Montañas Karakucuk
Una serie de factores como la solubilidad, la solidez a temperatura ambiente, la compatibilidad con los disolventes, los excipientes y la fotoestabilidad desempeñan un papel fundamental en la formulación eficaz de los medicamentos. Hasta la fecha, más del 40% de los nuevos componentes sintéticos que se producen a través de los sistemas de liberación de medicamentos son mezclas lipofílicas o poco solubles en agua. Existen numerosos métodos de formulación disponibles para abordar los problemas de baja solubilidad y baja biodisponibilidad de los medicamentos. Los métodos habituales incluyen la micronización, el uso de soluciones grasas, el uso de potenciadores de entrada o cosolventes, la estrategia de dispersión de surfactantes, el desarrollo de sales, la precipitación, etc., pero estos métodos tienen una utilidad limitada en la mejora de la solubilidad de medicamentos poco solubles. Otros métodos son la estructura vesicular como los liposomas, la dispersión de sólidos, las estrategias de emulsión y microemulsión y las estructuras de concentración con ciclodextrinas, que muestran un efecto beneficioso como sistema de liberación de medicamentos, pero los problemas graves de estos métodos son la falta de relevancia general para todos los medicamentos. Los problemas de escasa disolución de los átomos de los fármacos limitan la retención de los tranquilizantes por vía oral o dérmica y, en última instancia, reducen la biodisponibilidad debido a la hidrofobicidad. Además, es un gran desafío determinar si los fármacos con una disolución insuficiente pueden desarrollar una disolución que les permita actuar adecuadamente. Algunos nuevos fármacos candidatos, que están llegando a la geometría de la diana-receptor mediante pruebas de alto rendimiento, tienen una masa subatómica elevada y un valor de Log P elevado que aumenta la insolubilidad.
Según el Sistema de Clasificación Biofarmacéutica, los medicamentos de Clase II y IV se consideran poco solubles en agua. Se considera que los cambios físicos (micronización, desarrollo de polimorfos, dispersiones fuertes, estructuras de ciclodextrina, uso de solubles naturales), los cambios de composición (planificación de profármacos, estructuras de sal) o los enfoques nanotecnológicos (micelas, liposomas, nanoemulsiones, etc.) superan los problemas de baja solubilidad en agua. Los cambios físicos y de composición tienen algunos inconvenientes, por ejemplo, no son pertinentes a cada sustancia activa del medicamento, no brindan una adecuada solubilidad en inmersión ampliada o causan pérdida de acción. La nanotecnología se puede utilizar para solucionar los problemas relacionados con las diferentes metodologías descritas anteriormente. La nanotecnología se caracteriza por ser la ciencia y el diseño realizados en la nanoescala, es decir, 10–9 m.
In the most recent years, it is viewed as that tranquilize nanosuspensions are one the best ways to deal with figure ineffectively dissolvable mixes. Nanosuspensions are scattered frameworks which have nanometer extend, normally 200-600 nm, unadulterated medication particles. They contain least measure of settling specialists, for example, surfactants as well as polymers. Nanosuspensions can be delivered by precipitation, wet processing, high weight homogenization, or blend of these strategies. With remarkable properties of nanosuspensions by giving expanded surface region of medication articles, they can improve immersion solvency and disintegration pace of ineffectively dissolvable medications and thus oral or dermal bioavailability. The medication microparticles/micronized sedate powder is moved to tranquilize nanoparticles by methods like Bottom-Up Technology and Top-Down Technology. Nanosuspensions are submicron colloidal scatterings of nanosized tranquilize particles balanced out by surfactants. Nanosuspensions comprise of the ineffectively water-dissolvable medication with no grid material suspended in scattering. These can be utilized to upgrade the dissolvability of medications that are ineffectively solvent in water just as lipid media. Because of expanded solvency, the pace of flooding of the dynamic compound increments and the most extreme plasma level is arrived at quicker. This methodology is helpful for particles with helpless solvency, helpless porousness, or both, which represents a critical test for the formulators. The diminished molecule size delivers the chance of intravenous organization of inadequately dissolvable medications with no bar of the blood vessels. The suspensions can likewise be lyophilized and into a strong lattice. Aside from these points of interest, it additionally has the upsides of fluid definitions over others. Pharmaceutical nanosuspensions of medications are nanosized, heterogeneous watery scatterings of insoluble medication particles balanced out by surfactants. Conversely, nanoparticles are either polymeric or lipid colloidal transporters of medications. Nanosuspension procedure is the main alternative accessible, when a medication atom has numerous inconveniences, for example, failure to shape salt, huge sub-atomic weight and portion, high log P and softening point that obstruct them in creating appropriate details. Nanosuspensions can fathom such extraordinary medication conveyance issues related with the dynamic pharmaceutical fixings (API) by holding it in a translucent state while empower them with expanded medication stacking during detailing advancement. Obliging enormous medication sum with least portion volume has extra advantages in parenteral and ophthalmic medication conveyance framework inferable from the minimization of unnecessary utilization of unsafe non-watery solvents and extraordinary pH. Different focal points incorporate expanded dependability, continued arrival of medication, expanded viability through tissue focusing on, least first pass digestion and profound lung affidavit. The soundness of the submicron particles accomplished in the nanosuspension is for the most part ascribed to the uniform molecule size, which is shaped by various assembling procedures. Particles of nanosuspensions must stay unaltered in size all through its timeframe of realistic usability else it can start unconstrained precious stone development. In this manner, keeping up the uniform molecule size dispersion can frustrates the nearness of differing immersion dissolvability and accordingly repress any precious stone development because of Oswald aging impact. Nanosuspension of the medication can likewise be accomplished by weakening of emulsion, along these lines causing full dissemination of scattered stage into the constant stage bringing about the creation of nanosuspension. Microemulsion can be treated in comparative way for the creation of nanosuspensions. The impact of globule size and measure of surfactant (s) on the medication take-up of inward stage ought to be analyzed to create ideal medication stacking. Nanosuspension created by such strategies must be cleared from following solvents and different fixings by methods for ultrafiltration procedure to make it helpful for organization. Lyophilization of the nanosuspensions will be done to improve the physical and synthetic soundness and to conquer the incongruencies between the different detailing segments. Sanitization of the nanosuspensions should be possible either by film filtration (< 0.22 μm), steam heat cleansing or gamma illumination. Writing proposes that enhancement of base up nanosuspension approach requires fitting choice and setting appropriate convergence of excipients, for example, surfactant and polymer.
La capacidad específica de Qality by Design se conoce como Design of Experiment (DoE). El enfoque DoE analiza de manera objetiva las asociaciones entre los factores dentro del territorio del plan y permite el desarrollo de definiciones al considerar los atributos ideales del producto. El enfoque DoE ayuda a crear un plan de nanosuspensión al reducir la cantidad de pruebas, lo que resulta rentable y eficiente.
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