scholarly journals FORMULATION AND EVALUATION OF EFFERVESCENT GRANULES OF IBUPROFEN

Author(s):  
JINAN AL-MOUSAWY ◽  
ZAHRAA AL-HUSSAINY ◽  
MARYAM ALAAYEDI

Objective: The object of this investigation was to formulate and evaluate effervescent granules of ibuprofen, to increase its dissolution rate to get rapid analgesic and antipyretic effects. Methods: Five formulas (F1-F5) of effervescent ibuprofen granules were formulated by the wet granulation method. Croscarmellose sodium, powder of banana and other ingredients were used in the formulation of effervescent granules. Evaluation studies were carried out for all five formulas, these include: (compatibility study, flowability study, % of drug content, effervescent time and in vitro dissolution study). Results: The results show that the formulated granules have good flow properties with suitable bulk density for the uniting dose. FTIR study shows that there is no drug interaction with other ingredients in the formula. All five formulas have effervescent time less than 3 min, F5 show the best drug release 99.1±1 and effervescent time about 80 sec. Conclusion: Ibuprofen was successfully formulated and evaluated as effervescent granules by using a combination of croscarmellose sodium and banana powder.

Author(s):  
SUNDEEP MUPPARAJU ◽  
VIDYADHARA SURYADEVARA ◽  
SANDEEP DOPPALAPUDI ◽  
SASIDHAR REDDYVALLAM L. C. ◽  
RAMU ANNE ◽  
...  

Objective: The main objective of the current study is to enhance the solubility of Biopharmaceutical Classification System (BCS) Class-II drug Telmisartan using jack fruit seed starch as super disintegrant which increases drug release. Methods: Starches were extracted using alkali technique using sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations and water from Jack fruit seed powder. These starches were evaluated for various phytochemical and physicochemical tests. Fast dissolving tablets were prepared using Telmisartan, jack fruit seed starch and Croscarmellose sodium in various concentrations using wet granulation technique. Various pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) and accelerated stability studies. Results: Phytochemical tests revealed the presence of only starch in all the extracts. The starch prepared from 0.1% sodium hydroxide (JFS2) showed best physicochemical properties. From in vitro dissolution studies, it was observed that formulations F5 and F11 containing 15% w/w of JFS2 and 15% w/w of croscarmellose sodium showed faster disintegration and increased dissolution rate compared with other formulations. FTIR and DSC studies showed that there were no major interactions among drug and excipients. XRD studies revealed the nature of formulations. Accelerated stability studies revealed the stability of tablets. Conclusion: Thus, the tablets prepared using Jack fruit seed starch revealed the super disintegrant property of starch.


Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.


2019 ◽  
Vol 8 (2) ◽  
pp. 545-552

Ulcerative colitis is a chronic idiopathic inflammatory bowel disease that causes chronic inflammation and damage in the gastrointestinal (GI) tract that typically presents in the second or third decade of life with bloody diarrhoea and abdominal cramps. The objective of the present work was to formulate and evaluate of Prednisolone retention enema as a dispersible tablet and it is suspended in suitable vehicle for the treatment of ulcerative colitis. In the present work, an attempt has been made to formulate and evaluate Prednisolone retention enema as a dispersible tablet by using three different methods (direct compression (F1 to F3, wet granulation (F4 and F5) and slugging method (F6)). Prepared dispersible tablets were administered with the help of vehicle for the effective treatment of ulcerative colitis. Dispersible tablets were evaluated for various parameters. In vitro drug release and microbiological evaluation studies were performed to the best formulation in rectal suspension. Then the best formulation was subjected to carry out for stability studies at three different temperatures. Among the six formulations, F6 formulation showed better results. FT-IR study showed that there was no interaction between a drug and excipients. In vitro drug release and microbiological evaluation studies were performed for F6 formulation in rectal suspension. About 99.06 % of the drug was released at 60 min. and also it was found to be microbiologically stable. Results from the stability studies showed that F6 formulation alone and with rectal suspension was stable for a period of 90 days. It was concluded that F6 formulation in rectal suspension possesses a promising future for the treatment of ulcerative colitis.


