Deformation and Mechanical Characteristics of Compacted Binary Mixtures of Plastic (Microcrystalline Cellulose), Elastic (Sodium Starch Glycolate), and Brittle (Lactose Monohydrate) Pharmaceutical Excipients

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

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Compatibility Studies of Valsartan with Different Pharmaceutical Excipients

Revista de Chimie ◽

10.37358/rc.19.7.7386 ◽

2019 ◽

Vol 70 (7) ◽

pp. 2590-2600

Author(s):

Ioana Cristina Tita ◽

Lavinia Lupa ◽

Bogdan Tita ◽

Roxana Liana Stan ◽

Laura Vicas

Keyword(s):

Magnesium Stearate ◽

Dosage Forms ◽

Compatibility Studies ◽

Scanning Calorimetry ◽

Pharmaceutical Dosage Forms ◽

Lactose Monohydrate ◽

Pharmaceutical Excipients ◽

Solid Dosage ◽

Fourier Transformed Infrared Spectroscopy ◽

Ft Ir

Compatibility studies between active drugs and excipients are substantial in the pharmaceutical technology. Thermal analysis has been extensively used to obtain information about drug-excipient interactions and to perform pre-formulation studies of pharmaceutical dosage forms. The objective of the present study was to evaluate the compatibility of the valsartan (VALS) with pharmaceutical excipients of common use including diluents, binders, disintegrants, lubricants and solubilising agents. Thermogravimetry (TG), derivative thermogravimetry (DTG), but especially differential scanning calorimetry (DSC) were used for a first screening to find small variations in peak temperature and/or their associated enthalpy for six drug/excipient mixtures (starch, cross caramelose sodique, microcrystalline cellulose 102, povidone K30, lactose monohydrate and magnesium stearate), which indicate some degree of interaction. Additional methods using Fourier transformed infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRPD) confirmed the incompatibility of VALS with starch, povidone K30, lactose monohydrate and magnesium stearate. Those excipients should be avoided in the development of solid dosage forms.

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Influence of different types of commercially available microcrystalline cellulose on degradation of perindopril erbumine and enalapril maleate in binary mixtures / Vpliv različnih tipov komercialno dostopne mikrokristalne celuloze na razpad erbuminijevega perindoprilata in enalaprilijevega maleata v binarnih zmeseh

Acta Pharmaceutica ◽

10.2478/v10007-012-0039-5 ◽

2012 ◽

Vol 62 (4) ◽

pp. 515-528 ◽

Cited By ~ 6

Author(s):

Tanja Vehovec ◽

Andrej Gartner ◽

Odon Planinšek ◽

Aleš Obreza

Keyword(s):

Binary Mixtures ◽

Microcrystalline Cellulose ◽

Enzyme Inhibitors ◽

Angiotensin Converting Enzyme Inhibitors ◽

Converting Enzyme Inhibitors ◽

Enalapril Maleate ◽

Pharmaceutical Ingredients ◽

Perindopril Erbumine ◽

Different Types ◽

The Stability

Influence of some commercially available types of microcrystalline cellulose (MCC) on the stability of certain active pharmaceutical ingredients (APIs), when in contact, has been investigated. Two structurally similar APIs, perindopril erbumine (PER) and enalapril maleate (EM), both well-known angiotensin-converting enzyme inhibitors were used. The main properties of an MCC that could determine the stability for each API were measured and correlated to the stability of these two APIs in binary mixtures. The stability of these APIs differed when in contact with different types of MCC. The dominant properties of MCC from one manufacturer were surface features that influenced the stability of PER and acidity that influenced the stability of EM. In the case of MCC from other manufacturers, unbound water was stability determining for both substances.

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