scholarly journals STUDY OF DIRECT COMPRESSION METHOD FOR THE PREPARATION OF QUINAPRIL HYDROCHLORIDE TABLETS

2019 ◽  
pp. 202-211
Author(s):  
SHWETHA MARGRET JL ◽  
MADHAVI BLR
Keyword(s):  
Batch Size ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Compatibility Study ◽  
Direct Compression ◽  
Compression Method ◽  
Compression Technique ◽  
Blend Uniformity ◽  
Excipient Compatibility ◽  
Quinapril Hydrochloride

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.

scholarly journals FORMULATION AND OPTIMIZATION OF LEVAMISOLE CHEWABLE TABLETS

2019 ◽  
pp. 222-228
Author(s):  
PRADIP KUMAR CHAUDHARY ◽  
ABDUL RAHEEM T. ◽  
MANJUNATH U MACHALE ◽  
VASIA ◽  
SHAIK SADIK
Keyword(s):  
Drug Release ◽  
Compatibility Study ◽  
Direct Compression ◽  
Factorial Designs ◽  
Compression Method ◽  
Powder Blend ◽  
Dissolution Studies ◽  
Sodium Starch Glycolate ◽  
Chewable Tablets ◽  
Excipient Compatibility

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.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF BUSPIRONE USING COPROCESSED SUPERDISINTEGRANTS

2019 ◽  
pp. 31-37
Author(s):  
SHALLY SHARMA ◽  
NIMRATA SETH ◽  
NARESH SINGH GILL
Keyword(s):  
Water Absorption ◽  
Dosage Form ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Wetting Time

Objective: The present study aims to formulate and evaluate Fast dissolving tablet of Buspirone, the drug that is used for management of anxiety, by direct compression method using various Super disintegrants. Methods: Ten formulations (F1-F10) of fast dissolving tablets of Buspirone were prepared by using various Superdisintegrants. The prepared tablets were evaluated for hardness, friability, thickness, drug content uniformity, water absorption, wetting time, and disintegration time and in vitro dissolution study. Results: Among all the formulations, F10 (containing 5 mg of Coprocessed (CS: SSG 1:2) Superdisintegrants) was considered to be the best formulation, which released up to 98% drug in 20 min as compared to a marketed conventional dosage form which dissolves in approx 60 min. The results of stability study of formulation F10 after a period of two months indicated that the formulation was stable. Conclusion: It was concluded that a fast-dissolving tablet of Buspirone containing various Superdisintegrants is better and effective to meet patient compliance.

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

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.  

scholarly journals Formulation and evaluation of taste masked oral disintegrating tablets of lornoxicam

2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar
Keyword(s):  
Cation Exchange Resin ◽  
The Elderly ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Weight Variation ◽  
Croscarmellose Sodium

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders.  The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.

scholarly journals Formulation, Development and Evaluation of Bilayer Floating Tablet of Gemfibrozil

2019 ◽  
Vol 9 (4) ◽  
pp. 574-578
Author(s):  
Mohammad Faizan Mohammad Gufran ◽  
Sailesh Kumar Ghatuary ◽  
Reena Shende ◽  
Prabhat Kumar Jain ◽  
Geeta Parkhe
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Log P ◽  
Physical Parameters ◽  
Direct Compression ◽  
Formulation Development ◽  
Compression Technique

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).The aim of present study is to formulate Gemfibrozil (Gem) sustained release (SR) and immediate release (IR) bilayer tablet by different concentration of Hydroxypropyl methylcellulose (HPMC) and HPMC K 100 M to control the release pattern. The sustained release layer of Gem was prepared by using different grades of HPMC like, HPMC K-15, HPMC K-4 along with other excipients by direct compression technique. The immediate release layer of Gem was prepared by Cross carmellose sodium, Crospovidone and Sodium starch glycolate by direct compression technique. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. The both immediate release and sustained release layers of Gem were characterized by FT-IR and in vitro dissolution studies. The drug release study of Gem was evaluated using USP-II paddle type dissolution apparatus. The release rate of Gem in immediate release layer was studied for 15 min in 0.1 N HCL media and that of Gem in sustained release layer was studied for 12 h in 0.1 N HCL. From the nine batches F6 batch showed good release behaviour 99.85% of drug is released over 12 hours. Gem belongs to BCS Class II (log P 3.6) with poor solubility and high permeability resulting in limited and variable bioavailability. Total four trial batches of each drug have been manufactured to optimize and develop a robust and stable formulation, the stability studies of the products also comply with ICH guideline. Keywords: Bilayer floating tablets, Gemfibrozil, Biphasic drug release, HPMC K 15.

scholarly journals Formulation of Furosemide Oral Disintegrating Tablets Using Natural and Synthetic Superdisintegrants by SeDeM Expert Design System

