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BioMed Research International 2022Pharmaceutical excipients derived from natural sources like resins are nowadays meritoriously used in the formulation of drugs. Resins of natural origin have many...
Pharmaceutical excipients derived from natural sources like resins are nowadays meritoriously used in the formulation of drugs. Resins of natural origin have many advantages over chemically synthesized substances; they are safer, nontoxic, less expensive, biodegradable, and widely available. To our knowledge, resins from plants have been not sufficiently explored for application in pharmaceutical formulations. Thus, in the present study, a resin isolated from Engl was characterized for its potential use as a pharmaceutical excipient. . The resin was extracted from the oleo gum resin of Engl, which involved the removal of volatile oils, gum, and Boswellic acid contents. The dried resin powder was then characterized for its micromeritic properties, heavy metal contents, moisture content, moisture absorption power, pH, solubility, swelling property, and acute toxicity profile. Moreover, the crystal nature and the chemical functionality of the resin were evaluated by using X-ray diffraction and Fourier transform infrared spectrometry, respectively. . The yield of the neutral resin was 13.17%, and the powder was pale yellow and had irregular surfaces. The resin was freely soluble in organic solvents but almost insoluble in water. The moisture content of the dried extract was 2.5% while its moisture absorption capacity was 2.5%, 4%, and 5.47% at 40%, 60%, and 75% RH, respectively. Besides, the maximum swelling capacities of the resin observed were 40%, 37%, and 30% at 350C, 300C, and 250C, respectively. The bulk powder exhibited a 1.21 Hausner ratio, 36.497 angles of repose, and 17.03% Carr's index, indicating the fair flowability of the powder. Heavy metals such as zinc, chromium, and cobalt were detected at a low level while elements like copper, manganese, lead, and cadmium were absent. The X-ray diffraction study revealed that the crystallinity index of the powder was 42.7% with a crystal size of 994.5A. The resin could be safe in mice up to 3 g/kg of their body weight. In conclusion, the physicochemical properties of the resin powder investigated reveal its potential application as pharmaceutical additives in the formulation of modified release solid dosages forms like tablets and microcapsules.
Topics: Animals; Boswellia; Excipients; Mice; Powders; Resins, Plant; Tablets
PubMed: 35978631
DOI: 10.1155/2022/5791308 -
AIDS Patient Care and STDs Apr 2000Preferred microbicides are expected to inactivate most sexually transmitted viral and nonviral pathogens, including HIV-1, without affecting lactobacilli, components of... (Review)
Review
Preferred microbicides are expected to inactivate most sexually transmitted viral and nonviral pathogens, including HIV-1, without affecting lactobacilli, components of the natural defense system against sexually transmitted diseases (STDs), be widely available, be inexpensive, and have an established safety record for human use. We show here that cellulose acetate phthalate [C-A-P enteric coating polymer (Eastman)], a compound used for coating of enteric tablets, meets all these criteria.
Topics: Animals; Anti-Infective Agents; Controlled Clinical Trials as Topic; Disease Models, Animal; Excipients; HIV-1; Humans; Mice; Microbial Sensitivity Tests; Sexually Transmitted Diseases; Treatment Outcome
PubMed: 10806641
DOI: 10.1089/108729100317830 -
Nature Reviews. Drug Discovery Dec 2020
Topics: Drug Approval; Drug Compounding; Excipients; Humans; Pharmaceutical Preparations; United States; United States Food and Drug Administration
PubMed: 33168998
DOI: 10.1038/d41573-020-00201-1 -
International Journal of Molecular... Sep 2020The development of medicines designed for children can be challenging since this distinct patient population requires specific needs. A formulation designed for...
The development of medicines designed for children can be challenging since this distinct patient population requires specific needs. A formulation designed for paediatric patients must consider the following aspects: patient population variability; dose flexibility; route of administration; patient compliance; drug and excipient tolerability. The purpose of this Special Issue entitled "Paediatric Formulation: Design and Development" is to provide an update on both state-of-the-art methodology and operational challenges in the design and development of paediatric formulations. It aims at re-evaluating what is needed for more progress in the design and development of age-appropriate treatments for paediatric diseases, focusing on: formulation development; drug delivery design; efficacy, safety, and tolerability of drugs and excipients. This editorial, briefly, summarizes the objects of nine original research and review papers published in this Special Issue.
