Assessing the Enhancement of Aqueous Solubility of Efavirenz via Lyophilized Milk Based Solid Dispersion Formulations

2016 ◽  
Author(s):  
Nishikant Ambadas Raut
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility

Improvement of Aqueous Solubility and Dissolution Kinetics of Canrenone by Solid Dispersion in Sucroester

1988 ◽  
Vol 14 (6) ◽  
pp. 791-803 ◽  
Author(s):  
Augusta Obikili ◽  
Michel Deyme ◽  
Denis Wouessidjewe ◽  
Dominique Duchěne
Keyword(s):  
Solid Dispersion ◽  
Dissolution Kinetics ◽  
Aqueous Solubility ◽  
Kinetics Of

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals SOLID DISPERSIONS: A METHOD TO IMPROVE BIOAVAILABILITY OF ORAL DRUG DOSAGE FORM

2019 ◽  
Vol 8 (3) ◽  
Author(s):  
Ritika Puri ◽  
Manisha Bhatti
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Drug Dosage ◽  
Oral Drug ◽  
Surface Active Agents ◽  
Drug Dosage Form ◽  
Surface Active ◽  
Biopharmaceutical Classification System

Presently only few percent of drugs having high aqueous solubility, Number of drugs are belonging to biopharmaceutical classification system class II that means possessing  poor aqueous solubility  eventually  results in low level of drug in systemic circulation. To overcome this problem, various strategies have been come out into notion such as self emulsifying drug delivery system solid dispersions, use of surface active agents, complex formation. Solid dispersions is found to be promising approach to increase bioavailability by use of various polymers. This review focuses on the mechanism of drug release from solid dispersion with its method of preparation and applications. Key words: dissolution, particle size, solid dispersion

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.

Freeze dried solid dispersion of exemestane: A way to negate an aqueous solubility and oral bioavailability problems

2017 ◽  
Vol 107 ◽  
pp. 54-61 ◽  
Author(s):  
Shamandeep Kaur ◽  
Sunil K. Jena ◽  
Sanjaya K. Samal ◽  
Vaishali Saini ◽  
Abhay T. Sangamwar
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Aqueous Solubility ◽  
Freeze Dried

scholarly journals Development of a Ternary Solid Dispersion Formulation of LW6 to Improve the In Vivo Activity as a BCRP Inhibitor: Preparation and In Vitro/In Vivo Characterization

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 206 ◽  
Author(s):  
Rajiv Bajracharya ◽  
Sang Hoon Lee ◽  
Jae Geun Song ◽  
Minkyoung Kim ◽  
Kyeong Lee ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Amorphous State ◽  
Weight Ratio ◽  
Acid Methyl Ester ◽  
Systemic Exposure ◽  
Aqueous Solubility ◽  
Poloxamer 407 ◽  
Cancer Resistance ◽  
Ternary Solid Dispersion

LW6 (3-[2-(4-adamantan-1-yl-phenoxy)-acetylamino]-4-hydroxy-benzoic acid methyl ester) is a potent inhibitor of drug efflux by the breast cancer resistance protein (BCRP). However, its poor aqueous solubility leads to low bioavailability, which currently limits in vivo applications. Therefore, the present study aimed to develop ternary solid dispersion (SD) formulations in order to enhance the aqueous solubility and dissolution rate of LW6. Various SDs of LW6 were prepared using a solvent evaporation method with different drug/excipient ratios. The solubility and dissolution profiles of LW6 in different SDs were examined, and F8-SD which is composed of LW6, poloxamer 407, and povidone K30 at a weight ratio of 1:5:8 was selected as the optimal SD. The structural characteristics of F8-SD were also examined using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), and scanning electron microscopy (SEM). In the acidic to neutral pH range, F8-SD achieved rapid dissolution with a drug release of 76–81% within 20 min, while the dissolution of pure LW6 was negligible. The XRPD patterns indicated that F8-SD probably enhanced the solubility and dissolution of LW6 by changing the drug crystallinity to an amorphous state, in addition to the solubilizing effect of the hydrophilic carriers. Furthermore, F8-SD significantly improved the oral bioavailability of topotecan, which is a BCRP substrate, in rats. The systemic exposure of topotecan was enhanced approximately 10-fold by the concurrent use of F8-SD. In conclusion, the ternary SD formulation of LW6 with povidone K30 and poloxamer 407 appeared to be effective at improving the dissolution and in vivo effects of LW6 as a BCRP inhibitor.

