scholarly journals Formulation Development of Porous Mannitol carrier: Improving the dissolution of poorly soluble drugs

2019 ◽  
Vol 9 (6) ◽  
pp. 143-154
Author(s):  
Sharmila Shah ◽  
Roshan Bodhe ◽  
Ashish Gorle

Major challenges in the design of oral dosage forms are their low solubility and low bioavailability. Improving the dissolution of these oral dosage forms are one of the most challenging tasks for the formulation scientists as most of the drug candidates are highly lipophilic in nature. Telmisartan and Ezetimibe belongs to the BCS class II, having high lipophilicity, poor water solubility and poor dissolution. The objective of this work was to improve the dissolution rate of poorly water soluble drugs by using porous carrier drug delivery system. Templating based spray drying methodology was used to prepare porous mannitol. Drug (Telmisartan, Ezetimibe) loaded porous mannitol carriers then characterized by P-XRD, DSC, SEM, BET surface area analysis and ATR-FTIR. ATR-FTIR studies showed complete removal of templating agent from carrier. P-XRD and DSC studies confirmed nano- confinement of drug in crystalline form. In vitro dissolution study results indicated that porous mannitol prepared using tartaric acid as templating agent showed significant improvement in dissolution rate than pure drugs and respective physical mixtures .These results suggest that, these porous carriers can be useful as drug carriers for improving the dissolution of lipophilic drugs. Keywords: Templating agent, Spray drying, Mannitol, Surface area, Tartaric acid.

2013 ◽  
Vol 14 (3) ◽  
pp. 911-918 ◽  
Author(s):  
Anna Giulia Balducci ◽  
Enrico Magosso ◽  
Gaia Colombo ◽  
Fabio Sonvico ◽  
Nurzalina Abdul Karim Khan ◽  
...  

Author(s):  
Christina Karavasili ◽  
Angelos Gkaragkounis ◽  
Dimitrios G. Fatouros

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 411
Author(s):  
Abdul Latif Ershad ◽  
Ali Rajabi-Siahboomi ◽  
Shahrzad Missaghi ◽  
Daniel Kirby ◽  
Afzal Rahman Mohammed

A lack of effective intervention in addressing patient non-adherence and the acceptability of solid oral dosage forms combined with the clinical consequences of swallowing problems in an ageing world population highlight the need for developing methods to study the swallowability of tablets. Due to the absence of suitable techniques, this study developed various in vitro analytical tools to assess physical properties governing the swallowing process of tablets by mimicking static and dynamic stages of time-independent oral transitioning events. Non-anatomical models with oral mucosa-mimicking surfaces were developed to assess the swallowability of tablets; an SLA 3D printed in vitro oral apparatus derived the coefficient of sliding friction and a friction sledge for a modified tensometer measured the shear adhesion profile. Film coat hydration and in vitro wettability was evaluated using a high-speed recording camera that provided quantitative measurements of micro-thickness changes, simulating static in vivo tablet–mucosa oral processing stages with artificial saliva. In order to ascertain the discriminatory power and validate the multianalytical framework, a range of commonly available tablet coating solutions and new compositions developed in our lab were comparatively evaluated according to a quantitative swallowability index that describes the mathematical relationship between the critical physical forces governing swallowability. This study showed that the absence of a film coat significantly impeded the ease of tablet gliding properties and formed chalky residues caused by immediate tablet surface erosion. Novel gelatin- and λ-carrageenan-based film coats exhibited an enhanced lubricity, lesser resistance to tangential motion, and reduced stickiness than polyvinyl alcohol (PVA)–PEG graft copolymer, hydroxypropyl methylcellulose (HPMC), and PVA-coated tablets; however, Opadry® EZ possessed the lowest friction–adhesion profile at 1.53 a.u., with the lowest work of adhesion profile at 1.28 J/mm2. For the first time, the in vitro analytical framework in this study provides a fast, cost-effective, and repeatable swallowability ranking method to screen the in vitro swallowability of solid oral medicines in an effort to aid formulators and the pharmaceutical industry to develop easy-to-swallow formulations.


Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4518
Author(s):  
Raquel Sousa ◽  
Artur Figueirinha ◽  
Maria Teresa Batista ◽  
Maria Eugénia Pina

Cymbopogon citratus DC (Stapf.) is a perennial grass and it is distributed around the world. It is used as a condiment for food and beverage flavouring in the form of infusions and decoctions of its dried leaves. Our previous studies have shown antioxidant, anti-inflammatory and gastroprotective activities for the infusion and its phenolic fractions. The aim of the present work was to develop oral dosage forms from a Cymbopogon citratus extract to be used as a functional food with antioxidant properties. Initially, an essential oil-free infusion was prepared, lyophilized and characterized by HPLC-PDA. Total phenols were quantified with the Folin–Ciocalteu method and the antioxidant activity was assessed by DPPH assay. Gelatine capsules containing the extract with different excipients, selected after DSC and IR trials, were prepared. A formulation exhibiting better antioxidant behaviour in a gastric environment was attained. These results suggest that the proposed formulation for this extract could be a valuable antioxidant product and, consequently, make an important contribution to “preventing” and minimizing diseases related to oxidative stress conditions.


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