Enhanced release rate of the poorly water-soluble ginsenoside Rg3 with ordered meso/macroporous silica

2021 ◽  
Author(s):  
Ming Wu ◽  
Jing Xu ◽  
Xiong Lin ◽  
Xin Zhan ◽  
Kunyu Xiao ◽  
...  
Keyword(s):  
Release Rate ◽  
Water Soluble ◽  
Ginsenoside Rg3 ◽  
Macroporous Silica ◽  
Poorly Water Soluble

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

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.

scholarly journals DEVELOPMENT OF NATURAL AND MODIFIED GUM BASED SUSTAINED-RELEASE FILM-COATED TABLETS CONTAINING POORLY WATER-SOLUBLE DRUG

2019 ◽  
pp. 266-271
Author(s):  
AJAY KUMAR SHUKLA ◽  
RAM SINGH BISHNOI ◽  
MANISH KUMAR ◽  
C.P. JAIN
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
In Vitro Release ◽  
Release Profile ◽  
Water Soluble ◽  
The Core ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Seed Gum ◽  
Poorly Water Soluble Drug

Objective: The objective of this work was to the development of natural and modified gum based sustained-release film-coated tablets containing poorly water-soluble drug. Methods: Tamarind seed gum (TSG), fenugreek seed gum (FSG), sodium trimetaphosphate, hydroxypropyl methylcellulose (HPMC), sodium alginate (SA), and nifedipine (NFD) were used. The core tablets of nifedipine were prepared and evaluated for weight, diameters, thickness, hardness, and disintegration time. The core tablets were coated using 2% w/v solution of TSG, MTSG, FSG, and MFSG. The in vitro release rate of drug from these coated tablets was compared with the release rate of drug from the tablets coated with 2% w/v of HPMC. Results: The tablets coated with natural and modified TSG sustained the release of the drug up to 11 h and 14 h, respectively, and natural and modified FSG sustained release the drug up to 9 h and 11 h, respectively. The tablets coated with HPMC sustained released the drug up to 15 h. The drug release profile of tablets coated with modified TSG was comparable to the release profile of tablets coated with HPMC. Conclusion: On the basis of the release profile, it is concluded that unmodified and modified TSG can be used as release rate-controlling membrane.

NANO-SIZED SOLID DISPERSION OF A POORLY WATER-SOLUBLE DRUG

2012 ◽  
pp. 31-35
Author(s):  
Truong Dinh Thao Tran ◽  
Ha Lien Phuong Tran ◽  
Nghia Khanh Tran ◽  
Van Toi Vo
Keyword(s):  
Drug Release ◽  
Droplet Size ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Particle Size Reduction ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Purposes: Aims of this study are dissolution enhancement of a poorly water-soluble drug by nano-sized solid dispersion and investigation of machenism of drug release from the solid dispersion. A drug for osteoporosis treatment was used as the model drug in the study. Methods: melting method was used to prepare the solid dispersion. Drug dissolution rate was investigated at pH 1.2 and pH 6.8. Drug crystallinity was studied using differential scanning calorimetric and powder X-ray diffraction. In addition, droplet size and contact angle of drug were determined to elucidate mechanism of drug release. Results: Drug dissolution from the solid dispersion was significantly increased at pH 1.2 and pH 6.8 as compared to pure drug. Drug crystallinity was changed to partially amorphous. Also dissolution enhancement of drug was due to the improved wettability. The droplet size of drug was in the scale of nano-size when solid dispersion was dispersed in dissolution media. Conclusions: nano-sized solid dispersion in this research was a successful preparation to enhance bioavailability of a poorly water-soluble drug by mechanisms of crystal changes, particle size reduction and increase of wet property.

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

Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

2020 ◽  
Vol 15 ◽  
Author(s):  
Balaji Maddiboyina ◽  
Vikas Jhawat ◽  
Gandhi Sivaraman ◽  
Om Prakash Sunnapu ◽  
Ramya Krishna Nakkala ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Rate ◽  
Zero Order ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Crystalline Cellulose ◽  
Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

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