scholarly journals Compatibility Studies of Atorvastatin Calcium with Selected Excipients By Means of Thermal and FT-IR Spectroscopic Methods for the Development of Immediate Release Tablet

2016 ◽  
Vol 8 (03) ◽  
Author(s):  
Bipul Nath ◽  
Tushar Roy
Keyword(s):  
Sodium Lauryl Sulfate ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Crystalline Cellulose ◽  
Content Uniformity ◽  
Lauryl Sulfate ◽  
Atorvastatin Calcium ◽  
Weight Variation ◽  
Ft Ir ◽  
Release Tablet

The objectives of present investigation is to evaluate the compatibility of Atorvastatin calcium with immediate release excipients and to optimize the tablet which release is best comparable with innovator product by varying different super disintegrants. Various excipients used were sodium starch glycollate, cross carmellose sodium, cross-povidone, lactose, micro crystalline cellulose, mannitol, sodium lauryl sulfate, magnesium stearate, and stearic acid. Thermal characterization of the drug was done by DSC and FT-IR. From the DSC studies, the excipients such as microcrystalline cellulose (Avicel 101), magnesium stearate, mannitol, sodium lauryl sulfate were found to have physical interactions with Atorvastatin. Immediate release tablet was prepared by direct compression method and its release profile was compared with the marketed IR tablet. The prepared tablet have conform the pharmacopoeial limit for hardness, thickness, friability, weight variation and content uniformity. Formulation F11 containing two super disintegrants have shown the disintegration time less than 25 sec and better dissolution than all other formulations releasing more than 80% of the drug after 20 minutes. Kinetic data reveals that the drug release follows best order by Higuchi model, followed by korsemeyer peppas, zero order and first order mechanisms. The results of accelerated stability studies as per ICH guidelines indicated that the tablet was stable as there were no any significant physical changes after the study.

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.

scholarly journals Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DDP-4 Inhibitor

2021 ◽  
Vol 24 (2) ◽  
pp. 168-179
Author(s):  
Tanoy Saha ◽  
Md Mahbubul Alam ◽  
Dilshad Noor Lira ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
Dosage Forms ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Dosage ◽  
Release Tablet

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

scholarly journals Formulation, Development and Evaluation of Bilayer Tablet of Flurbiprofen

2019 ◽  
pp. 246-251
Author(s):  
Nitin A Gaikwad ◽  
Indrjeet V Mane ◽  
Manohar D Kengar ◽  
Ranjeet S Jadhav
Keyword(s):  
Immediate Release ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets ◽  
Bilayer Tablet ◽  
Weight Variation ◽  
Initial Release ◽  
Higuchi Model

In the Study of Formulation of Bilayer Tablet of Flurbiprofen the Following Materials Using sodium starch glycolate as immediate release and HPMC K15 in different ratios as release retardant materials using a wet granulation method. All tablets exhibited good physical properties with Respect to appearance, content uniformity, hardness, weight variation and Invitro dissolution data show at increasing proportions Of sodium starch glycolate for immediate release whereas HPMC K15sustaineddrugreleaserate. The bilayer tablets showed an initial release of drug In about1hr, then sustaining the release for 12h, The kinetic analysis of dissolution data showed that release was observe din these tablets. When data was fitted to the Higuchi model. Bilayer tablets of flurbiprofen can be successfully formulated Using sodium starch glycolate and HPMC K15 in different ratios as release retardant materials employing a wet granulation method.

Formulation and Development of Divalproex Sodium Bi-Layered Tablets using Superdisintegrants and Release Retardant Polymers

2017 ◽  
Vol 10 (2) ◽  
pp. 3669-3675
Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Immediate Release ◽  
Physical Parameters ◽  
Content Uniformity ◽  
Divalproex Sodium ◽  
In Vitro Drug Release ◽  
Weight Variation

Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.  

scholarly journals Production of Itraconazole Nanocrystal-Based Polymeric Film Formulations for Immediate Drug Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 960
Author(s):  
Anna Karagianni ◽  
Leena Peltonen
Keyword(s):  
Drug Release ◽  
Physicochemical Characterization ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Polymeric Film ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming

In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.

