Unmet Therapeutic Need
For a number of drug substances, lower bioavailability, high variability and adverse reactions are major limitations for achieving optimal therapeutic outcome. Different technologies have been developed to increase the solubility of the drug, however many of these employ either newer non-GRAS excipients or tedious non-conventional methods for manufacturing. A novel technology RubiEn® is therefore developed which can solubilise drugs using GRAS listed excipients and with conventional methods of manufacturing. . Depending upon the nature and solubility of the active agent a 2-10 fold increase in solubility can be achieved using this Technology.
Potential Drug Candidates for RubiEn®
Your Molecule ; Our Technology
Drug molecules which exhibit one or more of following properties are potential candidates for RubiEn®-
- Poor aqueous solubility
- Low bioavailability
- Too rapid an onset of action
- Significant side effects
- Opportunity for LCM
RubiEn® is a unique solubilization technology based on micellar solubilization. The technology involves treatment of a drug with selected GRAS listed excipients resulting in increase in the solubility leading to increased dissolution rate and complete dissolution . Thus RubiEn® increases the absorbable form of the drug resulting in an increase in the bioavailability of the drug. By increasing the solubility of a pH-dependent drug using RubiEn®, it may be possible to achieve a pH independent dissolution profile.
A number of in-vitro tools are employed for the performance evaluation of the system. Several in-vivo studies in human volunteers with an anti-hypertensive agent indicated increased bioavailability with a reduction in variability.
The basic technology is protected by patent applications filed in various countries. Additional patent applications have also been filed for expanding the scope of RubiEn® technology.
- Applicable to drugs having different effective doses
- Possible to develop dose weight similar/proportional formulations for multiple drug strengths
- Pharmacopoeial and GRAS listed excipients
- Conventional, robust method of manufacture
Bioenhanced formulation of an antihypertensive agent
The antihypertensive agent employed in the study had a low solubility in the acidic environment leading to low and variable bioavailability (~ 25%) for the marketed conventional dosage form. Treatment of this drug with solubility enhancing agents resulted in a four fold increase in solubility and a pH independent release profile. An in-vivo study in human volunteers resulted in a 1.6 fold increase in bioavailability with significantly reduced variability in pharmacokinetic parameters. Further Tmax for the RubiEn® formulation was reduced (1-2 hrs) compared to 3-4 hrs for the marketed formulation
Challenges and achievements
- 1.6 fold increase in bioavailability
- Lower variability
- Possibility of rapid onset of action