scholarly journals TRANSDERMAL DELIVERY OF CALCIUM CHANNEL BLOCKER: DEVELOPMENT AND CHARACTERIZATION

Author(s):  
Surya Teja S P ◽  
Manisha Khandelwal ◽  
Chitra V ◽  
Damodharan N

  Objective: Felodipine, a BCS class II calcium channel blocker, is used in the management of hypertension and angina pectoris. Due to the poor solubility and low bioavailability of the drug, there is a necessity to design an alternative route to achieve a constant plasma concentration of felodipine for its maximum therapeutic utility and can be achieved by transdermal route.Methods: In this study, matrix type transdermal patches were prepared using different combinations of hydrophilic polymer, namely, polyvinylpyrrolidone (PVP) and hydrophobic polymer, namely, ethyl cellulose (EC) by solvent evaporation technique and were subjected for characterization.Results: The Fourier transform infrared studies confirmed the compatibility between drug and polymers. Hydrophilic nature of the polymers greatly influenced physical characteristics and dissolution rate. Equal percentage of PVP and EC yielded patches with good folding endurance. The concentration of plasticizer present in the patches gave them desired folding endurance, and it increased with the presence of hydrophilic polymer. The formulation with highest PVP concentration, F3, exhibited a maximum drug release of 96.23% for 24 hrs. While the formulation with highest EC concentration, F5, exhibited only 74.45% drug release for 24 hrs.Conclusion: From the data, formulation F2 (PVP/EC, 2:1) can be concluded as best formulation due to its desired physical characteristics, good initial drug release, sustained release behavior, and good in vitro permeation. This formulation can be further studied in a clinical scenario.

Author(s):  
SHIFA SHAUKAT HAJU ◽  
SHEELA YADAV

Objective: Buccal drug delivery is the most suited route for local as well as systemic delivery of drugs. Cilnidipine is an L/N type dihydropyridine 4th generation calcium channel blocker (CCB), which decreases hypertension by blocking the N-type calcium channel to attenuate vascular sympathetic neurotransmission. It has high first-pass metabolism leading to low bioavailability. Hence the present research work was undertaken to formulate mucoadhesive buccal film of Cilnidipine with an objective to enhance therapeutic efficacy, bioavailability and was developed to administer into the unconscious and less-co-operative patients. Methods: Cilnidipine buccal films were prepared by a solvent-casting technique using various concentrations of mucoadhesive-polymers such as Hydroxyl propyl methylcellulose (HPMC) E15 and K4M and ethyl-cellulose as backing-layer, which acts like a patch providing unidirectional drug release. Prepared films were evaluated for their weight variation, thickness, surface-pH, swelling-index, drug content uniformity, in vitro residence time, folding endurance, tensile strength, in vitro release and permeability studies. Results: The infra-red (IR) spectra showed no interaction, and Physico-chemical characteristics were found within the limit. Swelling of the film increases with increasing concentration of polymers and %drug content of all formulations found to be in the range of 92.13%±0.94% to 97.92%±0.35%. The formulation F5, showed a promising tensile strength, folding endurance and in vitro drug release of about 95.18±0.03%, thus can be selected as an optimized formulation of mucoadhesive buccal film. Conclusion: The formulation of Cilnidipine mucoadhesive buccal film was found to be satisfactory and reasonable.


2011 ◽  
Vol 128 (2) ◽  
pp. 111-115 ◽  
Author(s):  
Juliana Q. Reimão ◽  
Fábio A. Colombo ◽  
Vera L. Pereira-Chioccola ◽  
André G. Tempone

2019 ◽  
Vol 9 (3) ◽  
pp. 51-59
Author(s):  
JESINDHA BEYATRICKS ◽  
, Dhananjaya

The aim of this study was to formulate and evaluate the oral fast-dissolving film of Vitamin B6 for the effective management of motion sickness and vomiting during pregnancy. Fast-dissolving films were prepared by the solvent-casting method using different polymers, HPMC-15 and Pullulan, along with Propylene glycol as a plasticizer. The Fourier-transform infrared study for the drug-polymer interaction was carried out. Evaluation of physical parameters such as physical appearance, surface texture, uniformity of weight, uniformity of strip thickness, surface pH, folding endurance, uniformity of drug content and percentage of moisture absorption were performed. Kinetic data analysis for the release study and the stability study were also performed. Results of uniformity of weight, thickness, folding endurance, surface pH, percentage drug content, tensile strength and percentage elongation of all the films were found to be satisfactory. The Fourier-transform infrared study indicated that there was no interaction between the drug and the polymers. The in-vitro drug release study showed that a better rate of drug release was achieved by formulations F4 and F8 compared with other formulations. The stability study did not show any significant difference in the external appearance, the drug content and the in-vitro drug release. In conclusion present study suggested that fast dissolving films has a better ability to cross the sublingual barrier at a faster rate, and hence the delivery system was found to be promising as it has the potential of overcoming the drawbacks associated with tablet formulations available in the market presently. Keywords: Fast-dissolving film, Vitamin B6, HPMC-15, Pullulan gum, Mango peel pectin, Crospovidone, solvent casting


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