Disintegration Rate and Properties of Active Pharmaceutical Ingredient Particles as Determined from the Dissolution Time Profile of a Pharmaceutical Formulation: An Inverse Problem

2014 ◽  
Vol 103 (2) ◽  
pp. 456-464 ◽  
Author(s):  
Stefan Horkovics-Kovats
Keyword(s):  
Inverse Problem ◽  
Active Pharmaceutical Ingredient ◽  
Time Profile ◽  
Pharmaceutical Formulation ◽  
Dissolution Time ◽  
Disintegration Rate

Pharmacokinetics and bioequivalence of generic etoricoxib in healthy volunteers

2021 ◽  
Vol 10 (3) ◽  
pp. 113-118
Author(s):  
Nishalini Harikrishnan ◽  
Ka-Liong Tan ◽  
Kar Ming Yee ◽  
Alia Shaari Ahmad Shukri ◽  
Nalla Ramana Reddy ◽  
...  
Keyword(s):  
Compartmental Analysis ◽  
Bioequivalence Study ◽  
Active Pharmaceutical Ingredient ◽  
Pharmacokinetic Profile ◽  
Time Profile ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Reference Drug ◽  
Test Formulation ◽  
R Ratio

Introduction/Study Objectives: A bioequivalence study was performed to compare the pharmacological profile of innovator etoricoxib (ETO) with a newly developed generic ETO, both in a 120 mg tablet formulation. A dissolution study was conducted to optimize the formulation process before evaluating physical changes in the active pharmaceutical ingredient and the formulated product. Methods: This was a randomized, open-label, balanced, two-treatment, two-period, two-sequence, single-dose, two-way crossover, truncated bioequivalence study involving a washout period of ten days. A total of 26 healthy male volunteers were recruited. The pharmacokinetic profile of the test formulation was compared with the reference formulation. Results/Discussion: The pharmacokinetic parameters of ETO were calculated based on the plasma drug concentration-time profile using non-compartmental analysis to determine its safety profile and tolerability. The Test/Reference (T/R) ratio of ETO was 104.36% (90% confidence interval (CI): 98.30%–110.80%) for area under curve (AUC)0-72 while the T/R ratio of maximum concentration (Cmax) was 101.39% (92.15%–111.56%). The 90% CI of the Cmax and AUC0-72 of ETO were within acceptable bioequivalence limits of 80%–125%. All values were within the predetermined limits of the Association of Southeast Asian Nation (ASEAN) bioequivalence guidelines. Conclusion: The test formulation was found to be bioequivalent with respect to the reference drug, according to ASEAN bioequivalence guidelines.

Verification of the mixing processes of the active pharmaceutical ingredient, excipient and lubricant in a pharmaceutical formulation using a resonant acoustic mixing technology

RSC Advances ◽  
2016 ◽  
Vol 6 (90) ◽  
pp. 87049-87057 ◽  
Author(s):  
Ryoma Tanaka ◽  
Naoyuki Takahashi ◽  
Yasuaki Nakamura ◽  
Yusuke Hattori ◽  
Kazuhide Ashizawa ◽  
...  
Keyword(s):  
Chemical Stability ◽  
Pharmaceutical Formulations ◽  
Active Pharmaceutical Ingredient ◽  
Pharmaceutical Formulation ◽  
Pharmaceutical Manufacturing ◽  
High Quality ◽  
Mixing Processes ◽  
Resonant Acoustic Mixing

Mixing processes are important for making high-quality pharmaceutical formulations and are related to dissolution and chemical stability in pharmaceutical manufacturing.

scholarly journals Solid State Stability and Kinetics of Degradation for Candesartan—Pure Compound and Pharmaceutical Formulation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 86
Author(s):  
Valentina Buda ◽  
Bianca Baul ◽  
Minodora Andor ◽  
Dana Emilia Man ◽  
Adriana Ledeţi ◽  
...  
Keyword(s):  
Candesartan Cilexetil ◽  
Active Pharmaceutical Ingredient ◽  
Pharmaceutical Formulation ◽  
Attenuated Total Reflection ◽  
Chemical Degradation ◽  
Npk Method ◽  
Ambient Conditions ◽  
Kinetics Of Degradation ◽  
The Impact ◽  
Kinetics Of

