scholarly journals IMPROVEMENT OF DISSOLUTION PROPERTIES OF ALBENDAZOLE FROM DIFFERENT METHODS OF SOLID DISPERSION

2018 ◽  
Vol 8 (5) ◽  
pp. 475-480 ◽  
Author(s):  
A.K. Azad ◽  
K Jahan ◽  
TS Sathi ◽  
R Sultana4 ◽  
SA Abbas ◽  
...  

Poor aqueous solubility of drugs results in poor absorption and bioavailability.  The objective of Solid dispersion technology is to increase the dissolution properties of highly lipophilic drugs, by using different hydrophilic carriers thereby improving their bioavailability. This technology is useful for enhancing the dissolution, absorption and therapeutic efficacy of drugs in dosage forms.  Albendazole is a broad-spectrum antihelminthic agent used for the treatment of a variety of parasitic worm infestations. It is practically insoluble in water but slightly soluble in solvents like chloroform, methanol, ethyl acetate, and acetonitrile. The aim of our study was to improve the dissolution profile of Albendazole using HPMC K 100 LV, Kollidon VA64 and Mannitol as carriers by solid dispersion techniques. From the prepared solid dispersion, formulation code CSF5 showed better result where carrier was HMPC K 100 LV at 1:10 ratio in solvent evaporation method. Among the carrier used here to conduct our study, HPMC K 100 LV showed better result for both kneading and solvent evaporation methods. And among the method employed here, solvent evaporation method showed better solubility of drug at 60 min also at 1:10 ratio which was 78.86%.

2019 ◽  
Vol 9 (01) ◽  
pp. 21-26
Author(s):  
Arif Budiman ◽  
Ayu Apriliani ◽  
Tazyinul Qoriah ◽  
Sandra Megantara

Purpose: To develop glibenclamide-nicotinamide cocrystals with the solvent evaporation method and evaluate their solubility and dissolution properties. Methods: Cocrystals of glibenclamide-nicotinamide (1:2) were prepared with the solvent evaporation method. The prediction of interactive cocrystals was observed using in silico method. The solubility and dissolution were performed as evaluation of cocrystals. The cocrystals also were characterized by differential scanning calorimetry (DSC), infrared spectrophotometry, and powder X-ray diffraction (PXRD). Result: The solubility and dissolution profile of glibenclamide-nicotinamide cocrystal (1:2) increased significantly compared to pure glibenclamide as well as its physical mixture. Characterization of cocrystal glibenclamide-nicotinamide (1:2) including infrared Fourier transform, DSC, and PXRD, indicated the formation of a new solid crystal phase differing from glibenclamide and nicotinamide. Conclusion: The confirmation of cocrystal glibenclamide-nicotinamide (1:2) indicated the formation of new solid crystalline phases that differ from pure glibenclamide and its physical mixture


2018 ◽  
Vol 6 (1) ◽  
pp. 26-34
Author(s):  
Pravin Kumar Sharma ◽  
Pankaj Kumar Sharma ◽  
Gajanan N Darwhekar ◽  
Birendra Shrivastava

Tadalafil is used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension. It is having low aqueous solubility thus it shows poor bioavailability of about 28% by after oral administration. To improve its solubility and dissolution profile solid dispersions (SDPs) of Tadalafil was prepared by physical mixing and solvent evaporation method using polyvinyl pyrollidone-K30 (PVP-30) as a hydrophilic polymeric carrier in different proportions with respect to drug (drug to polymer ratio 1:1 to 1:5). Drug and polymer compatibility studies were performed using FTIR study. The best suitable ratio and method was selected on the basis of enhanced aqueous solubility of drugs. Further selected SDPs were evaluated for various parameters like DSC analysis, percentage yield, percent drug content, saturation solubility, percent drug dissolution and stability studies. FTIR study indicated no incompatibility between Tadalafil and PVP-K30. SDPs prepared with drug to polymer ratio 1:3 and solvent evaporation method was found to be best as they shown significant increased (up to 10 fold) in aqueous solubility in comparison with that of others. DSC study also suggested the depression in the crystalline nature of Tadalafil. Selected SDPs exhibited good stability up to 3 months at 25 ± 2°C /60 ± 5% RH. Based on the results it can be concluded that, SDPs shown remarkable increase in the aqueous solubility and dissolution of Tadalafil and it may improve oral bioavailability of drug as compared with plain drug.


