In vitro testing of ciprofloxacin formulations and preliminary study on BCS biowaiver

Kyriacos, Soula; Boukarim, Chawki; Safi, William; Mroueh, Mohamad; Maroun, Aline Bou; El-Khoury, Ghada; Shehayeb, Rabih

doi:10.38212/2224-6614.2298

Cited by 4 publications

(5 citation statements)

References 6 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The single spots implied that there were no impurities. While this study indicated no impurities, Kyriacos and coworkers [26] found impurities ethylenediamine, desfluorociprofloxacin and fluoroquinolonic acid -which were not more than 0.2% and were therefore within limits. This study employed TLC while Kyriacos and co-workers utilized HPLC.…”

Section: Microbiological Evaluationcontrasting

confidence: 58%

See 1 more Smart Citation

Quality attributes of twenty-nine brands of ciprofloxacin: post-marketing in vitro analyses, microbiological assay and in vivo simulation

Muhammad¹,

Okpe²,

Olorunfemi³

et al. 2021

J. Pharm Bio.

View full text Add to dashboard Cite

Ciprofloxacin is a fluoroquinolone antibiotic employed to treat infections. There are over three hundred registered generic brands of ciprofloxacin in Nigeria. There has been an observed marked variation in therapeutic or clinical outcome with change in brands by health professionals and patients. In a previous study of six (6) brands we had reported a high degree of inequivalence. In this study, twenty-nine (29) brands of ciprofloxacin were extensively evaluated against compendia requirements. Microbial sensitivity against two test organisms was conducted. In-vitro drug release and in-vivo simulation were established. Analysis of the data generated indicated that all brands passed qualitative test using TLC and disintegration test, six failed hardness test, one failed friability, nine failed antimicrobial assay and six failed percentage content assay. Conclusions drawn from the study for evidence-based clinical decisionwould include the fact that three brands only were found to be bioequivalent to the innovator brand, Ciproxin; while eight brands were bio-inequivalent using the three models of similarity factor (f2), and difference factor (f1) in two media and dissolution efficiency (DE) in pH 4.5. The three brands (Cipro-All, Cifran And Ciprogem) may confidently be used interchangeably with the innovator brand Keywords: Bioequivalence; Ciprofloxacin Drug quality; Generic substitution; Post-marketing surveillance

show abstract

Section: Microbiological Evaluationcontrasting

confidence: 58%

“…Ciprofloxacin has been classified into the 4 classes of Biopharmaceutical Classification System (BCS) by various studies [26,[32][33][34][35][36][37][38][39]. The common class ciprofloxacin is attributed to is Class III (high solubility, low permeability).…”

Section: Microbiological Evaluationmentioning

confidence: 99%

Quality attributes of twenty-nine brands of ciprofloxacin: post-marketing in vitro analyses, microbiological assay and in vivo simulation

Muhammad¹,

Okpe²,

Olorunfemi³

et al. 2021

J. Pharm Bio.

View full text Add to dashboard Cite

show abstract

“…CIF is an efficient medicine widely prescribed for antibiotic therapy, but it has solubility limitations corresponding to biopharmaceutics classification system (BCS) class II or III depending on the pH range. 8 Therefore, to remove this disadvantage, multiple-component compounds such as solvates, co-crystals, or salts, has been employed. [9][10][11] Salts or other structural multi-components are an intensive technique for improving the physicochemical properties of active pharmaceutical compounds (APIs), particularly for solubility.…”

Section: Introductionmentioning

confidence: 99%

Improving aqueous solubility of ciprofloxacin: three different stoichiometric hydrated salt forms with oxalic acid

et al. 2023

View full text Add to dashboard Cite

show abstract

“…The ‘U-shape’ pH-solubility profile of CIP shows that its solubility increases at pH values higher than 8.7 (basic pKa) and lower than 6.1 (acidic pKa) [ 27 ], with the lowest solubility at neutral pH values. Therefore, CIP has been classified as an intermediate compound with BCS Class II/III classification [ 28 ]. In some cases, CIP has been classified as BCS class IV due it low solubility and low permeability, which leads to limited bioavailability [ 29 ].…”

Section: Introductionmentioning

confidence: 99%

Formation of Ciprofloxacin–Isonicotinic Acid Cocrystal Using Mechanochemical Synthesis Routes—An Investigation into Critical Process Parameters

et al. 2022

View full text Add to dashboard Cite

The mechanochemical synthesis of cocrystals has been introduced as a promising approach of formulating poorly water-soluble active pharmaceutical ingredients (APIs). In this study, hot-melt extrusion (HME) as a continuous process and grinding and ball milling as batch processes were employed to explore the feasibility of cocrystallization. Ciprofloxacin (CIP) and isonicotinic acid (INCA) were selected as the model API and coformer. CIP–INCA cocrystal was produced in all techniques. It was revealed that higher cocrystal content could be achieved at longer durations of grinding and ball milling. However, milling for more than 10 min led to increased co-amorphous content instead of cocrystal. A design of experiment (DoE) approach was used for deciphering the complex correlation of screw configuration, screw speed, and temperature as HME process parameters and their respective effect on final relative cocrystal yield. Statistical analysis showed that screw configuration, temperature, and their interaction were the most critical factors affecting cocrystallization. Interestingly, screw speed had minimal impact on the relative cocrystallization yield. Cocrystallization led to increased dissolution rate of CIP in phosphate buffer up to 2.5-fold. Overall, this study shed a light on the potential of mechanochemical synthesis techniques with special focus on HME as a continuous process for producing cocrystals.

show abstract

In vitro testing of ciprofloxacin formulations and preliminary study on BCS biowaiver

Cited by 4 publications

References 6 publications

Quality attributes of twenty-nine brands of ciprofloxacin: post-marketing in vitro analyses, microbiological assay and in vivo simulation

Quality attributes of twenty-nine brands of ciprofloxacin: post-marketing in vitro analyses, microbiological assay and in vivo simulation

Improving aqueous solubility of ciprofloxacin: three different stoichiometric hydrated salt forms with oxalic acid

Formation of Ciprofloxacin–Isonicotinic Acid Cocrystal Using Mechanochemical Synthesis Routes—An Investigation into Critical Process Parameters

Contact Info

Product

Resources

About