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Drug solubility in many formulations developed in the primary concern, but also the agents can effectively absorb one of the keys. Many drugs are organic compounds, are often difficult to dissolve in water, and some even the saturated solution is difficult to achieve effective therapeutic concentrations, so who have been eliminated. In drug screening, many in vitro pharmacological activity of the drug is highly insoluble, and how to increase the solubility of poorly soluble drugs is a focus of pharmaceutical research. In addition, the stability of pharmaceutical preparations to ensure safe and effective preparation is very important. Therefore, seeking safe, effective in improving the solubility of poorly soluble drugs and to improve the stability of the drug is very meaningful pharmaceutical research topic. Inclusion technique commonly used in the medicine to increase the drug solubility, improved stability of the formulation. Cyclodextrin (CD) of the annular hollow cylinder with a special structure, under certain conditions, with the guest molecule (such as drugs) to form inclusion complexes. CD is the most widely used β-CD, but the poor solubility of β-CD in the application process found a greater renal toxicity and hemolysis, so as to limit its application. The β-CD derivative to overcome the lack of β-CD. Melatonin (MLT) is an indole compound, insoluble in water, light sensitivity, low bioavailability. In this paper, β-CD, HP-β-CD, M-β-CD, SBE1-β-CD, SBE4-β-CD, SBE7-β-CD inclusion complexes of the MLT of their inclusion Preparation of tablets and parity. Experimental contents and results as follows: ① This concentration method using a continuous graded aggregate process for the packet MLT and β-CD, HP-β-CD, M-β-CD, SBE1-β-CD, SBE4-β-CD , SBE7-β-CD inclusion molar ratio, the molar ratio of inclusion 1:1,3:2,3:2,3:2,3:2,2:1 respectively. The inclusion method, using convenient, efficient ultrasonic method and by lyophilization processing package together solutions were prepared MLT-β-CD, MLT-HP-β-CD, MLT-M-β-CD, MLT- SBE1-β-CD, MLT-SBE4-β-CD, MLT-SBE7-β-CD inclusion complex six kinds. By microscopy, infrared spectroscopy, as well as physical and chemical characteristics of morphology proved MLT with six kinds of CD derivatives were formed inclusion. ② conditions by controlling the consistency of the preparation process to yield, drug content, encapsulation efficiency and dissolution four indicators for the evaluation of six kinds of CD derivatives MLT inclusion performance. Among them, the encapsulation efficiency and dissolution as the main evaluation index. Six kinds of CD derivatives on the encapsulation efficiency MLT size: SBE7-β-CD (94.481%) gt; SBE4-β-CD (93.531%) gt; SBE1-β-CD (92.994%) gt; M-β -CD (83.936%) gt; HP-β-CD (81.830%) gt; β-CD (75.756%). Six kinds inclusion dissolution order: SBE7-β-CD (96%) gt; SBE4-β-CD (93%) gt; SBE1-β-CD (91%) gt; M-β-CD (89 %) gt; HP-β-CD (85%) gt; β-CD (81%), MLT dissolution of the drug substance was 71%. Accordingly, MLT inclusion by six kinds of CD derivatives, its solubility been well improved. ③ determined by phase solubility of different concentrations of β-CD, HP-β-CD, M-β-CD, SBE1-β-CD, SBE4-β-CD, SBE7-β-CD solution at 25 ℃, 37 ℃, 45 ℃ constant temperature solubilization effect of MLT and inclusion equilibrium constant (K). Experimental results show that from solubilization effect, under the same conditions the six CD derivatives of the solubilization effect of the MLT: SBE7-β-CD gt; SBE4-β-CD gt; SBE1-β-CD gt; M-β-CD gt; HP-β-CD gt; β-CD, and the solubilization of each CD derivatives with the increase of concentration; addition, solubilization effect increases with the temperature. From the point of view of the inclusion of K results, K value greater easier for inclusion, more stable clathrate. At each temperature, SBE class inclusion K value is greater than β-CD, HP-β-CD, M-β-CD, which SBE7-β-CD inclusion complex K-value is max. ④ to MLT-SBE7-β-CD inclusion complex example, using uniform design optimized tablet formulations. In MLT tablets as control the quality of the two tablets were evaluated. The results showed that: both the visual inspection, the weight difference inspection, checking hardness and friability, disintegration inspection, content uniformity checks no significant differences are in line with requirements of the pharmacopoeia. But in dissolution inspections, MLT-SBE7-β-CD tablets significantly better than the MLT on the photo.
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