RESUMEN
Nintedanib is a competitive inhibitor of non-receptor tyrosine kinase (nRTKs) and receptor tyrosine kinase (RTKs). Nintedanib is a substrate for the P-glycoprotein transporter, which returns ingested substances to the gastrointestinal lumen. At present, Nintedanib is being prescribed for individuals diagnosed with idiopathic pulmonary fibrosis (IPF). This assessment provides a concise overview of the latest patents pertaining to Nintedanib. The patents covered in this analysis are categorized into sections, including patents related to the active ingredient, polymorph, formulation, and treatment method. The purpose of this compilation is to offer researchers convenient access to all the relevant patents in a single resource. Information was collected from diverse web databases, including both paid and free sources. Paid databases, such as Orbit® and SciFinder® were utilized as examples. On the other hand, free databases, such as the European Patent Office's Espacenet®, WIPO Patentscope® the Indian patent database, and Google Patents, were also accessed for data gathering purposes. The orange-book listed patents for Nintedanib are set to expire in July 2029. These patents explore various excipients to address the solubility issue in the long-term storage of the formulation. However, despite these efforts, there is still a need for further research to enhance the properties of the Nintedanib formulation. Extensive research has been conducted on multiple methods for manufacturing Nintedanib and its formulations. This dynamic study has the potential to create opportunities for numerous generic companies to enter the United States market. This, in turn, will improve healthcare accessibility by lowering costs.
Asunto(s)
Fibrosis Pulmonar Idiopática , Humanos , Estados Unidos , Fibrosis Pulmonar Idiopática/tratamiento farmacológico , Indoles/uso terapéutico , Proteínas Tirosina Quinasas Receptoras , Medicamentos GenéricosRESUMEN
BACKGROUND: Levothyroxine Sodium is a thyroid hormone replacement therapy for Hypothyroidism. Levothyroxine Sodium is approved to treat Hypothyroidisim, to suppress thyroid hormone release from cancerous thyroid nodules, and to prevent the growth of goiters. In addition, it is also used to treat conditions such as myxedema, cretinism, and obesity. OBJECTIVE: This assessment highlights the overview of the recent patents of Levothyroxine Sodium. This review includes patents grouped in sections like product patents, process patents, and composition-related patents, along with the treatment methodology. The objective of this article is to impel pseudoscientists to all existing patents in a solitary place. METHODS: Data were gathered from various internet-based resources, including Patentscope ® (WIPO), Worldwide Espacenet® (EPO), Google Patents, and InPASS (Indian patent database). RESULTS: Several new processes and composition-related patents of Levothyroxine Sodium have been reported. Further, due to the problem of photosensitivity, oxidation during development, and stability of Levothyroxine Sodium formulation, several excipients are tried in these patents to stabilize the same. However, the formulation of Levothyroxine Sodium with better characteristics needs to be developed. CONCLUSION: Extensive exposure has been carried out towards various processes for the preparation of Levothyroxine Sodium and the composition of the same. This sort of dynamic exploration will clear the path for many generic players, which will lead to the reduction of the expense of the composition and accordingly enhance global health care at a less expensive cost.
Asunto(s)
Hipotiroidismo , Tiroxina , Humanos , Tiroxina/uso terapéutico , Patentes como Asunto , Hipotiroidismo/tratamiento farmacológico , Terapia de Reemplazo de HormonasRESUMEN
BACKGROUND: Pemetrexed is a folate analogue metabolic inhibitor for mammalian cells. Pemetrexed is toxic to several cancer cells by interfering with their new biosynthesis of nucleotides, thus causing cell apoptosis. Presently, Pemetrexed is given to patients with Non-Small Cell Lung Cancer (NSCLC). OBJECTIVE: This review focuses on the recent patents of Pemetrexed. This assessment includes patents grouped in segments like crystalline form patent, composition related patents, product patents, as well as a method of treatment. The aim of this review is to simplify inventors with existing patents in a single place. METHODS: Data were searched from several available databases, including paid databases which include Orbit® and SciFinder®. Free databases include Worldwide Espacenet® (EPO), Patentscope® (WIPO), InPASS (Indian patent database) and Google Patents. RESULTS: Some new polymorph and composition-related inventions of Pemetrexed have been recently patented as its orange-book listed patents will soon expire in May 2022. Further, because of the problem of oxidation through the development and continuing storage of Pemetrexed composition, several excipients are experimented with within these patents to stabilize the same. Nevertheless, there is a need for further development of an improved composition of Pemetrexed with improved characteristics. CONCLUSION: Wide research has been conducted on different processes for preparing Pemetrexed and formulation thereof. Such type of active research may clear the track for the generic companies in the United States, producing the formulation at low prices and providing universal health care at economical prices.
