Effect of Binary Additive Combinations on Solution Crystal Growth of the Poorly Water-Soluble Drug, Ritonavir

2012 ◽  
Vol 12 (12) ◽  
pp. 6050-6060 ◽  
Author(s):  
Grace A. Ilevbare ◽  
Haoyu Liu ◽  
Kevin J. Edgar ◽  
Lynne S. Taylor
Keyword(s):  
Crystal Growth ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug ◽  
Solution Crystal Growth

scholarly journals Impact of Polymer Conformation on the Crystal Growth Inhibition of a Poorly Water-Soluble Drug in Aqueous Solution

Langmuir ◽  
2014 ◽  
Vol 31 (1) ◽  
pp. 171-179 ◽  
Author(s):  
Caitlin J. Schram ◽  
Stephen P. Beaudoin ◽  
Lynne S. Taylor
Keyword(s):  
Aqueous Solution ◽  
Crystal Growth ◽  
Growth Inhibition ◽  
Water Soluble ◽  
Polymer Conformation ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Crystal Growth Inhibition ◽  
Poorly Water Soluble Drug

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

scholarly journals In vivo evaluation of modified gum karaya as a carrier for improving the oral bioavailability of a poorly water-soluble drug, nimodipine

2002 ◽  
Vol 3 (2) ◽  
pp. 55-63 ◽  
Author(s):  
Gedela V. Murali Mohan Babu ◽  
Namballa R. Kumar ◽  
Kasina H. Sankar ◽  
Battu J. Ram ◽  
Namburu K. Kumar ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Water Soluble ◽  
In Vivo Evaluation ◽  
Gum Karaya ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals Effect of Grinding with Hydroxypropyl Cellulose on the Dissolution and Particle Size of a Poorly Water-Soluble Drug.

1999 ◽  
Vol 47 (9) ◽  
pp. 1311-1313 ◽  
Author(s):  
Tatsuhiko YAMADA ◽  
Noriyasu SAITO ◽  
Teruko IMAI ◽  
Masaki OTAGIRI
Keyword(s):  
Particle Size ◽  
Hydroxypropyl Cellulose ◽  
Water Soluble ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

scholarly journals 3D Printing of Dapagliflozin Containing Self-Nanoemulsifying Tablets: Formulation Design and In Vitro Characterization

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 993
Author(s):  
Mohammed S. Algahtani ◽  
Abdul Aleem Mohammed ◽  
Javed Ahmad ◽  
M. M. Abdullah ◽  
Ehab Saleh
Keyword(s):  
3D Printing ◽  
Solid Phase ◽  
Immediate Release ◽  
Water Soluble ◽  
Solid Matrix ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
3D Printing Technique ◽  
Poorly Water Soluble Drug

The 3D printing techniques have been explored extensively in recent years for pharmaceutical manufacturing and drug delivery applications. The current investigation aims to explore 3D printing for the design and development of a nanomedicine-based oral solid dosage form of a poorly water-soluble drug. A self-nanoemulsifying tablet formulation of dapagliflozin propanediol monohydrate was developed utilizing the semisolid pressure-assisted microsyringe (PAM) extrusion-based 3D printing technique. The developed formulation system consists of two major components (liquid and solid phase), which include oils (caproyl 90, octanoic acid) and co-surfactant (PEG 400) as liquid phase while surfactant (poloxamer 188) and solid matrix (PEG 6000) as solid-phase excipients that ultimately self-nanoemulsify as a drug encapsulated nanoemulsion system on contact with aqueous phase/gastrointestinal fluid. The droplet size distribution of the generated nanoemulsion from a self-nanoemulsifying 3D printed tablet was observed to be 104.7 ± 3.36 nm with polydispersity index 0.063 ± 0.024. The FT-IR analysis of the printed tablet revealed that no drug-excipients interactions were observed. The DSC and X-RD analysis of the printed tablet revealed that the loaded drug is molecularly dispersed in the crystal lattice of the tablet solid matrix and remains solubilized in the liquid phase of the printed tablet. SEM image of the drug-loaded self-nanoemulsifying tablets revealed that dapagliflozin propanediol monohydrate was completely encapsulated in the solid matrix of the printed tablet, which was further confirmed by SEM-EDS analysis. The in vitro dissolution profile of dapagliflozin-loaded self-nanoemulsifying tablet revealed an immediate-release drug profile for all three sizes (8 mm, 10 mm, and 12 mm) tablets, exhibiting >75.0% drug release within 20 min. Thus, this study has emphasized the capability of the PAM-based 3D printing technique to print a self-nanoemulsifying tablet dosage form with an immediate-release drug profile for poorly water-soluble drug.

Natural Polymers in Fast Dissolving Tablets

2021 ◽  
pp. 2859-2866
Author(s):  
Ratnaparkhi M.P. ◽  
Karnawat G.R. ◽  
Andhale R.S.
Keyword(s):  
Geriatric Patients ◽  
Nutritional Supplement ◽  
Synthetic Polymers ◽  
Oral Route ◽  
Water Soluble ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

Oral route is most preferable route of administration for various drugs, because it is convenient, economical, safest route. Fast dissolving tablets are popular nowadays, as they disintegrated in mouth within a few seconds without using water for swallow. Problems like Dysphagia in pediatric and geriatric patients have been overcome by formulating Fast dissolving tablet. Natural polymers are preferable because they are chemically inert, nontoxic, less expensive, biodegradable, and available easily than synthetic polymers. Natural polymers are obtained from the natural origin so they are devoid of any side effect. It is proved from the previous studies that Natural polymers are more-safe and effective than the synthetic polymers. Natural polymers improve the properties of tablet and they are used as binder, diluent, superdisintegrant, they also enhance the solubility of poorly water-soluble drug, decrease the disintegration time and provide nutritional supplement. The aim of the present article is to study various natural polymers used in fast dissolving tablets.

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