scholarly journals Design of Oral Sustained-Release Pellets by Modeling and Simulation Approach to Improve Compliance for Repurposing Sobrerol

Pharmaceutics ◽  
2022 ◽  
Vol 14 (1) ◽  
pp. 167
Author(s):  
Chu-Hsun Lu ◽  
Yu-Feng Huang ◽  
I-Ming Chu

Sobrerol, an oral mucolytic agent, in a recent study showed promise for treating multiple sclerosis. A human equivalent dose of 486 mg of sobrerol administered thrice daily (i.e., 1459 mg of daily dose) demonstrated the highest therapeutic efficacy for repurposing use, which also points out the poor compliance of administration. In this study, oral sustained-release pellets of sobrerol were successfully developed with evaluated manufacturing conditions and drug release kinetics. For design of the target drug product, we used a modeling and simulation approach to establish a predictive model of oral pharmacokinetic profile, by exploring the characteristics and correlations corresponding to the pharmacokinetics and pharmacodynamics of sobrerol, such as absorption lag time (0.18 h), time-scaling in vitro–in vivo correlation (tin-vitro = 0.494 tin-vivo − 0.0904), gastrointestinal transit time (8 h), minimum effective concentration (1.61 μg/mL), and duration of action (12.8 h). Results showed that the frequency of administration and the daily dose remarkably reduced by 33.3% (i.e., from thrice to twice daily) and 22.8%, respectively, which indicates that this prototype approach can be adopted for rapidly developing a modified-release dosage form of sobrerol, with improvement of compliance of administration and therapeutic efficacy.

2013 ◽  
Vol 2 (2) ◽  
pp. 70-79
Author(s):  
Umme Rahela ◽  
Md Mizanur Rahman Moghal ◽  
Sayed Masudur Rahman Dewan ◽  
Mohammad Nurul Amin

The present study was designed to evaluate the polymeric effect of METHOCEL K15MCR on the sustained release drug product of Carvedilol. Carvedilol matrix tablets were formulated by direct compression method using METHOCEL K15MCR polymer in various percentages. Physical parameters were tested and the dissolution procedure was performed by using USP (II) paddle method for eight hours to examine the release kinetics. In the study, METHOCEL K15MCR polymer was found to cause the strong retardation of the drug release. The release mechanism was explored and explained with zero order, first order, Higuchi and Korsmeyer-Peppas equations. In the context, it can be suggested with a satisfactory result that this sustained release Carvedilol tablets can be marketed to treat patient ensuring proper healthcare. DOI: http://dx.doi.org/10.3329/ijpls.v2i2.15452 International Journal of Pharmaceutical and Life Sciences Vol.2(2) 2013: 70-79


2015 ◽  
Vol 14 (2) ◽  
pp. 023505 ◽  
Author(s):  
Mihir Upadhyaya ◽  
Vibhu Jindal ◽  
Adarsh Basavalingappa ◽  
Henry Herbol ◽  
Jenah Harris-Jones ◽  
...  

1991 ◽  
Vol 29 (2) ◽  
pp. 7-8

Bromocriptine, lysuride (formerly lisuride, Revanil – Roche) and pergolide (not yet marketed in the UK) are dopamine agonists developed for use in the treatment of patients with Parkinson’s disease. Combination of a dopamine agonist with levodopa plus a dopa-decarboxylase inhibitor (‘co-dieldopa’)* may have advantages at all stages of the disease. The aim of combined co-dieldopa + agonist treatment is to limit some of the problems with prolonged co-dieldopa use alone; especially fluctuations in motor disability.1 It is still not clear how the three agonists compare with each other for therapeutic efficacy, duration of action, and side effects, nor how they are best combined with co-dieldopa.


1970 ◽  
Vol 8 (1) ◽  
pp. 31-38 ◽  
Author(s):  
Mohammad Nezab Uddin ◽  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Muhammad Rashedul Islam ◽  
Mohammad Habibur Rahman ◽  
...  

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)


2012 ◽  
Vol 468-471 ◽  
pp. 173-180
Author(s):  
Yi Ning Song ◽  
Zhi Li

The purpose of this paper is to explore the effective approach of Multi-Agent system(MAS) modeling and simulation. A detailed study of modeling and simulation of Space Information System has been carried out by combining controlled and intelligent requirements. To begin with we will provide a brief background on the Multi-Agent System concept and structure. Furthermore, grasp the model structure through vertical and longitudinal analysis with the consideration of emergence and collaboration. In addition, we described the Multi-agent model for Space Information System(SIS). Finally, algorithms of realizing the collaboration structures of the communication satellite system that presented in this paper were described.


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