فن پراکنش جامد برای افزایش حل‌پذیری داروهای کم‌محلول در آب

نوع مقاله : تالیفی

نویسندگان

1 عضو هیئت علمی / پژوهشگاه پلیمر و پتروشیمی ایران

2 پژوهشگاه پلیمر و پتروشیمی ایران

چکیده

حل­ پذیری و نفوذپذیری داروها از مهم­ترین خواص هر داروست که بر زیست­ فراهمی آن­ ها اثر می ­گذارد. در سامانه طبقه‌بندی زیست ­داروها (BCS) تعداد زیادی از مواد فعال دارویی با حل ­پذیری کم (گروه ­های IV و II) قرار دارند که به­ ندرت به بازار مصرف عرضه می­ شوند. بنابراین لازم است، راه ­حلی برای افزایش حل ­پذیری این نوع داروها ارائه شود. روش­ های زیادی برای فرمول­ بندی داروهای نامحلول در آب با هدف افزایش حل ­پذیری و به ­واسطه آن افزایش جذب دارو در دستگاه گوارش ارائه شده است. از این میان، روش پراکنش جامد از مهم­ترین روش ­ها محسوب می ­شود. از دهه 1960 میلادی، ایجاد فرمول­ بندی­ های دارویی برپایه روش پراکنش جامد دست­خوش پیشرفت­ های چشمگیری شده است. برای تهیه سامانه ­های حاوی دارو می ­توان به رویکردهای برپایه حلال و روش مذاب اشاره کرد. کاربرد بسترهای مختلف از حامل پلیمری منفرد تا حامل ­های چندتایی حاوی امولسیون ­کننده در طراحی فرمول­ بندی پراکنش جامد منجر به بهبود پایداری و عملکرد این سامانه­ ها شده است. در این مقاله، کاربرد فن پراکنش جامد برای تهیه فرمول­ بندی­ های دارویی معرفی شده و روش تهیه و پیشرفت ­های اخیر در این زمینه به­ طور خلاصه مرور می ­شود.

کلیدواژه‌ها

موضوعات

عنوان مقاله [English]

Solid Dispersion Technique to Enhance the Solubility of Poorly Water-Soluble Drugs

نویسندگان [English]

  • Arezou Mashak 1
  • Hamid Mobedi 2
1 -
2 Iran polymer and petrochemical institute
چکیده [English]

The solubility and permeability of drugs are the most important biopharmaceutical properties that affect their bioavailability. In the biopharmaceutics classification system (BCS), there are a large number of active pharmaceutical ingredients (APIs) with low solubility (BCS classes II and IV) that are rarely offered to the market. Therefore, it is necessary to provide a solution to increase thier solubility. There are many preparation methods to enhance the solubility and dissolution rate of drugs and thereby absorption in the gastrointestinal tract. Among them, the solid dispersion method is considered one of the most important methods. Since 1960s, the development of pharmaceutical formulations based on the solid dispersion method has undergone significant progress. Solvent-based and melting methods can be mentioned for the preparation of drug-containing systems. The use of different substrates from a single polymeric carrier to multiple carriers containing emulsifier in the design of solid dispersion formulations has led to the improvement of the stability and performance of these systems. In this article, the solid dispersion technique for the preparation of pharmaceutical formulations is introduced, and also a summary of the preparation methods and the recent advances in this field are briefly reviewed.
 

کلیدواژه‌ها [English]

  • solid dispersion system
  • poor water solubility drug
  • hydrophilic polymer
  • solvent evaporation method
  • solubility

مراجع

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