scholarly journals DEVELOPMENT OF NANOCRYSTAL FORMULATION WITH IMPROVED DISSOLUTION

2018 ◽  
Vol 8 (5) ◽  
pp. 118-129 ◽  
Author(s):  
Jaspreet Kaur Saini ◽  
Sandeep Kumar
Keyword(s):  
Dissolution Rate ◽  
Surface Area ◽  
Therapeutic Index ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Pharmaceutical Applications ◽  
Interesting Approach ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
The One

With the advancement in modern pharmaceutical technologies, Nanotechnology is the one of the most establish technology which is used to improve the therapeutic index and to overcome the formulation challenges of poorly water-soluble compounds. Nanocrystals, in nano range, is the interesting approach for poorly soluble drugs. Due to the small size, increased surface area enhanced the dissolution rate and solubility of drug. In this paper, current technologies and methods in nanocrystal preparation, stabilization, pharmaceutical applications and limitations of nanocrystal are reviewed. Keywords: Nanocrystal, limitations, stabilization, preparation, applications

scholarly journals Enhancement of solubility and dissolution rate of poorly water soluble raloxifene using microwave induced fusion method

2013 ◽  
Vol 49 (3) ◽  
pp. 571-578 ◽  
Author(s):  
Payal Hasmukhlal Patil ◽  
Veena Sailendra Belgamwar ◽  
Pratibha Ramratan Patil ◽  
Sanjay Javerilal Surana
Keyword(s):  
Dissolution Rate ◽  
Hydroxypropyl Methylcellulose ◽  
Microwave Treatment ◽  
Water Soluble ◽  
Fusion Method ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Wetting Properties ◽  
Poorly Soluble ◽  
Poorly Water Soluble

The objective of the present work was to enhance the solubility and dissolution rate of the drug raloxifene HCl (RLX), which is poorly soluble in water. The solubility of RLX was observed to increase with increasing concentration of hydroxypropyl methylcellulose (HPMC E5 LV). The optimized ratio for preparing a solid dispersion (SD) of RLX with HPMC E5 LV using the microwave-induced fusion method was 1:5 w/w. Microwave energy was used to prepare SDs. HPMC E5 LV was used as a hydrophilic carrier to enhance the solubility and dissolution rate of RLX. After microwave treatment, the drug and hydrophilic polymer are fused together, and the drug is converted from the crystalline form into an amorphous form. This was confirmed through scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) studies. These results suggested that the microwave method is a simple and efficient method of preparing SDs. The solubility and dissolution rate of the SDs were increased significantly compared with pure RLX due to the surfactant and wetting properties of HPMC E5 LV and the formation of molecular dispersions of the drug in HPMC E5 LV. It was concluded that the solubility and dissolution rate of RLX are increased significantly when an SD of the drug is prepared using the microwave-induced fusion method.

Combined Use of Polymers and Porous Materials to Enhance Cinnarizine Dissolution

2019 ◽  
Vol 25 (4) ◽  
pp. 331-337
Author(s):  
Maryam Maghsoodi ◽  
Fatemeh Shahi
Keyword(s):  
Porous Materials ◽  
Dissolution Rate ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Water Soluble Drug ◽  
Dissolution Behaviour ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Precipitation Inhibitor ◽  
Poorly Water Soluble

Background: Loading of poorly water-soluble drugs on the porous materials has attracted great interest as an effective approach for enhancement of dissolution rate of drugs. The Aerosil (Ae) with porous structure is expected to facilitate the dissolution of drugs which is generally associated with precipitation. Thus, the purpose of this investigation was thus to develop a formulation which combines a precipitation inhibitor and a poorly soluble drug loaded Ae. Methods: A poorly water-soluble drug, Cinnarizine (CNZ) was used as a model, and Eudragit L100 (Eu) was used as a precipitation inhibitor. Formulations were produced by solvent evaporation and characterized by FT-IR and differential scanning calorimetry (DSC). Dissolution experiments were carried out in phosphate buffer (pH 6.8) under non-sink conditions. Results: DSC thermograms revealed that no crystalline structure of CNZ was present in CNZ-loaded Ae formulations and no long-range order was arranged upon loading of CNZ into Ae. In dissolution test, the CNZ-loaded Ae physically blended with Eu achieved a remarkedly higher CNZ concentration over the plain CNZ and over the CNZ-Eu co-loaded Ae. The dissolution rate of CNZ from the CNZ-loaded Ae was enhanced with increasing Ae amount and the dissolution was maximum when the ratio of CNZ: Ae was 1:10 CNZ: Ae. In addition, the precipitation inhibition was increased when the amount of Eu was high. Conclusion: The results of this work revealed that the dissolution behaviour of CNZ-loaded Ae is enhanced by physically blending of Eu as a suitable precipitation inhibitor.

