Perspectives of in vitro dissolution tests in establishing in vivo/in vitro correlations

A dissolution test for mianserin hydrochloride in coated tablets containing 30 mg was developed and validated using a fast ultraviolet spectrophotometric method. The appropriate conditions were determinate after testing sink conditions, agitation spped and dissolution medium. The sink conditions tested showed that mianserin hydrochloride was soluble in 0.01 and 0.1 M hydrochloric acid (HCl), acetate buffer pH 4.1 and 5.0 and phosphate buffer pH 6.8. Then, dissolution tests were performed to investigate the drug release in each medium. Optimal conditions to carry out the dissolution test were 900 mL 0.1 M HCl and USP apparatus 2 (paddle) at 50 rpm stirring speed. The quantification method was also adapted and validated. The UV method showed specificity, linearity, precision and accuracy. The in vitro dissolution test can be used to evaluate the drug release profile and the data was used as an aid to establish a possible correlation with in vivo data.

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Finding Use for Sorghum Bicolor Leaf Sheath in Coating Technology

Pharmaceutical Fronts ◽

10.1055/s-0041-1736235 ◽

2021 ◽

Author(s):

Johnson Ajeh Isaac ◽

Kayode Ilesanmi Fasuba

Keyword(s):

Sorghum Bicolor ◽

Aqueous Extract ◽

Scientific Information ◽

Leaf Sheath ◽

In Vitro Dissolution ◽

Dependent Manner ◽

Coating Agent ◽

Dissolution Tests

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.

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In Vitro Dissolution Behavior of Custom Made CaP Scaffolds for Bone Tissue Engineering

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.361-363.7 ◽

2007 ◽

Vol 361-363 ◽

pp. 7-10 ◽

Cited By ~ 3

Author(s):

Saartje Impens ◽

Roosmarijn Schelstraete ◽

Steven Mullens ◽

Ivo Thijs ◽

Jan Luyten ◽

...

Keyword(s):

Tissue Engineering ◽

Calcium Phosphate ◽

Degradation Rate ◽

In Vitro Dissolution ◽

Dissolution Behavior ◽

Degradation Behavior ◽

Dissolution Tests ◽

Custom Made

The degradation rate of custom made calcium phosphate scaffolds, designed for bone tissue engineering applications, influences the healing process of critical size bone defects. An optimal degradation rate exists at which the neo-formed bone replaces the CaP (calcium phosphate) scaffold [1]. Consequently investigating the complex degradation behavior (dissolution, reprecipitation, osteoclast activity) of custom made CaP structures gains interest. In this work different in vitro dissolution experiments were performed to study the degradation behavior of 4 by composition different calcium phosphates. Ideally these experiments should have a predictive power regarding the in vivo degradation behavior. In vitro dissolution tests still lack standardization. Therefore this study focuses on the influence of two dissolution constraints: (i) the material’s macrostructure (porous - dense), (ii) the regenerated fluid flow (bath shaking - perfusion). From 4 different CaP compositions porous structures and as a reference dense disks were produced, using the same starting powder and heat treatment. To compare the different dissolution tests, all data was normalized to the CaP surface area. Results show that besides the structural appearances of the CaP structures, also the design of the dissolution test influences the in vitro dissolution behavior. Moreover there is a need to take the morphology of the dissolved material into account. The CaP perfusion tests show dissolution dynamics that resemble the in vivo reality more closely than the shaking bath experiments.

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Significance of In-Vitro and In-Vivo Correlation in Drug Delivery System

Research in Pharmacy and Health Sciences ◽

10.32463/rphs.2018.v04i04.23 ◽

2018 ◽

Vol 4 (4) ◽

pp. 523-531

Author(s):

Hina Mumtaz ◽

Muhammad Asim Farooq ◽

Zainab Batool ◽

Anam Ahsan ◽

Ashikujaman Syed

Keyword(s):

Dosage Form ◽

Pharmaceutical Preparations ◽

Pharmacokinetic Profile ◽

In Vitro Dissolution ◽

Time Saving ◽

Pharmaceutical Dosage Form ◽

Short Period ◽

Form Development

The main purpose of development pharmaceutical dosage form is to find out the in vivo and in vitro behavior of dosage form. This challenge is overcome by implementation of in-vivo and in-vitro correlation. Application of this technique is economical and time saving in dosage form development. It shortens the period of development dosage form as well as improves product quality. IVIVC reduce the experimental study on human because IVIVC involves the in vivo relevant media utilization in vitro specifications. The key goal of IVIVC is to serve as alternate for in vivo bioavailability studies and serve as justification for bio waivers. IVIVC follows the specifications and relevant quality control parameters that lead to improvement in pharmaceutical dosage form development in short period of time. Recently in-vivo in-vitro correlation (IVIVC) has found application to predict the pharmacokinetic behaviour of pharmaceutical preparations. It has emerged as a reliable tool to find the mode of absorption of several dosage forms. It is used to correlate the in-vitro dissolution with in vivo pharmacokinetic profile. IVIVC made use to predict the bioavailability of the drug of particular dosage form. IVIVC is satisfactory for the therapeutic release profile specifications of the formulation. IVIVC model has capability to predict plasma drug concentration from in vitro dissolution media.

