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Journal of Pharmaceutical Sciences May 2007There are many reports in the literature referring to the effect of microenvironmental pH on solid dosage form performance, particularly stability and dissolution... (Review)
Review
There are many reports in the literature referring to the effect of microenvironmental pH on solid dosage form performance, particularly stability and dissolution profiles. Several techniques have been proposed for the measurement of the microenvironmental pH. Those techniques use certain assumptions and approximations and many of them employ a solution calibration curve of a probe to predict hydrogen ion activity in a substantially dry solid. Despite the limitation of the methodology, it is clear from the literature that microenvironmental pH has a significant impact on stability of compounds which demonstrate pH dependent stability in solution. Degradation kinetics of such compounds, and in some cases degradation profile as well, are dependent on the microenvironmental pH of the solid. Modulation of the microenvironmental pH through the use of pH modifiers can hence prove to be a very effective tool in maximizing solid dosage form stability. Judicial selection of the appropriate pH modifier, its concentration and the manufacturing process used to incorporate the pH modifier is necessary to enhance stability. Control of microenvironmental pH to maximize stability can be achieved without the use of pH modifier in some cases if an appropriate counter ion is used to provide an inherently optimal pH for the salt. Microenvironmental pH modulation was also shown to control the dissolution profile of both immediate and controlled release dosage forms of compounds with pH dependent solubility. The pH modifiers have been used in conjunction with high energy or salt forms in immediate release formulations to minimize the precipitation of the less soluble free form during initial dissolution. Additionally, pH modifiers were utilized in controlled release dosage forms of weakly basic drugs which exhibit diminished release in dissolution media with high pH. The incorporation of acidic pH modifiers in the controlled release formulation increases the solubility of the basic drug even as the high pH dissolution medium enters into the dosage form hence increasing drug release rate.
Topics: Chemistry, Pharmaceutical; Delayed-Action Preparations; Dosage Forms; Drug Carriers; Drug Compounding; Drug Stability; Excipients; Hydrogen-Ion Concentration; Kinetics; Microspheres; Models, Chemical; Polymers; Solubility; Technology, Pharmaceutical
PubMed: 17455349
DOI: 10.1002/jps.20932 -
Critical Reviews in Therapeutic Drug... 2007Pelletized dosage forms date back to the 1950s, when the first product was introduced to the market. Since then, these dosage forms have gained considerable popularity... (Review)
Review
Pelletized dosage forms date back to the 1950s, when the first product was introduced to the market. Since then, these dosage forms have gained considerable popularity because of their distinct advantages, such as ease of capsule filling because of better flow properties of the spherical pellets; enhancement of drug dissolution; ease of coating; sustained, controlled, or site-specific delivery of the drug from coated pellets; uniform packing; even distribution in the GI tract; and less GI irritation. Pelletized dosage forms can be prepared by a number of techniques, including drug layering on nonpareil sugar or microcrystalline cellulose beads, spray drying, spray congealing, rotogranulation, hot-melt extrusion, and spheronization of low melting materials or extrusion-spheronization of a wet mass. This review discusses recent developments in the pharmaceutical approaches that have been used to prepare pelletized dosage forms using the extrusion-spheronization process over the last decade. The review is divided into three parts: the first part discusses the extrusion-spheronization process, the second part discusses the effect of varying formulation and process parameters on the properties of the pellets, and the last part discusses the different approaches that have been used to prepare pelletized dosage forms using the extrusion-spheronization process.
Topics: Chemistry, Pharmaceutical; Delayed-Action Preparations; Dosage Forms; Drug Compounding; Drug Delivery Systems; Excipients; Particle Size; Technology, Pharmaceutical
PubMed: 17430098
DOI: 10.1615/critrevtherdrugcarriersyst.v24.i1.10 -
Pharmaceutisch Weekblad. Scientific... Apr 1984When a drug meets the criteria which make incorporation into a controlled release dosage form rational, a proper dosage form has to be selected. Oral controlled release... (Review)
Review
When a drug meets the criteria which make incorporation into a controlled release dosage form rational, a proper dosage form has to be selected. Oral controlled release products, available on the Dutch market, are referred to in discussing the various methods used to control drug release by galenical means in order to achieve a prolonged therapeutic effect. The effects of some physiological variables of the alimentary tract on drug delivery from the various dosage forms, especially with regard to formulation and design, are reviewed.
