| Lappaconite hydrobromide is an effective component lapa-aconitine hydobromide which extracted from roots of Aconitum sinomontanum in crowfoot families. It is a pure natural unaddicitive pain relievers with single molecule. Lappaconite hydrobromide has strong analgesic action and is used in the treatment of moderate and above pain with the characters of wide adaptation and good analgesic effect, which can be used as a preferred therapeutic agent in the treatment of cancer pain. There exists lappaconite hydrobromide tablet and injection formulation registered and applied to clinical. It has been listed an mild painkiller on guiding principles of cancer patients three steps analgesic therapies, therefore, it is a good choice to research and develop dispersible tablets for improving drug curative effect in clinic.Lappaconite hydrobromide dispersible tablet formulation and production process: this product is a dispersible tablet. To design prescriptions, we consider rapidly disintegrating into small particles in water of pills, forming a uniform mixed suspension and uniform dispersion, and dissolution in accordance with the tablets requirements. Besides these, it should be accessible to get materials and easy to granulate and pellet, particles have good liquidity, and weight of each tablets have small difference. Taking hydrobromide into fine power, mixing with microcrystalline cellulose 301 and crosslinking povidone respectively through 120 mesh sieve twice, and then blending main medicine with microcrystalline cellulose andl/2 weight of 301 crosslinking povidone prescription through 80 mesh sieve twice, adding 70% ethanol fully blending to make soft materials through 20 mesh sieve,60℃ drying,20 mesh granulation, adding another 1/2 weight of crosslinking povidone and micro silica power blending, finally pressing into piece and getting the targets. Through the dissolve degree examination and influence factor investigation tests (illumination tests, high temperature tests, and high humidity tests) of the prescription, we optimized the product, obtained the simple and mature production process of lappaconite hydrobromide with good stability.Lappaconite hydrobromide dispersible tablet quality controls:according to the reference of Lappaconite hydrobromide dispersible tablet’ drug standard recorded on 5th volume of second part of ministry pharmaceutical standards and relevant provisions of dispersible tablets on the appendix of Chinese pharmacopoeia2010 version 2. We have done some quality controls to this product such asphysical and chemical characteristics, content identification test, relevant material, dissolving degrees, brittle broken degree, dispersion homogeneity, high performance liquid chromatograph (HPLC) method for the content determination and microbial limit inspection. Methods are quick, easy and comply with relevant standards.Lappaconite hydrobromide dispersible tablet stability study:according to chemical drug stability research technique guiding principles and the relevant requirements of the appendix in two parts of the 2010 edition Chinese Pharmacopeia. We did some stability research to this product. The results showed that removing the outer packing, this product’s complete index test results had not significantly changed in the conditions of strong light, high temperature and high humidity. The product stimulated listed packaging sample, placed by 40℃±2℃, RH 75%±5% for 6 months and 25℃±2℃, RH 60%±10% long-term tests for 9 months. The index of examination results had no change, neither. The product has basic stable physical and chemical properties. According to the stability study results and the national drug standards of lappaconite hydrobromide dispersible tablet, recommend that this product should be shading and sealing preservation. |
