Excipient celluloses

Excipients Cellulose, disodium hydrogen phosphate, hydroxypropyl cellulose, hydroxypropyl methylcellulose, lactose, mannitol, sodium lauryl sulfate, etc. 

Excipient Cellulose acetate, CA-398-10NF Manufacturer Eastman Chemical Co. 

Kibbe, A.H. Handbook of Pharmaceutical Excipients Cellulose, Silicified Microcrystalline American Public Health Association Washington, DC, 2000. 

The availabihty of spray-dried lactose, microcrystaUine cellulose, and other excipients allows for the use of granular rather than powdered phases. This eliminates some of the problems of particle segregation according to size (demixing) and even flow to the die. Direct compression eventually may be the preferred method of tablet preparation. 

The analysis of a pharmaceutical tablet (6) requires sample preparation that is little more complex as most tablets contain excipients (a solid diluent) that may be starch, chalk, silica gel, cellulose or some other physiologically inert material. This sample preparation procedure depends on the insolubility of the excipient in methanol. As the components of interest are both acidic and neutral, the separation was achieved by exploiting both the ionic interactions between the organic acids and the adsorbed ion exchanger and the dispersive interactions with the remaining exposed reverse phase. 

For thousands of years, nature has provided humankind with a large variety of materials for the most diversified applications for its survival, such as food, energy, medicinal products, protection and defense tools, and others. The pharmaceutical industry has benefitted from such diversity of biomaterials and has exploited the use of natural products as sources of both drugs and excipients. One example of a promising biomaterial for pharmaceutical use is xylan, a hemicellulose largely found in nature, being considered the second most abundant polysaccharide after cellulose. 

It may sometimes by necessary to supplement the properties of the drug so that it compresses more easily, and these needs have been realized by several manufacturers of excipients. Materials described as compression aids are now commercially available. Ideally, such adjuvants should develop mechanical strength while improving, or at least not adversely affecting, release characteristics. Among the most successful at meeting both these needs have been the microcrystalline celluloses (partially acid-hydrolyzed forms of cellulose). A number of grades are available based upon particle size and distribution. 

Measurements of particle porosity are a valuable supplement to studies of specific surface area, and such data are particularly useful in the evaluation of materials used in direct compression processes. For example, both micromeritic properties were measured for several different types of cellulosic-type excipients [53]. Surface areas by the B.E.T. method were used to evaluate all types of pore structures, while the method of mercury intrusion porosimetry used could not detect pores smaller than 10 nm. The data permitted a ready differentiation between the intraparticle pore structure of microcrystalline and agglomerated cellulose powders. 

The sorption of water by excipients derived from cellulose and starch has been considered by numerous workers, with at least three thermodynamic states having been identified [82]. Water may be directly and tightly bound at a 1 1 stoichiometry per anhydroglucose unit, unrestricted water having properties almost equivalent to bulk water, or water having properties intermediate between these two extremes. The water sorption characteristics of potato starch and microcrystalline cellulose have been determined, and comparison of these is found in Fig. 11. While starch freely adsorbs water at essentially all relative humidity values, microcrystalline cellulose only does so at elevated humidity values. These trends have been interpreted in terms of the degree of available cellulosic hydroxy groups on the surfaces, and as a function of the amount of amorphous material present [83]. 

Excipients Calcium carbonate, candeUUa wax, croscarmeUose sodium, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystaUine cellulose, polysorbate 80, simethicone emulsion... 

Formuiation The formulation consists of excipients such as carnauba wax, crospovidone, hydroxylpropyl cellulose, hydroxypropyl methylcellulose, lactose, magnesium stearate, microcrystalline cellulose, and other inactive ingredients. 

Spherical pellets containing 5% triamcinolone acetonide were prepared by Villar-Lopez and co-workers [59] by extrusion/spheronization following formulation with microcrystalline cellulose and/or a hydrophilic excipient like lactose, sodium earbox-ymethylcellulose, or P-cyclodextrin. Their suitability for coating, with a view toward colonic drug deliveiy, was assessed in terms of their size, sphericity, and dissolution test response. The best results were afforded by a 5 90 5 composition of microcrystalline cellulose, P-cyclodextrin, and triamcinolone acetonide, prepared by complex-ation of triamcinolone acetonide with P-cyclodextrin prior to the addition of microcrystalline cellulose. 

Fingerprint check for the identity of a drug and quality control of complex excipients such as lactose and cellulose used in formulation... 

Polyelectrolytes (most notably ionic cellulose derivatives and crosslinked polyacid powders) are also commonly used as matrices, binders and excipients in oral controlled release compositions. In these applications, the polyelectrolytes provide hydrophilicity and pH sensitivity to tablet dosage forms. Acidic polyelectrolytes dissociate and swell (or dissolve) at high pH values whereas basic polyelectrolytes (for instance, polyamines) become protonated and swell at low pH. In either case, swelling results in increased permeability [290], thereby allowing an incorporated drug to be released. 

Dissolution profiles from tablets containing 60% theophylline and 25% microcrystallme cellulose showed a smaller difference in the release rate of theophylline from heated and non-heated tablets (Fig. 3). Nevertheless, both of these tablets demonstrated a matrix-controlled release. These results suggest that the level of excipient in the tablet exerted a significant effect on the dissolution release properties of thermally and non-thermally treated tablets. As the microcrystalline cellulose content increased, the difference in release rates between heated and non-heated tablets became more pronounced. 

In this chapter, analysis of the excipient in Nasonex (mometasone naral spray) is used as a typical example to demonstrate how to select a proper analytical method. Nasonex Nasal Spray contains Mometasone Furoate, microcrystalline cellulose, and carboxymethylcellulose sodium NF, citric acid USP, sodium citrate USP, benzalkonium chloride solution NF, glycerin USP, polysorbate 80 NF, phenylethyl alcohol USP, and water USP. 

Sherwood BE, Becker JW. A new class of high functionality excipients silicified microcrystalline cellulose. Pharm Tech 1998 22(10) 78—88. 

Controlled optimal particle size and size distribution ensures superior flow properties of coprocessed excipients and reduced reliance on addition of glidants. The volumetric flow properties of SMCC were studied in comparison with those of the physical mixture of its parent excipients (42). The particle size range of the two test samples was found to be similar, but the flow of coprocessed excipient was better than that of the physical mixture. A comparison of the flow properties of Cellactose with its parent excipients was also performed (5) by measuring the angle of repose and Hausner ratio, and Cellactose was found to have better flow characteristics than lactose or a physical mixture of cellulose and lactose. The spray-dried coprocessed product had a spherical shape and even surfaces, which resulted in improved flow properties. On similar terms, mechanically coating the 2% CSD over microfine cellulose powder resulted in improving its flow properties (43). 

The most common problem manifested due to poor flow property is the variation in fill weight. This problem is much more serious in the case of DC excipients, but coprocessed excipients are devoid of this effect, when compared with the physical mixture of their parent excipients. This is because of the impregnation of one particle into the matrix of another, which reduces the rough particle surfaces and creates a near-optimal size distribution, causing better flow properties. Tablets prepared with M80K, a coprocessed cellulose powder with CSD, showed lesser weight variation than those prepared with Avicel (43). 

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