Formulation and evaluation of Diltiazem Extended-Release pellets

Abstract

Introduction: Diltiazem hydrochloride is one of the calcium channel blockers and is widely used for treating angina and high blood pressure and arrhythmias due to its low half-life, patients are required to take medicines several times a day, so it is necessary to prepare sustaine release form of medicine for ease of use and reduce the risk of forgetfulness of using the drug. Aim: The goal is to provide sustain-release pellets of diltiazem hydrochloride. Method: The method of making pellets in this study is the Extruder- Spheronizer method. In this method, an appropriate dough mass is obtained from the formulation and entered into the machine. The resulting pellets are finally checked in terms of physico chemical properties and appropriate pellets are selected. Result: The results of this study showed that formulations 6, 11 and 12 did not differ significantly in terms of particle size and drug loading in the pellets. Most pellets from these formulations have a particle size of 710-850 microns and the drug loading rate in these formulations was higher than 90%. In Formula 6, the drug was released at early times due to the formation of porosity in the RL PO eudragit during the dissolution test. Due to the high solubility of the drug in water, fatty excipients, such as stearyl alcohol, were used to sustain release formulations. After examining the formulations, the formulations containing 20% of stearyl alcohol released after 3 hours of the dissolution test above 30% of the drug, which should be below 25% for the USP. Thus, the amount of stearyl alcohol increased by 30%. In this formulation, after about 3 hours of the dissolution test, about 22% of the drug was released and after the end of 12 hours, the release of the drug in all three tubes was above 70%. Therefore, formulation 12, containing 20% of the drug and 30% of alcohol stearyl, was sustain released in terms of USP. Discussion and conclusion: Many factors involved in this formulation, some of which are related to the formulation, and some are related to the Extruder- Spheronizer. Some of the most important factors such as temperature, water consumption, speed and rotation time of the device were investigated in this study. Odegraditis and low percentages of stearyl alcohol did not slow down the release of soluble diltiazem water. Therefore, to formulate this formulation, not only the factors involved in the formulation must be optimized, but also the type, amount and proportion of the formulation components.