Porous calcium carbonate as a carrier material to increase the dissolution rate of poorly soluble flavouring compounds

2017 ◽  
Vol 8 (4) ◽  
pp. 1627-1640 ◽  
Author(s):  
Maria Lundin Johnson ◽  
David Noreland ◽  
Patrick Gane ◽  
Joachim Schoelkopf ◽  
Cathy Ridgway ◽  
...  
Keyword(s):  
Calcium Carbonate ◽  
Dissolution Rate ◽  
Amorphous State ◽  
Carrier Material ◽  
Enhanced Dissolution ◽  
Poorly Soluble ◽  
Porous Calcium Carbonate

Flavouring molecules stabilised in amorphous state when loaded in FCC show enhanced dissolution rate compared to the crystalline counterpart.

scholarly journals "Enhancement of solubility of a poorly soluble antiplatelet aggregation drug by cogrinding technique"

2018 ◽  
Vol 11 (10) ◽  
pp. 340
Author(s):  
Asmaa A Bayoumi
Keyword(s):  
Dissolution Rate ◽  
High Performance ◽  
Stability Study ◽  
Enhanced Dissolution ◽  
Antiplatelet Aggregation ◽  
Weight Variation ◽  
Accelerated Stability ◽  
Poorly Soluble ◽  
The Stability ◽  
Biopharmaceutical Classification System

Objective: The goal of this study was to formulate ticagrelor tablets with enhanced dissolution rate using cogrinding technique. However, it belongs to the biopharmaceutical classification system Class IV molecule, poorly soluble, and permeable.Methods: Various ratios (0.2:1–1.67:1) of povidone (PVP)/drug were used in the formulations. Ticagrelor was coground with different percentage of PVP K 25 (carrier) in a mortar with a pestle for 30 min, then mixed with the rest excipients. A high-performance liquid chromatography stability indicating assay was developed to test the stability of ticagrelor in the selected formulae.Results: The results showed that the presence of PVP in relatively high ratios compared to the drug is desirable for enhancing the dissolution rate of ticagrelor. The best-optimized formulae found were that F8 and F9 which showed good disintegration and dissolution rate of ticagrelor more than 92% after 30 min while the dissolution rate for ticagrelor standard was only 22% after 30 min. Stability studies were performed on the selected formulae F8 and F9. Conclusion: The optimized formulae were evaluated for thickness, weight variation, hardness, friability, dissolution, and accelerated stability study for a period of 6 months. Cogrinding using PVP K 25 proved to enhance the dissolution of ticagrelor which may be due to the formation of a soluble complex between ticagrelor and PVP. The selected formulae F8 and F9 showed good stability.

Enhanced Dissolution Rate of Glipizide by a Liquisolid Technique

2011 ◽  
Vol 3 (4) ◽  
pp. 1205-1213
Author(s):  
Hitendra S Mahajan ◽  
Manoj R Dhamne ◽  
Surendra G. Gattani, ◽  
Ashwini D Rasal ◽  
Hannan T Shaikh
Keyword(s):  
Thermal Analysis ◽  
Dissolution Rate ◽  
Immediate Release ◽  
X Ray Diffraction ◽  
Dissolution Rates ◽  
Polyethylene Glycol 400 ◽  
Disintegration Time ◽  
Peg 400 ◽  
Enhanced Dissolution ◽  
Poorly Soluble

This study aims to prepare immediate release glipizide liquisolid tablets using Avicel PH-102 and Aerosil 200 as the carrier and coating material respectively to increase dissolution rate of poorly soluble glipizide. This study also aims to evaluate treated Gellan gum as disintegrant in the preparation of liquisolid tablets. The solubility of glipizide was increased by use of liquisolid technique. The glipizide liquisolid tablets were evaluated for characteristics like drug content, friability, hardness, disintegration time, thermal analysis, X-ray diffraction (XRD) study and dissolution rates. The dissolution patterns of glipizide liquisolid tablets, carried out according to USP paddle method, and were compared with their commercial counterparts. The results obtained shows that all glipizide liquisolid tablets exhibits higher dissolution rates than those of marketed glipizide tablets. Dissolution rates increases with increasing concentration of liquid vehicles and maximum drug release achieved by formulations containing Polyethylene glycol 400 (PEG 400) as a liquid vehicle. The results of XRD and thermal analysis did not show any changes in crystallinity of drug and interaction between glipizide and excipients during the formulation process. 

