scholarly journals Dissolution study of Spironolactone by using solid dispersion technique

2012 ◽  
Vol 4 (2) ◽  
pp. 42-47
Author(s):  
Irwin Dewan ◽  
SM Ashraful Islam ◽  
Mohammad Shahriar
Keyword(s):  
Drug Delivery ◽  
Solid Dispersion ◽  
Release Rate ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dispersion Technique

The main objective of the current study was to formulate poorly water soluble drug Spirinolactone by using solid dispersion technique in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. Solid dispersions were prepared using two methods; solvent method and fusion method. Solid dispersion was prepared by using polymers, such as Hydroxy propylymethyl cellulose (HPMC 6cp), Hydroxy propyl cellulose (HPC), Sodium carboxymethylcellulose (Na-CMC), Povidone K12, Povidone K30, Poloxamer 407. Solid dispersions containing Spironolactone with HPC (96.81%), HPMC 6cp (93.05%), Poloxamer 407 (90.84%) and Na-CMC (89.93%) provided higher release rate than the release rate of solid dispersion containing only Spironolactone (35.27%), and Spironolactone with Povidone K12 (76.17%), Povidone K30 (67.92%). So the present study revealed that the solid dispersion may be an ideal means of drug delivery system for poorly water soluble drugs. Further study in this field was required to establish these drug delivery systems so that in future it can be used effectively in commercial basis.DOI: http://dx.doi.org/10.3329/sjps.v4i2.7776S. J. Pharm. Sci. 4(2) 2011: 42-47

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 Solid Dispersions : An Approach to Enhance the Bioavailability of Poorly Water-Soluble Drugs

2013 ◽  
pp. 37-46
Author(s):  
Sanjoy Kumar Das
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Historical Background ◽  
Solid Dosage ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Inert Carrier ◽  
Dispersion Technique

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.

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

scholarly journals NANOSUSPENSION: A MODERN TECHNOLOGY USED IN DRUG DELIVERY SYSTEM

2019 ◽  
pp. 1-3
Author(s):  
HRISHAV DAS PURKAYASTHA ◽  
S. K. IMANUR HOSSIAN
Keyword(s):  
Drug Delivery ◽  
Matrix Material ◽  
Modern Technology ◽  
Water Soluble ◽  
Promising Alternative ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
High Pressure Homogenizer ◽  
Poorly Water Soluble Drug

Nanosuspension consists of the pure poorly water-soluble drug without any matrix material suspended in dispersion. The formulation as nanosuspension is an attractive and promising alternative to solve these problems. Nanosuspension technology solved the problem of drugs which are poorly aqueous soluble and less bioavailability. Stability and bioavailability of the drugs can be improved by Nanosuspension technology. Nanosuspensions are promising candidates that can be used for enhancing the dissolution of poorly water-soluble drugs. Preparation of Nanosuspension is simple and applicable to all drugs which are aqueous insoluble. Nanosuspensions are prepared by using wet mill, high-pressure homogenizer, emulsion‐solvent evaporation, melt emulsification method and supercritical fluid techniques. Nanosuspension can be prepared by using stabilizers, organic solvents and other additives such as buffers, salts, polyols, osmogent and cryoprotectant. Nanosuspensions can be delivered by oral,parenteral, pulmonary and ocular routes. Nanosuspensions can also be used for targeted drug delivery when incorporated in the ocular inserts and mucoadhesive hydrogels.

scholarly journals An Overview on Recent Patents and Technologies on Solid Dispersion

2020 ◽  
Vol 14 (1) ◽  
pp. 63-74 ◽  
Author(s):  
Ritu Kaushik ◽  
Vikas Budhwar ◽  
Deepak Kaushik
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Bioavailability Enhancement ◽  
Molecular Arrangement ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Cryogenic Processing

The oral bioavailability enhancement of poorly water-soluble medicaments is still one of the most complicated aspects of the formulation development. Various approaches are currently available for solubility and rate of dissolution enhancement such as salt formation, solubilization and reduction of particle size, each with its own limitations and advantages. Solid dispersion is one of the most suitable approaches for the formulation development of poorly water-soluble drugs. The popularity of solid dispersion is evident from the increasing number of patent applications and patents granted in this field during recent years. This article reviews the various approaches for the preparation of solid dispersion such as a solvent melting, hot-melt extrusion method, solvent evaporation method, cryogenic processing approaches etc. from the perspective of patents filed or granted for these techniques. Some of the aspects taken into account before the preparation of solid dispersions are carrier selection and physicchemical testing along with an insight into the molecular arrangement of medicaments in solid dispersion. The manuscript further highlights various commercial patented technology platforms such as Solumertm, Hovione and Kinetisol which are based on the concept of solid dispersions.

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.

REVIEW ON FAST DISSOLVING TABLET BY SOLID DISPERSION APPROACH

2021 ◽  
pp. 2840-2845
Author(s):  
V. Namitha
Keyword(s):  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
And Performance ◽  
High Level ◽  
Determining Factor ◽  
Mouth Dissolving Tablet

Tablet is found to be the most popular dosage form among all existing dosage form. However, in certain occurrences as a result of the huge size of dosage forms, and in the uncooperative, pediatric and dysphasia patients, it might make a few problems, to avoid this issues, another type of dosage form is created, which is known as fast dissolving tablet or mouth dissolving tablet. These are the high level dosage form which breaks down within seconds when placed on the toungue. Mouth dissolving tablets have become impressive consideration as a better option in contrast to others because of better convenience to patients. This review discusses the method of preparation, properties, mechanisms; capsules to be incorporated inside the mouth dissolving pill and evaluation of the drugs are emphasized. The solid dispersion is one of the established solubilization techniques for poorly water-soluble drugs. It is basically the interaction between drug and polymer, and hence it is found to be the determining factor in its design and performance. This review additionally summarizes our knowledge on solid dispersions both in the solid as well as liquid state.

Nano-sized Solid Dispersions for Improving the Bioavailability of Poorly Water-soluble Drugs

2020 ◽  
Vol 26 (38) ◽  
pp. 4917-4924
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Release Rate ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Water Soluble ◽  
Drug Bioavailability ◽  
Poorly Water Soluble Drugs ◽  
High Drug ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

It has been well established that solid dispersions have a high potential to increase the release rate of poorly water-soluble drugs, resulting in high drug bioavailability. Solid dispersions have been vigorously investigated with various practical approaches in recent decades. Improvements in wettability, molecular interactions and drugs being held in an amorphous state in solid dispersions are the main mechanisms underlying the high drug release rate. Moreover, the synergistic effect of incorporating nanotechnology in solid dispersions is expected to lead to an advanced drug delivery system for poorly water-soluble drugs. However, to date, there is still a lack of reviews providing outlooks on the nano-sized solid dispersions that have been substantially investigated for improving the bioavailability of poorly water-soluble drugs. In the current review, we aim to overview key advantages and approaches for producing nano-sized solid dispersions. The classification of key strategies in developing nano-sized solid dispersions will advance the creation of even more efficient solid dispersions, which will translate into clinical studies.

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