scholarly journals PREPARATION, CHARACTERIZATION AND DISSOLUTION STUDY OF SPRAY DRIED SOLID DISPERSIONS OF SIMVASTATIN WITH PVP K25 AND AEROSIL 200

2021 ◽  
Vol 10 (6) ◽  
pp. 3806-3812
Author(s):  
Pritam Singh
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Drying Method ◽  
Bcs Class Ii ◽  
Enhanced Dissolution ◽  
Amorphous Nature ◽  
Characterization Studies

BCS class II is well-known for the drugs, having poor aqueous solubility and high permeability. Simvastatin is also categorized as BCS class II, suffering from poor aqueous solubility, affecting its bioavailability. In an attempt to resolve this problem, solid dispersions of simvastatin were prepared by spray-drying method. Solid dispersions of simvastatin with PVP K25 and aerosol in ratio (1:1:1 to 1:5:1) and without aerosil 200 (1:1 to 1:5) were prepared by spray drying method. The dissolution test showed the enhancement of dissolution as compared to the pure drug and nearly equal to marketed formulation “SIMVOTIN 20mg” in both types of formulation, but formulations with aerosil 200 showed faster drug release as compared to the simple formulations without aerosil. The formulation containing the 1:3:1 (simvastatin: PVP K25: Aerosil 200) showed the faster drug release as compared to other formulation that do not contain the Aerosil 200. Other characterization studies were also performed such as FTIR, differential scanning colorimetry and powdered X-ray crystallographic studies. These studies showed the increased amorphous nature of the drug in the formulation, which explain the enhanced dissolution rate of the drug for these formulations.

Central composite designed ezetimibe solid dispersion for dissolution enhancement: synthesis and in vitro evaluation

2019 ◽  
Vol 10 (10) ◽  
pp. 643-658 ◽  
Author(s):  
Neelam Sharma ◽  
Sukhbir Singh
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Solvent Evaporation ◽  
Dissolution Enhancement ◽  
Great Promise ◽  
Bcs Class Ii ◽  
Evaporation Technique ◽  
Central Composite

Aim: The current research is focused on increasing aqueous solubility and dissolution of BCS class II drug by using modified solvent evaporation technique to produce solid dispersions of ezetimibe (EZSD) using gelucire 50/13 and polyvinyl pyrollidone K30. Methodology & results: Central composite design analyzed the effect of gelucire 50/13 and polyvinyl pyrollidone K30 on the percentage of drug released in 5 and 30 min. Ezetimibe (EZ) aqueous saturation solubility (4.56 ± 0.94 μg/ml) was increased 25-fold in EZSD (115 ± 3.41 μg/ml). Cumulative drug release from EZ and optimized EZSD were observed 24.67 and 87.54% within 1 h, respectively. Conclusion: Manufacturing EZSD using modified solvent evaporation technique using rotary evaporator holds great promise for enhancing EZ's solubility and dissolution.

scholarly journals Formulation Development and Evaluation of Liposphere of Poor Water Soluble Drug for Hyperlipidemia

2021 ◽  
Vol 11 (2) ◽  
pp. 23-30
Author(s):  
Anil Kumar ◽  
Umesh K. Jain ◽  
Ajay Patel
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Water Soluble ◽  
Fibric Acid Derivative ◽  
Formulation Development ◽  
Bcs Class Ii ◽  
Paraffin Oil

Lipospheres offer a new approach to improve an aqueous solubility of BCS class-II drugs. Simvastatin is a third generation fibric acid derivative belonging to this class, employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. An attempt was made to improve aqueous solubility of Simvastatin by aid of stearic acid and Paraffin oil. The factorial batches of the Simvastatin lipospheres were formulated by melt dispersion technique using 32 factorial design with variables X1- concentration of stearic acid and X2- concentration of paraffin oil and responses Y1 - % Drug Entrapment (% DE) and Y2 - % Drug Release (% DR). From the surface response graphs the optimized batch was formulated and evaluated for saturation solubility, in-vitro drug release studies. Significant improvement in the aqueous solubility of the drug in the Simvastatin lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs. Keywords: Linospheres; Simvastatin; Drug release; Hyperlipidemic; Drug entrapment.

Improved Efficacy of Lovastatin from Soluplus-PEG Hybrid Polymer- Based Binary Dispersions

2020 ◽  
Vol 16 (8) ◽  
pp. 1164-1171
Author(s):  
Radhika Verma ◽  
Manju Nagpal ◽  
Thakur G. Singh ◽  
Manjinder Singh ◽  
Geeta Aggarwal
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Class Ii ◽  
Hybrid Polymer ◽  
In Vitro Drug Release ◽  
In Vivo Efficacy ◽  
Bcs Class Ii ◽  
Individual Polymer

