scholarly journals FORMULATION AND EVALUATION OF SOMATOSTATIN ANALOGUE TABLETS

2019 ◽  
pp. 220-223
Author(s):  
ZOYA SHPRAKH ◽  
OLGA ORLOVA ◽  
NATALYA OBOROTOVA ◽  
NATALYA BUNYATYAN
Keyword(s):  
Magnesium Stearate ◽  
Wet Granulation ◽  
Somatostatin Analogue ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Long Term Study ◽  
Weight Variation ◽  
Powder Properties ◽  
Pharmaceutical Properties

Objective: This study was undertaken with the aim of the formulation and evaluation of hypothalamic hormone somatostatin analogue tablets, which are intended for neuroendocrine tumours treatment. Methods: Tablets were prepared by using the wet granulation method and evaluated for weight variation, resistance to crushing, friability, disintegration time, content and content uniformity. Stability tests have been performed. Results: Characteristics of somatostatin analogue cyphetrylin powder have been investigated, and the wet granulation method has been chosen to prepare tablets. Technical pharmaceutical properties of formulations of different compositions and obtained tablets were estimated and the best formulation CF11 has been established with appropriate characteristics: disintegration time less than 15 min, resistance to crushing more than 30 kg·m·s−2, weight variation ˂7.5 %, active substance content closed to the nominal quantity and consistent cyphetrylin distribution in the batch. Performed examinations showed cyphetrylin tablets stability in the long-term study. Conclusion: Because of somatostatin analogue cyphetrylin powder properties tablets were prepared by the wet granulation method with starch, lactose, povidone, talc, microcrystalline cellulose, calcium stearate and magnesium stearate as excipients. The best formulation including povidone has characteristics corresponding to requirements of European Pharmacopoeia (PhEur) and State Pharmacopoeia of the Russian Federation (PhRu). Examination of cyphetrylin tablets showed its quality and stability within the time of observation–12 mo.

DESIGN AND CHARACTERIZATION OF ACECLOFENAC FAST DISSOLVING TABLETS USING SUPER DISINTEGRATING AGENTS

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (01) ◽  
pp. 34-40
Author(s):  
V.L Narasaiah ◽  
◽  
Ch. Praneetha ◽  
P Mallika ◽  
K. Pullamma ◽  
...  
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Disintegration Time ◽  
First Order ◽  
Drug Content ◽  
Weight Variation

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.

scholarly journals Optimization of Immediate Release Tablet of Raloxifene Hydrochloride by Wet Granulation Method

2009 ◽  
Vol 1 (01) ◽  
Author(s):  
Rai V. K. ◽  
Pathak N. ◽  
Bhaskar R. ◽  
Nandi B. C. ◽  
Dey S. ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Weight Variation ◽  
Raloxifene Hydrochloride ◽  
Vitro Release ◽  
Release Tablet

The purpose of this research is to prepare Raloxifene Hydrochloride immediate release tablet by wet granulation technique. In order to obtain the best, optimized product six different formulations were developed. Different filler, binder, disintegrant and lubricant were taken as variables. Weight variation, thickness, hardness, friability, disintegration time, in-vitro release and pharmaceutical assay were studied as response variables. Sticking was observed when the formulation containing stearic acid and sodium stearyl fumarate. However, in the remaining four formulation containing magnesium stearate, no sticking was observed. The formulation NP061 was selected as an optimized product. The different physical properties and in-vitro release profile showed best comparable with reference product. Optimization has proven as an effective tool in product development.

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. 