Topics: Administration, Oral; Biological Availability; Capsules; Delayed-Action Preparations; Dosage Forms; Fats; Humans; Ion Exchange; Osmosis; Polymers; Resins, Plant; Tablets, Enteric-Coated; Waxes
PubMed: 6374610
DOI: 10.1007/BF01953956 -
Molecular Pharmaceutics Apr 2024Oral dosage forms are the most widely and frequently used formulations to deliver active pharmaceutical ingredients (APIs), due to their ease of administration and... (Review)
Review
Oral dosage forms are the most widely and frequently used formulations to deliver active pharmaceutical ingredients (APIs), due to their ease of administration and noninvasiveness. Knowledge of intragastric release rates and gastric mixing is crucial for predicting the API release profile, especially for immediate release formulations. However, knowledge of the intragastric fate of oral dosage forms to date is limited, particularly for dosage forms administered when the stomach is in the fed state. An improved understanding of gastric food processing, dosage form location, disintegration times, and food effects is essential for greater understanding for effective API formulation design. standard and controlled modeling has played a significant role in predicting the behavior of dosage forms . However, discrepancies are reported between and disintegration times, with these discrepancies being greatest in the fed state. Studying the fate of a dosage form is a challenging process, usually requiring the use of invasive methods, such as intubation. Noninvasive, whole body imaging techniques can however provide unique insights into this process. A scoping review was performed systematically to identify and critically appraise published studies using MRI to visualize oral solid dosage forms in healthy human subjects. The review identifies that so far, an all-purpose robust contrast agent or dosage form type has not been established for dosage form visualization and disintegration studies in the gastrointestinal system. Opportunities have been identified for future studies, with particular focus on characterizing dosage form disintegration for development after the consumption food, as exemplified by the standard Food and Drug Administration (FDA) high fat meal.
Topics: Humans; Administration, Oral; Stomach; Gastrointestinal Tract; Contrast Media; Magnetic Resonance Imaging; Dosage Forms; Solubility; Tablets
PubMed: 38440796
DOI: 10.1021/acs.molpharmaceut.3c01123 -
The Journal of Pharmacy and Pharmacology Jul 2012This review focuses on the evolution and current status of biorelevant media and hydrodynamics, and discusses the usefulness of biorelevant performance testing in the... (Review)
Review
OBJECTIVES
This review focuses on the evolution and current status of biorelevant media and hydrodynamics, and discusses the usefulness of biorelevant performance testing in the evaluation of specific dosage form related lumenal processes.
KEY FINDINGS
During the last 15 years our knowledge of the gastrointestinal environment (including the lower gut) has improved dramatically and biorelevant media composition and, to a lesser extent, biorelevant hydrodynamics, have been refined. Biorelevant dissolution/release testing is useful for the evaluation of formulation and food effects on plasma levels after administration of immediate release dosage forms containing low solubility compounds and after administration of extended release products. Lumenal disintegration times of immediate release dosage forms and the bile acid sequestering activity of resins in the lumen can also be successfully forecasted with biorelevant in vitro testing.
SUMMARY
Biorelevant in-vitro performance testing is an important tool for evaluating intralumenal dosage form performance. Since the formulation of new active pharmaceutical ingredients for oral delivery is more challenging than ever before, efforts to improve the predictability of biorelevant tests are expected to continue.
Topics: Administration, Oral; Chemistry, Pharmaceutical; Delayed-Action Preparations; Dosage Forms; Gastrointestinal Tract; Hydrodynamics; Pharmaceutical Preparations; Quality Control; Solubility
PubMed: 22686340
DOI: 10.1111/j.2042-7158.2012.01474.x -
International Journal of Molecular... Sep 2010Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release... (Review)
Review
Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development.
Topics: Biocompatible Materials; Biodegradable Plastics; Delayed-Action Preparations; Drug Carriers
PubMed: 20957095
DOI: 10.3390/ijms11093298 -
Journal of Pharmaceutical Sciences Jan 1977
Topics: Delayed-Action Preparations; Dosage Forms; Pilocarpine; Terminology as Topic
PubMed: 833719
DOI: 10.1002/jps.2600660103 -
International Journal of Pharmaceutics Aug 2022In order to expand the limited portfolio of available polymer-based excipients for fabricating three-dimensional (3D) printed pharmaceutical products, Lipid-based...
