Evaluation of heat-conduction microcalorimetry in pharmaceutical stability studies. IV. The influence of microcrystalline cellulose on the hydration rate of anhydrous lactose

Objective: The present study aimed to improve the rate of dissolution of furosemide by solid dispersion technique. Methods: Solid dispersion of furosemide was prepared by using hydrogel isolated from the seeds of Lepidium sativum as a novel carrier by the solvent evaporation method. Solid dispersion was evaluated to study the improvement in the rate of dissolution. Molecular dispersion of furosemide in the novel carrier was studied by DSC and FTIR studies. Solid dispersion was filled in capsules after stability studies and the formulation was optimized by adopting factorial design. Results: Solid dispersion of furosemide exhibited dissolution improvement from 13.54 % (plain furosemide) to 69.12% (solid dispersion) in the first 60 min. Improvement in dissolution efficiency was found to be retained after stability studies. Capsules were filled with the formulation of solid dispersion using two different grades of lactose-α lactose monohydrate and anhydrous lactose and were found stable after stabilization studies. Conclusion: The dissolution improvement of furosemide was attributed to its molecular dispersion in the novel carrier selected for this study. The recrystallization of furosemide was prevented due to intermolecular interaction between the novel carrier and furosemide. This was confirmed by FTIR. Evaluation of the dissolution data of factorial batches was analyzed by ANOVA. Analysis of the data revealed that selected levels of α lactose monohydrate and anhydrous lactose would be useful to navigate design space.

Download Full-text

Novel Co-processed Spray Dried Super Disintegrants Designing of Fast Dissolving Tablets Using

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v15i2.30933 ◽

2017 ◽

Vol 15 (2) ◽

pp. 167-172

Author(s):

SB Shirsand ◽

RT Gumate ◽

V Jonathan ◽

Shailashri

Keyword(s):

Drug Release ◽

Microcrystalline Cellulose ◽

Phosphate Buffer ◽

Angle Of Repose ◽

Stability Studies ◽

Drying Method ◽

In Vitro Drug Release ◽

Conventional Tablet ◽

Tablet Formulations

In the present study, novel co-processed superdisintegrants were developed by spray drying method using microcrystalline cellulose and mannitol in different ratios (1:1, 1:2 and 1:3) for use in the fast dissolving tablet formulations. The developed excipients were evaluated for angle of repose, Carrs index and Hausners ratio in comparison with physical mixture of superdisintegrants. The angle of repose of the developed excipients was found to be < 30o, Carrs index in the range of 9-15 % and Hausners ratio in the range of 1.12-1.16. Fast dissolving tablets of glibenclamide were prepared using the above co-processed superdisintegrants and evaluated for pre-compression and post-compression parameters. Based on in vitro dispersion time (approximately 22.23 sec), promising formulation MCM3 was tested for in vitro drug release pattern in pH 6.8 phosphate buffer and stability (at 400C/75 % RH for 3 months), drug excipients interaction (IR spectroscopy) were studied. Among the designed formulations, the formulation (MCM3) containing 8 % w/w of co-processed superdisintegrant (1:3 mixture of microcrystalline cellulose and mannitol) emerged as the overall best formulation (t50% 1.6 min) based on drug release characteristics in pH 6.8 phosphate buffer compared to commercial conventional tablet formulation (t50% 6 min). Stability studies on promising formulation indicated that there were no significant changes in drug content and in vitro dispersion time (p<0.05).Dhaka Univ. J. Pharm. Sci. 15(2): 167-172, 2016 (December)

Download Full-text

Factorial Designs in Pharmaceutical Stability Studies

Journal of Pharmaceutical Sciences ◽

10.1002/jps.2600720410 ◽

1983 ◽

Vol 72 (4) ◽

pp. 362-366 ◽

Cited By ~ 22

Author(s):

Sanford Bolton

Keyword(s):

Factorial Designs ◽

Stability Studies ◽

Pharmaceutical Stability

Download Full-text

Beyond-Use Dates Assignment for Pharmaceutical Preparations: Example of Low-Dose Amiodarone Capsules

Journal of Pharmacy Technology ◽

10.1177/87551225211015566 ◽

2021 ◽

pp. 875512252110155

Author(s):

Damien Brun ◽

Christophe Curti ◽

Edouard Lamy ◽

Christophe Jean ◽

Pierre Bertault-Peres ◽

...