2019 ◽  
Vol 9 (6) ◽  
pp. 55-63 ◽  
Author(s):  
Mulchand A. Shende ◽  
Kajal D Chavan
Keyword(s):  
Active Pharmaceutical Ingredient ◽  
In Vitro Dissolution ◽  
Design System ◽  
Direct Compression ◽  
Compression Technique ◽  
Drug Content ◽  
Weight Variation ◽  
Preformulation Studies ◽  
Natural And Synthetic

SeDeM design expert technique used to evaluate the risks of poor flow of pharmaceutical powders under preformulation studies which reveals direct compression suitability and prepare robust composition of active pharmaceutical ingredient (API) and excipient in tablets formulation. The purpose of this study was to develop oral disintegrating tablets of Furosemide using different concentration of natural and synthetic superdisintegrants by means of SeDeM design technique. Oral disintegrating tablets (ODT) of Furosemide were prepared by direct compression technique using isolated banana powder and croscarmellose sodium (Ac-di-sol) together with microcrystalline cellulose as superdisintegrants. SeDeM design was performed to check suitability and deficient of excipients and drug for optimized composition derived based on IPP value. These tablets were evaluated for hardness, friability, drug content, weight variation, wetting time and in-vitro dissolution. All the formulations showed low weight variation with dispersion time less than 173.5±0.70 seconds and rapid in-vitro dissolution. The drug content of all the formulations was within the acceptable limits. Lubricated blend composition of F4 found average radius value 5.24, 0.66 and 5.509 for IGC, IP and IPP respectively, compressed tablet shown good physical properties. The optimized formulation F4 showed good release profile with 99.25 percentage drug release compared to other trial batches. It was concluded that natural superdisintegrant (banana powder) showed better disintegrating property than synthetic super disintegrant (Ac-di-sol) in the formulations of ODTs. Keywords: Furosemide, Oral disintegrating tablets, SeDeM expert system, Superdisintegrants

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

2018 ◽  
Vol 10 (8) ◽  
pp. 67
Author(s):  
Naveen Goyal ◽  
Anil Kumar
Keyword(s):  
Ethyl Cellulose ◽  
Extended Release ◽  
Research Work ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Salbutamol Sulphate ◽  
Modified Polymers

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).

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

2021 ◽  
pp. 93-101
Author(s):  
Srikumar Billa ◽  
Saibabu Ch ◽  
Malyadri T
Keyword(s):  
Research Work ◽  
Immediate Release ◽  
Direct Compression ◽  
Compatibility Studies ◽  
Compression Method ◽  
First Order ◽  
First Order Kinetics ◽  
Croscarmellose Sodium ◽  
Physical Changes ◽  
Excipient Compatibility

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.

IMPROVEMENT OF DISSOLUTION RATE OF FEBUXOSTAT USING HYBRID TECHNIQUE OF SPHERICAL CRYSTALLIZATION AND SOLID DISPERSION

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (09) ◽  
pp. 32-39
Author(s):  
D. B Tandel ◽  
◽  
P. A Shah ◽  
K. G. Patel ◽  
M. C Gohel ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Hybrid Technique ◽  
Spherical Crystallization ◽  
Spherical Agglomerates ◽  
Pvp K30 ◽  
Excipient Compatibility

The present study was carried out with an aim to improve dissolution rate of febuxostat (FBX, BCSclass II) drug. Spherical agglomerates were prepared by hybrid technique of spherical crystallization and solid dispersion using different ratios of FBX and polymer (PVP K30, HPMC E3LV and chitosan). Drug excipient compatibility study was evaluated by Fourier transform infrared spectroscopy and X-ray diffractometry. Scanning electron microscopy was used for measurement of size of agglomerate. In vitro dissolution study of prepared spherical agglomerates was compared with untreated FBX and marketed formulation in phosphate buffer pH 6.8. The ratio of drug to polymer also affected the drug dissolution results. Drug excipient compatibility study showed no interaction between FBX and PVP K30 (1:5) polymer. The use of PVP K30 (1:5) resulted in partial amorphization and improved drug dissolution. Direct compression method can be adopted in manufacturing to simplify the validation efforts. The performance of the formulated product was superior to the marketed product in the in vitro dissolution test.

Formulation and Evaluation of Fast Dissolving Tablet of Ondansetron by Utilizing Liquisolid Compact Technique

2021 ◽  
pp. 163-168
Author(s):  
Sanket Jain ◽  
Sujit Pillai ◽  
Rampal Singh Mandloi ◽  
Nikhlesh Birla
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Dissolution Studies ◽  
Drug Content ◽  
Ftir Studies ◽  
Site Of Action

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.

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