scholarly journals Liquisolid Tablets Formulation of Atorvastatin Calcium Using Polyethylene Glycol 400 as Solvent and Some Carrier Materials

2020 ◽  
Author(s):  
Yulias Ninik Windriyati ◽  
Matsniyyatul Badriyah ◽  
Diar Arum Kusumaningtyas ◽  
Rian Lesta Riesmalia
Keyword(s):  
Coating Material ◽  
Ftir Analysis ◽  
High Permeability ◽  
Polyethylene Glycol 400 ◽  
Atorvastatin Calcium ◽  
Peg 400 ◽  
Bcs Class Ii ◽  
Carrier Materials ◽  
Low Solubility ◽  
Neusilin Us2

The dissolution of atorvastatin calcium need to be improved since included BCS Class II drugs with low solubility and high permeability, meaning that the dissolution affects the bioavailability of drugs. This research aimed to develop a formulation of a liquisolid tablet using PEG 400 as a solvent and some carrier materials in various compositions to increase the dissolution of atorvastatin calcium. Different formulations of liquisolid tablets were conducted using different quantities of carrier and coating material for adsorbing liquid solvent to produce a free-flowing and compressible powder. Avicel PH 101, Avicel PH 102, Neusilin US2 were employed as the carrier and Aerosil 200 as the coating material. A disintegrant and lubricant were then added to the formed liquisolid system and compressed into tablets by the direct compressing method. The liquisolid tablets were characterized for their tableting properties and possible drug-excipient interaction by XRD and FTIR analysis. The tableting characteristics of atorvastatin calcium liquisolid tablets were within the acceptable limits criteria. The dissolution of AA4 and NA1 liquisolid tablets was higher compared to marketed tablets. Based on the XRD and FTIR analysis, no interactions between drug and excipient.  

scholarly journals CONTROLE DE QUALIDADE DE CÁPSULAS MANIPULADAS CONTENDO ATORVASTATINA CÁLCICA

2020 ◽  
Vol 12 (2) ◽  
pp. 59-69
Author(s):  
Diego da Silva Ribeiro ◽  
Nayra Mendes da Silva ◽  
Ana Julia Pereira Santinho Gomes
Keyword(s):  
Oral Absorption ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
High Permeability ◽  
Pharmaceutical Dosage Forms ◽  
Atorvastatin Calcium ◽  
Pharmaceutical Ingredients ◽  
Continuous Use ◽  
Low Solubility

Atorvastatin calcium (ATC) is one of the most used drugs in the treatment of dyslipidemia. The compounding of capsules containing ATC has often been requested as it is an exceptionaldispensing drug (continuous use and high cost). ATC presents low solubility and high permeability, therefore, pharmaceutical ingredients are capable of interfering with its solubility. The aim of this work was to evaluate the quality of ATC capsules prepared incompoundingpharmacies in Divinópolis,Brazil.Fourier Transform Infrared spectroscopy (FTIR) was used to identify the ATC. Tests for weight determination (WD), content uniformity (CU) and dissolution were also carried out. The FTIRconfirmed the authenticity of ATC. All batches were approved in relation to the WD, however only 67% were approved in relation to the CU, although all have been approved for acceptance value.It was also observed that 1/3 of the products did not display the specified dissolution rate. This is due to the excipient composition impacting on a significantly slower dissolution profile compared to the others. It was noted that the choice of a specific excipient for ATC together with an appropriate encapsulation procedure play key roles in ensuring the quality of an exceptional dispensing drug, whose dissolution behaviorcan influence oral absorption. In conclusion, the importance of monitoring the compounding process was demonstrated, expanding the relevance of the constant evaluation of the quality of pharmaceutical dosage forms, bringing to light the difficulties of the compounding sector, as well as the effectiveness of the approval criteria employed to date.

scholarly journals Intestinal absorption of BCS class II drugs administered as nanoparticles: A review based on in vivo data from intestinal perfusion models

ADMET & DMPK ◽  
2020 ◽  
Author(s):  
David Dahlgren ◽  
Erik Sjögren ◽  
Hans Lennernäs
Keyword(s):  
Class Ii ◽  
Intestinal Perfusion ◽  
Oral Drug ◽  
High Permeability ◽  
In Vivo Models ◽  
Fed State ◽  
Bcs Class Ii ◽  
Mucus Barrier ◽  
Low Solubility

An established pharmaceutical strategy to increase oral drug absorption of low solubility–high permeability drugs is to create nanoparticles of them. Reducing the size of the solid-state particles increases their dissolution and transport rate across the mucus barrier and the aqueous boundary layer. Suspensions of nanoparticles also sometimes behave differently than those of larger particles in the fed state. This review compares the absorption mechanisms of nano- and larger particles in the lumen at different prandial states, with an emphasis on data derived from in vivo models. Four BSC class II drugs—aprepitant, cyclosporine, danazol and fenofibrate—are discussed in detail based on information from preclinical intestinal perfusion models.

