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

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.

scholarly journals Efficient validated method of HPLC to determine amlodipine in combinated dosage form containing amlodipine, enalapril and bisoprolol and in vitro dissolution studies with in vitro/ in vivo correlation

Pharmacia ◽  
2020 ◽  
Vol 67 (2) ◽  
pp. 55-61
Author(s):  
Liliya Logoyda
Keyword(s):  
Dosage Form ◽  
Hplc Method ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Buffer Solution ◽  
Pharmaceutical Dosage Form ◽  
Dissolution Studies ◽  
Ultraviolet Detector

Aim. A rapid and reproducible HPLC method has been developed for the determination of amlodipine in experimental combined dosage forms containing amlodipine, bisoprolol and enalapril and for drug dissolution studies. Materials and methods. The separation was done using a column Phenomenex Polar Synergi, 5 μm, 4.6×50 mm and a mobile phase of methanol:phosphate buffer solution (65:35, v/v), flow-rate of 1.0 mL/min. The injection volume was 100 μL and the ultraviolet detector was set at 240 nm. Results. The method was validated as per ICH guidelines. Under these conditions, amlodipine was eluted at 1.89 min. Total run time was shorter than 2.5 min. The linearity of the method had a good correlation with concentration and peak area. The correlation coefficient of amlodipine was found to be not less than 0.9991, which indicates good linear relationship over concentration range 0.625 mg/mL–5.000 mg/mL (1.250 mg/mL–5.000 mg/mL at pH 4.5). The % RSD values in intra-day and inter-day precision study were found to be less than 0.267 for amlodipine, which indicate method was precise. Hence, the present developed method was said to be suitable for the analysis of drugs in their pharmaceutical dosage form. Also, in vitro dissolution of amlodipine containing tablets were performed to validate the suitability of the proposed method. The dissolution pattern complies with the FDA standards, indicating suitability of the proposed method for the dissolution study of amlodipine. It will allow conducting comparative studies in vitro to confirm the equivalence of tablets containing amlodipine. Conclusion. A simple and sensetive HPLC method was developed for the estimation of amlodipine in tablets containing amlodipine, enalapril and bisoprolol. The proposed method was applied successfully for quality control assay of amlodipine in experimental tablets and in vitro dissolution studies. In vitro / in vivo correlation of amlodipine has been conducted.

scholarly journals OPTIMIZATION OF STATISTICALLY DESIGNED ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH GLUTAMATE AS A NOVEL SUPERDISINTEGRANT

2019 ◽  
pp. 77-88
Author(s):  
R. SANTOSH KUMAR ◽  
SAHITHI MUDILI
Keyword(s):  
Drug Release ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
In Vitro Dissolution ◽  
Pharmacokinetic Studies ◽  
Disintegration Time ◽  
Short Period ◽  
Dissolution Efficiency

Objective: To optimize aceclofenac fast dissolving tablets employing starch glutamate as novel superdisintegrant by 23factorial design to improve bioavailability and enhance patient compliance. Methods: Starch glutamate was prepared by the esterification process. Starch glutamate physical and micromeritics properties had been evaluated and the prepared starch glutamate was used as a superdisintegrant for the formulation of the fast dissolving tablets of aceclofenac by direct compression method and optimized by employing 23factorial design. The prepared aceclofenac fast dissolving tablets were evaluated for post compression parameters as well as in vitro and in vivo release characteristics. Optimized formulation stability studies were performed at accelerated conditions for 6 mo as per ICH and WHO guidelines. Results: The prepared starch glutamate was amorphous, insoluble in aqueous and organic solvents were tested. Fast dissolving tablets of aceclofenac were formulated by employing starch glutamate as a superdisintegrant showed good tablet properties and showed an increased dissolution efficiency of the drug. Among all the formulations (F1 to F8), the formulation F8 containing 5% concentration of starch glutamate, croscarmellose sodium and, crospovidone as a superdisintegrants showed 99.7±0.15% of drug release within 5 min. Whereas the formulation F2 containing 5% concentration of starch glutamate, drug release characters were comparable to the formulation F8. Optimized formulation F2 attained peak plasma concentration within a short period and showed increased relative bioavailability of the drug. Conclusion: From the physical properties, disintegration time, in vitro dissolution studies and pharmacokinetic studies, it was concluded that fast dissolving tablets of aceclofenac tablets formulated by employing starch glutamate as a superdisintegrant enhanced the dissolution efficiency and improved the bioavailability of the drug as compared to the pure drug and stable.