Keyword(s):

Microcrystalline Cellulose ◽

Low Dose ◽

Pharmaceutical Preparations ◽

The United States ◽

Stability Study ◽

Potential Drug ◽

Stability Studies ◽

United States Pharmacopoeia ◽

Amiodarone Hydrochloride

Background: Beyond-use dates (BUDs) in compounding practice are assigned from stability studies. The United States Pharmacopoeia (USP 42 NF 37) suggested to assign a 6 months BUD for dry oral forms. A new pediatric formula of amiodarone capsules was implemented in our hospital, with 3 dosages (5 mg, 20 mg, and 50 mg). Objective: BUD of these new formulas had to be determined by stability study. Methods: The method for the determination of amiodarone content was validated to be stability indicating, and a stability study was performed. Different excipients commonly used for capsule compounding were compared. Results: We found that, with microcrystalline cellulose as excipient, 50 mg amiodarone capsules were stable for 1 year, whereas 5 mg and 20 mg capsules were not. This difference was studied, and lactose or mannitol were found to be better excipients for 5 mg amiodarone capsules, despite their potential side effects. A potential drug-excipient interaction between microcrystalline cellulose and amiodarone hydrochloride is described. Conclusion: Amiodarone hydrochloride/microcrystalline cellulose capsules have a BUD of 1 month for 5 mg capsules, 6 months for 20 mg, and 1 year for 50 mg.

Download Full-text

Formulation, Development and Scale-Up of Fixed-Dose Combination Tablets Containing Zidovudine, Lamivudine and Nevirapine

Current HIV Research ◽

10.2174/1570162x17666190927162155 ◽

2019 ◽

Vol 17 (5) ◽

pp. 360-367 ◽

Cited By ~ 1

Author(s):

Zênia Maria Maciel Lavra ◽

Flávia Patrícia Morais de Medeiros ◽

Rosali Maria Ferreira da Silva ◽

Talita Atanazio Rosa ◽

Victor de Albuquerque Wanderley Sales ◽

...

Keyword(s):

Microcrystalline Cellulose ◽

Corn Starch ◽

Scale Up ◽

Hiv Treatment ◽

Fixed Dose Combination ◽

Fixed Dose ◽

Wet Granulation ◽

Stability Studies ◽

Formulation Development ◽

Dose Combination

Background: The development of antiretroviral associations in a single dosage form aims to ensure improved efficacy, low costs and better adherence to treatment. Objective: This work performed the pharmacotechnical development, coating, and stability studies of fixed-dose combination tablets of zidovudine, lamivudine and nevirapine (300 + 200 + 150 mg, respectively). Methods: Qualitative and quantitative planning of diluents (101 and 250 microcrystalline cellulose, spray-dried monohydrate lactose and corn starch) and coating polymers (Opadry white II HP® and Instacoat Aqua Moistshield II®) were analyzed, and direct compression (DC) and wet granulation (WG) methods were tested aiming the development of the pharmaceutical form. Quality control was carried out according to the specifications set by official compendia. The chosen formulation was scaled-up and the industrial batches were submitted to accelerated and long-term stability studies. Results: The batches obtained by WG met the requirements, using 101 microcrystalline cellulose, corn starch and Opadry white II HP® as excipients. The DC trial was not possible due to the need of a greater ratio of excipients to improve formulation properties. Conclusion: Thus, this study brings a new therapeutic alternative for HIV treatment, contributing to the development of another possibility to simplify drug administration.

Download Full-text