scholarly journals Enhancement of Aqueous Solubility and Dissolution Profile of Atorvastatin Calcium: In vitro Evaluation of Solid Dispersion

2021 ◽  
pp. 1-7
Author(s):  
Pawar AR ◽  
◽  
Mehetre JS ◽  
Keyword(s):  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Lipid Lowering ◽  
Dissolution Profile ◽  
High Permeability ◽  
Onset Of Action ◽  
Atorvastatin Calcium ◽  
Lipid Lowering Agent ◽  
Low Solubility

Purpose: The objective of the present study was to formulate solid dispersions (SD) of Atorvastatin calcium to improve the aqueous solubility and dissolution rate to facilitate faster onset of action. Atorvastatin calcium is a lipid lowering agent belonging to BCS-II having low solubility and high permeability.

scholarly journals FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

2020 ◽  
pp. 34-41
Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
Bioavailability Enhancement ◽  
Disintegration Time ◽  
Peg 400 ◽  
Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

scholarly journals FORMULATION AND EVALUATION OF ATORVASTATIN CALCIUM NANOCRYSTALS CONTAINING P-GLYCOPROTEIN INHIBITORS FOR ENHANCING ORAL DELIVERY

2021 ◽  
pp. 19-23
Author(s):  
SARAH LABIB ◽  
MOHAMED NASR ◽  
MOHAMED NASR
Keyword(s):  
Polyethylene Glycol ◽  
Oral Drug Delivery ◽  
Tween 80 ◽  
Degree Of Crystallinity ◽  
Oral Drug ◽  
Tween 20 ◽  
Atorvastatin Calcium ◽  
Peg 400 ◽  
P Glycoprotein ◽  
Saturated Solubility

Objective: The main objective of this study was to develop atorvastatin calcium (ATR) as an oral drug delivery system for a P-glycoprotein (P-gp) substrate drug using different pharmaceutical excipients that inhibit P-glycoprotein and evaluate the influence of nanocrystals on the dissolution characteristics and bioavailability compared to the plain drug. Methods: A nanosuspension was prepared by Solvent-antisolvent precipitation method using a solvent containing stabilizer that act as a p-gp inhibitor dissolved in distilled water as polyethylene glycol 300, polyethylene glycol 400 (PEG 300, PEG 400), tween 20 and tween 80 while the solvent selected for atorvastatin calcium was methanol. The concentrations were as follows: PEG 300 and 400 = 0.25% w/v, tween 20 and 80 = 0.75% v/v. Nanocrystals were extracted from the suspension and characterized. Results: Particle size of the drug was 1307±127.79 nm while the formulas prepared ranged from 223±17.67 to 887±58.12 nm. Pure ATR had a saturated solubility of 0.059±0.005 mg/ml and the prepared nanocrystals ranged from 0.32±0.021 to 0.88±0.019 mg/ml. The Percentage of drug released of plain atorvastatin calcium reached 41.49% while the formula ranged from 44.32 to 61.5%. Both XRD and SEM discussed the degree of crystallinity as follows: F1<F2<F4<F3<ATR. Conclusion: 0.3% of PEG 300 and PEG 400 were not enough to formulate proper nanocrystals while 0.75% tween 20 and tween 80 achieved acceptable formulas. F4 which is prepared with tween 80 exhibited the highest enhancement in saturated solubility, dissolution rate and subsequently expected to have improved oral bioavailability.

scholarly journals Self-microemulsifying drug delivery systems of Moringa oleifera extract for enhanced dissolution of kaempferol and quercetin

2020 ◽  
Vol 70 (1) ◽  
pp. 77-88 ◽  
Author(s):  
Namfa Sermkaew ◽  
Thipapun Plyduang
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Moringa Oleifera ◽  
Delivery Systems ◽  
Polyethylene Glycol 400 ◽  
Peg 400 ◽  
Enhanced Dissolution ◽  
Promising Strategy ◽  
Herbal Medicinal ◽  
Percentage Ratio

AbstractThe aim of the present study was to develop self-microemulsifying drug delivery systems (SMEDDS) of the extract of Moringa oleifera, a herbal medicinal plant. Kaempferol and quercetin, the flavonoids present in the leaf extract of M. oleifera, were chosen as markers for quantification. The optimized formulation of SMEDDS consisted of propylene glycol dicaprylocaprate, polysorbate 80, and polyethylene glycol 400 (PEG 400) in a percentage ratio of 20:60:20 (m/m). SMEDDS emulsified immediately (within 20 s) after dilution in water, resulting in transparent microemulsions with a droplet size of 49 nm. SMEDDS could increase the solubility of kaempferol and quercetin to nearly 100 % within 15 min, whereas only a 30 % improvement in solubility was achieved in the case of crude extract. These results demonstrated SMEDDS to be a promising strategy to improve the solubility of M. oleifera extract-derived drugs, which, in turn, could prove beneficial to the herbal medicine field.

