scholarly journals Novel Application of Mixed Solvency Concept to Develop and Formulate Dry Powder Injection for Reconstitution of a Poorly Water Soluble Drug, Amlodipine Besylate and their Evaluations

2021 ◽  
Vol 11 (4-S) ◽  
pp. 101-108
Author(s):  
Yashi Thakur ◽  
R.K. Maheshwari
Keyword(s):  
Water Soluble ◽  
Oral Dosage ◽  
Poloxamer 407 ◽  
Powder Injection ◽  
Amlodipine Besylate ◽  
Dry Powder ◽  
Synergistic Enhancement ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

In the recent generation of pharmaceutical research, it has been observed that many newly designed and discovered drug products have less water solubility. Thus, leading to difficulties in several developmental, manufacturing and administrative processes. Furthermore, the clinical trials of these drugs have witnessed a great failure due to their poor pharmacokinetics. The lineup of our research work was promotion of mixed solvency concept by formulating the dry powder injection for reconstitution of poorly water-soluble drug amlodipine besylate by decreasing the solubilisers concentration in small proportion for expected synergistic enhancement of drug solubility in water. Solubilisers used are sodium benzoate, sodium caprylate, PVPK-25, sodium citrate, niacinamide, poloxamer 407, sodium acetate, L-arginine, benzoic acid, β-cyclodextrin and lysine hydrochloride to developed the dry powder injection for reconstitution of amlodipine besylate. The reconstitution time of amlodipine besylate injections were found 58 sec, 36 sec and 1 min 10 sec in selected blends. This drug is slightly soluble in water, and it comes in various forms, including tablets and other oral dosage forms. However, no amlodipine besylate dry powder injection or ready-made injections are currently available in the market. Dry powder injection for reconstitution of amlodipine besylate was formulated successfully and mixed solvency concept has been successfully employed. Keywords: Mixed solvency concept, Amlodipine besylate, Dry powder injection for reconstitution, Solubilisers, Solubility.

scholarly journals TECHNOLOGY DVELOPMENT FOR POLYMER MODIFICATION TO ENHANCE SOLUBILITY OF POORLY SOLUBLE DRUG

2018 ◽  
Vol 1 (1) ◽  
pp. 5-9
Author(s):  
Biresh Kumar Sarkar ◽  
Suraj Kumar Mishra ◽  
Suraj Kumar Mishra ◽  
Ajay Krishna Gupta ◽  
Shailendra S Solanki
Keyword(s):  
Dosage Form ◽  
Guar Gum ◽  
Water Soluble ◽  
Oral Dosage ◽  
In Vitro Dissolution ◽  
Polymer Modification ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Water Soluble Drug

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.

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 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.

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