-vitro dissolution results revealed that the drug release of F5 formulation tablets was more than 90% for Pioglitazone and near to 70% for Cilnidipine within 30 minutes. Stability studies were performed on F5 formulation tablets showed no significant changes in color, disintegration time and in-vitro dissolution which showed that appearance of tablets was having no effect. Conclusion: Fast dissolving tablets of Pioglitazone and Cilnidipine can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of both drugs. Keywords: Pioglitazone, Cilnidipine, diabetes induced hypertension, fast dissolving tablets, direct compression.


2019 ◽  
Vol 9 (3) ◽  
pp. 95-98
Author(s):  
Ravi U Gaware ◽  
Gayatri R Waykar ◽  
Madhuri K Yewale ◽  
Rutuja B Mhaske ◽  
Poonam S Mhaske

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.


2016 ◽  
Vol 8 (3) ◽  
pp. 107
Author(s):  
A Thirupathaiah ◽  
R Shyam Sunder

<p>Investigation of <em>in vitro/in vivo</em> behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard. </p>


2015 ◽  
Vol 18 (2) ◽  
pp. 132-136 ◽  
Author(s):  
Md Shamsul Alam ◽  
Jakir Ahmed Chowdhury ◽  
Sams Mohammad Anowar Sadat ◽  
Md Selim Reza

Ethyl cellulose (EC) microcapsules containing Salbutamol sulphate (SS) were prepared through emulsion-solvent evaporation technique. Microcapsules were compressed and in-vitro release profiles were studied from both microcapsules and their compressed matrix tablets. Different amounts of drug were added in order to obtain various drugs to polymer ratios and it was found that the size of microcapsules reduced with the increase in core loading. In the preparation of formulations, Tween 80 was used as an emulsifying or dispersing agent and light liquid paraffin (LLP) was used as oil phase. The in-vitro release of EC microcapsules was studied in distilled water at 37º ± 0.5°C. A biphasic release behavior of SS from microcapsules was observed. In case of microcapsules, an immediate release was observed but for their compressed tablet form, initially a burst effect and then slow release were observed which was extended for 8 hours. In order to further investigate the type of drug release mechanism, the dissolution data were plotted according to the different kinetic models. In-vitro dissolution studies showed that zero-order and square-root of time (Higuchi model) release characteristics were exhibited.Bangladesh Pharmaceutical Journal 18(2): 132-136, 2015


INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (08) ◽  
pp. 84-87
Author(s):  
S Kumar ◽  
J. V. Kumar ◽  
P Singhal ◽  

The aim of the present investigation was to prepare solid dispersion (SD) of the water insoluble drug. Loratadine using super disintegrants as carrier and formulate it as fast dissolving tablets (FDTs) with an objective to improve solubility and enhance dissolution of drug. The SD’s of the drug were prepared by melt dispersion technique using polyethylene glycol (PEG) 6000 in diferent ratios 1 : 2.5, 1 : 5 and 1 : 7.5. The prepared SD formulations were characterized for equilibrium solubility, Fourier Transform Infrared spectroscopy (FTIR) and in vitro dissolution study. The batch containing SD formulation of loratadine showed fastest dissolution (99.87% drug release in 60 min). In this study, fast dissolving tablets were prepared by direct compression method using Croscarmellose sodium, sodium starch glycolate and polyplasdone XL as the super disintegrants. Effect of various super disintegrants on dissolution behavior of tablets was evaluated in phosphate buffer pH 6.8.