Solubility and Thermodynamics of 6-Phenyl-4,5-dihydropyridazin-3(2H)-one in Various (PEG 400+Water) Mixtures

2019 ◽  
Vol 233 (2) ◽  
pp. 273-287 ◽  
Author(s):  
Mohd. Imran
Keyword(s):  
Polyethylene Glycol ◽  
Thermodynamic Analysis ◽  
Mole Fraction ◽  
Solubility Data ◽  
Polyethylene Glycol 400 ◽  
Isothermal Method ◽  
Peg 400 ◽  
Neat Water

Abstract The aim of this study was to determine the solubility of pyridazinone derivative 6-phenyl-4,5-dihydropyridazin-3(2H)-one (PDP-6) in different “polyethylene glycol 400 (PEG 400)+water” mixtures at temperatures “T=293.2 K to 313.2 K” and pressure “p=0.1 MPa”. The solubilities of PDP-6 were determined using an isothermal method and correlated with Apelblat, van’t Hoff and Yalkowsky–Roseman models. The maximum solubilities of PDP-6 in mole fraction were obtained in neat PEG 400 (8.46×10−2 at T=313.2 K). However, the minimum one was recorded in neat water (7.50×10−7 at T=293.2 K). Apparent thermodynamic analysis showed an endothermic dissolution of PDP-6 in all (PEG 400 water) mixtures. Based on the solubility data of the current study, PDP-6 has been considered as practically insoluble in water and soluble in PEG 400.

Effects of polyethylene glycol 400 (PEG 400) following 13 weeks of gavage treatment in fischer-344 rats

1995 ◽  
Vol 33 (2) ◽  
pp. 139-149 ◽  
Author(s):  
S.J. Hermansky ◽  
D.A. Neptun ◽  
K.A. Loughran ◽  
H.W. Leung
Keyword(s):  
Polyethylene Glycol ◽  
Fischer 344 Rats ◽  
Polyethylene Glycol 400 ◽  
Fischer 344 ◽  
Peg 400

scholarly journals Synthesis, Characterization and Solubility Determination of 6-Phenyl-pyridazin-3(2H)-one in Different Pharmaceutical Solvents

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3404 ◽  
Author(s):  
Faiyaz Shakeel ◽  
Mohd Imran ◽  
Nazrul Haq ◽  
Sultan Alshehri ◽  
Md. Khalid Anwer
Keyword(s):  
Isopropyl Alcohol ◽  
Molecular Level ◽  
Research Work ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 400 ◽  
X Ray ◽  
Peg 400 ◽  
Cardiovascular Agent ◽  
Solubility Determination

The current research work proposed the solubility data and solution thermodynamic properties of the cardiovascular agent 6-phenylpyridazin-3(2H)-one [PPD] in twelve pharmaceutical solvents at “T = 298.2 K to 318.2 K” and “p = 0.1 MPa”. The measured solubilities of PPD were regressed well with “van’t Hoff and Apelblat models”. The solid phases of pure and equilibrated PPD were characterized using differential scanning calorimetry and powder X-ray differactometry, and the results suggested no transformation of PPD into solvates/hydrates/polymorphs after equilibrium. The solubilities of PPD in a mole fraction at “T = 318.2 K” were noted at a maximum in dimethyl sulfoxide (DMSO, 4.73 × 10−1), followed by polyethylene glycol-400 (PEG-400, 4.12 × 10−1), Transcutol® (3.46 × 10−1), ethyl acetate (EA, 81 × 10−2), 2-butanol (2.18 × 10−2), 1-butanol (2.11 × 10−2), propylene glycol (PG, 1.50 × 10−2), isopropyl alcohol (IPA, 1.44 × 10−2), ethylene glycol (EG, 1.27 × 10−2), ethanol (8.22 × 10−3), methanol (5.18 × 10−3) and water (1.26 × 10−5). Similar tendencies were also noted at other studied temperatures. The results of the “apparent thermodynamic analysis” showed an endothermic and entropy-driven dissolution of PPD in all pharmaceutical solvents. The results of the activity coefficients suggested a maximum interaction at the molecular level in PPD-DMSO, PPD-PEG-400 and PPD-Transcutol, compared with other combination of the solute and solvents.

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