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

The Effect of Superdisintegrants on the Dissolution of Promethazine. HCl Fast Dissolving Tablets

2010 ◽  
Vol 3 (1) ◽  
pp. 867-871
Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Angle Of Repose ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Enhanced Dissolution ◽  
Weight Variation ◽  
Compressibility Index ◽  
Chemoreceptor Trigger Zone ◽  
Trigger Zone ◽  
Standard Limit

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 

Enhanced oral bioavailability of Etodolac by liquisolid compact technique: optimisation, in-vitro and in-vivo evaluation

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhumin K. Pathak ◽  
Meenakshi Raghav ◽  
Arti R. Thakkar ◽  
Bhavin A. Vyas ◽  
Pranav J. Shah
Keyword(s):  
Dissolution Rate ◽  
Amorphous State ◽  
Immediate Release ◽  
Angle Of Repose ◽  
Oral Suspension ◽  
Load Factor ◽  
In Vivo Evaluation ◽  
Rate Of Dissolution ◽  
Q 30

Background: Poor dissolution of Etodolac is one of the major challenges in achieving the desired therapeutic effect in oral therapy. Objective: This study aimed to assess the potential of liquisolid compact technique in increasing the rate of dissolution of Etodolac and thus its bioavailability. Methods: Liquisolid compacts were prepared using PEG 400, Avicel PH-200 and Aerosil 200 as non-volatile liquid, carrier and coating material respectively. Optimisation was carried out by applying a 32 full factorial design using Design expert software 11.0.3.0 to examine the effects of independent variables (load factor and carrier: coating ratio) on dependent variables (angle of repose and % cumulative drug release at 30 min [Q 30 min]).Assessment of bioavailability was based on pharmacokinetic study in rabbits and pharmacodynamics evaluation in rats respectively. Results: The formulation M3 was identified as the optimised formulation based on the better flow (lower angle of repose) and a higher rate of dissolution (Q 30 min >95%). The higher dissolution rate could be due to conversion of Etodolac into an amorphous molecularly dispersed state, availability of larger surface area, enhancement of aqueous solubility and enhanced wetting of drug particles. Studies with DSC, XRD, and SEM verified the transformation of Etodolac from crystalline to amorphous state, a key factor responsible for improving the dissolution rate. Pharmacokinetic profile of M3 was prominent, demonstrating higher absorption of Etodolac in comparison of oral suspension and immediate-release conventional tablets in rabbits. Liquisolid formulation exhibited 27% increment in paw thickness as compared to 57% and 46% increments for oral suspension and immediate-release conventional tablets respectively, after 7 hrs in carrageenan-induced paw model in rats. Conclusion: The results indicated liquisolid compact technique to be a promising strategy to enhance the bioavailability of Etodolac.

Controlled precipitation for enhanced dissolution rate of flurbiprofen: development of rapidly disintegrating tablets

2017 ◽  
Vol 43 (9) ◽  
pp. 1430-1439 ◽  
Author(s):  
Ebtessam A. Essa ◽  
Amira O. Elmarakby ◽  
Ahmed M. A. Donia ◽  
Gamal M. El Maghraby
Keyword(s):  
Dissolution Rate ◽  
Enhanced Dissolution ◽  
Controlled Precipitation

The Influence of Thermal and Mechanical Preparative Techniques on the Amorphous State of Four Poorly Soluble Compounds

2005 ◽  
Vol 94 (9) ◽  
pp. 1998-2012 ◽  
Author(s):  
James E. Patterson ◽  
Michael B. James ◽  
Angus H. Forster ◽  
Robert W. Lancaster ◽  
James M. Butler ◽  
...  
Keyword(s):  
Amorphous State ◽  
Poorly Soluble
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