2019 ◽  
Vol 22 (2) ◽  
pp. 228-234 ◽  
Author(s):  
Sreebash Chandra Bhowmik ◽  
Marzia Alam ◽  
Md Saiful Islam Pathan

The purpose of the current study was to develop a fast dissolving polymeric oral thin film containing palonosetron hydrochloride having good mechanical properties, fast disintegration, dissolution and good drug content uniformity. Solvent casting method was used to prepare the films. Compatibility between drugs and excipients were studied using FTIR and HPLC. Nine different formulations of film from F1 to F9 were prepared using different concentration of polymer A at drug-polymer A ratio (1:26), (1:28), (1:30), (1:32), (1:34), (1:36), (1:38), (1:40), (1:42) and at polymer A-plasticizer B of (65:10), (70:10), (75:10), (40:10), (42.5:10), (45:10), (47.5:10), (50:10), (52.5:10), respectively. The in vitro dissolution study was carried out in phosphate buffer (pH 6.8) at 37±0.5oC and 50 rpm using USP XXIV paddle method. Physicochemical evaluations of all the batches were performed including weight variation, thickness, folding endurance, pH, in vitro disintegration and drug release, FTIR and content uniformity test. Maximum and minimum drug dissolution were found in F6 (108.7%) and in F1 (98.5%), respectively. The maximum and minimum disintegration time were in F9 (43.8 sec) and F1 (25 sec), respectively which demonstrated that disintegration of the film was directly proportional to the polymer A and plasticizer B concentration. It is quite evident from the present research work that the film prepared using polymer A-plasticizer B were smooth, mechanically strong and easy to peel out. Among all the batches, formulation F5 showed best results with respect to disintegration (33 sec), drug dissolution (105%), content uniformity (98.51%) and folding endurance (731). Therefore, it can be said that combination of polymer A and plasticizer B can be prospectively used for the preparation of palonosetron hydrochloride oral thin film. Bangladesh Pharmaceutical Journal 22(2): 228-234, 2019


2020 ◽  
Vol 10 (3-s) ◽  
pp. 17-25
Author(s):  
Inder Kumar ◽  
Dipima Chaudhary ◽  
Bhumika Thakur ◽  
Vinay Pandit

Objective: In the present research work, fast dissolving tablets of Piroxicam were formulated by two different techniques i.e. direct compression method and sublimation method using different superdisintegrants. Methods: Twelve formulations were prepared (PXM1 to PXM12) in which first six formulation were prepared by direct compression technique and other six formulation were prepared by sublimation method by using camphor as a sublimating agent. Result and Discussion: All the formulations were subjected for precompression, post compression parameters, and shows all the data within the specific limits. Formulation PXM4 containing 5 % crospovidone showed 99.480 ± 0.291 % drug release in 20 min which was more than the drug release of rest of the formulations. The optimized formulation PXM4 was compared with the marketed formulation and it revealed that drug release of PXM4 was found to be 99.397 ± 0.751 % in 20 min, which was greater than the marketed formulation. Finally, results were statistically analysed by the application of one way ANOVA and t-test. The stability study of the optimized formulation PXM4 showed no significant changes in, drug content, disintegration time and in-vitro drug release. Conclusion: Piroxicam can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of the drug. Keywords: Direct compression, fast dissolving tablets, sublimation, Piroxicam.


Author(s):  
Manish Khadka ◽  
Dharma Prasad Khanal ◽  
Deepti Piya Baniya ◽  
Prakash Karki ◽  
Saurav Shrestha

Orally disintegrating tablets of Furosemide were prepared, evaluated and the comparison of the action of different concentrations of disintegrants on disintegration and dissolution of the tablets were studied. Direct compression method was used to prepare the orally disintegrating tablets containing 20 mg of Furosemide. The formulation was conducted using different concentrations of crospovidone, croscarmellose and sodium starch glycolate as superdisintegrants and their interactions with Furosemide were also evaluated using FTIR.  FTIR studies using the drug and its mixtures with the excipients showed that the peaks correlate with one another which signify that there is no interaction between the drug molecule and the excipients used. The obtained results revealed that the disintegration time of ODTs were between 9 to 59 seconds. The percentage drug content of tablets in all the formulations was found between 91.51% to 106.69%, which complies with the limits established in pharmacopoeia. The in-vitro dissolution studies show maximum release of 89.47% in formulation F3 and minimum of 77.64% in formulation F12. Higher concentration of crospovidone and croscarmellose in formulations F3 and F6 showed better dissolution properties than SSG. So by varying the concentrations of superdisintegrants, oral disintegrating tablets can be formulated.


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