Background: Lovastatin is a statin drug used for lowering cholesterol in those with hypercholesterolemia to reduce the risk of cardiovascular disease. It is a BCS class II drug i.e. it has low aqueous solubility and high permeability. Objective: Improvement of solubility and in vivo efficacy was investigated by formulating binary solid dispersions. Methods: Binary solid dispersions of lovastatin were formulated in the current study using two polymers i.e. Soluplus and PEG 4000. Seven batches of solid dispersions were prepared (S1, P1, SP1, SP2, SP3, SP4, and SP5) via the solvent evaporation method. The prepared dispersions were evaluated for equilibrium solubility, FTIR, XRD, DSC, SEM studies, and further in vitro drug release were evaluated. The results revealed significant enhancement in the solubility of drug-using polymer hybrids as compared to that of individual polymer dispersion batches. Results: A significant solubility enhancement was observed with SP5 (approx 40 times) having a higher concentration of Soluplus. FTIR studies indicated no drug to polymer interaction. DSC studies revealed complete amorphization of polymer and also X-RD data is also in compliance with DSC results. In vitro drug release studies showed almost 100% release in 2h in polymer hybrid batches in comparison to individual polymer batch (S1 and P1). The best dissolution characteristics were observed in SP3 and SP5 which is also in compliance with solubility data. Further in vivo efficacy studies revealed a significant reduction in LDL, HDL, TG, AST, and ALT levels in comparison to pure drug lovastatin group and hypercholesterolemia control group. Conclusion: Hybrid polymer may be a prospective carrier system for the enhancement of solubility of BCS class II drugs.

Enhanced dissolution rate of celecoxib using PVP and/or HPMC-based solid dispersions prepared by spray drying method

2013 ◽  
Vol 43 (3) ◽  
pp. 205-213 ◽  
Author(s):  
Jung Hwan Lee ◽  
Min Jeong Kim ◽  
Hyeon Yoon ◽  
Cho Rok Shim ◽  
Hyun Ah Ko ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Spray Drying ◽  
Solid Dispersions ◽  
Drying Method ◽  
Enhanced Dissolution

scholarly journals Development of Fenofibrate Solid Dispersions for the Plausible Aqueous Solubility Augmentation of this BCS Class-II Drug

2021 ◽  
Vol 13 (10) ◽  
pp. 107-116
Author(s):  
Purushottam S. Gangane ◽  
Vaibhav M. Mule ◽  
Debarshi Kar Mahapatra ◽  
Nilesh M. Mahajan ◽  
Harigopal S. Sawarkar
Keyword(s):  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Bcs Class Ii

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

Inhalable Spray Dried Pro-Liposome Powder Containing Budesonide for Pulmonary Delivery

2021 ◽  
Vol 14 (4) ◽  
pp. 5538-5548
Author(s):  
Aliasgar J Kundawala ◽  
Khushbu S Chauhan ◽  
Harsha V Patel ◽  
Swati K Kurtkoti
Keyword(s):  
Drug Release ◽  
Spray Drying ◽  
Entrapment Efficiency ◽  
Geometric Standard Deviation ◽  
Drying Method ◽  
Dry Powder ◽  
Liposomal Drug ◽  
Vesicle Size ◽  
Aerodynamic Properties ◽  
Spray Dried

Budesonide is an anti-asthmatic agent which is used to control the symptoms of asthma like bronchospasm, oedema. Drug delivered to lung through inhalation will provide systemic and local drug delivery at lower dose in chronic and acute diseases. Dry powder inhalers are the best choice for targeting the anti-asthmatic drugs through pulmonary route. The objective of the present study is to prepare inhalable lipid coated budesonide microparticles by spray drying method so effective delivery of budesonide to the lungs can be achieved. The microparticles in the form of dry powder were obtained by either spray drying liposomal drug suspension or lipid drug suspension. The liposomes were initially prepared by solvent evaporation method using Hydrogenated Soyabean Phosphatidylcholine and Cholesterol (1:1, 1:2, 2:1) as lipid carrier and then spray dried later with mannitol as bulking agent at different lipid to diluent ratio (1:1.25, 1:2.5 & 1:5). The liposomes and liposomal dry powder were evaluated for vesicle size, % entrapment efficiency, in vitro drug release studies, powder characteristics, aerosol performance and stability studies. The liposomes prepared showed vesicle size (2-8 µm), Entrapment efficiency (92.22%) at lipid: drug ratio of (2.5:1) and observed 80.41 % drug release in 24 hrs. Pro-liposomes prepared by spray drying of liposomal drug suspension (LSD1) showed emitted dose, mean mass aerodynamic diameter, geometric standard deviation and fine particle fraction of 99.01%, 3.12 µm, 1.78 and 43.5% along with good powder properties. The spray dried powder was found to be stable at 4 ± 2 °C & 65% ± 5 % RH. The inhalable microparticles containing Budesonide containing lipid dry powder was successfully prepared by spray drying method that showed good aerodynamic properties and stability with mannitol as diluent. The microparticles produced with this novel approach could deliver drug on target via inhalation route and also ease manufacture process at large scale in fewer production steps.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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