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.

scholarly journals Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet

2021 ◽  
Vol 11 (1) ◽  
pp. 63-69
Author(s):  
Anjam H. Abdalla ◽  
Anoosh B. Hagop ◽  
Dina A. Boya
Keyword(s):  
Drug Release ◽  
Sodium Lauryl Sulfate ◽  
Fourier Transforms ◽  
Critical Role ◽  
Tween 80 ◽  
Release Profile ◽  
Oral Drug ◽  
Content Uniformity ◽  
Lauryl Sulfate ◽  
Significant Difference

The oral drug delivery is the most generally used route of administration that has been explored for the delivery of drugs through various pharmaceutical products. Solubility of drug plays critical role in achieving the optimum therapeutic levels of the drug in blood and thus bioavailability. There are many drugs of various therapeutic categories fall in Biopharmaceutics Classification System Classes II and IV as they lack solubility. For all these drugs, dissolution is the big issue for the absorption process. Valsartan is an effective antihypertensive agent and it can be used for the treatment of hypertension in most cases. The objective of this study is to prepare Valsartan as an oral sachet which can be used as an alternative dosage form after improvement of drug solubility using solubilizing agents such as sodium lauryl sulfate and tween 80. Three different formulas of Valsartan sachet were prepared by conventional technique of wet granulation method named conventional formula (Fc), sodium lauryl sulfate formula (Fs), and tween 80 formula (Ft) then compared with the available marketed product of Valsartan tablet (Fd) as a reference. The preformulations studies were conducted to exclude drug excipients interaction. Evaluation was performed in terms of weight variation, dose content uniformity, and drug release study using dissolution test apparatus. Fourier Transforms Infrared Spectroscopy reveals no drug excipient interaction and the drug release profile for Fs and Ft formulas within 30 min was 100.16% and 104.16%, respectively, while for Fc only 57.55% of the drug was released. This difference in the release profile was statistically significant (P < 0.05) between Fs and Ft with Fc, but a non- significant difference (P > 0.05) was observed between Fs and Ft with the marketed Valsartan tablet (Fd). The results support the possibility of using the prepared formulas Fs and Ft as a Valsartan sachet for the oral administration alternative to conventional Valsartan tablets Fd.

scholarly journals FORMULATION OF IMMEDIATE RELEASE (IR) ATORVASTATIN CALCIUM PELLETS AND SUSTAINED RELEASE (SR) GLIBENCLAMIDE FOR FIXED-DOSE COMBINATION DOSAGE FORM

2018 ◽  
Vol 11 (12) ◽  
pp. 159
Author(s):  
Kowshik K ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu
Keyword(s):  
Sustained Release ◽  
Guar Gum ◽  
Immediate Release ◽  
Fixed Dose ◽  
Locust Bean Gum ◽  
Atorvastatin Calcium ◽  
Dsc Studies ◽  
Ft Ir ◽  
Locust Bean

Objective: The objective of the present research was to develop fixed-dose combinations for the treatment of dyslipidemia, associated with type-II diabetes mellitus for improvement of glucose tolerance.Methods: Multiple unit pellet systems (MUPSs) consisting immediate release atorvastatin calcium pellets and sustained release glibenclamide were formulated by spheronization technique. The characterization of formulated pellets was done by Fourier transform infrared (FT-IR) and differential scanning calorimetry (DSC) studies, and formulated pellets were evaluated for solubility, viscosity, pH, and in vitro studies.Results: From FT-IR and DSC studies, it was confirmed that no chemical interaction existed between the drug and the natural polymers used. Solubility of glibenclamide was found to be 4.38 and 18.24 and atorvastatin calcium was found to be 6.84, 214.67, and 287.43 g/L. The viscosity of 1% w/v of locust bean gum, guar gum, and ghatti gum was found to be 169 cP, 124 cP, and 31 cP in distilled water. The pH of locust bean gum, guar gum, and gum ghatti solutions was found to be 5.6±0.49, 5.2±0.27, and 4.7±0.51. The in vitro studies suggested that glibenclamide pellets had shown a sustained release till 12 h, while atorvastatin calcium had shown immediate release of drug due to rapid disintegration of pellets.Conclusion: Thus, MUPS can be considered as an alternative approach to treat diabetes induced dyslipidemia.

