Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.


2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.


2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014


2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.


2018 ◽  
Vol 13 (2) ◽  
pp. 79
Author(s):  
Bassam Abduh Ali ◽  
Mohammed Gameel Al-haddad ◽  
Abdullah Ahmed Areqi

Clopidogrel is a medication to reduce the risk of heart disease and taken orally. Quality of drug characterizes the production process and every phamaceutical company strives for it but often it is very difficult to achieve. This study was to investigate quality control parameters of some marketed Clopidogrel tablets. To assess the quality, eight different marketed brands of Clopidogrel 75 mg tablets available in Yemeni market collected from different pharmacies in Hodeida city. Different quality parameters like weight variation, hardness, thickness and friability were determined according to established protocols. Then the in-vitro dissolution test, potency, disintegration time were also carried out. UV-spectrophotometer was used to determine the percentage released and assay at 218 nm. All the brands comply the requirements of Pharmacopoeia as they showed acceptable weight variation range. Friability of all brands was less than 1% and no significant differences in disintegration times as they disintegrated within 15 minutes. In case of dissolution profile, all brands except C6 showed acceptable dissolution time as they released more than 60% of drug in 45 minute. The hardness of only two brands was within the range. All brands also meet the potency specifications. This study suggested that most commercially Clopidogrel tablets in Yemen maintain the quality and comply with the pharmacopeia specifications.


2015 ◽  
Vol 3 (01) ◽  
pp. 11-17
Author(s):  
Krishnamurthy A. Kamalapurkar ◽  
Mahesh P. Chitali ◽  
Revansidh R. Pujari

The objective of this study was formulation development and evaluation of Oxcarbazepine Fast Dissolving Tablets (FDTs) prepared by sublimation technique where different sublimating agents like camphor and menthol were used with L-HPC and crospovidone as a superdisintegrants. Oxcarbazepine is an anticonvulsant drug used in the treatment of epilepsy and bipolar disorder. Each sublimating agent was used in concentration of 10-20 mg per tablet. Tablets were first prepared and then kept in hot air oven for sublimation. The prepared FDTs were evaluated for weight variation, thickness, drug content, friability, hardness, wetting time, water absorption ratio, in-vitro dispersion time, in-vitro disintegration time and in-vitro dissolution time. All formulations showed disintegration time ranging from 8 to 332sec. Optimized batch (SA6) was selected for the stability studies. The results of stability studies revealed that there was no remarkable difference in the tested parameters of promising formulation after storage for 3 months at 400 c ± 20 c 75% ± 5%RH and at room temperature 65% ± 5%RH as compared to initial results All the prepared formulae complied with Pharmacopoeia requirements of drug contents.


Author(s):  
JOGABRATA TRIPATHY ◽  
SUBHASHREE SAHOO ◽  
AFRASIM MOIN ◽  
SIDDARAMAIAH ◽  
D. V. GOWDA

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin. Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study. Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min. Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance.


INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 34-40
Author(s):  
V.L Narasaiah ◽  
◽  
Ch. Praneetha ◽  
P Mallika ◽  
K. Pullamma ◽  
...  

The aim of this project was to develop fast dissolving tablets (FDT) of aceclofenac by wet granulation using super disintegrating agents such as cross carmellose sodium (CCS), Crospovidone (CP) and sodium starch glycolate (SSG) were formulated and evaluated. The tablets evaluated for thickness, hardness, friability weight variation, drug content, water absorption ratio, wetting time, disintegration time and in vitro dissolution studies. The in vitro release studies were conducted in pH 7.4 phosphate buffer. Different release models like zero order, first order, Higuchi and Korsmeyer-Peppas were applied to in vitro drug release data in order to evaluate drug release mechanisms and kinetics. The formulation ‘F4’ showed satisfactory physico-chemical properties and drug content uniformity. The formulation ‘F4’ follows first order kinetics and the mechanism of drug release was governed by Higuchi. The ‘n’ value showed between <0.5, it was followed that Fickian transport. The FTIR studies were conducted and it shows that there is no interaction between drug and excipients.


2021 ◽  
Vol 11 (1) ◽  
pp. 42-47
Author(s):  
Pooja Kanathe ◽  
Ruchi Jain ◽  
Nilesh Jain ◽  
Surendra Kumar Jain

The purpose of this research work is to formulate and evaluate the Orodispersible tablet of Fluvastatin Sodium to enhance the bioavailability and effectiveness of the drug. The objectives of the drug work were to formulate and evaluate Orodispersible tablets of Fluvastatin Sodium, having adequate mechanical strength, rapid disintegration, and fast action. Precompression parameters like angle of repose, bulk density, tapped density, compressibility index & post-compression parameters like wetting time, water absorption ratio, in-vitro disintegration, and in-vitro dispersion time were studied. The hardness, friability, and drug content of all the formulations were found to be within the limits. The best formulation PK09 has shown good disintegration time, dissolution time, and dispersion time. The optimized formulation of batch PK9 gave the best in-vitro release of 99.60% in 3min in phosphate buffer pH 6.8. The release of the drug followed the matrix diffusion mechanism as compared to the commercial formulation. Formulation PK9 gives quick disintegration and better drug release. Hence it can be concluded that the formulation of PK9 is stable and effective for quick action and it is an alternative to the conventional tablets. Keywords:  Orodispersible Tablets, Fluvastatin Sodium, Fast dissolving/disintegrating tablets, GIT, bioavailability, first-pass metabolism, superdisintegrants


Author(s):  
Dr. Dilip Agrawal ◽  
Dr. Rakesh Goyal ◽  
Dr. Mukesh Bansal ◽  
Ashok Kumar Sharma ◽  
Mohit Khandelwal

The demands for fast dissolving tablets have received ever increasing day by day during the last decade. In the present projected study, the effect of natural Super disintegrants was compared with synthetic Super disintegrants and conventional Super disintegrants in the of fast dissolving tablet formulation of Meclofenamate Sodium. Meclofenamate sodium NSAID is used for the treatment of mild to moderate pain in various conditions like (e.g., dental pain, osteoarthritis) and to decrease pain and blood loss during menstrual periods. It is also used for other treatments like reducing pain, swelling, and joint stiffness caused with rheumatoid arthritis. In the present work 9 formulations of FDT (Fast dissolving tablet) of Meclofenamate Sodium were prepared by using Super disintegrants was evaluated and compiles with the official parameters and specifications. Various formulations were prepared using four different super disintegrants namely natural super disintegrant Banana Powder, sodium starch glycolate, crosscarmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose, bulk density, tapped density, and then tablet evaluated with various post-compression parameters like thickness, drug content, hardness, weight variation, wetting time, friability, disintegration time, dissolution time, drug release study. Formulation F2 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation F2 showed 98.55% drug release at the end of 3 minutes. The best formulations among these were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline.


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