scholarly journals Design, development and in vivo pharmacokinetic of telmisartan loaded oral disintegration tablets

2020 ◽  
Vol 11 (4) ◽  
pp. 8108-8118
Author(s):  
Arindam Chatterjee ◽  
Shaik Mohammad Abdulla ◽  
Nagarajan G ◽  
Birendra Shrivastava
Keyword(s):  
Angle Of Repose ◽  
Wet Granulation ◽  
Average Weight ◽  
Content Uniformity ◽  
Design Development ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Elimination Half ◽  
Powder Characteristics

Orodispersible Tablets (ODT) is a novel tableting technology which is formulated, and it overcomes the difficulties of other multi compressed tablets. Telmisartan has a bioavailability of 42-100 percent and a 24-hour elimination half-life. It excretes the majority of drugs through the faeces, which accounts for 97 percent of total drug excretion. The objective of this research is to formulate and evaluate Telmisartan loaded ODT and to prove the enhancement of dissolution and bioavailability of Telmisartan. From the DSC studies, it was confirmed that Telmisartan and excipients used in the formulation are compatible to each other and suitable for the manufacturing process. Telmisartan loaded ODT was formulated by wet granulation technique and evaluated for powder characteristics and release characteristics. About 9 formulations were formulated in each ODT, and all the formulation obeys a good powder flow characteristic from the angle of repose, Carr’s index and Hausner’s ratio. All the experimental formulation batches have been subjected to various evaluations viz, average weight, friability, disintegration, thickness, hardness, dissolution, content uniformity. Among this nine Telmisartan ODT formulations (F1-F9), F7 possess an expected release pattern and disintegration time in a short time period (i.e., 101.8 ± 2.72 in 5th min and disintegration time at 5 seconds), which may fastens the absorption and bioavailability of Telmisartan. It was concluded that ODT was a suitable dosage form to enhance the solubility at the same time the bioavailability of BCS class II drugs like Telmisartan.

The Effect of Superdisintegrants on the Dissolution of Promethazine. HCl Fast Dissolving Tablets

2010 ◽  
Vol 3 (1) ◽  
pp. 867-871
Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Angle Of Repose ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Enhanced Dissolution ◽  
Weight Variation ◽  
Compressibility Index ◽  
Chemoreceptor Trigger Zone ◽  
Trigger Zone ◽  
Standard Limit

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 

scholarly journals EVALUATION OF MUSA ACUMINATA FRUIT AS A NATURAL SUPERDISINTEGRANT FOR TABLET FORMULATION

2018 ◽  
Vol 11 (10) ◽  
pp. 167
Author(s):  
Gopinath E
Keyword(s):  
Nutritive Value ◽  
Low Cost ◽  
Cost Effective ◽  
Musa Acuminata ◽  
Tablet Formulation ◽  
Angle Of Repose ◽  
Average Weight ◽  
Disintegration Time ◽  
Solubility Study ◽  
Orodispersible Tablet

Objective: The objective of the present work was to develop and evaluate a new, low-cost effective superdisintegrant from Musa acuminata fruit for tablet formulation.Methods: The study involved collection of M. acuminata fruit powdered and evaluated for physicochemical properties. Propranolol Hcl was used as a model drug for tablet formulation. Different concentrations of M. acuminatea powder were used as superdisintegrant, and orodispersible tablet is prepared and evaluated. In the present study, sodium starch glycolate was used as synthetic superdisintegrant for comparative study.Result: The powder was dark brownish and did not change throughout the study. The percentage porosity of powder was found to be 42.88% and angle of repose of was found to be 33.69°. The solubility study shows that the powders are sparingly soluble in water and disperse into individual particles. Total ash and acid insoluble ash values of powder were found to be 2.61 and 2.11% w/w, respectively. The average weight of tablets was ranged from 101.42 to 103.52 mg and averaged hardness was found to be 3.4 kg/cm2. Moreover, the tablets exhibited acceptable friability. Disintegration time of all formulations was found to be in the range of 22–80 s and wetting time was found to be 07–18 s.Conclusion: From the study, it was concluded that M. acuminatea powder in the range of 2–12% can be used as superdisintegrant in orodispersible tablet formulation and shall be preferred as having nutritive value as well as cost profit in the development of orodispersible tablet than synthetic polymer.

