Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach

Abstract

Low solubility causing low dissolution in gastrointestinal tract is the major problem for drugs meant for systemic action after oral administration, like cinnarizine. Pharmaceutical products of cinnarizine are commercialized globally as immediate release preparations presenting low absorption with low and erratic bioavailability. Approaches to enhance bioavailability are widely cited in the literature. An attempt has been made to review the bioavailability complications and clinical therapeutics of poorly water soluble drug: cinnarizine. The interest of writing this paper is to summarize the pharmacokinetic limitations of drug with special focus on strategies to improvise bioavailability along with effectiveness of novel dosage forms to circumvent the obstacle. The paper provides insight to the approaches to overcome low and erratic bioavailability of cinnarizine by cyclodextrin complexes and novel dosage forms: self-nanoemulsifying systems and buoyant microparticulates. Nanoformulations need to systematically explored in future, for their new clinical role in prophylaxis of migraine attacks in children. Clinical reports have affirmed the role of cinnarizine in migraine prophylaxis. Research needs to be dedicated to develop dosage forms for efficacious bioavailability and drug directly to brain.

Design of Organic Macrocycle‐Modified Iron Oxide Nanoparticles for Drug Delivery

“…CDs have been used extensively for drug‐delivery applications because of their stability, biocompatibility, and ease of structural modification . Various studies have shown that CDs increase drug solubility and stability, contribute to sustained drug release, enhance membrane permeability and bioavailability, and minimize toxicity . As a result of these favorable properties and the ability of their hydroxyl groups to interact with iron oxide, many systems for targeted drug delivery, including IONPs, have incorporated CDs.…”

Cinnarizine Liquid Solid Compacts: Preparation Evaluation

“…A large number of new chemical entities which have high potential to be developed as useful drugs have failed to reach the public merely due to the poor dissolution rate which results in unsatisfactory bioavailability. An orally administered drug must be insolubilized state and be able to cross the gastrointestinal tract (GIT) membrane to show its therapeutic effects [1]. The therapeutic effect of a drug relies on the bioavailability which is highly dependent on the solubility factor as well as the dissolution rate of the drug.…”

Optimization of the Method for Obtaining Nanocapsules, Development of the Methods of Determining the Degree of Cinnarizine Inclusion in a Prolonged Dosage Form Based on Poly-D, L-Lactid-Co-Glicolide, and Its Validation

“…Основной группой лекарственныхпрепаратов, назначаемых при данной патологии, являются блокаторы кальциевых каналов,в частности циннаризин, эффективность которого доказана многочисленными клиническими исследованиями [5]. Существующие лекарственные формы цин-наризина имеют ряд недостатков, а именно: частота приема, наличие побочных эффектов [6,7]. Решением по нивелированию данных нежелательных факторов является разработка пролонгированной формы циннаризина, позволяющей уменьшить частоту приемов и тем самым избежать резких изменений концентрации препарата в организме, то есть способной поддерживать концентрацию препарата в организме относительно постоянной и терапевтический эффективной.…”