In order to expand the limited portfolio of available polymer-based excipients for fabricating three-dimensional (3D) printed pharmaceutical products, Lipid-based excipients (LBEs) have yet to be thoroughly investigated. The technical obstacle of LBEs application is, however their crystalline nature that renders them very brittle and challenging for processing via 3D-printing. In this work, we evaluated the functionality of LBEs for filament-based 3D-printing of oral dosage forms. Polyglycerol partial ester of palmitic acid and polyethylene glycols monostearate were selected as LBEs, based on their chemical structure, possessing polar groups for providing hydrogen-bonding sites. A fundamental understanding of structure-function relationship was built to screen the critical material attributes relevant for both extrusion and 3D-printing processes. The thermal behavior of lipids, including the degree of their supercooling, was the critical attribute for their processing. The extrudability of materials was improved through different feeding approaches, including the common powder feeding and a devised liquid feeding setup. Liquid feeding was found to be more efficient, allowing the production of filaments with high flexibility and improved printability. Filaments with superior performance were produced using polyglycerol ester of palmitic acid. In-house designed modifications of the utilized 3D-printer were essential for a flawless processing of the filaments.
Topics: Dosage Forms; Drug Liberation; Esters; Excipients; Palmitic Acid; Powders; Printing, Three-Dimensional; Tablets; Technology, Pharmaceutical
PubMed: 35839981
DOI: 10.1016/j.ijpharm.2022.122013 -
Current Pharmaceutical Design 2015Cohesive powders are problematic in the manufacturing of pharmaceutical solid dosage forms because they exhibit poor flowability, fluidization and aerosolization. These... (Review)
Review
Cohesive powders are problematic in the manufacturing of pharmaceutical solid dosage forms because they exhibit poor flowability, fluidization and aerosolization. These undesirable bulk properties of cohesive powders represent a fundamental challenge in the design of efficient pharmaceutical manufacturing processes. Recently, mechanical dry coating has attracted increasing attention as it can improve the bulk properties of cohesive powders in a cheaper, simpler, safer and more environment-friendly way than the existing solvent-based counterparts. In this review, mechanical dry coating techniques are outlined and their potential applications in formulation and manufacturing of pharmaceutical solid dosage forms are discussed. Reported data from the literature have shown that mechanical dry coating holds promise for the design of superior pharmaceutical solid formulations or manufacturing processes by engineering the interfaces of cohesive powders in an efficient and economical way.
Topics: Dosage Forms; Drug Compounding; Excipients; Humans; Particle Size; Pharmaceutical Preparations; Powders; Technology, Pharmaceutical
PubMed: 26446461
DOI: 10.2174/1381612821666151008151001 -
European Journal of Rheumatology and... 1987Patient acceptance of medications often depends upon individual and cultural preferences for particular dosage forms. A variety of dosage forms also provides the patient... (Clinical Trial)
Clinical Trial
Patient acceptance of medications often depends upon individual and cultural preferences for particular dosage forms. A variety of dosage forms also provides the patient and the physician with greater convenience and flexibility. Thus, multiple formulations increase the clinical utility of a drug. In addition to the capsule, dosage forms of piroxicam now available or in an advanced stage of clinical development include a suppository, dispersible tablet, topical gel, and parenteral formulation. (Ed.: The parenteral and topical formulations were launched after the symposium was held, and are now available). The piroxicam suppository offers an alternative to the oral route of administration. Pharmacokinetic studies demonstrate that the 20-mg suppository is bioequivalent to the 20-mg capsule, and clinical studies have shown that it is equal to the capsule in efficacy and toleration. Piroxicam is the only non-steroidal anti-inflammatory drug (NSAID) that is available as a dispersible tablet. This dosage form is also well tolerated by patients and equally effective as the capsule. Intramuscular administration of piroxicam is in development. All these dosage forms offer the convenience of once-a day administration. Piroxicam topical gel (0.5%) has been demonstrated to have anti-inflammatory activity in several animal models. In double-blind clinical trials involving patients with osteoarthritis of the knee, the topical gel was found to be significantly more effective than placebo and well tolerated.
Topics: Administration, Topical; Animals; Arthritis; Clinical Trials as Topic; Dogs; Gels; Humans; Injections, Intramuscular; Piroxicam; Suppositories; Tablets
PubMed: 3305038
DOI: No ID Found