Formulation and Evaluation of Bilayered Tablets Containing Immediate Release Layer of Glimepiride Complexed with Mangifera indica Gum and Sustained Release Layer Containing Metformin HCL by Using HPMC as Release Retardant

2017 ◽  
Vol 9 (6) ◽  
Author(s):  
Hemalatha S. ◽  
Srikanth P. ◽  
Mounica Sai G.
Keyword(s):  
Sustained Release ◽  
Mangifera Indica ◽  
In Vitro Release ◽  
Model Fitting ◽  
Immediate Release ◽  
Wet Granulation ◽  
Content Uniformity ◽  
Weight Variation ◽  
Uniform Dispersion

In present investigation an attempt has been made to design and develop the Bilayered tablet of Glimepiride and Metformin using Mangifera Indica Gum (MIG) and HPMC as Immediate Release and Sustained Release Layer polymers. Glimepiride and Metformin are oral-hypoglycaemic drugs which lower blood glucose level and have been selected to prepare Bilayered tablets. Glimepiride immediate release layer was prepared using MIG by wet granulation technique and Metformin sustained release layer was prepared using HPMC by dry granulation technique. Prepared Bilayered tablets were evaluated for parameters like thickness, diameter, weight variation, hardness, friability, disintegration and in-vitro release studies. All the prepared tablets were of smooth surface and elegant texture. The weights of the tablets were in the range of 540±0.551 mg. The thicknesses of the tablet were in the range of 4±0.05mm. The drug content uniformity study showed uniform dispersion of drug throughout the formulation in the range of 97.16±0.50%. The hardness was in the range of 4.0±0.5 kg/cm2 and friability is in the range of 0.67±0.06%. The bilayered tablets were also subjected to model fitting analysis to know the order and mechanism of drug release from the formulation by treating the data according to zeroorder, first-order, Higuchi and peppas equations.The bioequivalence studies conducted between prepared and marketed (Glycomate) bilayered tablet showed the similarity factor value of 70.120 for IR layer and 57.689 for SR layer.

ASSESSMENT OF THE TOXICITY AND HAZARD OF SODIUM LAURYL SULFATE AT DIFFERENT EXPOSURE ROUTES

2020 ◽  
pp. 56-59
Author(s):  
M. V. Bidevkina ◽  
M. I. Golubeva ◽  
A. V. Limantsev ◽  
I. N. Razumnaya ◽  
T. N. Potapova ◽  
...  
Keyword(s):  
Sodium Lauryl Sulfate ◽  
Exposure Level ◽  
Hazardous Substance ◽  
Lauryl Sulfate ◽  
Upper Respiratory Tract ◽  
Mucous Membranes ◽  
Chloroprene Rubber ◽  
Upper Respiratory ◽  
Exposure Routes ◽  
Number Of Cells

Sodium lauryl sulfate is the most common surfactant used in the production of detergents, chloroprene rubber, plastics, artificial furs and in pharmaceutical industry. Sodium lauryl sulfate is a moderately hazardous substance when introduced into the stomach (DL50 for white mice and rats is in the range of 2086-2700 mg/kg), has a pronounced local irritant effect on the skin and mucous membranes of the eyes, has a skin-resorptive, sensitizing and pronounced cumulative effects. The threshold for acute inhalation action is set at 15,3 mg/m3 for changes in the function of the nervous system and irritating effects on the mucous membranes of the upper respiratory tract (an increase in the total number of cells in the nasal flushes).Recommended for approval tentative safe exposure level of sodium lauryl sulfate in the air of the working area is 0.2+ mg/m3 (aerosol).

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