scholarly journals Preparation of solid dispersion of rutin by spay drying

2019 ◽  
Vol 35 (2) ◽  
Author(s):  
Nguyen Van Khanh ◽  
Ta Thi Thu ◽  
Hoang Anh Tuan
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Flow Rate ◽  
Solid Dispersions ◽  
Tween 80 ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Pvp K30

Abstract: The poor solubility of rutin leads to poor bioavailability. The present study is aimed to increase the solubility and bioavailability of rutin using solid dispersion technique. The solid dispersions of rutin were prepared by spray-dried method using β-CD, HPMC E6, HPMC E15, PVP K30, SLS, poloxamer 188 and Tween 80 as carriers. The interaction of rutin with the carriers was evaluated by using methods such as dissolved measurement, Fourier-transformation infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The optimization of formulation was carried out by using Central Composite Face design. Independent variables include PVP K30/rutin ratio, Tween 80/rutin ratio, inlet air temperature, and feed flow rate. Dependent variables are the dissolution and product yield. The optimized preparation conditions for rutin solid dispersions were obtained as PVP K30: rutin at a ratio of 5.77, Tween 80: rutin at a ratio of 0.14, inlet temperature of 110.05, flow rate of 1370.9 ml per hour. The results of this study indicate that the solid dispersion of rutin increases significantly the dissolution of rutin in comparison with rutin. The results of the DSC and XRD studies prove the state transition of rutin from crystalline to amorphous. Keywords Rutin, solid dispersion, spray drying, PVP K30, dissolution. References [1] Beatriz Gullón, Thelmo A. Lú-Chau, María Teresa Moreira, Juan M. Lema, Gemman Eibes, Rutin: A review on extraction, identification and purification methods, biological activities and approaches to enhance its bioavailability, Trends in Food Science & Technology 67 (2017) 220-235. https://doi.org/10.1016/j.tifs.2017.07.008.[2] Carla Aparecida Pedriali, Adjaci Uchoa Fernandes, Leandra de Cássia Bernusso, Bronislaw Polakiewicz, The synthesis of a water-soluble derivative of rutin as an antiradical agent, Química Nova 31(8) (2008) 2147-2151. http://dx.doi.org/10.1590/S0100-40422008000800039.[3] Chiou, Win Loung, Riegelman, Sidney, Pharmaceutical applications of solid dispersion systems, Journal of pharmaceutical sciences 60(9) (1971) 1281-1302. https://doi.org/10.1002/jps.2600600902.[4] Xingwang Zhang, Huijie Xing,Yue Zhao, Zhiguo Ma, Pharmaceutical Dispersion Techniques for Dissolution and Bioavailability Enhancement of Poorly Water-Soluble Drugs, Pharmaceutics 10(3) (2018) 1-33. https://doi.org/10.3390/pharmaceutics10030074.[5] Ladan Akbarpour Nikghalb, Gurinder Singh, Gaurav Singh, Kimia Fazaeli Kahkeshan, Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs, Journal of Applied Pharmaceutical Science 2(10) (2012) 170-175. https://doi.org/10.7324/JAPS.2012.2103.[6] Amrit Paudel, Zelalem Ayenew Worku, Joke Meeus, Sandra Guns, Guy Van den Mooter, Manufacturing of solid dispersions of poorly water soluble drugs by spray drying: formulation and process considerations, International Journal of Pharmaceutics 453(1) (2013) 253-284. https://doi.org/10.1016/j.ijpharm.2012.07.015.[7] P.B. Dalvi, A.B. Gerange, R. IngaleP, Solid dispersion: strategy to enhance solubility, Journal of Drug Delivery & Therapeutics 5(2) (2015) 20-28. https://doi.org/10.22270/jddt.v5i2.1060.[8] Chau Le Ngoc Vo, Chulhun Park, Beom Jin Lee, Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs. European Journal of Pharmaceutics and Biopharmaceutics 85(3) (2013) 799-813. https://doi.org/10.1016/j.ejpb.2013.09.007.[9] I.V. Koval’skii, I.I. Krasnyuk, I.I. Krasnyuk, O.I. Nikulina, A.V. Belyatskaya, Yu. Ya. Kharitonov, N.B. Fel’dman, S.V. Lutsenko, V.V. Grikh, Studies of the Solubility of Rutin from Solid Dispersions, Pharmaceutical Chemistry Journal 47(11) (2014) 612-615. https://doi.org/10.1007/s11094-014-1020-z.  

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

scholarly journals NOVEL APPLICATION OF MIXED HYDROTROPIC SOLUBILIZATION TECHNIQUE IN THE FORMULATION AND EVALUATION OF SOLID DISPERSION OF FLUPIRTINE MALEATE

2018 ◽  
Vol 8 (5) ◽  
pp. 481-488
Author(s):  
Nisha Kumari Yadav ◽  
Tripti Shukla ◽  
Neeraj Upmanyu ◽  
Sharad Prakash Pandey ◽  
Mohammad Azaz Khan
Keyword(s):  
Particle Size ◽  
Solid Dispersion ◽  
Sodium Benzoate ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Evaporation Technique ◽  
Poorly Water Soluble

Flupirtine is an amino pyridine derivative that functions as a centrally acting non-opioid, non-steroidal analgesic. It is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Its muscle relaxant properties make it popular for back pain and other orthopedics uses. In the present investigation, recently developed mixed hydrotropic solid dispersion technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. Mixed-hydrotropic solubilisation technique is the experience to increase the solubility of poorly water soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. The Flupirtine loaded solid dispersion was prepared by a solvent evaporation technique using sodium benzoate and a niacinamide hydrotropic mixture. The prepared solid dispersions were valuated regarding their solubility, mean particle size, in-vitro drug release. The prepared solid dispersions were found very stable (chemically). The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability. Keywords: Flupirtine, Solid dispersion, Mixed-hydrotropic solubilisation, Solvent evaporation technique, Sodium benzoate, Niacinamide

