Formulation and Pharmacokinetic Evaluation of Polymeric Dispersions Containing Valsartan

Chella, Naveen; Daravath, Bhaskar; Kumar, Dinesh; Tadikonda, Rama Rao

doi:10.1007/s13318-015-0290-5

Cited by 9 publications

(6 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Another publication evaluated the dissolution parameters of Eudragit E 100 based ASDs at pH 1. In this case, the angiotensin II receptor antagonist agent valsartan was released over 2 h in a gradual manner . The discrepancy in the data might be explained by the dissimilar design of these experiments: sink versus nonsink conditions for valsartan and indomethacin, respectively.…”

Section: Importance Of Polymers In Amorphous Solid Dispersionsmentioning

confidence: 91%

Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms

2016

View full text Add to dashboard Cite

Over the last few decades, polymers have been extensively used as pharmaceutical excipients in drug delivery systems. Pharmaceutical polymers evolved from being simply used as gelatin shells comprising capsule to offering great formulation advantages including enabling controlled/slow release and specific targeting of drugs to the site(s) of action (the "magic bullets" concept), hence hold a significant clinical promise. Oral administration of solid dosage forms (e.g., tablets and capsules) is the most common and convenient route of drug administration. When formulating challenging molecules into solid oral dosage forms, polymeric pharmaceutical excipients permit masking undesired physicochemical properties of drugs and consequently, altering their pharmacokinetic profiles to improve the therapeutic effect. As a result, the number of synthetic and natural polymers available commercially as pharmaceutical excipients has increased dramatically, offering potential solutions to various difficulties. For instance, the different polymers may allow increased solubility, swellability, viscosity, biodegradability, advanced coatings, pH dependency, mucodhesion, and inhibition of crystallization. The aim of this article is to provide a wide angle prospect of the different uses of pharmaceutical polymers in solid oral dosage forms. The various types of polymeric excipients are presented, and their distinctive role in oral drug delivery is emphasized. The comprehensive know-how provided in this article may allow scientists to use these polymeric excipients rationally, to fully exploit their different features and potential influence on drug delivery, with the overall aim of making better drug products.

show abstract

Section: Importance Of Polymers In Amorphous Solid Dispersionsmentioning

confidence: 91%

Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms

2016

View full text Add to dashboard Cite

show abstract

“…Cumulative % drug release in 20 min (Q 20 ), mean dissolution time (MDT),dissolution efficiency (%DE) and relative dissolution rate (RDR) were determined to compare the optimized SDs with marketed tablets and conventional formulation of FPN as discussed in our previous article (Chella et al, 2016).…”

Section: Dissolution Data Treatmentmentioning

confidence: 99%

Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

Daravath

Chella

Vemula

et al. 2018

Braz. J. Pharm. Sci.

Self Cite

View full text Add to dashboard Cite

The intent of the current work is to study the effect of polyethylene glycol 8000 and polyethylene glycol 10000 as hydrophilic carriers on dissolution behaviour of flurbiprofen. In the present study, solvent evaporation method was used to prepare flurbiprofen solid dispersions and evaluated for physicochemical properties, drug-carrier compatibility studies and dissolution behaviour of drug. Solubility studies showed more solubility in higher pH values and formulations SD4 and SD8 were selected to prepare the fast dissolving tablets. FTIR and DSC study showed no interaction and drug was dispersed molecularly in hydrophilic carrier. XRD studies revealed that there was change in the crystallinity of the drug. The results of In vitro studies showed SD8 formulation confer significant improvement (p<0.05) in drug release, Q 20 was 99.08±1.35% compared to conventional and marketed tablets (47.31±0.74% and 56.86±1.91%). The mean dissolution time (MDT) was reduced to 8.79 min compared to conventional and marketed tablets (25.76 and 22.22 min.) indicating faster drug release. The DE (% dissolution efficiency) was increased by 2.5 folds (61.63%) compared to conventional tablets (23.71%). From the results, it is evident that polyethylene glycol solid dispersions in less carrier ratio may enhance the solubility and there by improve the dissolution rate of flurbiprofen.

show abstract

“… From t = 0.5 h to 2 h, absorption would be faster than dissolution, which could correspond with an absorption window, similarly to that observed for valsartan with similar physicochemical characteristics. [ 38 , 39 ] In that period, dissolution is the limiting factor. These in vivo times correspond to the in vitro times 0.150 h and 1.100 h that, as can be observed on Figure 5 (upper plot), correspond to the period in which dissolution rate showed the highest differences between reference and test products.…”

Section: Discussionmentioning

confidence: 99%

Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool

et al. 2020

View full text Add to dashboard Cite

The main objective of this investigation was to develop an in vitro–in vivo correlation (IVIVC) for immediate release candesartan cilexetil formulations by designing an in vitro dissolution test to be used as development tool. The IVIVC could be used to reduce failures in future bioequivalence studies. Data from two bioequivalence studies were scaled and combined to obtain the dataset for the IVIVC. Two-step and one-step approaches were used to develop the IVIVC. Experimental solubility and permeability data confirmed candesartan cilexetil. Biopharmaceutic Classification System (BCS) class II candesartan average plasma profiles were deconvoluted by the Loo-Riegelman method to obtain the oral fractions absorbed. Fractions dissolved were obtained in several conditions in USP II and IV apparatus and the results were compared calculating the f2 similarity factor. Levy plot was constructed to estimate the time scaling factor and to make both processes, dissolution and absorption, superimposable. The in vitro dissolution experiment that reflected more accurately the in vivo behavior of the products of candesartan cilexetil employed the USP IV apparatus and a three-step pH buffer change, from 1.2 to 4.5 and 6.8, with 0.2% of Tween 20. This new model was able to predict the in vivo differences in dissolution and it could be used as a risk-analysis tool for formulation selection in future bioequivalence trials.

show abstract

Formulation and Pharmacokinetic Evaluation of Polymeric Dispersions Containing Valsartan

Abstract: Eudragit E 100 can be used to improve the dissolution of drugs that show low solubility at lower pH and thereby enhancing the bioavailability.

Cited by 9 publications

References 31 publications

Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms

Applications of Polymers as Pharmaceutical Excipients in Solid Oral Dosage Forms

Solubility and dissolution enhancement of flurbiprofen by solid dispersion using hydrophilic carriers

Candesartan Cilexetil In Vitro–In Vivo Correlation: Predictive Dissolution as a Development Tool

Contact Info

Product

Resources

About