ABSTRACT
Abstract The goal of the present study was to develop inclusion complexes and polymers dispersions of ramipril prepared by physical mixing, kneading, co-evaporation, and solvent evaporation methods to enhance drug solubility and dissolution rate, and thereby to reduce drug dose and side effects using selected hydrophilic carriers such as β-CD, PVP-K25, PEG 4000, and HPMC K100M. The prepared formulations were characterized for solubility and in-vitro drug release studies. The systematic optimization of formulations was performed using I-Optimal experimental design by selecting factors such as type of carriers (X1), drug: carrier ratio (X2), and method of preparation (X3), and response variables including percent yield (Y1), solubility (Y2), Carr's index (Y3) and drug release in 30 min (Y4). Mathematical modeling was carried out using a quadratic polynomial model. The inclusion complex formulation (F27) was selected as an optimized batch by numerical desirability function and graphical optimization with the help of design space. The inclusion complex prepared by the co-evaporation method showed maximum drug solubility and released in pH 6.8 phosphate buffer compared to pure and other formulations. The inclusion complex is a feasible approach to improve the solubility, dissolution rate, bioavailability, and minimization of drugs' gastrointestinal toxicity upon oral administration of ramipril.
ABSTRACT
Rasamanikya prepared from Shodhita Haritala is one of the effective and economical medicines used in different skin and respiratory disorders. Different methods are explained in the classics for the preparation of Rasamanikya and few adopted methods are also developed from scholars of Rasashastra depending upon their experience. Present study is aimed at exploring all these methods in detail and any modifications if needed. The Patra Haritala is subjected to different Shodhana procedures in different media, the changes observed are discussed in the article. The yield of Shodhita Haritala was 92% to 96% in different Shodhana methods. Rasmanikya is prepared in six different methods. Sharava samputa method (Method III & IV) can be considered as suitable methods for pharmaceutical preparation of Rasamanikya in large quantity as there was loss of only 11% to 13% drug was noticed. Chemical analysis and X-Ray diffraction of Patra Haritala and Rasamanikya prepared from all the methods is carried as a part of standardization. In Analytical study of all the methods, 44% to 47% of Arsenic and 22 to29% of Sulphur was present in Rasamanikya. X-RD study of Haritala and Rasamanikya samples revealed that crystalline form of Haritala was changed to relatively amorphous form in Rasamanikya prepared by I, II, III and IV methods, which indicates quick and better absorption of the drug Rasamanikya on administration making it one of the economical and potent medicine. Chemically Rasamanikya can be considered as a complex compound of As2S3 and As2O5.