![]() In our study, we will interpret the effect of formulating Tel in surface solid dispersions (Tel-SSDs) using different hydrophilic polymers, superdisintegrants and combined matrix. Several studies report the incorporation of some additives as surfactants, additional hydrophilic polymers and superdisintegrants to achieve more enhanced drug release. ![]() SDs not only provide a more amorphous state for the drug, but also increase the wettability of the drug associated with the presence of hydrophilic polymers. Nowadays, more than 30% of market drugs that require solubility enhancement are formulated in a solid dispersion form. Solid dispersions (SDs) have been proven to cause significant enhancement in the solubility of poorly soluble drugs, since active pharmaceutical ingredients dispersed inside the carrier matrix in an amorphous form. Additionally, some studies included the use of alkalinizers, which proved to be effective but can cause instability problems. There are many successful approaches to enhance Tel solubility, yet most include expensive and multistep techniques. However, the main problem of Tel is its poor aqueous solubility in biological fluids. Another superior characteristic is its high lipophilicity that ensures more effective distribution and tissue penetration. Tel has the longest half-life (24 h) compared to other angiotensin II receptor blockers. Telmisartan (Tel) is a potent, non-peptide antagonist of the angiotensin II type-1 receptor that is indicated for the treatment of hypertension. ![]() Consequently, the prevention and treatment of hypertension are of social significance. Hypertension is one of the main causes of heart disease, and in recent years, the age adjusted hypertension and hypertension disease death rates are increasing. Formulation of Tel SSDs using combined carriers proved to be effective in enhancing the aqueous solubility and dissolution rates of Tel, as well as showing good stability upon aging. The effect of aging results proved a non-significant difference in the drug content and dissolution profiles between fresh and aged samples. Combined surface solid dispersions employing superdisintegrant croscarmellose sodium with either hydrophilic polymer PEG 4000 or Poloxamer 407 gave remarkable enhancement in solubility and dissolution rates of Tel where more than 90% of the drug was released within 20 min. Tel-SSDs showed pertinent enhancement related to the carrier used. All Tel-SSDs showed acceptable physical properties. Effect of aging was studied by comparing the drug content and dissolution profiles of freshly prepared SSDs with aged samples. Dissolution profiles were studied using model dependent and independent approaches and were subjected to the pair-wise procedure using the DDsolver software program. Saturation, aqueous solubility, and dissolutions rates were determined. Both drug content and percentage yield were calculated to judge the efficiency of the preparation technique used. Tel-SSDs were evaluated optically and thermally to reveal a complete loss of the crystalline nature of the drug. Compatibility between Tel and different carriers was examined via FT-IR. Tel-SSDs were formulated using thesolvent evaporation method. This study adopted the use of surface solid dispersions (SSDs) employing superdisintegrants, hydrophilic polymers and combined carriers including a superdisintegrant with a hydrophilic polymer. Our aim was to improve Tel solubility and dissolution rates without the need for expensive multistep procedures, and without inclusion of alkalinizers. Telmisartan (Tel) is a potent antihypertensive drug with a very poor aqueous solubility, especially in pH ranging from 3 to 9 (i.e., biological fluids) that results in poor bioavailability.
0 Comments
Leave a Reply. |
Details
AuthorWrite something about yourself. No need to be fancy, just an overview. ArchivesCategories |