scholarly journals A Review on Solubility Enhancement by Solid Dispersion Method

2021 ◽  
Vol 11 (1) ◽  
pp. 182-187
Author(s):  
Laxmikant B. Dhande ◽  
Madhuri T. Deshmukh ◽  
Abhijit N. Khopade ◽  
Rajkumar V. Shete ◽  
Vaibhavi V. Kunjir

The issues of solubility for the targeted drug delivery of the new drug affects, the delivery many existing drug. The minimum 40% of the novel drug from the pharmaceutical industries are showing poor ability of solubilization in water. Hence to increase the solubility of such drug in waters and to increase their bioavailabilities are the major challenges to the scientists. So to overcome such problems and increase dissolution, development of solid dispersion with carriers having good water solubility is beneficiary. Hence solid dispersion methods are found to be an effective method to develop the solubility factor of the drug which showing poor solubility in water. The review highlights the various aspect of solid dispersion type, rational, advantages, limitation and manufacturing processes for the limited commercialization of solid dispersion. Keywords: Solid dispersions, hydrophilic, carrier, solubility, polymer, bioavailability.

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


2018 ◽  
Vol 6 (02) ◽  
pp. 43-52 ◽  
Author(s):  
R. Bhaskar ◽  
Monika OLA ◽  
Ravindra M. Ghongade

Nearly 40% of novel drugs comes in pharmaceutical industries are showing poor capability of solubilization in water. Therefore enhancing the solubilization of such drugs in water to enhance their bioavailability be the major challenge to formulation scientists. So the preparation of solid dispersion from the drug which shows poor solubility in water with carriers having good water solubility has decrease the occurrence of such problems and increase dissolution. Hence solid dispersion found to be attention-grabbing method for solubility enhancing of drugs which showing poor solubility in water. This review, shows an overview on the different solid dispersion types, rationale, their advantages, limitations, manufacturing processes as well as its characterization methods.


Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.


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 .


2021 ◽  
Vol 10 (3) ◽  
pp. 2929-2932
Author(s):  
Sachin N Kothawade

Spray drying methods were used to make solid dispersions of the medication Eprosartan Mesylate, which is poorly water-soluble. X-ray Powder diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were used to characterize the products' physicochemical features as well as drug-polymer interactions. Eprosartan Mesylate was shown to be dispersed amorphously in both solid dispersion systems, with a drug to polymer weight ratio of 1:4.The drug and polymer created hydrogen bonds, according to the spectrum data. Both techniques utilized in this investigation enhanced Eprosartan Mesylate solubility. Solid dispersions, on the other hand, performed significantly better, dissolving completely in 5 minutes and at a rate that was about 20 times faster than API within the first 15 minutes. Spray drying is a good way to boost the bioavailability of drugs that are poor water solubility.


Author(s):  
Preeti Mehra ◽  
Vishal Kapoor ◽  
Naveen Gupta ◽  
Dharmendra Singh Rajpoot ◽  
Neeraj Sharma

Rofecoxib, a new non-steroidal anti-inflammatory agent mainly used for the treatment of osteoarthritis and rheumatoid arthritis. The major drawback of Rofecoxib is its very low water solubility, which results in poor bioavailability after oral administration. Hence, an attempt was made to formulate fast dissolving tablets of Rofecoxib. The solid dispersions of Rofecoxib were prepared with PEG-4000 and PVP K30 by solvent evaporation method. The characterization of prepared solid dispersions by FTIR, XRPD and DSC, which reveals lack of interaction with carriers and dictates amorphous state of solid dispersions. Solid dispersion of Rofecoxib with PVP K30 (1:6) showed maximum dissolution, therefore compressed into tablets by using microcrystalline cellulose, lactose and crosspovidone. The dissolution profile of developed fast dissolving tablets containing solid dispersion of Rofecoxib (1:6) was studied. The formulated formulations showed optimum dissolution efficiency.


2011 ◽  
Vol 418-420 ◽  
pp. 2231-2234 ◽  
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Yvonne Ibold

Resveratrol (Res) is a polyphenolic secondary natural substance and can be used as anti-inflammatory, anti-aging, anti-heart disease and anti-cancer agent. However, Res has low water solubility which causes a low bioavailability in human body. In order to increase solubility we have prepared different inclusion complexes with native ((α, β, γ) and modified (2-hydroxypropyl-beta, dimethyl-beta) cyclodextrins (Cd) as well as solid dispersions using several surfactants (Imwitor 742, Imwitor 928, PEG 6000, Span 40, Span 60, Solutol HS15) with Res. The solubility of all mixtures was determined by UV-VIS spectroscopy at the wavelength of 305 nm. Regarding the Cd, the complex of Res with 2-hydroxypropyl-beta-Cd at a ratio of 1:3 showed the highest water solubility (248210 g/l). Concerning the surfactants, the solid dispersion from Res and Solutol HS15 showed the highest water solubility (16140 g/l). The complexation and the solid dispersion phase were confirmed by DSC. The results will be a basis for better formulation of resveratrol with higher bioavailability.


2017 ◽  
Vol 2 (1) ◽  

The objective of this study was to formulate and prepare gliclazide capsule by solid dispersion method using different surfactants and their in vitro evaluation. Solubilising capacity of polyethylene glycol (PEG 6000, PEG 20000) and polyvinylpyrrolidone (PVP K 30) was determined at 2% concentration where gliclazide was used as a model drug and water was used as control for comparison. Results showed that PVP K 30 exhibited maximum solubilising capacity. Fusion method of solid dispersion was adopted for preparation of capsules using PEG 6000 & PEG 20000 in different ratios. Although these agents are claimed to be good surfactants but our results showed that, the highest cumulative drug release was 1.81 % for gliclazide and PEG 6000 in a ratio of 1:6. The flow property of capsule granules was determined by angle of repose. The capsules were also subjected to weight uniformity test, disintegration test and moisture permeation test and the chemical analysis of solid dispersions were done by FTIR. From this study, it can be concluded that it is possible to formulate and prepare gliclazide capsule by using solid dispersion method.


Author(s):  
SHRADHA S. TIWARI ◽  
SHAILESH J. WADHER ◽  
SURENDRA G. GATTANI

Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.


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