Asunto(s)
Adenocarcinoma del Pulmón/tratamiento farmacológico , Carcinoma de Células Grandes/tratamiento farmacológico , Carcinoma de Pulmón de Células no Pequeñas/tratamiento farmacológico , Antagonistas del Ácido Fólico/administración & dosificación , Neoplasias Pulmonares/tratamiento farmacológico , Patentes como Asunto , Pemetrexed/administración & dosificación , Antagonistas del Ácido Fólico/uso terapéutico , Humanos , Pemetrexed/uso terapéuticoRESUMEN
CONTEXT: Conventional ophthalmic solutions often eliminate rapidly after administration and cannot provide and maintain an adequate concentration of drug in the pre-corneal area. OBJECTIVES: Above problem can be overcome by the use of in situ gel forming systems that are instilled as drops in to the eye and undergo a sol-gel transition in the cul-de-sac. METHODS: An ion sensitive polymer gellan gum was used as gelling agent which formed immediate gel and remained for extended time period. Nanoparticles of moxifloxacin, prepared by solvent evaporation, were separated by freeze drying. The rheological properties and in vitro drug release test of in situ gel loaded with nanoparticles were evaluated and compared with marketed preparation. In vitro release study demonstrated diffusion controlled release for moxifloxacin from formulations over a period of 12 h. RESULTS: The developed formulation was stable and showed enhanced contact time minimizing the frequency of administration. Confocal microscopy showed clear permeation of drug loaded nanoparticles across L/S of cornea. CONCLUSION: The formulation of moxifloxacin was found liquid at the formulated pH and formed gel in the presence of mono or divalent cations. The gel formed in situ showed sustained drug release over a period of 10-12 h. The formulations were less viscous before instillation and formed strong gel after instilling it into cul-de-sac. It is thus concluded that by adopting a systematic formulation approach, an optimum point can be reached in the shortest time with minimum efforts to achieve desirable rheological and in vitro release property for in situ gel forming system.
Asunto(s)
Córnea/metabolismo , Sistemas de Liberación de Medicamentos/métodos , Fluoroquinolonas/química , Geles/química , Transporte Iónico/efectos de los fármacos , Soluciones Oftálmicas/química , Ácidos Polimetacrílicos/metabolismo , Polisacáridos Bacterianos/química , Córnea/química , Preparaciones de Acción Retardada , Fluoroquinolonas/administración & dosificación , Moxifloxacino , Nanopartículas , Soluciones Oftálmicas/farmacología , Ácidos Polimetacrílicos/química , Polisacáridos Bacterianos/metabolismoRESUMEN
CONTEXT: Conventional sustained dosage form of ranitidine hydrochloride (HCl) does not prevent frequent administration due to its degradation in colonic media and limited absorption in the upper part of GIT. OBJECTIVES: Ranitidine HCl floating tablet was formulated with sublimation method to overcome the stated problem. METHODS: Compatibility study for screening potential excipients was carried out using Fourier transform infrared spectroscopy (FT-IR) and differential scanning chromatography (DSC). Selected excipients were further evaluated for optimizing the formulation. Preliminary screening of binder, polymer and sublimating material was based on hardness and drug release, drug release with release kinetics and floating lag time with total floatation time, respectively. Selected excipients were subjected to 3(2) factorial design with polymer and sublimating material as independent factors. Matrix tablets were obtained by using 16/32" flat-faced beveled edges punches followed by sublimation. RESULTS: FT-IR and DSC indicated no significant incompatibility with selected excipients. Klucel-LF, POLYOX WSR N 60 K and l-menthol were selected as binder, polymer and sublimating material, respectively, for factorial design batches after preliminary screening. From the factorial design batches, optimum concentration to release the drug within 12 h was found to be 420 mg of POLYOX and 40 mg of l-menthol. Stability studies indicated the formulation as stable. CONCLUSION: Ranitidine HCl matrix floating tablets were formulated to release 90% of drug in stomach within 12 h. Hence, release of the drug could be sustained within narrow absorption site. Moreover, the dosage form was found to be floating within a fraction of second independent of the pH of media ensuring a robust formulation.