Topics: Chemistry, Pharmaceutical; Child; Drug Compounding; Drug Delivery Systems; Drug Development; Excipients; Humans; Periodicals as Topic
PubMed: 32992469
DOI: 10.3390/ijms21197118 -
Carbohydrate Polymers Oct 2021Alginic acid and its sodium salt are well-accepted pharmaceutical excipients fulfilling several roles in the development of solid oral dosage forms. Although they have... (Review)
Review
Alginic acid and its sodium salt are well-accepted pharmaceutical excipients fulfilling several roles in the development of solid oral dosage forms. Although they have attractive advantages as safety, abundance, relatively low cost and biodegradability, these natural polysaccharides possess a high variability that may limit their use as excipients for tablet formulation. Thus, to obtain robust formulations and high-quality drug products with consistent performance a complete understanding of the structure-property relationship becomes necessary as the structure of alginates affects both, technological and biopharmaceutical properties. This review compiles the compaction studies carried out that relate the structure of alginates to their mechanical and dissolution performances. The different analytical methods used to determine the chemical composition, primary structure and molecular weight distribution, major factors affecting the behavior of alginates in direct compression, are also exposed. Finally, different strategies reported to improve the properties of alginic acid as direct compression excipient are discussed.
Topics: Alginates; Alginic Acid; Drug Compounding; Drug Liberation; Excipients; Humans; Magnetic Resonance Spectroscopy; Molecular Weight; Particle Size; Solubility; Structure-Activity Relationship; Tablets
PubMed: 34364633
DOI: 10.1016/j.carbpol.2021.118399 -
Expert Opinion on Drug Delivery Dec 2014Compritol® 888 ATO is a lipid excipient that is generally used in cosmetic industry as a surfactant, emulsifying agent and viscosity-inducing agent in emulsions or... (Review)
Review
INTRODUCTION
Compritol® 888 ATO is a lipid excipient that is generally used in cosmetic industry as a surfactant, emulsifying agent and viscosity-inducing agent in emulsions or creams. Based on its chemical composition, Compritol 888 ATO is a blend of different esters of behenic acid with glycerol.
AREAS COVERED
Recently, there has been great interest in the multiple roles that Compritol 888 ATO plays in various pharmaceutical delivery systems. Accordingly, this review aimed at summarizing the current and potential applications of Compritol 888 ATO in various drug delivery areas.
EXPERT OPINION
Different researches have highlighted the feasibility of using Compritol 888 ATO as a lubricant or coating agent for oral solid dosage formulations. It has also been explored as a matrix-forming agent for controlling drug release. At present, the most common pharmaceutical application of Compritol 888 ATO is in lipid-based colloidal drug delivery system such as solid lipid microparticles, solid lipid nanoparticles and nanostructured lipid carriers. Although, Compritol 888 ATO has acceptable regulatory and safety profiles and although the number of articles that emphasize on its applicability as an innovative excipient in pharmaceutical technology is continuously increasing, it is not widely used in the pharmaceutical market products and its use is limited to its sustain release ability in extended release tablets.
Topics: Animals; Delayed-Action Preparations; Drug Carriers; Excipients; Fatty Acids; Humans; Kinetics; Nanoparticles
PubMed: 25152197
DOI: 10.1517/17425247.2014.935335 -
International Journal of Pharmaceutics Nov 2017Poor aqueous solubility of drugs is becoming an increasingly pronounced challenge in the formulation and development of drug delivery systems. To overcome the... (Review)
Review
Poor aqueous solubility of drugs is becoming an increasingly pronounced challenge in the formulation and development of drug delivery systems. To overcome the limitations associated with these problematic drugs, formulation scientists are required to use enabling strategies which often demands the use of new excipients. Cellulose nanofibers (CNFs) is such an excipient and it has only recently been described in the pharmaceutical field. In this review, the use of CNF in drug formulation with a focus on poorly soluble drugs is featured. In particular, the aim is to describe and discuss the many unique properties of CNFs, which make CNFs attractive as excipients in pharmaceutical sciences. Furthermore, the use of CNF as stabilizers for crystalline drug nanoparticles, as a matrix former to obtain a long-lasting sustained drug release over several weeks and as a film former with immediate release properties for poorly soluble drug are reported. Finally, the preparation of pharmaceutical CNF foams together with poorly soluble drugs is highlighted; foams, which offer a sustained drug delivery system with positive buoyancy.
