scholarly journals Formulation, Characterisation and Evaluation of the Ethosuximide Oral Immediate Release Tablets

2020 ◽  
Vol 11 (2) ◽  
pp. 1807-1813
Author(s):  
Naga Sujan M ◽  
Kunal K Mehta ◽  
Amit B Patil ◽  
Anusha Vajhala
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Immediate Release ◽  
Rice Starch ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Release Studies

The present study is aimed to formulate, characterization, and evaluate oral immediate-release tablets of Ethosuximide. It is employed as an anti-epileptic agent used in the treatment of epilepsy, in all the age groups who were≥ 1 year. The dosage form is formulated by directly compressing the blend and granulating the powder blend by wet granulation methods. The optimized formulation is achieved by the trial and error method by changing the concentration of lactose monohydrate and di-basic calcium phosphate dehydrate as diluents, sodium starch glycolate as Super-dis-integrant, rice Starch as an intra-granular binder, hydroxypropyl cellulose as binder talc as a lubricant. Evaluation parameters such as micrometric properties, disintegration time along with in-vitro drug release studies were performed for characterizing the dosage form. In-vitro drug release studies were carried out using 0.1 N HCl as dissolution media with 75 rpm and temperature of 370C ± 50C by employing USP apparatus II (Paddle type). Estimation of the % drug release of the tablet was carried out using the UV method. The prepared formulation and the marketed formulation were tested for the in-vitro drug release profile and the prepared formulation was compared with the marketed formulation. All the evaluated result was found to be within the specifications. Therefore, from the obtained evaluation results F6 trail was selected as the best formulation.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

Development and In Vivo Evaluation of Mesalazine Colon Targeted Tablets

2019 ◽  
Vol 12 (3) ◽  
pp. 4552-4558
Author(s):  
Rawoof MD ◽  
Rajnarayana K ◽  
Ajitha M
Keyword(s):  
Drug Release ◽  
Wet Granulation ◽  
Time Intervals ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Ph Dependent ◽  
Rapid Hydrolysis

The main objective of the present study was to develop colon-targeted tablets of mesalazine by wet granulation method using 33 Response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16 % of mesalazine after 24 h, whereas marketed product drug release was 92.02 ± 2.15 after  24 h. From in vivo bioavailability studies, after oral administration of colon targeted tablet containing 400 mg mesalazine, the Cmax, Tmax, and AUC0–∞ of optimized formulation and marketed product was found to be 683.21 ± 0.03 ng/mL, 6.01 ± 0.04 h, 4150.12 ± 5.12 ng*h/mL and 445.34 ± 3.22 ng/mL, 4.00 ± 0.01 h, 3457.18 ± 5.32 ng*h/mL respectively. Cmax, Tmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of mesalazine for the treatment of disease at colon region.

scholarly journals The Effects of Lubricants on the Disintegration and Dissolution Profile of Metronidazole Tablets Formulated Using Sida acuta Gum as a Binder

2021 ◽  
pp. 350-362
Author(s):  
Sinodukoo Eziuzo Okafo ◽  
Avbunudiogba John Afokoghene ◽  
Christian Areruruoghene Alalor ◽  
Deborah Ufuoma Igbinake
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Sodium Lauryl Sulphate ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Sida Acuta ◽  
Drug Content

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder. Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release. Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35% Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.

scholarly journals DEVELOPMENT OF ORALLY DISINTEGRATING TABLETS OF MEMANTINE HYDROCHLORIDE-A REMEDY FOR ALZHEIMER’S DISEASE

2019 ◽  
pp. 147-152
Author(s):  
IMRAN S. GHOGARI ◽  
PRITAM S. JAIN
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Drug Release ◽  
Immediate Release ◽  
Tablet Formulation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orally Disintegrating Tablet ◽  
Accelerated Stability

Objective: The study is directed towards the development of an orally disintegrating drug delivery system of memantine hydrochloride which can be commercially exploited for the well-being of society for the treatment of Alzheimer’s disease, which is a most common form of dementia. Methods: Orally disintegrating immediate-release tablets of memantine hydrochloride were prepared and optimized for disintegration time and in vitro drug release. The top spray granulation method was used for the preparation of granules. Subsequently, these granules were compressed to tablets. The levels of diluent, disintegrant and taste-masking agents were optimized using the design of experiments. The resulting tablets were evaluated for disintegration time and in vitro drug release. The optimized formulation was subjected to accelerated stability study for 3 mo. Results: The optimized orally disintegrating tablet formulation exhibited a disintegration time of 2-3 min and complete drug release i.e. more than 85 % drug release within 10 min while performing in vitro drug release study. This is a prerequisite for faster action in the case of patients suffering from Alzheimer’s disease. Accelerated stability studies indicated good physical and chemical stability of the optimized formulation. Conclusion: Developed orally disintegrating tablet formulation of memantine hydrochloride could release the drug faster compared to conventional immediate-release tablets which is useful in paediatric, geriatric and psychiatric patients.