scholarly journals Application of Solid Dispersion Technique to Improve Solubility and Sustain Release of Emamectin Benzoate

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4315
Author(s):  
Bin Bin Huang ◽  
Dong Xu Liu ◽  
De Kun Liu ◽  
Gang Wu
Keyword(s):  
Solid Dispersion ◽  
Rotational Speed ◽  
Mixing Time ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Feed Ratio ◽  
Emamectin Benzoate ◽  
Wettable Powder ◽  
Dispersion Technique ◽  
Pvp K30

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.

scholarly journals Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 407
Author(s):  
Sooho Yeo ◽  
Jieun An ◽  
Changhee Park ◽  
Dohyun Kim ◽  
Jaehwi Lee
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Dispersion System ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

scholarly journals Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization

2021 ◽  
Vol 20 (2) ◽  
pp. 149-158
Author(s):  
Shimul Halder ◽  
MAK Azad ◽  
Hrishik Iqbal ◽  
Madhabi Lata Shuma ◽  
Eva Rahman Kabir
Keyword(s):  
Solid Dispersion ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Drug Carriers ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Enhanced Solubility

Bioavailability of a poorly water-soluble drug, e.g., widely used anthelmintic drug Albendazole (ABZ), is very low and thus, to obtain an optimized therapeutic efficacy, the aqueous solubility of such drugs needs to be enhanced. The objective of this study was to develop an effective high drug-loaded solid dispersion (SD) of ABZ with two biocompatible drug carriers, namely Soluplus® and Ludiflash® to improve its physicochemical characteristics. Equilibrium solubility study was performed to choose the optimum polymer ratio among the formulations and it showed up to 50-fold enhanced solubility compared to crystalline ABZ in water. X-Ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) studies of SD-ABZ showed reduced crystallinity of ABZ in the SD. The polymeric carriers, notably Soluplus®, are thought to play a key role in the reduction of crystallinity and molecular polydispersity of ABZ. The dissolution studies in water showed improved dissolution of SD-ABZ compared to crystalline ABZ, with a quick onset of drug release followed by gradual dissolution. However, due to high drug-loading and retention of crystalline ABZ in the sample, the dissolution behavior was not as expected, and may require further studies to optimize the SD-ABZ formulation. Dhaka Univ. J. Pharm. Sci. 20(2): 149-158, 2021 (December)

scholarly journals Heightening the solubility of poorly soluble fenofibrate by Solid Dispersion Technique

2020 ◽  
Vol 11 (1) ◽  
pp. 663-668
Author(s):  
Yasmin Begum M ◽  
Prathyusha Reddy G
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Gastric Fluid ◽  
Lipid Lowering ◽  
Solid Inclusion ◽  
Gastrointestinal Fluid ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Lowering Drug

The intention of the current study was to boost the solubility of Fenofibrate by solid dispersion technique which is an efficient technique in improving the solubility and hence the dissolution rate of poorly soluble drugs in the form of eutectic mixtures by producing fine dispersion when in contact with gastrointestinal fluid and also the technique offers the choices of carriers to be combined with drug conveniently to improve the solubility to a considerable extent. Fenofibrate a BCS class II Antihyperlipidemic drug belongs to fibrate class and it is a lipid-lowering drug used in the treatment of hyperlipidemia. Fenofibrate is insoluble in water and hence shows poor dissolution in gastric fluid with reduced absorption characteristics. In order to improve the solubility, dissolution rate, gastrointestinal absorption and oral bioavailability, it was decided to prepare fenofibrate solid dispersion and evaluated. They were prepared using poly ethylene glycol 4000, 6000, 8000 and β-cyclodextrin by fusion technique and optimized solid dispersion was also lyophilized. Physical characterization of solid inclusion complex of fenofibrate was studied and showed that there were no drug excipients interactions. Dissolution studies showed a momentous rise in a dissolution of Fenofibrate when dispersed in polymers. Inturn aqueous solubility was enlarged linearly as a function of the concentration of β- Cyclodextrin.

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