Topics: Cellulose; Drug Delivery Systems; Excipients; Nanofibers; Pharmaceutical Preparations; Solubility
PubMed: 28951349
DOI: 10.1016/j.ijpharm.2017.09.064 -
Advanced Drug Delivery Reviews Oct 2011The purpose of this review is to demonstrate the critical importance of understanding protein-excipient interactions as a key step in the rational design of formulations... (Review)
Review
The purpose of this review is to demonstrate the critical importance of understanding protein-excipient interactions as a key step in the rational design of formulations to stabilize and deliver protein-based therapeutic drugs and vaccines. Biophysical methods used to examine various molecular interactions between solutes and protein molecules are discussed with an emphasis on applications to pharmaceutical excipients in terms of their effects on protein stability. Key mechanisms of protein-excipient interactions such as electrostatic and cation-pi interactions, preferential hydration, dispersive forces, and hydrogen bonding are presented in the context of different physical states of the formulation such as frozen liquids, solutions, gels, freeze-dried solids and interfacial phenomenon. An overview of the different classes of pharmaceutical excipients used to formulate and stabilize protein therapeutic drugs is also presented along with the rationale for use in different dosage forms including practical pharmaceutical considerations. The utility of high throughput analytical methodologies to examine protein-excipient interactions is presented in terms of expanding formulation design space and accelerating experimental timelines.
Topics: Drug Design; Drug Stability; Excipients; High-Throughput Screening Assays; Humans; Hydrogen Bonding; Proteins; Static Electricity; Technology, Pharmaceutical
PubMed: 21855584
DOI: 10.1016/j.addr.2011.07.006 -
Polimery W Medycynie 2020Co-processing starch with clay nanocomposite has been shown to yield a new class of materials, potentially with better properties than pristine starch, that could be...
BACKGROUND
Co-processing starch with clay nanocomposite has been shown to yield a new class of materials, potentially with better properties than pristine starch, that could be used as directly compressible excipients in tablet formulations.
OBJECTIVES
In this study, starches from 3 botanical sources, i.e., millet starch from Pennistum glaucum (L) RBr grains, sorghum starch from Sorghum bicolor L. Moench grains and cocoyam starch from Colocasia esculenta L. Schott tubers, were co-processed with montmorillonite clay (MMT) and evaluated as a directly compressible excipient in tramadol tablet formulations. The effects of different starch-to-clay ratios on the material and drug release properties of the resulting tablets were evaluated.
MATERIAL AND METHODS
The starch-clay composites were prepared by heating a dispersion of the starch in distilled water, then precipitating the dispersion with an equal volume of 95% ethanol. The starch-clay composites were characterized and used as direct compression excipients for the preparation of tramadol tablets. The mechanical and drug release properties of the tablets were evaluated.
RESULTS
Co-processing MMT with the starches yielded starch-clay composites with different material and tablet properties than the pristine starches. The co-processed starch-MMT biocomposites exhibited improved flowability and compressibility over the pristine starches. The mechanical and drug release properties of tramadol tablets containing starch-clay composites were significantly better than those containing only pristine starches. The properties of the starch-clay composites were not related to the botanical source of the starches.
CONCLUSIONS
The study showed that starch-clay biocomposites could be used in the controlled release of tramadol.
Topics: Clay; Drug Compounding; Excipients; Solubility; Starch; Tablets; Tramadol
PubMed: 33125195
DOI: 10.17219/pim/128473 -
International Journal of Pharmaceutics Sep 2016A β-cyclodextrin (β-CD) polymer obtained by crosslinking β-CD with citric acid in its water-insoluble (PCD-I) and soluble (PCD-S) forms was used as a multifunctional...
A β-cyclodextrin (β-CD) polymer obtained by crosslinking β-CD with citric acid in its water-insoluble (PCD-I) and soluble (PCD-S) forms was used as a multifunctional direct compression excipient for tablet designing. PCD-I powder was obtained after grinding the solid fraction through a 200μm grid. PCD-S powder was recovered after lyophilization or spray drying of the PCD-S aqueous solutions, eventually followed by a wet granulation step. Both PCD-I and PCD-S powders were characterized, separately and mixed in variable ratios, based on dynamic water vapor sorption, SEM, particle size distribution, tapped density, compressibility, and flowability. PCD-I and spray dried and lyophilized/wet granulated PCD-S, as well as the mixture PCD-I/PCD-S=90/10, presented optimal free flowing characteristics. Then, PCD-I or PCD-S powders - separately or mixed in variable ratios - were used for tablets preparation by direct compression without adding any other excipient (e.g. binder, lubricant, disintegrant etc). As PCD-I decreased, tablets resistance to crushing and disintegration time increased from 15s to 15min (against 30min for β-CD), showing the improved disintegrant functionality of PCD-I, that rapidly swelled once in contact with water. Finally, PCD was force-fed to Sprague-Dawley rats (2g/kg) which were then observed during 14days for any clinical signs of toxicity.
Topics: Animals; Body Weight; Cellulose; Citric Acid; Cyclodextrins; Drug Compounding; Excipients; Particle Size; Rats; Rats, Sprague-Dawley; Tablets; X-Ray Diffraction
PubMed: 27473278
DOI: 10.1016/j.ijpharm.2016.07.059