Surface Solid Dispersion – A Review

2013 ◽  
Vol 6 (1) ◽  
pp. 1915-1925
Author(s):  
Sadhna Khatry ◽  
Neha Sood ◽  
Sandeep Arora
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
High Surface ◽  
High Surface Area ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Water Soluble

Preparation of an effective formulation of poorly water-soluble drugs is a key challenge in pharmaceutical technology. Dissolution rate and solubility are the rate- limiting steps for increasing the bioavailability of poorly water‐soluble drugs. Solid dispersion is an efficient technique for improving dissolution rate and subsequently, the bioavailability of poorly water‐soluble drugs. Surface sSolid dDispersion is a novel technique of solid dispersion for dispersing one or more active ingredients on a water insoluble carrier of high surface area in order to achieve increased dissolution rates and bioavailability of insoluble drugs. The Vvarious polymers used in this technique are Avicel, Crosspovidone, sSodium starch glycolate, pPregelatinized starch, Cab-o-sil, Ac-di-sol, KyronT-314, Primojel and pPotato sStarch. This article reviews the various methods of preparation and characterization of surface solid dispersion and compiles some of the drugs formulated as surface solid dispersions. Some of the practical aspects to be considered for preparing surface solid dispersion are selection of a suitable carrier and method of preparation of surface solid dispersion.

scholarly journals SOLID DISPERSION - A NOVEL APPROACH FOR BIOAVAILABILITY ENHANCEMENT OF POORLY WATER-SOLUBLE DRUGS IN SOLID ORAL DOSAGE FORMS

2019 ◽  
pp. 17-26
Author(s):  
PURNACHANDRA REDDY GUNTAKA ◽  
SRINIVAS LANKALAPALLI
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Oral Dosage ◽  
Bioavailability Enhancement ◽  
Poorly Water Soluble Drugs ◽  
Novel Approach ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of the bioavailability of poorly water-soluble drugs is a challenging task in drug development. Currently 40% of new chemical entities are discovered as poorly water-soluble drugs. Solid dispersion is one of the best technology for improving solubility, dissolution rate, and bioavailability. Solid dispersion techniques are more useful for enhancing drug solubility for a combination of drug and inert carrier to improve wettability, reduced particle size, and converting amorphous particles. This article reviews various advantages, methods of solid dispersions, carriers used in solid dispersion, characterization, and marketed products.

Modulation of Drug Crystallization and Molecular Interactions by Additives in Solid Dispersions for Improving Drug Bioavailability

2019 ◽  
Vol 25 (18) ◽  
pp. 2099-2107 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Wei Duan ◽  
Beom-Jin Lee ◽  
Thao T.D. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Drug Bioavailability ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Potential Applications ◽  
Poorly Water Soluble ◽  
The Right

Background:: An increase in poorly water-soluble drugs makes the design of drug delivery systems challenging. Methods:: Currently, a number of prospective solid dispersions have been investigated with potential applications for delivering a variety of poorly water-soluble drugs. A number of traditional solid dispersions and modifiedsolid dispersions offer attractive advantages in the fabrication, design and development of those drugs for effective therapeutics. Results:: Although traditional solid dispersions can produce a higher release rate, resulting in higher bioavailability compared to conventional dosage forms, this method is not always a promising approach. Modified-solid dispersion has demonstrated both the ability of its polymers to transform drug crystals into amorphous forms and molecular interactivity, thereby improving drug dissolution rate and bioavailability, especially with tough drugs. However, the classification of modified-solid dispersion, which guides the selection of the right strategy in solid dispersion preparation, remains ill-defined. Conclusions:: This review focused on effective strategies in using additives in solid dispersion for improving drug bioavailability.

ENHANCED DISSOLUTION OF A POORLY WATER-SOLUBLE DRUG BY SOLID DISPERSIONS (SOLVENT EVAPORATION) TECHNIQUE

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 13-19
Author(s):  
R. O Sonawane ◽  
◽  
S. Nayak ◽  
M. D. Chaudhari ◽  
V. V. Pande
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Differential Scanning Calorimetric ◽  
Maximum Enhancement ◽  
Enhanced Dissolution ◽  
Water Soluble Drugs ◽  
Fusion Methods ◽  
Poorly Water Soluble

The poorly water soluble drugs tend to have low bioavailability and this can be improved by several methods. Solid dispersion is a promising formulation approach to improve solubility and dissolution and ultimately oral bioavailability of these drugs. The aim of this study was to prepare and characterize solid dispersion of anti-diabetic glimepiride, a BCS class II drug, with the hydrophilic carrier PVP K30 by solvent evaporation and microwave induced fusion methods. Scanning electron microscopy (SEM), X–ray powder diffractometry (XRD) and differential scanning calorimetric (DSC) were used to evaluate the physical state of the drug. The solid dispersions were also evaluated for drug content, solubility and dissolution studies. Solid dispersions prepared by solvent evaporation method were showed maximum enhancement of solubility and dissolution in comparison to that prepared by other method.

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: RESUSCITATING ORAL DELIVERY OF HYDROPHOBIC DRUGS

2019 ◽  
pp. 213-217
Author(s):  
RUCHI AGRAWAL ◽  
ABID RAZA ◽  
OM PRAKASH PATEL
Keyword(s):  
Oral Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Future Trends ◽  
Hydrophobic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Viable Method

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

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