scholarly journals Design Optimization and In Vitro-In Vivo Evaluation of Orally Dissolving Strips of Clobazam

2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Rajni Bala ◽  
Sushil Khanna ◽  
Pravin Pawar
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Content Uniformity ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
Significant Difference ◽  
Film Formulation ◽  
Test Film

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.

scholarly journals Isolation and preliminary evaluation of Mulva Neglecta mucilage: a novel tablet binder

2016 ◽  
Vol 52 (1) ◽  
pp. 201-210 ◽  
Author(s):  
Haroon Rahim ◽  
Abdul Sadiq ◽  
Shahzeb Khan ◽  
Kamran Ahmad Chishti ◽  
Fazli Amin ◽  
...  
Keyword(s):  
Binding Capacity ◽  
Diclofenac Sodium ◽  
Angle Of Repose ◽  
Binding Potential ◽  
Wet Granulation ◽  
Preliminary Evaluation ◽  
Disintegration Time ◽  
Tablet Dosage ◽  
Tapped Density ◽  
Pvp K30

ABSTRACT The aim of this study was to evaluate binding potential of Mulva neglecta mucilage (MNM) with subsequent comparison to PVP K30. Eight batches of Diclofenac sodium tablets were prepared by wet granulation technique keeping different concentrations (4, 6, 8 & 10% w/w) of Mulva neglecta mucilage (extracted from leaves of Mulva neglecta) and PVP K30 as standard binder. The granules of formulated batches showed bulk density (g/mL) 0.49 ± 0.00 to 0.57 ± 0.00, tapped density (g/mL) 0.59 ± 0.01 to 0.70 ± 0.01, Carr's index 09.27 ± 0.95 to 19.65 ± 0.59, Hausner's ratio 1.12 ± 0.00 to 1.24 ± 0.01 and angle of repose 30.37 ± 2.90 °C to 36.86 ± 0.94 °C. Tablets were compressed to hardness 7.50 to 7.95 kg/cm2. The tablets showed 0.39 ± 0.02 to 0.39 ± 0.01% friability and 7:20 to 14:00 min disintegration time. Granules and post-compression evaluation revealed that parameters assessed were all found to be within the pharmacopoeial limits. The results (hardness, disintegration and dissolution) proved that Mulva neglecta mucilage has better binding capacity for preparation of uncoated tablet dosage form as compared to PVP K30. Among all the formulations, MN-1 to MN-4 showed slow release as compared to PV-1 to PV-4 and thereby Mulva neglecta mucilage exhibited satisfactory drug release phenomenon tablets of diclofenac sodium.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF VALDECOXIB

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
K Kareemuddin Ansari ◽  
Neeraj Sharma
Keyword(s):  
Dissolution Rate ◽  
Methyl Cellulose ◽  
Aqueous Solubility ◽  
Angle Of Repose ◽  
Content Uniformity ◽  
Carboxy Methyl Cellulose ◽  
Compression Technique ◽  
Disintegration Time ◽  
Enhanced Dissolution ◽  
Carboxy Methyl