2018 ◽  
Vol 6 (1) ◽  
pp. 26-34 ◽  
Author(s):  
Pravin Kumar Sharma ◽  
Pankaj Kumar Sharma ◽  
Gajanan N Darwhekar ◽  
Birendra Shrivastava

Tadalafil is used for the treatment of the erectile dysfunction (ED) and pulmonary arterial hypertension. It is having low aqueous solubility thus it shows poor bioavailability of about 28% by after oral administration. To improve its solubility and dissolution profile solid dispersions (SDPs) of Tadalafil was prepared by physical mixing and solvent evaporation method using polyvinyl pyrollidone-K30 (PVP-30) as a hydrophilic polymeric carrier in different proportions with respect to drug (drug to polymer ratio 1:1 to 1:5). Drug and polymer compatibility studies were performed using FTIR study. The best suitable ratio and method was selected on the basis of enhanced aqueous solubility of drugs. Further selected SDPs were evaluated for various parameters like DSC analysis, percentage yield, percent drug content, saturation solubility, percent drug dissolution and stability studies. FTIR study indicated no incompatibility between Tadalafil and PVP-K30. SDPs prepared with drug to polymer ratio 1:3 and solvent evaporation method was found to be best as they shown significant increased (up to 10 fold) in aqueous solubility in comparison with that of others. DSC study also suggested the depression in the crystalline nature of Tadalafil. Selected SDPs exhibited good stability up to 3 months at 25 ± 2°C /60 ± 5% RH. Based on the results it can be concluded that, SDPs shown remarkable increase in the aqueous solubility and dissolution of Tadalafil and it may improve oral bioavailability of drug as compared with plain drug.


Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.


1970 ◽  
Vol 3 (2) ◽  
pp. 43-46
Author(s):  
Riaz Uddin ◽  
Farzana Ali ◽  
Subrata Kumar Biswas

Key Words: Solid dispersions; solvent evaporation method; atorvastatin; HPMCDOI: http://dx.doi.org/10.3329/sjps.v3i2.8036 S.J. Pharm. Sci 3(2): 43-46


Author(s):  
Sanjesh G. Rathi ◽  
Dhruv B. Chaudhari

The solid dispersions of Bilastine with HPMC, PVP K30 and HPC have been prepared in different weight ratios by using solvent evaporation method. DSC was used to characterize the samples of solid dispersions and pure drug. Drug found compatible with the excipients. The highest improvements in solubility and in-vitro drug release were observed in solid dispersion prepared with HPC (F14) by solvent evaporation method. The increased dissolution rate of drug from solid dispersion may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion with the HPC carrier considered as most satisfactory among all solid dispersions.


2019 ◽  
Vol 11 (1) ◽  
pp. 241 ◽  
Author(s):  
D. Christopher Vimalson ◽  
S. Parimalakrishnan ◽  
N. S. Jeganathan ◽  
S. Anbazhagan

Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.


2020 ◽  
Vol 14 (1) ◽  
pp. 75-89 ◽  
Author(s):  
Sandip Pawar ◽  
Pravin Shende

Background: : Currently, the most important challenge in the development of therapeutics and actives is their poor aqueous solubility and bioavailability. Objective: : The low aqueous solubility, poor pharmacokinetic properties, and bioavailability associated with novel actives manifest in numerous challenges in the formulation of conventional dosage forms like tablets, capsules, suspensions, emulsions, etc. Nanosponges are a novel class of drug delivery system capable of encapsulating or entrapping both lipophilic and hydrophilic drugs. Target-specific drug delivery and controlled drug release are the advantages offered by nanosponges which make them a promising anti-tumor drug delivery system. Methods: Nanosponges are colloidal structures comprising solid nanoparticles with cavities and meshlike structures for encapsulation of wide varieties of substances like antineoplastic agents, proteins and peptides, volatile oils, genetic material, etc. The methods of preparation of β-cyclodextrin-based nanosponges include solvent evaporation method, emulsion solvent evaporation method, ultrasound-assisted synthesis, hyper cross-linked cyclodextrin and interfacial phenomenon method. A large variety of nanosponges- based formulations are available in the market and some formulations of prostavastin, brexin, glymesason, mena-gargle, etc. are under clinical trials. Results: : Nanosponges possess potential applications in target site-specific drug delivery to liver, spleen, and lungs. Due to the surface functionalization, nanosponges show broad applications in water purification, protein delivery, chemical sensors, detection of explosives, agriculture, etc. In the near future, nanosponges-based products will capture a huge market for commercialization due to their improved properties and advantages. Conclusion: : This review provides an account of the patents related to nanosponges (2006-2018) and covers the broad applications of β-cyclodextrin-based nanosponges, their roles in vaccine delivery, cancer therapy, fire engineering, water purification, etc.


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