scholarly journals Enhancement of Solubility Ibuprofen by Solid Dispersion Technique on Natural Mucilage

Author(s):  
Mr. Shikalgar S. S. ◽  

In this study generally solid dispersions (SDs) of ibuprofen were prepared by for all intents and purposes melt dispersion technique using natural mucilage of Lemon seed as carrier, which really is quite significant. Physical mixtures (PMs) of ibuprofen literally were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile, which generally is fairly significant. The solid dispersions and kind of physical mixtures for all intents and purposes were investigated for drug loading, saturation solubility and dissolution behavior in a subtle way. Saturation solubility study really actually was basically carried out in phosphate buffer (pH 7.4), 0.1 N HCL solution and distilled water, which kind of literally is quite significant. Solid dispersions for all intents and purposes particularly were mostly really found definitely fairly effective to literally kind of enhance the solubility of ibuprofen significantly in all the media, which actually is quite significant. Dissolution test specifically was mostly carried out in two different media, phosphate buffer (pH 7.4) and 0.1 N HCL. Solid dispersion containing Lemon seed mucilage at the ratio of 1:1.5 (drug: carrier) basically showed faster and sort of definitely higher drug release and basically was specifically really found to for the most part actually be most sort of effective among all the very actually solid dispersions in a generally big way, which kind of is fairly significant. Drug carrier interactions specifically specifically were studied by comparing Fourier definitely mostly Transform generally Infrared Spectroscopy (FT-IR) of particularly solid dispersions with pure drug which essentially revealed that the SDs specifically were kind of really stable in a pretty big way, which is fairly significant. So, fairly very solid dispersion may particularly be an definitely really effective technique to specifically enhance dissolution rate of ibuprofen, which kind of literally is fairly significant in a fairly big way.

2012 ◽  
Vol 11 (1) ◽  
pp. 1-6 ◽  
Author(s):  
Md Abdullah Al Masum ◽  
Florida Sharmin ◽  
S M Ashraful Islam ◽  
Md Selim Reza

In this study solid dispersions (SDs) of ibuprofen were prepared by melt dispersion technique using macrogol 4000 and macrogol 6000 as carrier. Physical mixtures (PMs) of ibuprofen were also prepared with the same carrier and in the same drug-carrier ratio (1:0.5, 1:1 and 1:1.5) to compare the dissolution profile. The solid dispersions and physical mixtures were investigated for drug loading, saturation solubility and dissolution behavior. Saturation solubility study was carried out in phosphate buffer (pH 7.2), 0.1 N HCl solution and distilled water. Solid dispersions were found effective to enhance the solubility of ibuprofen significantly in all the media. Dissolution test was carried out in two different media, phosphate buffer (pH 7.2) and 0.1 N HCl. Solid dispersion containing macrogol 6000 at the ratio of 1:1.5 (drug: carrier) showed faster and higher drug release and was found to be most effective among all the solid dispersions. Drug carrier interactions were studied by comparing Fourier Transform Infrared Spectroscopy (FT-IR) of solid dispersions with pure drug which revealed that the SDs were stable. So, solid dispersion may be an effective technique to enhance dissolution rate of ibuprofen. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12480 Dhaka Univ. J. Pharm. Sci. 11(1): 1-6, 2012 (June)


2017 ◽  
Vol 15 (2) ◽  
pp. 195-201
Author(s):  
Md Zahir Uddin ◽  
Jakir Ahmed Chowdhury ◽  
Ikramul Hasan ◽  
Md Selim Reza

This study was carried out to improve the dissolution properties of loratadine by solid dispersion technique. A series of solid dispersions of loratadine in PVP K-30 (1:1, 1:3 and 1:5) were prepared by kneading technique. The prepared solid dispersions were characterized by various physicochemical properties (fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy) and the dissolution characteristics were compared with loratadine and the physical mixtures of loratadine. It was revealed from the physicochemical analyses that there was a good compatibility between drug and carrier. On the other hand, the drug release from the prepared binary solid dispersions was significantly enhanced in comparison to both drug alone and the physical mixtures. Finally solid dispersion of loratadine: PVP K-30 prepared as 1:5 ratio was found to be described by non-Fickian release mechanism and was selected as the best formulation in this study.Dhaka Univ. J. Pharm. Sci. 15(2): 195-201, 2016 (December)