Valdecoxib is a selective COX- II inhibitor with anti – inflammatory, analgesic and antipyretic properties. The poor aqueous solubility of the drug leads to variable dissolution rates. In the present study an attempt has been made to prepare fast dissolving tablets of Valdecoxib in the oral cavity with enhanced dissolution rate. The fast dissolving tablets of Valdecoxib was prepared with some carriers (polymers) and super disintegrants such as Polyvinyl Pyrrolidone (PVP), Sodium Carboxy Methyl Cellulose (SCMC), Crospovidone NF and β – Cyclodextrin. The above mentioned all carriers and superdisintegrants were taken in different proportions of 5, 10, and 15%. All the formulations of the fast dissolving tablets of Valdecoxib were prepared by direct compression technique. The blend was examined for Angle of repose, Bulk density, Compressibility index and Hausner’s ratio. The prepared tablets were evaluated for hardness, drug content uniformity, friability, disintegration time and dissolution rate. An effective pleasant testing formulation released 99.88% drug within 10 minutes. The prepared formulations drug release was found to be comparable with the marketed dispersible tablets. Keywords: Fast dissolving tablets, Super-disintegrants, Valdecoxib, Crosspovidone, Sodium Carboxy Methyl Cellulose.

scholarly journals FORMULATION AND CHARACTERIZATION OF HERBAL TABLETS FOR THE MANAGEMENT OF DENGUE

2021 ◽  
pp. 104-113
Author(s):  
Shikha Thakur ◽  
Brisha Bhardwaj ◽  
Shouvik Kumar Nandy
Keyword(s):  
Carica Papaya ◽  
Hardness Test ◽  
Herbal Extract ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Weight Variation ◽  
Phosphorus Iron ◽  
Fresh Pulp ◽  
Tapped Density

Tablets are used as formulation and are prepared by using plant extracts i.e., Carica papaya and Embelica officinalis. These tablets were prepared by using wet granulation method. In this article the extract of leaves of Carica papaya and fruits of Embelica officinalis were used for making herbal tablets. Extracts of leaves of Carica papaya was obtained by cold extraction and through maceration method and the extract of fruits of Embelica officinalis was obtained by maceration process. Both extracts were dried and mixed. These extracts were then impregnated with the excipients like diluents, binding agents, super disintegrating agent, lubricants, etc. to make granules. These granules were then evaluated by using various parameters like Angle of repose, tapped density, bulk density, Carr’s Index, Hausner’s Ratio and void volume. These granules were then used for the making of tablets of desired size and shape by punching in the machine. After preparation of the tablets their evaluation parameters were studied like physical appearance, weight variation, friability, disintegration time, hardness test and thickness. Also the parameters for the acceptance of the tablets is also done like flavor and sweetness. Recent studies have shown that herbal extract of leaves of papaya has beneficial effect as an anti-inflammatory agent, for its wound healing properties, anti-tumor as well as Immunomodulatory effects and as an antioxidant. Amla fruit is a rich natural source of vitamin C (Ascorbic acid) and contains 600-750 mg/100 g of the fresh pulp. Also it is rich in minerals matters like phosphorus, iron and calcium. Amla is used as an Immunomodulatory agent and hence enhance the immunity of the patient. Aim of the study is to design develop and optimize the dosage form to cure dengue and is based on the use of natural plant ingredients to intermingle with chemical as well as synthetic ingredients to develop an effective unit dosage forms for better patient compliance. KEYWORDS: Papaya, Amla, Extracts, Herbal tablet, Dengue, Immunomodulatory, Platelets.

scholarly journals CHARACTERIZATION OF HYDROXYPROPYL CELLULOSE PRODUCED FROM α-CELLULOSE BETUNG BAMBOO (DENDROCALAMUS ASPER) AND IT’S APPLICATION IN TABLET FORMULATION

2019 ◽  
pp. 123-129
Author(s):  
Herman Suryadi ◽  
Harmita . ◽  
Muhammad Herpi Akbar ◽  
Pingkan Lestari ◽  
Pingkan Lestari
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Hydroxypropyl Cellulose ◽  
Tablet Formulation ◽  
Average Weight ◽  
Average Particle ◽  
Disintegration Time ◽  
Particle Size Analyzer ◽  
Size Uniformity ◽  
Powder Characteristics

