Search results for "Availability"
showing 10 items of 510 documents
Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Aciclovir
2008
Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing (biowaiver) for the approval of immediate release (IR) solid oral dosage forms containing aciclovir are reviewed. Aciclovir therapeutic use and therapeutic index, pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability (BA) studies were also taken into consideration in order to ascertain whether a biowaiver can be recommended. According to the Biopharmaceutics Classification System (BCS) and considering tablet strengths up to 400 mg, aciclovir would be BCS Class III. However, in some countries also 800 mg tablets are available which …
Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Metformin Hydrochloride.
2021
Abstract Data are examined regarding possible waiver of in vivo bioequivalence testing (i.e. biowaiver) for approval of metformin hydrochloride (metformin) immediate-release solid oral dosage forms. Data include metformin's Biopharmaceutics Classification System (BCS) properties, including potential excipient interactions. Metformin is a prototypical transporter-mediated drug and is highly soluble, but only 50% of an orally administered dose is absorbed from the gut. Therefore, metformin is a BCS Class III substance. A BCS-based approval approach for major changes to marketed products and new generics is admissible if test and reference dosage forms have the identical active pharmaceutical …
Subcutaneous Injection of Drugs: Literature Review of Factors Influencing Pain Sensation at the Injection Site.
2019
The subcutaneous administration route is widely used to administer different types of drugs given its high bioavailability and rapid onset of action. However, the sensation of pain at the injection site might reduce patient adherence. Apart from a direct effect of the drug itself, several factors can influence the sensation of pain: needle features, injection site, volume injected, injection speed, osmolality, viscosity and pH of formulation, as well as the kind of excipients employed, including buffers and preservatives. Short and thin needles, conveniently lubricated and with sharp tips, are generally used to minimize pain, although the anatomic injection site (abdomen versus thigh) also …
Ion-pair approach coupled with nanoparticle formation to increase bioavailability of a low permeability charged drug.
2018
Abstract Atenolol is a drug widely used for the treatment of hypertension. However, the great drawback it presents is a low bioavailability after oral administration. To obtain formulations that allow to improve the bioavailability of this drug is a challenge for the pharmaceutical technology. The objective of this work was to increase the rate and extent of intestinal absorption of atenolol as model of a low permeability drug, developing a double technology strategy. To increase atenolol permeability an ion pair with brilliant blue was designed and the sustained release achieved through encapsulation in polymeric nanoparticles (NPs). The in vitro release studies showed a pH-dependent relea…
Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine.
2020
Abstract Literature relevant to assessing whether BCS-based biowaivers can be applied to immediate release (IR) solid oral dosage forms containing carbamazepine as the single active pharmaceutical ingredient are reviewed. Carbamazepine, which is used for the prophylactic therapy of epilepsy, is a non-ionizable drug that cannot be considered “highly soluble” across the range of pH values usually encountered in the upper gastrointestinal tract. Furthermore, evidence in the open literature suggests that carbamazepine is a BCS Class 2 drug. Nevertheless, the oral absolute bioavailability of carbamazepine lies between 70 and 78% and both in vivo and in vitro data support the classification of ca…
Biowaiver monograph for immediate-release solid oral dosage forms: acetylsalicylic acid.
2012
A biowaiver monograph for acetylsalicylic acid (ASA) is presented. Literature and experimental data indicate that ASA is a highly soluble and highly permeable drug, leading to assignment of this active pharmaceutical ingredient (API) to Class I of the Biopharmaceutics Classification System (BCS). Limited bioequivalence (BE) studies reported in the literature indicate that products that have been tested are bioequivalent. Most of the excipients used in products with a marketing authorization in Europe are not considered to have an impact on gastrointestinal motility or permeability. Furthermore, ASA has a wide therapeutic index. Thus, the risks to the patient that might occur if a nonbioequi…
Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Cephalexin Monohydrate.
2019
Literature data and results of experimental studies relevant to the decision to allow waiver of bioequivalence studies in humans for the approval of immediate release solid oral dosage forms containing cephalexin monohydrate are presented. Solubility studies were performed in accordance with the current biowaiver guidelines of the Food and Drug Administration, World Health Organization and European Medicines Agency, taking the degradation at some pH values into consideration. Together with solubility and permeability data for cephalexin monohydrate from the literature, it was demonstrated to be a Biopharmaceutics Classification System Class 1 drug. The pharmacokinetic behavior, results of b…
Physical methods to promote drug delivery on mucosal tissues of the oral cavity.
2013
Introduction: The successful of drug delivery through the mucosal tissue of the oral cavity represents a current challenge as well as a great future perspective. The need for more rapid onset of action and improved absorption of medications has resulted in great development of drug delivery technologies that use physical methods to overcome the barrier properties of oral mucosae. Areas covered: This review discusses the various physical techniques which have been, and are being, explored to sustain drug delivery in the oral cavity. In particular, supersaturation, eutectic formation, iontophoresis, electroporation, sonophoresis, laser radiation, photomechanical waves, and needleless injectio…
Invasion biology in non‐free‐living species: interactions between abiotic (climatic) and biotic (host availability) factors in geographical space in …
2013
In invasion processes, both abiotic and biotic factors are considered essential, but the latter are usually disregarded when modeling the potential spread of exotic species. In the framework of set theory, interactions between biotic (B), abiotic (A), and movement-related (M) factors in the geographical space can be hypothesized with BAM diagrams and tested using ecological niche models (ENMs) to estimate A and B areas. The main aim of our survey was to evaluate the interactions between abiotic (climatic) and biotic (host availability) factors in geographical space for exotic symbionts (i.e., non-free-living species), using ENM techniques combined with a BAM framework and using exotic Entoc…
In Vitro Dialyzability of Zinc from Different Salts Used in the Supplementation of Infant Formulas
1999
Seven zinc salts--acetate, chloride, lactate, sulfate, citrate, gluconate, and oxide--were added to milk--and soy-based infant formulas to estimate possible differences in zinc availability depending on the type of salt used. For this purpose, an in vitro method that estimates the dialyzability of the element (i.e., the fraction available for absorption) was applied. Zinc dialyzability is always higher in milk-based products than in soy products, even when the total zinc contents are higher in the latter. The salts can be classified according to the zinc dialyzability in the two types of formulas as follows: oxidegluconate = chloride = lactatecitrate = acetatesulfate. Therefore, according t…