2013 ◽  
Vol 16 (1) ◽  
pp. 45-52 ◽  
Author(s):  
Sharmi Islam ◽  
Laboni Rani Dey ◽  
Mohammad Shahriar ◽  
Irin Dewan ◽  
SM Ashraful Islam

In this study solid dispersion (SDs) of gliclazide were prepared by solvent evaporation technique using poloxamer 407 as carrier. Drug carrier weight ratio were 1:1, 1:3 and 1:5. Physical mixtures of the same ratio were also prepared for comparison. The solid dispersions were investigated for drug loading and dissolution behavior and were found effective to enhance the solubility of gliclazide in dissolution medium significantly. Evaluation of the properties of the SDs was also performed by using Fourier-transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) studies. The FTIR spectroscopic studies showed the stability of gliclazide and absence of interaction between gliclazide and poloxomer 407. The XRD studies indicated the amorphous state of gliclazide in SDs. Dissolution data of SDs were compared by using both model dependant and model independent techniques. No significant difference in % DE (dissolution efficiency) was found among the SDs. But the drug release rate from SDs differs from that of physical mixture. So, solid dispersion technique may be an effective way to enhance dissolution rate of gliclazide. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14490 Bangladesh Pharmaceutical Journal 16(1): 45-52, 2013


2012 ◽  
Vol 1 (12) ◽  
pp. 423-430 ◽  
Author(s):  
Md. Sariful Islam Howlader ◽  
Jayanta Kishor Chakrabarty ◽  
Khandokar Sadique Faisal ◽  
Uttom Kumar ◽  
Md. Raihan Sarkar ◽  
...  

The aim of the present study was to improve the solubility and dissolution rate of a poorly water-soluble drug by a solid dispersion technique, in order to investigate the effect of these polymers on release mechanism from solid dispersions. Diazepam was used as a model drug to evaluate its release characteristics from different matrices. Solid dispersions were prepared by using polyethylene glycol 6000 (PEG-6000), HPMC, HPC and Poloxamer in different drug-to-carrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solid dispersions were prepared by solvent method. The pure drug and solid dispersions were characterized by in vitro dissolution study. Distilled water was used as dissolution media, 1000 ml of distilled water was used as dissolution medium in each dissolution basket at a temperature of 37°C and a paddle speed of 100 rpm. The very slow dissolution rate was observed for pure Diazepam and the dispersion of the drug in the polymers considerably enhanced the dissolution rate. This can be attributed to improved wettability and dispersibility, as well as decrease of the crystalline and increase of the amorphous fraction of the drug. SEM (Scanning Electron microscope) studies shows that the solid dispersion having a uniform dispersion. Solid dispersions prepared with PEG-6000, Poloxamer showed the highest improvement in wettability and dissolution rate of Diazepam. Solid dispersion containing polymer prepared with solvent method showed significant improvement in the release profile as compared to pure drug, Diazepam.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12453 International Current Pharmaceutical Journal 2012, 1(12): 423-430


Author(s):  
EMAN HUSSAIN ELMUBARAK ◽  
ZUHEIR ABDELRAHMAN OSMAN ◽  
MOHAMMED ABDELRAHMAN

Objective: The objective of the present study was to improve the aqueous solubility and dissolution characteristics of the loop diuretic furosemide (FUR); a class IV drug in the Biopharmaceutical Classification System (BCS) using solid dispersion technique. Methods: Solvent evaporation and kneading methods were used to produce solid dispersions of FUR in different ratios with the hydrophilic carrier polyvinylpyrrolidone K-30 (PVP-K30). The prepared solid dispersions were evaluated in terms of solubility study, percentage yield, drug content and Fourier transform infrared spectroscopic study (FT-IR). Tablets containing the optimized formula of solid dispersions ( were formulated and their dissolution characteristics were compared with commercial furosemide tablets. Results: The prepared solid dispersions showed an increase in aqueous solubility, especially those formulated in a 1:2 drug: carrier ratio using solvent evaporation method ( it showed a four-fold increase in solubility compared to the parent drug. The absence of drug-carrier chemical interactions that could affect the dissolution was proved by FT-IR. Solid dispersion tablets exhibited a better dissolution profile in simulated gastric fluid pH 1.2 at 37°C ± 0.5 than the commercial FUR tablets in terms of mean dissolution time (8.44 min) and dissolution efficiency in 30 min (42.54%). Both FUR solid dispersions and commercial tablets followed Weibull and Krosmeyer models as the two best models of drug release kinetics proving that they were immediate release. Conclusion: According to the results obtained in this study, solid dispersion techniques could be successfully used for the enhancement of aqueous solubility and dissolution rate of FUR.


