Preformulation Study of a Poorly Water-Soluble Drug, α-Pentyl-3-(2-quinolinylmethoxy)benzenemethanol: Selection of the Base for Dosage Form Design

Solubilization of poorly soluble drugs is a frequently encountered challenge in screening studies of newchemical entities as well as in formulation design and development. Solubility of some drugs is very less; thesedrug molecules are often lipophilic and hence dissolution may be a problem in drug absorption from solid oraldosage forms. The increasing interest of the technology of dosage form with natural biopolymers has becomethe reason for undertaking present investigation on the possibility of modification of guar gum application inthe preparation of an oral solid dosage form of a poorly water soluble drug. Present study examines the effect ofmodified guar gum on the solubility of a poorly water-soluble Nevirapine. Modified guar gum was preparedusing heat treatment (110-120oC for 2 hours) method. It was characterized for viscosity and swelling index etc.The physical and co-grinding mixtures of Nevirapine with modified guar gum were prepared in 1:4 drugs togum ratio. The physical and co-grinding mixtures were characterized by DSC and FT-IR study. The studiesconfirmed that there was no interaction between drug and carrier. Prepared mixtures were evaluated forsolubility study and in vitro dissolution studies. The results of present investigation indicated that modified guargum can be a used for the development of oral dosage form with increased solubility and hence improveddissolution and oral bioavailability of poorly water soluble drug.

Download Full-text

Formulation and development of vaginal films of poorly water soluble drug, metronidazole, using mixed solvency concept and their evaluations

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i6.2085 ◽

2018 ◽

Vol 8 (6) ◽

pp. 41-48 ◽

Cited By ~ 2

Author(s):

Neha Gahlot ◽

Rajesh Kumar Maheshwari

Keyword(s):

Dosage Form ◽

Research Work ◽

Cost Effective ◽

Stability Study ◽

Water Soluble ◽

High Concentration ◽

Disintegration Time ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

Aim: To deliver antibacterial therapy in an efficacious way, film dosage form has been proposed for drug delivery in vagina which can overcome bioavailability issues of poorly water soluble drugs. The present research work is aimed to explore the application of mixed solvency concept to increase solubility of poorly water soluble drug, metronidazole. Materials and Methods: Metronidazole, a slightly soluble drug in water was tried to be solubilized by employing the combination of solubilizers like niacinamide, sodium benzoate, sodium caprylate, caffeine and urea to endeavour its fast dissolving film formulations. The procured sample of drug was characterized by UV, IR and DSC studies. The formulations were evaluated for various properties of film such as thickness, folding endurance, surface pH, disintegration time and thin layer chromatography. Stability studies of vaginal films of metronidazole were performed for ten weeks at room temperature, and refrigerated conditions. Results and Discussion: It was found that 97.54% and 97.58% of drug was remaining after stability study at respective temperatures in batch F1 and 98.53% and 96.57% in batch F4.Conclusion: It was concluded that the approach of mixed solvency concept is novel, safe, cost-effective and user friendly. It also eliminates the problem of toxicity associated with high concentration of water-soluble solubilizers. So, it may be employed in dosage form development of drugs with poor solubility to overcome bioavailability issues. Keywords: Solubility, metronidazole, vaginal films, mixed solvency concept.

Download Full-text

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

Journal of Medicine and Pharmacy ◽

10.34071/jmp.2012.5.4 ◽

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.

Download Full-text

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.4.6 ◽

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

Download Full-text