scholarly journals METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS ESTIMATION OF LAMIVUDINE, DOLUTEGRAVIR AND TENOFOVIR DISOPROXIL FUMARATE IN BULK AND PHARMACEUTICAL DOSAGE FORM USING RP-HPLC AND ITS APPLICATION TO IN-VITRO DISSOLUTION STUDY

2021 ◽  
Vol 10 (4) ◽  
pp. 3202-3207
Author(s):  
K. Nihila
Keyword(s):  
Tenofovir Disoproxil Fumarate ◽  
Dosage Form ◽  
Method Development ◽  
In Vitro Dissolution ◽  
Simultaneous Estimation ◽  
Pharmaceutical Dosage Form ◽  
Dissolution Study ◽  
Rp Hplc ◽  
Tablet Dosage

A simple, rapid, and economical method has been developed for the simultaneous estimation of the latest FDA approved antiviral drug combination, Dolutegravir, Lamivudine, and tenofovir disoproxil fumarate in tablet dosage form using Shimadzu LC-20 AT HPLC with a Phenomenex Luna column compartment., the method was developed using HPLC graded methanol with o-phosphoric acid as a mobile phase and successfully validated the developed method as per the ICH guidelines. The method was found to be linear, accurate, precise, robust, and rugged. The limit of detection and the limit of quantification was found to be 2.6μg/ml and 8.18μg/ml for Dolutegravir, 14.63 μg/ml and 44.35 μg/ml for Lamivudine and 16.43 μg/ml and 49.81 μg/ml for tenofovir disoproxil fumarate respectively. The retention time was found to be 3.0, 2.3 and 2.7 min for Dolutegravir, Lamivudine and tenofovir disoproxil fumarate respectively. All of assessed parameters complied with the acceptance criteria hence indicated the usefulness of the RP-HPLC method for the determination of assay and in-vitro dissolution study for tablet dosage form which contains lamivudine, tenofovir disoproxil fumarate, and dolutegravir active substances. Hence the method can be applied for routine quality control of the drugs.

Acceleration of in vitro dissolution studies of sustained release dosage form of theophylline and in vitro–in vivo evaluations in terms of correlations

2011 ◽  
Vol 36 (4) ◽  
pp. 243-248 ◽  
Author(s):  
Gökhan Ertan ◽  
Ercüment Karasulu ◽  
Işık Özgüney ◽  
Yeşim Karasulu ◽  
Şebnem Apaydın ◽  
...  
Keyword(s):  
Sustained Release ◽  
Dosage Form ◽  
In Vitro Dissolution ◽  
Dissolution Studies

scholarly journals Multivariate optimization of liquid chromatographic conditions for determination of dapagliflozin and saxagliptin, application to an in vitro dissolution and stability studies

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Sunitha Gurrala ◽  
Shiva Raj ◽  
C. V. S. Subrahmanyam ◽  
Panikumar D. Anumolu
Keyword(s):  
Flow Rate ◽  
Mobile Phase ◽  
Dosage Form ◽  
Hplc Method ◽  
In Vitro Dissolution ◽  
Simultaneous Estimation ◽  
Stability Studies ◽  
Experimental Conditions ◽  
Pharmaceutical Dosage Form

