Preparation and evaluation of flurbiprofen dry elixir as a novel dosage form using a spray-drying technique

The conventional “top-down”, “bottom-up” and “combination” approaches of generating drug nanocrystals produce a “nanosuspension” (NS). It requires significant downstream processing for drying the liquid by suitable means followed by its granulation to develop an oral solid dosage form (OSD). In this paper, we used a novel, spray drying-based NanoCrySP technology for the generation of drug nanocrystals in the form of nanocrystalline solid dispersion (NCSD). We hypothesized that the NCSD would require minimal downstream processing since the nanocrystals are obtained in powder form during spray drying. We further compared downstream processing of NS and NCSD of diclofenac acid (DCF) prepared by wet media milling and NanoCrySP technology, respectively. The NS and NCSD were characterized for crystallinity, crystal size, assay and dissolution. The NCSD was physically mixed with 0.3% Aerosil® 200, 1.76% croscarmellose sodium (CCS) and 0.4% sodium stearyl fumarate (SSF) and filled into size 0 hard gelatin capsules. The NS was first wet granulated using Pearlitol® SD 200 (G1 granules) and Celphere® 203 (G2 granules) in a fluidized bed processor, and the resulting granules were mixed using the same extra granular excipients as NCSD and filled into capsules. A discriminatory dissolution method was developed to monitor changes in dissolution behavior due to crystal growth during processing. Cost analysis and comparison of process efficiency was performed using an innovation radar tool. The NS and NCSD were successfully fabricated with a crystal size of 363 ± 21.87 and 361.61 ± 11.78, respectively. In comparison to NCSD-based capsules (65.13%), the G1 and G2 granules showed crystal growth and decrease in dissolution to 52.68% and 48.37%, respectively, in 120 min. The overall cost for downstream processing of NCSD was up to 80% lower than that of NS. An innovation radar tool also concluded that the one-step NanoCrySP technology was more efficient and required less downstream processing than the two-step wet media milling approach for conversion of nanocrystals to OSD.

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Práškové částice pro plicní podání

Chemické listy ◽

10.54779/chl20220028 ◽

2022 ◽

Vol 116 (1) ◽

pp. 28-34

Author(s):

Jakub Karas ◽

David Vetchý ◽

Jan Gajdziok

Keyword(s):

Drug Delivery ◽

Present Article ◽

Spray Drying ◽

Active Ingredient ◽

Active Substance ◽

Porous Particles ◽

Production Processes ◽

Effective Option ◽

Aerodynamic Parameters ◽

Preparation And Evaluation

The deposition of a drug to its required destination is crucial for effective lung treatment. It is important to design a suitable formulation that delivers the active ingredient to the desired site and resists the natural cleansing mechanisms of the airways. Large porous particles used as active substance carriers appear to be the most effective option for lung drug delivery. The present article provides a basic overview of the mechanisms of deposition of dry inhalable powders and methods of their preparation and evaluation. Spray drying together with micronization and crystallization techniques are among the most used methods of preparation of the discussed particles. Besides, these techniques can be combined with other production processes (encapsulation, emulsification, etc.). The evaluation of the properties of particles suitable for pulmonary application is based on specific requirements for their density, porosity, shape, aerodynamic parameters, and deposition in the lungs, which can now be simulated on an accurate model of artificial lungs.

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Preparation and evaluation of granisetron chewable pediatric oral jelly

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v9i3.4 ◽

2019 ◽

Vol 9 (o3) ◽

Author(s):

Zahraa Mohammed Kadhim* ◽

Wedad K. Ali*

Keyword(s):

Dosage Form ◽

Physical Stability ◽

Drug Efficacy ◽

Content Uniformity ◽

Solid Dosage Forms ◽

Solid Dosage ◽

Natural Substances ◽

Evaluation Test ◽

Preparation And Evaluation ◽

General Appearance

The aim of this study was to formulate granisetron (GSN) in a new dosage form using natural substances and to improve pediatric patient compliance to achieve maximum drug efficacy. GSN is a 5HT3 receptor antagonist that used as prophylaxis for prevention of nausea and vomiting before radiotherapy and chemotherapy. This dosage form was selected because of sharing both the advantages of liquid and solid dosage forms. In this study, two types of natural jellifying agents have been used in different concentrations. The natural jellifying agents which have been used were gelatin and caragennan (CRG). The effect of jellifying agent and their concentrations have been investigated. Six formulations of (GSN) oral jellies were prepared by heat and congealing method and the prepared jellies were evaluated by measuring their pH, content uniformity, drug-polymer compatibility, syneresis, physical stability, general appearance and production yield. Among the prepared formulations, formulation F1 with 4.5% gelatin was considered the best one, since it gave the highest drug release 99.4% in 15 min with acceptance results for all other evaluation test.

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