Mathematical prediction of pharmacokinetic parameters-an in-vitro approach for investigating pharmaceutical products for IVIVC

Rastogi, Vaibhav; Yadav, Pragya; Lal, Niharika; Rastogi, Pallavi; Singh, B.K.; Verma, Navneet Kumar; Verma, Anurag

doi:10.1016/j.fjps.2018.03.001

Cited by 15 publications

(12 citation statements)

References 15 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…where F and V d are bioavailability and volume of distribution and % PE is percent predicted error. 7…”

Section: Mathematical Expressionmentioning

confidence: 99%

“…A key aspect of the development of a product is to find in vitro characteristics of potential formulation that reflect in vivo performance. 7 Dissolution test determines the rate and extent of drug absorption and subsequent therapeutic outcome. In vitro dissolution is conducted to predict assumption regarding in vivo behavior of drugs.…”

Section: In Vitro-in Vivo Correlation Studymentioning

confidence: 99%

“…It is well known that the process of getting drug profiles from dissolution results is referred to as convolution, while extracting dissolution profile from a blood profile is called deconvolution. 7 The convolution technique, though not a very popular in vitro-in vivo correlation (IVIVC) method, is preferred over the deconvolution method, because it does not require human study, and there is no need to define experimental conditions of an appropriate dissolution test for multiple products with different in vivo release properties. 8 Then, we utilized a mathematical concept, and the convolution IVIVC technique to reveal the relationship between drug release extent of the coated tablets and their amount of drug absorbed.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Finding Use for Sorghum Bicolor Leaf Sheath in Coating Technology

Isaac

Fasuba

2021

Pharmaceutical Fronts

View full text Add to dashboard Cite

This study aimed to investigate the potential use of aqueous extract of Sorghum bicolor leaf sheath (SBLS) as a coating agent for paracetamol tablets. The mechanical properties of the coated tablets were assessed using crushing strength and friability test, while the release properties of the tablet were evaluated using disintegration and dissolution tests. The physicochemical properties of the coated tablets did not show any striking differences when compared with the uncoated tablet as par compendium specifications, which formed the basis for performing further in vitro dissolution study. Our data showed that SBLS enhanced the hardness and friability of the tablets in a dose-dependent manner. Tablets coated with 3, 5, and 7.5% of SBLS disintegrated in 8.13, 6.25, and 4.13 minutes, respectively, while the uncoated tablet disintegrated in 0.7 minutes. Furthermore, 3, 5, and 7.5% of SBLS-coated tablets exhibited slower release of their active ingredient (releasing 21, 16, and 17%, respectively) than that of the uncoated tablet (releasing 40%) in 5 minutes. Besides, comparison between the dissolution profiles was successfully achieved using difference factor (f1) and similarity factor (f2). The apparent dissimilarity between our coated tablets and the uncoated one led to further study of convolution in vitro–in vivo correlation, with the aim to obtain data that converted into mathematical prediction of in vivo data. For all batches, the percent predictable errors of C max and T max were within the acceptable limit of no more than 10%. In summary, SBLS aqueous extract is a potential and protective coat agent for paracetamol tablets. The in vitro established dissolution of the coated tablets provided scientific information for the prediction of the in vivo plasma drug profile.

show abstract

“…where F and V d are bioavailability and volume of distribution and % PE is percent predicted error. 7…”

Section: Mathematical Expressionmentioning

confidence: 99%

Section: In Vitro-in Vivo Correlation Studymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Finding Use for Sorghum Bicolor Leaf Sheath in Coating Technology

Isaac

Fasuba

2021

Pharmaceutical Fronts

View full text Add to dashboard Cite

show abstract

“…In order to avoid animal experiments at this initial stage of development, plasma drug concentration profiles after intramuscular administration of the PLGA MS were predicted by using the convolution technique, a method used for predicting in vivo pharmacokinetic behavior and in vitro-in vivo correlation, as described previously [41,42]. We assumed 1.58 mg PLGA MS (corresponding to 0.25 mg donepezil) for intramuscular administration into the human body.…”

Section: Prediction Of Plasma Drug Concentration Profiles By Using Comentioning

confidence: 99%

“…As for the initial burst release, we could infer that the drug loaded in the pore structure of the PLGA MS with high concentrations might be initially released from the partly thinly coated or partly non-coated pore space of the calcium alginate membrane. Figure 7 shows the predicted plasma concentration-time profiles obtained by using the convolution method [41,42], on the basis of the in vitro drug release data and the pharmacokinetic parameters established from previous clinical studies [10,44,45]. The peak concentration (C max ) was predicted to be reached within the first day of injection for all the porous (F6) and pore-closed PLGA formulations (F7-9) due to the initial burst release of donepezil, after which the predicted drug concentrations declined gradually.…”

Section: In Vitro Releasementioning

confidence: 99%

PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride

et al. 2020

View full text Add to dashboard Cite

As the main symptom of Alzheimer’s disease-related dementia is memory loss, patient compliance for donepezil hydrochloride (donepezil), administered as once-daily oral formulations, is poor. Thus, we aimed to design poly(lactic-co-glycolic acid) (PLGA) microspheres (MS) with alginate-coated large pores as an injectable depot of donepezil exhibiting sustained release over 2–3 weeks. The PLGA MS with large pores could provide large space for loading drugs with high loading capacity, and thereby sufficient amounts of drugs were considered to be delivered with minimal use of PLGA MS being injected. However, initial burst release of donepezil from the porous PLGA MS was observed. To reduce this initial burst release, the surface pores were closed with calcium alginate coating using a spray-ionotropic gelation method. The final pore-closed PLGA MS showed in vitro sustained release for approximately 3 weeks, and the initial burst release was remarkably decreased by the calcium alginate coating. In the prediction of plasma drug concentration profiles using convolution method, the mean residence time of the pore-closed PLGA MS was 2.7-fold longer than that of the porous PLGA MS. Therefore, our results reveal that our pore-closed PLGA MS formulation is a promising candidate for the treatment of dementia with high patient compliance.

show abstract

Dissolution

Batchelor

Butler

2021

Biopharmaceutics

View full text Add to dashboard Cite

Mathematical prediction of pharmacokinetic parameters-an in-vitro approach for investigating pharmaceutical products for IVIVC

Cited by 15 publications

References 15 publications

Finding Use for Sorghum Bicolor Leaf Sheath in Coating Technology

Finding Use for Sorghum Bicolor Leaf Sheath in Coating Technology

PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride

Dissolution

Contact Info

Product

Resources

About