Abstract Background Analytical quality by design driven HPLC method has been optimized for simultaneous estimation of dapagliflozin and saxagliptin in pharmaceutical dosage form. Response surface methodology was employed for optimization of experimental conditions using three factors such as organic phase (%), pH of aqueous phase, and flow rate of mobile phase. Results Virtuous separation of analytes was achieved with mobile phase consisted of acetonitrile: phosphate buffer, pH 5.8 (26:74% v/v) with flow rate 0.96 mL/min using SPOLAR C18 column (250 × 4.6 mm, 5 μ) with run time 6 min and UV detection at 236 nm. Retention time for dapagliflozin and saxagliptin were found to be 3.5 and 5.0 min, respectively. Method was validated as per ICH guidelines. The plot between peak area vs concentration for dapagliflozin and saxagliptin were rectilinear in the range of 0.2-300 μg/mL and 0.1-150 μg/mL respectively with detection and quantification limits were 0.061 and 0.18 μg/mL for dapagliflozin and 0.014 and 0.043 μg/mL for saxagliptin, respectively. Conclusion The proposed method was exploited for assay, in vitro dissolution, and stability studies of target drugs in marketed dosage form.

scholarly journals Luminal Fluid Motion Inside an In Vitro Dissolution Model of the Human Ascending Colon Assessed Using Magnetic Resonance Imaging

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1545
Author(s):  
Connor O’Farrell ◽  
Caroline L. Hoad ◽  
Konstantinos Stamatopoulos ◽  
Luca Marciani ◽  
Sarah Sulaiman ◽  
...  
Keyword(s):  
Magnetic Resonance Imaging ◽  
Magnetic Resonance ◽  
Dosage Form ◽  
In Vitro Dissolution ◽  
Ascending Colon ◽  
Resonance Imaging ◽  
Dissolution Model ◽  
Luminal Flow

Knowledge of luminal flow inside the human colon remains elusive, despite its importance for the design of new colon-targeted drug delivery systems and physiologically relevant in silico models of dissolution mechanics within the colon. This study uses magnetic resonance imaging (MRI) techniques to visualise, measure and differentiate between different motility patterns within an anatomically representative in vitro dissolution model of the human ascending colon: the dynamic colon model (DCM). The segmented architecture and peristalsis-like contractile activity of the DCM generated flow profiles that were distinct from compendial dissolution apparatuses. MRI enabled different motility patterns to be classified by the degree of mixing-related motion using a new tagging method. Different media viscosities could also be differentiated, which is important for an understanding of colonic pathophysiology, the conditions that a colon-targeted dosage form may be subjected to and the effectiveness of treatments. The tagged MRI data showed that the DCM effectively mimicked wall motion, luminal flow patterns and the velocities of the contents of the human ascending colon. Accurate reproduction of in vivo hydrodynamics is an essential capability for a biorelevant mechanical model of the colon to make it suitable for in vitro data generation for in vitro in vivo evaluation (IVIVE) or in vitro in vivo correlation (IVIVC). This work illustrates how the DCM provides new insight into how motion of the colonic walls may control luminal hydrodynamics, driving erosion of a dosage form and subsequent drug release, compared to traditional pharmacopeial methods.

scholarly journals Solubility enhancement of glimperide: Development of solid dispersion by solvent melt method, characterization and dosage form development

2018 ◽  
Author(s):  
Suchitra Kaushik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Accelerated Stability ◽  
Form Development

The aim of the present work was to develop immediate release dosage form of the solid dispersion of glimperide (GLIM) for potential enhancement in the bioavailability. The solid dispersions of GLIM were prepared with PEG6000, PVP K30 and Poloxamer 188, in 1:1, 1:3 and 1:5 %w/w ratio by using solvent wetting and solvent melt method. The in vitro dissolution parameters (%DE10min, %DE30min, %DE60min, T50% and DP30) were used to select the optimized solid dispersion that was characterized by IR, PXRD, DSC and SEM. The optimized solid dispersion of GLIM (GSDSM3) was used as drug component for immediate release (IR) tablets that were evaluated for physical and pharmacopoeial parameters. The in vitro drug release studies identified G4 as the optimized tablet with a cumulative drug release (CDR) of 99.34% in 30 min in phosphate buffer, pH 7.4. The CDR was higher than the marketed tablet (91.15%, Amaryl®, Sanofiaventis), However, the f1 and f2 were 10.6 and 52 respectively, which confirmed similarity of the dissolution profile(s). Accelerated stability studies confirmed stability up to 6 months at 40°C/75% condition in the HDPE bottle pack.

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