Pharmacosomes as Drug Delivery System: An Overview

2021 ◽  
pp. 122-127
Author(s):  
Nikita D. Gidde ◽  
Indrayani D. Raut ◽  
Manojkumar M. Nitalikar ◽  
Shrinivas K. Mohite ◽  
Chandrakant S. Magdum
Keyword(s):  
Chemical Structure ◽  
Complex Form ◽  
Colloidal Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Phospholipid Ratio ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
The Cost ◽  
Harmful Effects

Pharmacosomes are the colloidal dispersions of drugs covalently bound to lipids and can exist, depending on the chemical structure, as ultrafine vesicular, micellar, or hexagonal aggregates. Because of the linking of a drug (pharmakon) to a carrier (soma), they are rightly termed "pharmacosomes."Pharmacosomes can be characterized as a neutral molecule with both positive and negative charges, water-loving and fat-loving characteristics, and in complex form, an ideal polyphenol-to-phospholipid ratio. Pharmacosomes are amphiphilic lipid vesicular systems that have demonstrated their ability to increase the bio-accessibility of poorly water-soluble and poorly lipophilic medicines. Drug pharmacosomes provide an effective method of delivering the drug directly to the infection site, which contributes to a lowering in drug toxicity without harmful effects, and also lowers the cost of therapy by improving the drug's bioavailability, particularly in the case of poorly soluble drugs. Pharmacosomes are appropriate to incorporate both hydrophilic and lipophilic drugs. Pharmacosomes have been designed for multiple anti-inflammatory medications that are non-steroidal, neurological, and antineoplasty.

scholarly journals Enhancement of solubility of poorly soluble drugs by solid dispersion: An Overview

2017 ◽  
Vol 5 (04) ◽  
pp. 17-23
Author(s):  
Katta Manogna ◽  
P. Nagaveni ◽  
K. Thyagaraju
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Drug Solubility ◽  
Solid Dosage Forms ◽  
Preparation Methods ◽  
Solid Dosage ◽  
Poorly Soluble ◽  
Poorly Water Soluble

Most of the newly invented chemical drug moieties are poorly water soluble. According to BCS classification, class II and IV drugs are considered as poorly water soluble. So enhancement of oral absorption and bioavailability of solid dosage forms remains a challenge to formulation scientists due to their solubility criteria. Therefore many techniques are being explored to enhance the solubility of poor soluble drugs. Solid dispersion is one of the most important method for enhance the solubility (dissolution rate) and hence oral bioavailability of poorly soluble drugs. In solid dispersion the particle size of drug is reduced or a crystalline pure drug is converted into amorphous form and hence the solubility is increased. Polymer incorporating in solid dispersion technology is usually hydrophilic in nature and also showing compatibility with the drug to enhance the drug solubility. This review mainly discus about solid dispersion, preparation methods, and finally characterization.

scholarly journals Solid Dispersion: Solubility Enhancement Technique of Poorly Water Soluble Drug

2020 ◽  
Vol 10 (1) ◽  
pp. 173-177 ◽  
Author(s):  
, Ikram ◽  
Kapil Kumar
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Inert Carrier ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Solid dispersion is a technique which is widely and successfully applied to improve the solubility, dissolution rates and consequently the bioavailability of poorly soluble drugs. Dispersion of one or more active ingredients (hydrophobic) is done with an inert carrier (hydrophilic) at solid-state prepared by fusion method, solvent, and melting solvent method. In this review article, we have focused on the methods of preparation, advantages, disadvantages and characterization of the solid dispersions. Keywords: Solid dispersion; dissolution; solubility.

scholarly journals A Review on Self Micro Emulsifying Drug Delivery System: An Approach to Enhance the Oral Bioavailability of Poorly Water Soluble Drug

1970 ◽  
Vol 8 (3) ◽  
pp. 202-208
Author(s):  
Mamta Patil ◽  
Shobha Palde ◽  
Amol Deshmukh
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Oral Bioavailability ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
The One ◽  
Lipid Vehicle ◽  
Poorly Water Soluble Drug

Self-micro emulsifying drug delivery framework is the one of the methodology for improving the solvency of the hydrophobic medication. The medications which are insoluble in water can be formulated in this technique by solubilizing it in the lipid vehicle to absorb through the membrane. The lipid and surfactants are utilized to build the solvency of the drug and improve absorption. This improves the dissolution rate of the drug by expanding its solubility. A large number of the obstacles and arrangements are depicted in this article. This system picked up consideration as it likewise improves the bioavailability of the drug. This article has total survey about SMEDDS for present work and for future viewpoint too.  

Enhancement of Solubility and Dissolution Rate of Poorly Water Soluble Drug using Cosolvency and Solid Dispersion Techniques

1970 ◽  
Vol 1 (4) ◽  
pp. 349-356
Author(s):  
Meka Lingam ◽  
Vobalaboina Venkateswarlu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

The low aqueous solubility of celecoxib (CB) and thus its low bioavailability is a problem.    Thus, it is suggested to improve the solubility using cosolvency and solid dispersions techniques. Pure CB has solubility of 6.26±0.23µg/ml in water but increased solubility of CB was observed with increasing concentration of cosolvents like PEG 400, ethanol and propylene glycol. Highest solubility (791.06±15.57mg/ml) was observed with cosolvency technique containing the mixture of composition 10:80:10%v/v of water: PEG 400: ethanol. SDs with different polymers like PVP, PEG were prepared and subjected to physicochemical characterization using Fourier-transform infrared (FTIR) spectroscopy, X-ray diffractometry (XRD), differential scanning calorimetry (DSC), solubility and dissolution studies. These studies reveals that CB exists mainly in amorphous form in prepared solid dispersions of PVP, PEG4000 and PEG6000 further it can also be confirmed by solubility and dissolution rate studies. Solid dispersions of PV5 and PV9 have shown highest saturation solubility and dissolution rate

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