scholarly journals FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF DONEPEZIL HYDROCHLORIDE

2020 ◽  
pp. 45-51
Author(s):  
P. V. KAMALA KUMARI ◽  
Y. SRINIVASA RAO
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Wet Granulation ◽  
High Concentration ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Orodispersible Tablets ◽  
Weight Variation ◽  
Donepezil Hydrochloride

Objective: The present study was aimed to develop the formulation and in vitro evaluation of Orodispersible tablets by wet granulation method using Donepezil HCl as a model drug to enhance patient compliance. Methods: In the wet granulation method, a mixture of microcrystalline cellulose and hydroxypropyl methylcellulose were used along with superdisintegrants, i.e., croscarmellose sodium and crospovidone. The prepared granules were subjected to both pre and post-compression evaluation parameters including; FTIR spectroscopy, micromeritics properties, tablet weight variation, hardness, friability, drug content, disintegration time and in vitro drug release. Results: FTIR studies indicated that there was nointeraction between the drug and the excipients used. The formulation containing high concentration of crospovidone and mixture as the best formulation F2 based on in vitro drug release characteristics of tablet formulation. Conclusion: The results of this work suggested that orodispersible tablets of Donepezil hydrochloride with rapid disintegration time, fast drug release and good hardness can be efficiently and successfully formulated by wet granulation method.

FORMULATION AND EVALUATION OF THYROID HORMONE (T4) IMMEDIATE RELEASE TABLETS

2022 ◽  
Vol 2 (1) ◽  
pp. 389-393
Author(s):  
Madhivardhana P ◽  
Rajalakshmi A N ◽  
Padmapriya S
Keyword(s):  
Thyroid Hormone ◽  
Drug Release ◽  
Research Work ◽  
Immediate Release ◽  
Flow Property ◽  
Direct Compression ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Good Flow

The aim of this research work is to formulate and evaluate Levothroxine sodium immediate release tablets prepared by direct compression method . Five formulations were evaluated for different pre and post compression parameter and in vitro drug release studies.The results of pre compression parameters of formluation 1 to 5 were compared with prescribed limits. It showed that formulation 1 to 5 powder blend exhibit good flow property and compressibility property. The disintegration time of all formulation was found to be in the range 2mins 09 secsto 4mins 03 secs.Thus, based on evaluation of different parameters it was concluded that formulation of immediate release tablet Levothyroxine sodium was successfully done and F-5 showed almost 93% drug release at 45 mins in Alkaline borate buffer( pH 10). Keywords: Thyroid hormone (T4), Immediate release tablets, Direct compression, Dissolution.

scholarly journals Formulation and evaluation of orally disintegrating clopidogrel tablets

2016 ◽  
Vol 52 (2) ◽  
pp. 309-318 ◽  
Author(s):  
Gamal Mohamed Mahrous ◽  
Mohamed Gabr Kassem ◽  
Mohamed Abbas Ibrahim ◽  
Sayed Hassan Auda
Keyword(s):  
Drug Release ◽  
Content Uniformity ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Orally Disintegrating Tablets ◽  
Release Studies ◽  
Mouth Feel

ABSTRACT Recent advances in drug delivery systems have aimed to achieve better patient compliance. One of these advances is the formulation of orally disintegrating tablets (ODTs) that dissolve instantaneously, releasing drugs within a few seconds without the need of water. The main objective of this paper was to prepare and develop ODTs of clopidogrel. The ODTs were prepared by direct compression. The effect of three superdisintegrants, namely crospovidone, croscarmellose sodium, and sodium starch glycolate, using three different disintegration times on the dissolution rate was investigated. The prepared tablets were evaluated for hardness, friability, disintegration time and in vitro drug release. Furthermore, the interaction of clopidogrel with the formulation excipients was studied using differential scanning calorimetry (DSC). DSC studies revealed that there were no interactions between the drug and the excipients used. All tablets had hardness values in the range 4.0-5.2 kp and friability lower than 1%. The weight and drug content uniformity of all formulations was within official limits according to BP. In vitro drug release studies of the ODTs showed that more than 90% of the drug was released within ten minutes. A palatability test in human volunteers showed acceptable taste and mouth feel. Thus, the obtained results conclusively demonstrated successful rapid disintegration of the formulated tablets and acceptable palatability.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

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