2020 ◽  
Vol 10 (3-s) ◽  
pp. 142-149
Author(s):  
Inder Kumar ◽  
Sandeep Verma ◽  
Amit Chaudhary

Objective: The present work based on formulation of Ramipril tablets containing solid dispersion employing selective polymers. The objective of the preparation is to prepare the solid dispersion of the Ramipril, which has more responsive value in terms of the dissolution rate. Method: Solid dispersion complex was prepared with two different carriers PEG 6000 and PVP K30. Nine formulations were developed and each formulation were subjected to pre compression and post compression parameters. Result and Discussion:  Pre-compression and post compression parameters were studied which had shown good flow property and compiled the standard data. In-vitro dissolution studies shows more than 90 % drug release in phosphate buffer pH 6.8 in 30 min. Out of all formulation F4 showed 92.55±0.67 % drug release with in 30min which was the best result rest of the formulation. Conclusion: Ramipril tablets were successfully prepared and evaluated. F4 formulation shows the greater dissolution rate in phosphate buffer pH 6.8 as compared to other formulations. When compared with marketed formulation it also shows better results. Therefore, Ramipril solid dispersion tablets enhanced the dissolution rate and can be more efficacious for improving oral bioavailability of Ramipril. Keywords: Solid dispersion, Ramipril, Solvent Evaporation Technique.


2014 ◽  
Vol 1 (1) ◽  
pp. 8-23 ◽  
Author(s):  
Sarmila Shrestha ◽  
Dharma Prasad Khanal ◽  
Panna Thapa

Twenty three different tablet formulations of alprazolam were prepared using Polymer like hydroxypropylmethyl cellulose (HPMC K4M, HPMC K15M and HPMC K100M) in the concentration of 5 – 50 % of total weight of tablets and combination of HPMC K15M and HPMC K100M with ethyl cellulose (EC) was formulated by using wet granulation method. Drug formulation containing 1.0 mg, 1.5 mg, 5 mg, 10 mg and 15 mg alprazolam per tablet maintaining constant HPMC K15M concentration was also developed.The in-vitro dissolution studies of the formulated and marketed product in USP type II apparatus showed that the drug release is dependent upon the drug: polymer ratio; also molecular weight of the polymer and solubility of loaded drug. With increasing concentration and molecular weight of polymer, drug release was found to be decreased. When formulating the tablets the method used whether direct compression or wet granulations also affect the release of the drug from matrix. Wet granulation method by using 40 % HPMC K15M in combination with 5 % EC was found to be most suitable controlled release alprazolam tablet as drug release was found to be appreciable in this formulation. When loading dose of alprazolam was increased, drug release was found to be tremendously decreased because of the poor solubility of alprazolam in water. When one-way ANOVA was applied for various formulated and marketed tablets it was found that there is no significant difference (p > 0.05) in drug release rate among formulation similarly model independent methods was also applied such as similarity and dissimilarity factor and found that there is no significant difference between these formulations.DOI: http://dx.doi.org/10.3126/jmmihs.v1i1.9896 Journal of Manmohan Memorial Institute of Health Sciences Vol.1(1) 2011; 8-23


Author(s):  
Yella Sirisha ◽  
Gopala Krishna Murthy T E ◽  
Avanapu Srinivasa Rao

