Formulation, Development, Evaluation and Solubility Enhancement of Lercanidipine Hydrochloride by Solid Dispersion Techniques

Background: Solid dispersions (SDs) are the dispersion of hydrophobic drugs in an inert hydrophilic carrier. SDs are prepared to improve the dissolution properties and bioavailability of slightly water-soluble drug molecules by dispersing them into an inert hydrophilic carrier. Aims and Objective: Evaluate the dissolution and solubility of Solid Dispersion of Lercanidipine Hydrochloride (LER). Materials and Methods: To study the effect of polymer, dissolution and solubility studies were carried out. Solid state characterizations of prepared solid dispersions were performed by differential scanning calorimetry (DSC).Drug- carrier interactions were studied by FT-IR spectroscopy, whereas X-ray diffraction of powder was done to demonstrate the crystal structure of the dispersions. Results: The prepared solid dispersion exhibited 94% drug release at 30 minutes which is higher than both LER pure and LER MKT. Better dissolution characteristic of solid dispersion was confirmed by 9.86 min MDT and 63.12% DE30 which is higher than that of LER MKT (13.64 MDT, 46.92 % DE30) Solid state characterization revealed that enhancement of dissolution is the result of conversion of crystalline form of LER to less crystalline and/or amorphous form. Conclusion: Solid dispersion of LER can successfully be prepared with the PEG6000 in the ratio of 1:6 using solvent evaporation technique. It is a successful and easy approach for the increase in onset of action of drug after administration and facilitates treatment of cardiovascular diseases.

FABRICATION AND ASSESSMENT OF LERCANIDIPINE HYDROCHLORIDE SOLID DISPERSIONS FOR SOLUBILITY PREFERMENT USING POLYMER COMBINATION

Objective: An attempt has made in fabricating solid dispersions (SDs) by taking lercanidipine hydrochloride (LCD) as a model drug. Methods: The SDs were made using a poly mix of poly vinyl pyrrolidone (PVP) K-30, Poloxamer-188, and hydroxy propyl methyl cellulose (HPMC) K4M. Different proportions of LCD: polymer mix in 1:1, 1:3, 1:5, and 1:7 ratios were fabricated as SDs by solvent evaporation and melting method, further compressed into tablets. The LCD SDs were assessed for physicochemical, and LCD release possessions. Results: The results were observed to be attractive with the increase in solubility LCD SD (F-3 and F-7) with 1:5 ratios of LCD. Conclusion: The study concludes that the poly mix of PVP K-30, Poloxamer-188, and HPMC K4M and was found to be a better combination for elevating the solubility and release of LCD from the SDs.

Fabrication and Characterization of Lercanidipine Hydrochloride Solid Dispersions by Fusion Technique

The authors aimed to design solid dispersions with Lercanidipine Hydrochloride (LCD) with PVP K-30, Poloxamer-188, and HPMC K4M as carriers. Various mixtures of LCD and Polymers (PVP K-30, Poloxamer-188, and HPMC K4M) were made in 1:1, 1:3, 1:5 and 1:7 ratios, and the solid dispersion was prepared by melting tactic, later compressed into tablets. Drug excipient compatibility studies were examined by DSC and FTIR studies. LCD was found to compatible with carriers used. The LCD solid dispersion was measured for physicochemical quality both in solid dispersions SD, and tablet states. The LCD solid dispersions found to have excellent flow possessions and compression assets. The yield of prepared solid dispersion was observed to be more than 90%), and the formulation LPOX-3 has showed a good yield of 98.9±1.95%, The tablets which were compressed from solid dispersions were found to have a uniform in size, shape, color, and consistency. The tablets were observed to have a uniform in thickness, and weight and ranged from 300.2±1.64 to 301.7±1.64 mg. The loss on friability was less than 1%, and the hardness was more than 4 Kg/cm2 indicates significant mechanical strength and the LCD content was also found to be uniform (96.8±1.35 to 99.9±2.34). The solubility of LCD was found to be good in 0.1N HCl and diminished with an increase in pH of the buffer. LCD released from the tablets were firstly by eruption followed by zero order. The dissolution was found to be good in solid dispersions with LCD: Poloxamer-188 at the ratio of 1:5. The results obtained were satisfactory. The study concludes that LCD solid dispersions (LPOX-3) with 1:5 ratios of LCD and Poloxamer-188 was found to be a better carrier than PVP K-30, and HPMC K4M in increasing the solubility of LCD from the solid dispersions.

Pharmacokinetic and bioavailability study of lercanidipine hydrochloride fast disintegrating tablets in rabbits by high-performance liquid chromatography

In the present study, fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) were tested in vivo in the buccal cavity of the rabbits. Various pharmacokinetic parameters were analysed in the study, including maximum measured plasma concentration (Cmax), time of maximum measured plasma concentration (tmax) and area under the plasma concentration vs time curve (AUC). Also, the comparative study of the Lercanidipine Hydrochloride fast disintegrating tablets (LFDT) was performed with the marketed conventional tablets of the drug (LMKT). The technique selected for the bioanalytical analysis of the blood samples of the rabbits for pharmacokinetic data computation was High-Performance Liquid Chromatography. An already well-established and validated method was used to analyse the blood samples of the rabbits. The results revealed that the rate of absorption was improved for fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) as compared to the marketed conventional tablets of the drug (LMKT). This indicated that drug was rapidly absorbed from the fast disintegrating tablet and attained elevated plasma concentration in a short interval after dosing than the marketed formulation. However, the value of tmax was drastically shorter for LFDT than the LMKT. The average peak plasma concentration also designated a rise in the extent of absorption (AUC). From the present study, it was concluded that the fast disintegrating tablet batch (LFDT) had much more improved pharmacokinetic parameters as compared to its conventional marketed counterpart (LMKT).