Volume 9, Number 19, January - March, 2017


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About the Cover

Tamoxifen Citrate (TC) is BCS Class–II, anticancer, antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxyl tamoxifen. In other tissues such as the endometrium, it behaves as an agonist, and thus may be characterized as a mixed agonist/antagonist. Tamoxifen is the used in endocrine (anti-estrogen) therapy for hormone receptor-positive breast cancer in pre-menopausal women, and is also a standard in post-menopausal women although aromatase inhibitors frequently used in that setting. Breast cancer is the most common cause of cancer related deaths among women worldwide. Liquisolid compacts technique is a new and promising method that can enhance the dissolution rate of water insoluble drugs. According to the liquisolid compacts techniques, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non-volatile liquid vehicles can be converted into acceptably flowable and compressible powders by blending with selected powder excipients. According to solubility of TC in various non-volatile liquid vehicles (Oils) Propylene glycol was selected. Avicel PH 112, Aeroperl 300 were selected as carrier and coating material respectively. For optimized batch, pre-compressible and post-compressible parameters were evaluated & found that all were under the standard limits. In-Vitro drug release of the optimized tablets was compared with the marketed preparation and showed better release. The stress study of API and optimized Liquisolid compacts formulation was also done and it showed better result. From this, it was concluded that the liquisolid technique is a promising alternative for improvement of dissolution of water-insoluble drugs (Ref: Pandya DT. Formulation development and evaluation of Tamoxifen Citrate by Liquisolid Techniques. Discovery Pharmacy, 2017, 9(19), 1-10).

ANALYSIS

Formulation development and evaluation of Tamoxifen Citrate by Liquisolid Techniques

Pandya DT

Tamoxifen Citrate (TC) is BCS Class–II, anticancer, antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxyl tamoxifen. In other tissues such as the endometrium, it behaves as an agonist, and thus may be characterized as a mixed agonist/antagonist. Tamoxifen is the used in endocrine (anti-estrogen) therapy for hormone receptor-positive breast cancer in pre-menopausal women, and is also a standard in post-menopausal women although aromatase inhibitors frequently used in that setting. Breast cancer is the most common cause of cancer related deaths among women worldwide. Liquisolid compacts technique is a new and promising method that can enhance the dissolution rate of water insoluble drugs. According to the liquisolid compacts techniques, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non-volatile liquid vehicles can be converted into acceptably flowable and compressible powders by blending with selected powder excipients. According to solubility of TC in various non-volatile liquid vehicles (Oils) Propylene glycol was selected. Avicel PH 112, Aeroperl 300 were selected as carrier and coating material respectively. For optimized batch, pre-compressible and post-compressible parameters were evaluated & found that all were under the standard limits. In-Vitro drug release of the optimized tablets was compared with the marketed preparation and showed better release. The stress study of API and optimized Liquisolid compacts formulation was also done and it showed better result. From this, it was concluded that the liquisolid technique is a promising alternative for improvement of dissolution of water-insoluble drugs.

Discovery Pharmacy, 2017, 9(19), 1-10

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