Formulation and Evaluation of Atenolol and Indapamide SR Matrix Tablets for Treatment of Hypertension

2014 ◽  
Vol 7 (2) ◽  
pp. 2450-2458
Author(s):  
Sarika Pundir ◽  
Ashutosh Badola
Keyword(s):  
Kinetic Studies ◽  
Film Coating ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Simultaneous Estimation ◽  
Matrix Tablet ◽  
Release Agent ◽  
Disintegration Time ◽  
Weight Variation

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.

scholarly journals FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Rapid Release ◽  
Weight Variation ◽  
Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 

scholarly journals FORMULATION AND EVALUATION OF FUROSEMIDE LIQUISOLID COMPACT

2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim
Keyword(s):  
Dissolution Rate ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 400 ◽  
Coating Materials ◽  
Disintegration Time ◽  
Weight Variation ◽  
R Ratio

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

scholarly journals Evaluating the Flow and Release Profiles of Ibuprofen Formulations by Increasing the Binder Concentration

2021 ◽  
Vol 16 (2) ◽  
pp. 111-117
Author(s):  
B.B. Mohammed ◽  
E.J. John ◽  
G.T. Abdulsalam ◽  
K.P. Bahago
Keyword(s):  
Release Rate ◽  
Active Drug ◽  
Release Profile ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Dissolution ◽  
Tablet Formulations ◽  
Release Profiles

Background: Tablets must be able to release the active drug in the gastrointestinal tract for absorption. The release profile of solid pharmaceutical dosage formulations can be quantified by assessing the disintegration and dissolution times tests. Binders are adhesives either from sugar or polymeric material that are added to tablet formulations to provide the cohesiveness required for the bonding together of the granules under compaction to form tablets.Objective: The objective of the study was to formulate and assess ibuprofen tablets using different concentrations of binders (Acacia and Gelatin).Methods: The granules were prepared using wet granulation method and analysed for flow properties based on USP/NF protocols. After granule compression, the tablets release profiles were thereafter assessed via the tablet dissolution and disintegration tests.Results: Weight variation, thickness and diameter were within the acceptable values for all batches indicative of a uniform flow. Batches with binder concentrations of 10 % and 20 % failed disintegration test due to a disintegration time above 15 min while the release rate for batches 1 and 4 was about 88 % in 60 min as against the other batches whose release rate was less than 50 % in 60 min as a result of increasing their binder concentrations.Conclusion: The study concluded that increasing the concentration of acacia and gelatin above 5% led to a decrease in percentage of drug released and an increase in disintegration time above 30 mins because 5% batches gave the best release profiles.

scholarly journals EFFECT OF MALTODEXTRIN RATIO TO KLUTUK BANANA FRUIT EXTRACT (MUSA BALBISIANA COLLA) COMBINED WITH ITS PSEUDOSTEM EXTRACT ON ANTI-DYSENTERY GRANULE PERFORMANCE AND EFFECTIVITY

2018 ◽  
Vol 10 (6) ◽  
pp. 187
Author(s):  
Sri Agung Fitri Kusuma ◽  
Soraya Ratnawulan Mita ◽  
Ratna Fitria Ermawati
Keyword(s):  
Shigella Dysenteriae ◽  
Potassium Content ◽  
Wet Granulation ◽  
Banana Fruit ◽  
Banana Plant ◽  
Fruit Extract ◽  
Disintegration Time ◽  
Musa Balbisiana ◽  
Weight Variation ◽  
Dried Fruit

Objective: The objective of this study was to determine the best ratio of maltodextrin and extract concentration on performance of anti-dysentery granule containing Klutuk banana fruit extract (Musa balbisiana Colla) as an effective antimicrobial to treat dysentery caused by Shigella dysenteriae and combined with its pseudostem extract to supply potassium needed for supporting dehydration impact caused by dysentery.Methods: The dried fruit and pseudostem of the Klutuk banana plant were each extracted by maceration method. Each granule formula was optimized in different ratio of extract and maltodextrin concentration (1:2 (F1); 1:3 (F2); and 1:4 (F3) respectively. Then, the anti-shigellosis granule were formulated using the wet granulation method and evaluated for 30 d. The appearance of the granule, weight variation, loss on drying value, flowability, granule solubility, disintegration time, pH, and anti-dysentery activity of each formula was observed. The potassium content determination of each granule formula was done using an atomic absorption spectrophotometer method. Results: All formulated granules showed good flow properties and antidysentery activity. Concerning to the solubility, maltodextrin addition showed the increasing solubility of all formulated granule. The F3 achieved the best-improved granule characteristic and had good anti-dysentery effectivity, but had the lowest potassium content (0.362 g/l) among all formulas. The potassium content of F1 and F2 were 0.625 g/l and 0.444 g/l, respectively. Conclusion: Maltodextrin can improve the usefulness of granule that containing the Klutuk banana fruit and its pseudostem extracts in dysentery treatment and the dehydration impact.

