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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Rao, Monica R. P. Bhingole, Rohini C. |
| Description | Country affiliation: India Author Affiliation: Rao MR ( a Department of Pharmaceutics , AISSMS College of Pharmacy , Pune , India.); Bhingole RC ( a Department of Pharmaceutics , AISSMS College of Pharmacy , Pune , India.) |
| Abstract | CONTEXT: Gabapentin was selected to formulate oral controlled release dry suspension because of short biological half life of 5-7 h and low bioavailability (60%). Gabapentin is a bitter drug so an attempt was made to mask its taste. OBJECTIVE: To formulate and evaluate controlled release dry suspension for reconstitution to increase the bioavailability and to control bitter taste of drug. MATERIALS AND METHODS: Cyclodextrin based nanosponges were synthesized by previously reported melt method. The nanosponge-drug complexes were characterized by FTIR, DSC and PXRD as well as evaluated for taste and saturation solubility. The complexes were coated on Espheres by a suspension layering technique followed by coating with ethyl cellulose and Eudragit RS-100. A dry powder suspension for reconstitution of the microspheres was formulated and evaluated for taste, redispersibility, in vitro dissolution, sedimentation volume, leaching and pharmacokinetics. RESULTS AND DISCUSSION: The complexes showed partial entrapment of drug nanocavities. Significant decrease in solubility (25%) was observed in the complexes than pure drug in different media. The microspheres of nanosponge complexes showed desired controlled release profile for 12 h. Insignificant drug leaching was observed in reconstituted suspension during storage for 7 days at 45 °C/75% RH. Nanosponges effectively masked the taste of Gabapentin and the coating polymers provided controlled release of the drug and enhanced taste masking. The results of in vivo studies showed increase in bioavailability of controlled release suspension by 24.09% as compared to pure drug. CONCLUSION: The dry powder suspension loaded with microspheres of nanosponges complexes can be proposed as a suitable controlled release drug delivery for Gabapentin. |
| File Format | HTM / HTML |
| ISSN | 03639045 |
| Issue Number | 12 |
| Volume Number | 41 |
| e-ISSN | 15205762 |
| Journal | Drug Development and Industrial Pharmacy |
| Language | English |
| Publisher | Taylor & Francis |
| Publisher Date | 2015-01-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Amines Administration & Dosage Pharmacokinetics Cyclohexanecarboxylic Acids Nanoparticles Metabolism Gamma-aminobutyric Acid Administration, Oral Adult Chemistry Animals Chemistry, Pharmaceutical Delayed-action Preparations Dose-response Relationship, Drug Humans Male Rats Rats, Wistar Suspensions Taste Drug Effects Physiology X-ray Diffraction Young Adult Journal Article |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Drug Discovery Pharmacology Pharmaceutical Science |
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