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Enhancement of Solubility and Dissolution Rate of Bcs Class Ii Drug Ritonavir Using Liquisolid Technique
| Content Provider | Semantic Scholar |
|---|---|
| Author | Bonthagarala, Brahmaiah Dasari, Varun Kotra, Vijay |
| Copyright Year | 2019 |
| Abstract | BCS class II drugs usually suffer inadequate bioavailability as a dissolution step is the absorption rate-limiting step. In this work, the effect of solubility increase at the main absorption site for these drugs was investigated using ritonavir as a drug model. The liquidsolid technique was applied to prepare ritonavir per-oral tablets of high dissolution rate using versatile non-ionic surfactants of high solubilizing ability [Transcutol HP, labrasol and labrasol/labrafil (1:1) mixture] as liquid vehicles at different drug concentrations (10–30%) and fixed (R). The prepared liquisolid tablets were fully evaluated, and the dissolution rate at pH 1.2 was investigated. The formula of higher dissolution rate was subjected to solid state characterization using Differential Scanning Calorimetric (DSC), Infrared Spectroscopy (IR). Results showed that liquisolid tablet prepared using labrasol/labrafil (1:1) mixture as a liquid vehicle containing 10% ritonavir is a compatible formula with a higher dissolution rate (100% in 35 min). This led to the conclusion that liquisolid technique efficiently improved the drug solubility and dissolution rate of BCS class II drugs. INTRODUCTION: To get a significant plasma drug concentration a desired pharmacological action is required. The plasma drug concentration is related to solubility in GI fluids 1 . The presence of the drug in solution form is important for drug absorption mechanisms from GIT 2 . According to BCS classification system, poorly water-soluble drugs are categorized as Class-II. In these, dissolution is the rate-limiting step in the absorption process. QUICK RESPONSE CODE DOI: 10.13040/IJPSR.0975-8232.10(5).2430-38 The article can be accessed online on www.ijpsr.com DOI link: http://dx.doi.org/10.13040/IJPSR.0975-8232.10(5).2430-38 For such drugs improvement of drug solubility and dissolution is the main challenge after oral administration 3 . Till date, different techniques had been designed for improving the solubility characteristics of poorly water-soluble drugs. Some of these include solvent change coprecipitation 4 , solid dispersion 5 , inclusion complexes with β-cyclodextrins 6 , nanosuspensions 7 , microencapsulation 8 , soluble salts formation 9 , lyophilization 10 and liquisolid technique 11 . The liquisolid technique is a recent one for the improvement of solubility of insoluble drugs. In this technique for the preparation of liquid medication, the poorly soluble drug is dissolved or suspended in a water-miscible non-volatile solvent. As per mathematical model described by Spireas 12 |
| File Format | PDF HTM / HTML |
| DOI | 10.13040/ijpsr.0975-8232.10(5).2430-38 |
| Alternate Webpage(s) | http://ijpsr.com?action=download_pdf&postid=51417 |
| Alternate Webpage(s) | http://ijpsr.com/?action=download_pdf&postid=51417 |
| Alternate Webpage(s) | https://doi.org/10.13040/ijpsr.0975-8232.10%285%29.2430-38 |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
