Improvement of Solubility and Dissolution of Rilpivirine Solid Dispersions by Solvent Evaporation Technique and Novel Carriers

2018 ◽  
Vol 11 (4) ◽  
pp. 4177-4184
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Vishwa M
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Immediate Release ◽  
Solvent Evaporation ◽  
Onset Of Action ◽  
Enhanced Solubility ◽  
Evaporation Technique

Rilpivirine benzonitrile is a pharmaceutical drug used for the treatment of HIV infection it is characterized with poor solubility that limits its absorption and dissolution rate, which delays onset of action. In the present study, immediate release solid dispersion of antiretroviral Rilpivirine was formulated by solvent evaporation technique. Eighteen solid dispersions were prepared with 1:1:1, 1:2:1 and 1:3:1 ratios of drug: carrier: surfactant. There was significant improvement in the rate of drug release from all 18 solid dispersions and the formulation (SE12) comprising Rilpivirine: Kolliwax GMS II: SLS in 1:3:1 by solvent evaporation process has shown enhanced solubility about 30 folds and significant improvement in the rate of drug release. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Rilpivirine has been converted into an amorphous form from crystalline within the solid dispersion formulation. 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 Rilpivirine.   

scholarly journals Preparation and Evaluation of Solid Dispersion of Nebivolol Using Solvent Evaporation Method

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
A. Laxmi Raj ◽  
Y. Shravan Kumar
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Enhanced Solubility

Nebivolol is a pharmaceutical drug used for the treatment of Hypertension. It is characterized with poor solubility which limits its absorption and dissolution rate which delays onset of action. In the present study, fifteen formulations of solid dispersions were prepared with 1:1:1, 1:5:2 and 1:3:1.5 ratios of drug: carrier: surfactant by solvent evaporation method. There was significant improvement in the rate of drug release from all 15 solid dispersions and the formulation (SD14) comprising Nebivolol: Kleptose HPB: SLS in 1:5:2 ratio has shown enhanced solubility about 42 folds and significant improvement in the rate of drug release i.e. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Nebivolol has been converted into an amorphous form from crystalline within the solid dispersion formulation. The present study demonstrated that formulation of Nebivolol solid dispersion is a highly effective strategy for enhancing the bioavailability of poorly water soluble drug Nebivolol.

scholarly journals STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

2020 ◽  
pp. 187-190
Author(s):  
MAHAPARALE PR ◽  
THORAT VP
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Poloxamer 188 ◽  
Evaporation Method ◽  
Enhanced Solubility

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

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.

scholarly journals Solubility Enhancement of Diclofenac Using Solid Dispersions

2021 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
Mohd. Aamir Mirza ◽  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
Active Pharmaceutical Ingredient ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Limiting Factor ◽  
Formulation Development ◽  
Enhanced Solubility ◽  
Evaporation Technique

Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

scholarly journals FORMULATION OF SOLID DISPERSIONS FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN

2021 ◽  
pp. 94-100
Author(s):  
PAYAL D. BORAWAKE ◽  
KAUSLYA ARUMUGAM ◽  
JITENDRA V. SHINDE
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Fourier Transforms ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Pvp K30

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate. Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data. Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation. Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30.

scholarly journals Formulation and Evaluation of Solid Dispersion Incorporated Fast Disintegrating Tablets of Tenoxicam Using Design of Experiment

2019 ◽  
Vol 11 (1) ◽  
Author(s):  
Hafsa Mohammadi ◽  
V Hemanath Kumar
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Immediate Release ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Efficient Management ◽  
High Concentrations ◽  
Fast Disintegrating Tablets

The aim of the present work is to develop fast dissolving tablets from the solid dispersion of Tenoxicam for enhancement of solubility. The solid dispersions of Tenoxicam were prepared with Kollidon CL, PVP K30 and Poloxamer 127, in 1:1:1, 1:2:1 and 1:3:1 by using solvent evaporation method. The prepared solid dispersions were analyzed for all the physical parameters, drug: carrier interactions like FTIR, SEM, XRD. Solid dispersions showed a better dissolution compared to the pure drugs and among all the other formulations SD9 shows high percentage drug release i.e. 99.11 ± 5.17% for 90 min and selected as an optimized formulation for the preparation of fast disintegrating tablets of Tenoxicam. Gellan Gum, Fenugreek Seed Mucilage and L-HPC (low, middle and high concentrations) used in the preparation of fast disintegrating tablets prepared by direct compression method using 33 Response surface method. The post compression parameters of all the prepared tablets were within the limits. TF13 was selected as optimized formulation based on its highest disintegration time 36 sec and drug release 99.68 ± 1.52% for 10 min. Drug-excipients characterization also revealed that there is no interaction. Hence it concluded that solid dispersions incorporated fast disintegrating tablets is very useful approach for immediate release of Tenoxicam in the efficient management of inflammation and pain.

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.

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.

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 DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

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