The aim of this work was to assess the impact of an excipient in a pharmaceutical formulation containing candesartan cilexetil over the decomposition of the active pharmaceutical ingredient and to comparatively investigate the kinetics of degradation during thermolysis in an oxidative atmosphere under controlled thermal stress. To achieve this, the samples were chosen as follows: pure candesartan cilexetil and a commercial tablet of 32 mg strength. As a first investigational tool, Universal attenuated total reflection Fourier transform infrared (UATR-FTIR) spectroscopy was chosen in order to confirm the purity and identity of the samples, as well as to check if any interactions took place in the tablet between candesartan cilexetil and excipients under ambient conditions. Later on, samples were investigated by thermal analysis, and the elucidation of the decomposition mechanism was achieved solely after performing an in-depth kinetic study, namely the use of the modified non-parametric kinetics (NPK) method, since other kinetic methods (American Society for Testing and Materials—ASTM E698, Friedman and Flynn–Wall–Ozawa) led to inadvertencies. The NPK method suggested that candesartan cilexetil and the tablet were degraded by the contribution of two steps, the main being represented by chemical degradation and the secondary being a physical transformation. The excipients chosen in the formulation seemed to have a stabilizing effect on the decomposition of the candesartan cilexetil that was incorporated into the tablet, relative to pure active pharmaceutical ingredient (API), since the apparent activation energy for the decomposition of the tablet was 192.5 kJ/mol, in comparison to 154.5 kJ/mol for the pure API.

AN INVERSE PROBLEM IN THE DYNAMICAL REATOR THEORY

1982 ◽  
Vol 2 (1) ◽  
pp. 9-16 ◽  
Author(s):  
Dexing Feng ◽  
Guangtian Zhu
Keyword(s):  
Inverse Problem

FORMULATION AND DEVELOPMENT OF FAST DISSOLVING TABLET OF METOCLOPRAMIDE: AN ANTI-EMETIC DRUG

2019 ◽  
Vol 8 (6) ◽  
Author(s):  
Avilash Carpenter ◽  
M.K. Gupta ◽  
Neetesh Kumar Jain ◽  
Urvashi Sharma ◽  
Rahul Sisodiya
Keyword(s):  
Mechanical Strength ◽  
Standard Procedure ◽  
Flow Property ◽  
Storage Conditions ◽  
Angle Of Repose ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Powder Blend ◽  
Standard Curve ◽  
The Stability

Aim: The main of the study is to formulate and develop orally disintegrating fast dissolving tablet of Metoclopramide hydrochloride. Material & Methods: Before formulation and development of selected drug, the standard curve in buffer was prepared and absorbance at selected maxima was taken. Then two different disintegrating agents were selected and drug was mixed with disintegrating agents in different ratio. Various Preformulation parameters and evaluation of tablet i.e. disintegration time, dissolution time, friability, hardness, thickness were measured by standard procedure. Result & Discussion: The angle of repose for all the batches prepared. The values were found to be in the range of 30.46 to 36.45, which indicates good flow property for the powder blend according to the USP. The bulk density and tapped density for all the batches varied from 0.49 to 0.54 g/mL and 0.66 to 0.73, respectively. Carr’s index values were found to be in the range of 23.33 to 25.88, which is satisfactory for the powders as well as implies that the blends have good compressibility. Hausner ratio values obtained were in the range of 1.22 to 1.36, which shows a passable flow property for the powder blend based on the USP. The results for tablet thickness and height for all batches was found to range from 4.45 to 4.72 mm and 3.67 to 3.69 mm, respectively. Hardness or breaking force of tablets for all batches was found to range from 32.8 to 36.2 N. Tablet formulations must show good mechanical strength with sufficient hardness in order to handle shipping and transportation. Friability values for all the formulations were found to be in the range of 0.22 % to 0.30 %. Conclusion: Orally disintegrating tablets were compressed in order to have sufficient mechanical strength and integrity to withstand handling, shipping and transportation. The formulation was shown to have a rapid disintegration time that complied with the USP (less than one minute). The data obtained from the stability studies indicated that the orally disintegrating mini-tablets of MTH were stable under different environmental storage conditions. Keywords: Formulation & Development, Fast Dissolving Tablet, Metoclopramide, Anti-Emetic Drug, Oral Disintegrating Tablet

Sign in / Sign up

Export Citation Format

Share Document