Pharmaceutical dosage forms contain both pharmacologically active compounds and excipients added to aid the formulation and manufacture of the subsequent dosage form for administration to patients. Indeed, the properties of the final dosage form (i.e. its bioavailability and stability) are, for the most part, highly dependent on the excipients chosen, their concentration and interaction with both the active compound and each other. No longer can excipients be regarded simply as inert or inactive ingredients, and a detailed knowledge not only of the physical and chemical properties but also of the safety, handling and regulatory status of these materials is essential for formulators throughout the world. In addition, the growth of novel forms of delivery has resulted in an increase in the number of the excipients being used and suppliers of excipients have developed novel coprocessed excipient mixtures and new physical forms to improve their properties. The Handbook of Pharmaceutical Excipients has been conceived as a systematic, comprehensive resource of information ​ on all of these topics. URI http://repositorio.ub.edu.ar/handle/123456789/5143 Collections Libros Farmacia www.ub.edu.ar | biblioteca.ub.edu.ar Contact Us | Send Feedback Handbook of pharmaceutical excipients 

Handbook of Pharmaceutical Excipients

Purpose. To study the molecular structure of indomethacin-PVP amorphous solid dispersions and identify any specific interactions between the components using vibrational spectroscopy.

Spectroscopic characterization of interactions between PVP and indomethacin in amorphous molecular dispersions.

Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles.

Fast disintegrating tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The popularity and usefulness of the formulation resulted in development of several FDT technologies. This review describes various formulations and technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. In particular, this review describes in detail FDT technologies based on lyophilization, molding, sublimation, and compaction, as well as approaches to enhancing the FDT properties, such as spray-drying, moisture treatment, sintering, and use of sugar-based disintegrants. In addition, taste-masking technologies, experimental measurements of disintegration times, and clinical studies are also discussed.

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Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies.

General principles of pharmaceutical solid polymorphism: a supramolecular perspective.

In order to make a compressed tablet which can rapidly disintegrate in the oral cavity, microcrystalline cellulose and low-substituted hydroxypropylcellulose were used as disintegrants, and ethenzamide and ascorbic acid were chosen as poorly and easily water soluble model drugs, respectively. The mixture of microcrystalline cellulose and low-substituted hydroxypropylcellulose was compressed at 100--500 kgf in the absence of an active ingredient. The properties of these tablets, such as hardness, porosity, the time required for complete wetting of a tested tablet (wetting time), water uptake and disintegration time determined by a new disintegration apparatus, were investigated to elucidate the wetting and disintegration characteristics of these tablets, When the MCC/L-HPC ratio was in the range of 8:2 to 9:1, the shortest disintegration time was observed. The disintegration of tablets containing ethenzamide or ascorbic acid was examined next. Tablet disintegration time in the oral cavity was also tested, and good correlation between the disintegration behaviors in vitro and in the oral cavity was recognized.

Preparation and Evaluation of a Compressed Tablet Rapidly Disintegrating in the Oral Cavity

To make rapidly disintegrating tablets with sufficient mechanical integrity as well as a pleasant taste, microcrystalline cellulose (MCC), Tablettose (TT), and crosslinked sodium carboxymethyl cellulose (Ac-di-sol) or erythritol (ET) were formulated. Tablets were made by a direct compression method (1). Tablet properties such as porosity, tensile strength, and disintegration time were determined. The tensile strength and disintegration time were selected as response variables, tablet porosity and parameters representing the characteristics of formulation were selected as controlling factors, and their relation was determined by the polynomial regression method. Response surface plots and contour plots of tablet tensile strength and disintegration time were also constructed. The optimum combination of tablet porosity and formulation was obtained by superimposing the contour diagrams of tablet tensile strength and disintegration time. Rapidly disintegrating tablets with durable structure and desirable taste could be prepared within the obtained optimum region.

Evaluation of Rapidly Disintegrating Tablets Prepared by a Direct Compression Method

Rapidly disintegrating tablets prepared by the wet compression method: Mechanism and optimization

We found that ibuprofen (IPF) became amorphous when the crystalline powder was merely mixed with polyvinylpyrrolidone (PVP), using a test tube mixer, and allowed to stand at appropriate temperatures. The crystallinity of the mixture was evaluated from the X-ray diffraction spectra by Ruland's method. The degree of decrease in crystallinity (A), defined as the ratio of the decrease in crystallinity to the value calculated by assuming additivity of crystallinity, increased gradually with time for the IPF-PVP system. We found that the higher the storage temperature, the higher the weight ratio of PVP in the mixture and the lower the molecular weight of PVP, the greater was the degree of decrease in crystallinity. The effect of PVP particle size was observed in 1 : 1 and 1 : 3 IPF/PVP mixtures.The interaction of IPF with PVP in the solid state was investigated by IR and 13C-NMR analyses, and the molecular geometry of 1-ethyl-2-pyrrolidone (EtP, a model compound for PVP) was calculated by the molecular orbital method (PM3). Our findings suggested that EtP undergoes O-protonation, forming a hydrogen bond at the carbonyl oxygen, in preference to N-protonation.

https://www.jstage.jst.go.jp/article/cpb1958/43/6/43_6_988/_pdf

Yorinobu Yonezawa

Papers

Preparation and Evaluation of a Compressed Tablet Rapidly Disintegrating in the Oral Cavity

Evaluation of Rapidly Disintegrating Tablets Prepared by a Direct Compression Method

Rapidly disintegrating tablets prepared by the wet compression method: Mechanism and optimization

Solid-State Interaction of Ibuprofen with Polyvinylpyrrolidone

Measurement and evaluation of the adhesive force between particles by the direct separation method.