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Biopharmaceutical and Preclinical Studies of Zaleplon as Semisolid Dispersions with Self-emulsifying Lipid Surfactants for Oral Delivery

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2016.9.1.5 ◽

1970 ◽

Vol 9 (1) ◽

pp. 3102-3111

Author(s):

Narendar Dudhipala ◽

Arjun Narala ◽

Dinesh Suram ◽

Karthik Yadav Janga

Keyword(s):

Oral Delivery ◽

Molecular State ◽

In Vivo Studies ◽

In Vitro Dissolution ◽

Content Uniformity ◽

Phase Solubility ◽

Microscopic Studies ◽

Pure Drug

The objective of this present study is to develop a semisolid dispersion (SSD) of zaleplon with the aid of self-emulsifying lipid based amphiphilic carriers (TPGS E or Gelucire 44/14) addressing the poor solubility of this drug. A linear relationship between the solubility of drug with respect to increase in the concentration of lipid surfactant in aqueous medium resulting in AL type phase diagram was observed from phase solubility studies. Fusion method was employed to obtain semisolid dispersions (SSD) of zaleplon which showed high content uniformity of drug. The absence of chemical interactions between the pure drug, excipients and formulations were conferred by Fourier transmission infrared spectroscopic examinations. The photographic images from polarized optical microscopic studies revealed the change in crystalline form of drug to amorphous or molecular state. The superior dissolution parameters of zaleplon from SSD over pure crystalline drug interpreted from in vitro dissolution studies envisage the ability of these lipid surfactants as solubility enhancers. Further, the caliber of TPGS E or Gelucire 44/14 in encouraging the GI absorption of drug was evident with the higher human effective permeability coefficient and fraction oral dose of drug absorbed from SSD in situ intestinal permeation study. In conclusion, in vivo studies in Wister rats demonstrated an improvement in the oral bioavailability of zaleplon from SSD over control pure drug suspension suggesting the competence of Gelucire 44/14 and TPGS E as conscientious carriers to augment the dissolution rate limited bioavailability of this active

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Formulation and Evaluation of Nanosuspension of Simvastatin

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.2.9 ◽

2015 ◽

Vol 8 (2) ◽

pp. 2858-2873

Author(s):

Rupali L. Shid ◽

Shashikant N. Dhole ◽

Nilesh Kulkarni ◽

Santosh L Shid

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Factorial Design ◽

Dissolution Rate ◽

In Vitro Dissolution ◽

Total Drug ◽

23 Factorial Design ◽

Rate Of Dissolution

Poor water solubility and slow dissolution rate are issues for the majority of upcoming and existing biologically active compounds. Simvastatin is poorly water-soluble drug and its bioavailability is very low from its crystalline form. The purpose of this study wasto increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspension by emulsification solvent diffusion method at laboratory scale. Prepared nanosus-pension was evaluated for its particle size and in vitro dissolution study and characterized by zeta potential,differential scanning calorimetry (DSC) and X-Ray diffractometry (XRD), motic digital microscopy, entrapment efficiency, total drug content, saturated solubility study and in vivo study. A 23 factorial design was employed to study the effect of independent variables, amount of SLS (X1), amount of PVPK-30 (X2) and poloxamer-188 (X3) and dependent variables are total drug content and polydispersity Index. The obtained results showed that particle size (nm) and rate of dissolution has been improved when nanosuspension prepared with the higherconcentration of PVPK-30 with the higher concentration of PVP K-30 and Poloxamer-188 and lower concentration of SLS. The particle size and zeta potential of optimized formulation was found to be 258.3 nm and 23.43. The rate of dissolution of the optimized nanosuspension was enhanced (90% in 60min), relative to plain simvastatin (21% in 60 min), mainly due to the formation of nanosized particles. These results indicate the suitability of 23 factorial design for preparation of simvastatin loaded nano-suspension significantly improved in vitro dissolution rate and thus possibly enhance fast onset of therapeutic drug effect. In vivo study shows increase in bioavailability in nanosuspension formulation than the plain simvastatin drug.

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