scholarly journals Tablet Formula Optimization From Helminthostachys Zaylanica Extract Using A Simplex Lattice Design

2021 ◽  
Vol 6 (3) ◽  
pp. 131-136
Author(s):  
Fitrya Fitrya ◽  
Najma Annuria Fithri ◽  
Budi Untari ◽  
Aprililianti
Keyword(s):  
Physical Properties ◽  
Toxicity Tests ◽  
Dissolution Time ◽  
Wet Granulation ◽  
Disintegration Time ◽  
Lattice Design ◽  
Simplex Lattice Design ◽  
Weight Variation ◽  
Simplex Lattice ◽  
Helminthostachys Zeylanica

Helminthostachys zeylanica extract has pharmacological activities such as antioxidant, antiinflamatory, and antihyerucemia. This extract is nontoxic substance from the acute and subchronic toxicity tests. This extract has a potency to be formulated into tablet dosage forms. This study aims to optimize a tablet formula from Helminthostachys zeylanica extract. Disintegrant and binder concentrations were independent variables, while physical properties and dissolution time of the tablets were dependent variables. The tablet was prepared by a wet granulation method. Formula was optimized by Simplex Lattice Design. Physicochemical propertiesof granule, physical properties and dissolution of tablet were then analyzed with One Way ANOVA (p = 0.05). Based on granule analysis, specification of physicochemical parameters, such as hausner’s ratio, compressibility index, flowability, repose angle, and water content, met standard British Pharmacopeia. In addition, the starch and PVA concentrations influenced thickness, weight variation, hardness, friability, disintegration time and dissolution of the tablets (p <0.05), except for friability (p> 0.05). Based on this study, the starch and PVA concentrations for the optimum tablet formula were 19.5% and 1.05%, respectively.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILM OF ANTI-ALLERGIC DRUG

2018 ◽  
Vol 6 (3) ◽  
pp. 5-16 ◽  
Author(s):  
ABRAHAM LINKU ◽  
JOSEPH SIJIMOL
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Moisture Loss ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Permeation Study ◽  
Weight Variation

The aim of present work was the development of fast dissolving oral film of Loratadine to overcome the limitations of current routes of administration, to provide immediate action and increase the patient compliance. To improve the bioavailability of the drug, fast dissolving oral film were formulated using different grades of Hydroxy Propyl Methyl Cellulose(HPMC) and various plasticizers like Polyethylene Glycol(PEG) 400, glycerol, Propylene glycol(PG) by solvent casting method. The formulated films were evaluated for film thickness, surface pH, folding endurance, weight variation, % moisture loss, exvivo permeation study, tensile strength, % elongation, drug content uniformity, in vitro dissolution studies,in vitro disintegration test and in vivo study. The optimized formulation (F9) containing HPMC E5 and glycerol showed minimum disintegration time (10.5 s), highest in vitrodissolution (92.5%) and satisfactory stability. Ex vivo permeation study of optimized formulation showed a drug release of 80.6% within 10 min. The milk induced leucocytosis inrat proved that fast dissolving oral films of Loratadine produced a faster onset of action compared to the conventional tablets. These findings suggest that fast dissolving oral film of Loratadine could be potentially useful for treatment of allergy where quick onset of action is required.

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