2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N

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.


Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .


Author(s):  
Sanjoy Kumar Das

Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. Therefore increase in dissolution of poorly soluble drugs by solid dispersion technique presents a challenge to the formulation scientists. Solid dispersion techniques have attracted considerable interest of improving the dissolution rate of highly lipophilic drugs thereby improving their bioavailability by reducing drug particle size, improving wettability and forming amorphous particles. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic inert carrier or matrix and a hydrophobic drug. This article reviews historical background of solid dispersion technology, limitations, classification, and various preparation techniques with its advantages and disadvantages. This review also discusses the recent advances in the field of solid dispersion technology. Based on the existing results and authors’ reflection, this review give rise to reasoning and suggested choices of carrier or matrix and solid dispersion procedure.


2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude

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.


Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4315
Author(s):  
Bin Bin Huang ◽  
Dong Xu Liu ◽  
De Kun Liu ◽  
Gang Wu

The solid dispersion technique, which is widely used in the medical field, was applied to prepare a pesticide dosage form of emamectin benzoate (EM). The preparation, physicochemical characterization, aqueous solubility, release dynamics, photolytic degradation, bioactivity, and sustained-release effects of the prepared EM solid dispersions were studied by a solvent method, using polymer materials as the carriers. Water-soluble polyvinyl pyrrolidone (PVP) K30 and water-insoluble polyacrylic resin (PR)III were used as the carriers. The influence of various parameters, such as different EM:PVP-K30 and EM:PRIII feed ratios, solvent and container choices, rotational speed and mixing time effects on pesticide loading, and the entrapment rate of the solid dispersions were investigated. The optimal conditions for the preparation of EM-PVP-K30 solid dispersions required the use of methanol and a feed ratio between 1:1 and 1:50, along with a rotational speed and mixing time of 600 rpm and 60 min, respectively. For the preparation of EM-PRIII solid dispersions, the use of methanol and a feed ratio between 1:4 and 1:50 were required, in addition to the use of a porcelain mortar for carrying out the process. Under optimized conditions, the prepared EM-PVP-K30 solid dispersions resembled potato-like, round, and irregular structures with a jagged surface. In contrast, the EM-PRIII solid dispersions were irregular solids with a microporous surface structure. The results of X-ray powder diffraction (XRD), differential scanning calorimetry (DSC), ultraviolet (UV) spectrometry, and infrared (IR) spectrometry showed that the solid dispersions were formed by intermolecular hydrogen bonding. The solid dispersion preparation in PVP-K30 significantly improved the solubility and dissolution rate of EM, particularly the aqueous solubility, which reached a maximum of 37.5-times the EM technical solubility, when the feed ratio of 1:10 was employed to prepare the dispersion. Importantly, the wettable powder of EM-PVP-K30 solid dispersion enhanced the insecticidal activity of EM against the Plutella xylostella larvae. Furthermore, the solid dispersion preparation in PRIII afforded a significant advantage by prolonging the EM technical release in water at a pH below 7.0, especially when the PRIII content in solid dispersions was high. While the amplified toxicity of the wettable powder of EM-PRIII solid dispersions against the P. xylostella larvae showed no significant differences from that of the EM technical, the long-term toxicity under the field condition was much better than that of the commercially available EM 1.5% emulsifiable concentrate. Notably, solid dispersions with both the PVP-K30 and PRIII carriers reduced the effect of UV photolysis.


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