Objective: This study aimed to obtain the physicochemical properties of hydroxypropyl cellulose (HPC) powder from α-cellulose Betung bamboo and its characteristics in tablet formulation. Methods: HPC was prepared by hydroxypropylation of α-cellulose using 25% (w/v) sodium hydroxide and 10 ml propylene oxide (based on 1 g α-cellulose) at 70 °C for 3 h. HPC of Betung bamboo (HPC BB) was characterized using fourier transform infrared (FTIR) spectrometry, particle size analyzer (PSA), x-ray diffraction (XRD), scanning electron microscope (SEM) and compared to HPC grade SL (HPC SL) as the reference. Then, HPC BB was used as a binder in tablet formulation by direct compression method and the resulted tablets were evaluated. The tablets evaluation including weight and size uniformity, hardness, friability and disintegration time. Results: The results showed HPC BB powder was yellowish white, odorless and tasteless, pH 7.49, residue on ignition 0.68%, hydroxypropoxy groups content 54.75%, average particle size 37.39 μm, loss on drying 1.09%, and moisture content 3.34%. Flow properties of powder fulfilled the requirements based on literature. Infrared spectrum and diffraction pattern of HPC BB were relatively similar to HPC SL. The tablets have average weight 403.495 mg, diameter 12.16 mm, thickness 3.11 mm, hardness 4.11 KPa, friability 2.04% and disintegration time 24.88 s. Conclusion: Based on the comparison of powder characteristics and tablets evaluation, HPC BB has a great potential in tablet formulation which showed similar characteristics to reference.

scholarly journals CINNARIZINE LIQUID SOLID COMPACTS: PREPARATION EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 150
Author(s):  
Sreenivas Patro Sisinthy ◽  
Shubbaneswarei Selladurai
Keyword(s):  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Weight Variation ◽  
Drug Concentrations ◽  
R Value

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

scholarly journals Physicochemical Characterization and Evaluation of the Binding Effect of Acacia etbaica Schweinf Gum in Granule and Tablet Formulations

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla
Keyword(s):  
Water Solubility ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hot Water ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Binding Effect ◽  
Tablet Formulations

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.

scholarly journals Postruminal Delivery System for Amino Acids and Proteins in Cattle

2007 ◽  
Vol 76 (4) ◽  
pp. 547-552 ◽  
Author(s):  
T. Sýkora ◽  
M. Rabišková ◽  
J. Třináctý ◽  
D. Vetchý ◽  
A. Häring ◽  
...  
Keyword(s):  
Amino Acids ◽  
Small Intestine ◽  
Low Cost ◽  
Ph Sensitive ◽  
Wet Granulation ◽  
Average Weight ◽  
Disintegration Time ◽  
The Core ◽  
Ph Sensitive Polymer

The purpose of this experiment was to develop an effective postruminal transport system (PTS) with a high content of suitable vegetable proteins and amino acids. PTS serves for nutrient delivery to the abomasum and small intestine of dairy cows in order to increase the milk yield. Direct addition of proteins and amino acids to the diet is not useful as the ruminal microbes will utilize active substances before they reach absorption sites in the small intestine. PTS has several advantages, e.g. a possibility of the direct application in a food, low cost, and nutritional and therapeutical improvement. PTS consists of a core (pellets, small tablets) and a coating, which protects the core against the environment of rumen and enables to release the core content in the environment of abomasum and small intestine. Lenticular tablets - cores of PTS were prepared by wet granulation method and compression. Qualitative indicators of tablets (average weight, weight uniformity, hardness, friability, disintegration time) were determined according to valid Czech and European Pharmacopoeias. Cores were subsequently coated with several types of coating - ethylcellulose, stearic acid and pH sensitive polymer poly-(2-vinylpyridine-co-styren), alone or in combination of various rates. Nine samples of coated protein tablets exhibiting appropriate characteristics in vitro were prepared. The presence of the pH sensitive polymer at least in 10% concentration of the coating and the coating amount of 9.0 to 12.6% per tablet were necessary to ensure the requested PTS properties.

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