 Objective: The present research work is an attempt to determine the effect of various diluents and superdisintegrants on drug release of eletriptan orodispersible tablets and designs an optimized formulation using 22 factorial design. Further, evaluate the tablets for various pre-compression and post-compression parameters.Methods: The drug excipient compatibility study was conducted by infrared spectroscopy, differential scanning colorimetry and X-ray diffraction studies were conducted to test the purity of the drug. The tablets were formulated by direct compression method using spray dried lactose, mannitol, microcrystalline cellulose, starch as diluents and crospovidone, croscarmellose sodium, and sodium starch glycolate as superdisintegrants. The powder formulations were evaluated for pre-compression parameters such as bulk density, tapped density, Carr’s Index, Hausner’s ratio, and angle of repose. The tablets were evaluated for post-compression parameters such as the hardness, thickness, friability, weight variation, and disintegrating time in the oral cavity, in vitro drug release kinetics studies, and accelerated stability studies. The formulations were optimized by 22 factorial design.Results: The drug and excipients were compatible, and no interaction was found. The drug was pure, and all the pre-compression parameters were within Indian Pharmacopoeial Limits. Post-compression parameters were also within limits. The disintegration time was found to be 27 s for the formulation F29 containing Croscarmellose sodium (5%) and Mannitol as diluent, and in vitro drug release was found to be 99.67% in 30 min and follows first-order kinetics. This was also the optimized formulation by 22 factorial design with a p=0.013.Conclusion: The orodispersible tablets of eletriptan were successfully formulated, and the optimized formulation was determined that can be used in the treatment of migraine.


Author(s):  
Dinesh V. Panpaliya ◽  
Atish Y. Sahare ◽  
Priyanka Lanje ◽  
Pooja Dhoke

The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity


2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.


2012 ◽  
Vol 1 (11) ◽  
pp. 376-383 ◽  
Author(s):  
M Mallikarjuna Gouda ◽  
A Ramakrishna Shabaraya ◽  
S M Shanta Kumar

Current study is to develop the colon targeted matrix tablet using the natural polysaccharide sterculia gum as carrier and model drug ciprofloxacin HCl. The matrix tablets were prepared by wet granulation technology using the various proportions of sterculia gum with carbopol 934 P, sterculia gum and ethyl cellulose polymer blends. Granules of all formulations were evaluated for rheological, post compressional properties and in vitro dissolution study in different pH buffers of pH 1.2 , pH 7.4 , pH 6.8 (saline phosphate buffer) without and with 4% rat cecal content in order to mimic GIT condition . Formulation SGC2 to SGC4 and SGE7 to SGE9 has released 13.6% to 38.9% in the initial 5h and released more amount of drug in stomach and small intestine than colon. Formulation SGC5 containing 45% of sterculia gum and 25% carbopol 934 p and Formulation SGE10 containing 45% of sterculia gum and 25% ethyl cellulose has released minimum 10.91 % to 13.04 % in the initial 5h and sustained the drug release up to 24 h and at the end of study released 75% to 79.99%. Formulations with 4% rat cecal content at the end of 24 h study drug released is 90.44% to 95.33% indicating higher amount of drug release is due to enzymatic break down of sterculia gum in the matrix tablet. Hence the above results conclude that the formulation SGC5 and SGE10 are potential in targeting the drug to colon to treat irritable bowel disease.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12064 International Current Pharmaceutical Journal 2012, 1(11): 376-383


Author(s):  
Ningule Ganesh M. ◽  
Nagoba Shivappa N. ◽  
Shaikh Atiya L. ◽  
Wadulkar Raghunath D. ◽  
Deshmukh Aditye Y.

The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Glimepride with different ratios of hydrophilic and hydrophobic polymeric systems by the solvent evaporation technique. Different concentrations of oleic acid and isopropyle myristate were used to enhance the transdermal permeation of glimipride. Matrix type transdermal patches prepared by using different ratio of Eudragit RS100, HPMC100M, by using solvent evaporation techniques. All the prepared formulation were subjected to evaluation studies i.e., weight variation, thickness, drug content, moisture content, moisture uptake, flatness and in-vitro drug release. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Compatibility study between drug and polymer can be done by FTIR. From the all formulation batch F3 was optimized formula. Shows linear zero order release for 24 hrs with cumulative % drug diffusion of 88.34% from 4cm2 patches. It is concluded that concentration of polymer (HPMC100M) when increases into primary layer, then In-vitro diffusion rate also increases and concentration of Eudragit Rs100 when increases, the drug diffusion decreases. It provides better controlled drug release for patch.


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