Study On Physicochemical Properties Of Calamine Before And After Processing,and Peparation Of Calcined Calamine Dispersible Tablets

Calamine has a long history of medicine, first recorded in the Foreign Dan Herbal, named differ very stone, sweet stone, floating sweet stone.Calamine from Smith sonitum in calcite of the carbonate minerals, or Hydrozincite [Zn5(CO3)2(OH)6] in a single monoclinic system of hydrous carbonate minerals. Property and flavor is sweet, flat. Meridian distribution to stomach. It has the effect of detoxication, improving eyesight, eliminating dampness, alleviate itching and anti-itch sore. At present, Calamine is processed to very fine powder to prepare Calamine lotion or Calamine gel in clinic. Due to Calamine extremely insoluble, easy to precipitate, unpleasant feeling, uneven distribution, so it affects clinical efficacy.Dispersible tablets as a new dosage form developed in recent years for insoluble drugs, easy to disintegrate in water to form a homogeneous suspension solution. In order to provide experimental basis for the convenient use of Calamine, this paper puts Calamine as the object of study to study physicochemical properties of Calamine before and after processing, and peparation of calcined Calamine dispersible tablets.This study provided a new application form for clinical application of Calamine. The contents and results were as follows.1. The resources survey and samples identification of CalamineCalamine is mainly produced in Sixiang from Miaoshan Autonomous County, Chang Anlu from Rongan County and Ge Jiatang from Guilin in Guangxi. Distributing in Guilin, Shanxi, Guizhou and other places. This study collected13batches of samples from Yulin(Guangxi), Rongan(Guangxi), Sichuan, Guizhou, Anhui and Shanxi. Use X-ray diffraction(XRD) and titration to identify. The XRD method showed only one batch of samples was genuine. It was monoclinic system of [Zn5(CO3)2(OH)6] and orthorhombic system of Zn4Si2(OH)2. The others were CaCO3. The method of titration showed only one batch of ZnO content was qualified. Results were consistent. But XRD method was simple and fast. Therefore, XRD method could be as a fast inspection method to test mineral drugs.These results suggest that commercial goods of Calamine for sale are complex and more are adulterants. Some batches of samples from some (GMP) certified productions are also problems. It is imperative to establish strict quality management and standards to ensure the safety of clicical drugs.2. Study on the processing technology of CalamineThe processing methods of Calamine have Ming Duan, water flying, and San Huangtang quenching. The clinical uses fine powder after calcining. But existing processing technology of Calamine varies, to be lack of processing technology parameters and uniform standards. In this study, the processing technology of Calamine was optimized by central composite design-response surface method using the content of ZnO as index. The dynamic observation of its shape and particle size was conducted to optimize the water grind processing of Calamine for the first time. The optimal processing technology was as follows:taking24mesh Calamine, calcining4h at400℃, adding5-fold water to grind drug into paste, then adding40-fold water to stir, resting for above8min to pour out the suspension. The number of water grind processing was six times, then the suspension was placed for21h before drying at120℃.This study provided experimental basis for the processing mechanism of Calamine.3. Study on chemical composition and main phase of Calamine before and after processingThe processing of Calamine was not only the crushing process, but also the process of transformation from ZnCO3/[Zn5(CO3)2(OH)6] to the active ingredient of ZnO. The study of chemical composition about Calamine before and after processing showed:main phase of Calamine after processing changed from monoclinic system of [Zn5(CO3)2(OH)6] to hexagonal system of ZnO, and orthorhombic system of Zn4Si2(OH)2din not change. This study provided experimental basis for the processing mechanism of Calamine.4. Raw materials selection of calcined Calamine dispersible tabletsIn order to make Calamine quickly and uniformly dispersed, and reach the purpose of save time, effort, preventing dust emission, this study prepared calcined Calamine dispersible tablets.4.1Comparative study on physicochemical properties of Calamine different particle sizesThe particle size distribution of the Calcined Calamine Powder with different sizes was measured by laser analyzer.The structure was characterised by the surface and pore size analyzer and the scanning electron microscope.The element was analysed by IR. Results:physical and chemical properties of different particle sizes were no significant differences.With the particle size decreasing, the Calamine gradually uniform and size distribution range gradually narrow. The true density, porosity and pore diameter decreased with particle size decreasinig. But titration results showed the content of ZnO made by calcining and water flying was relatively high. Pharmacological effects of Calamine related to the content of ZnO and its size, so using vibration milling to piece200mesh made by calcining and water flying to1000mesh or finer. It not only made the content of ZnO higher, but also increased pharmacological effects and reduced skin irritation.4.2Comparative on in vitro transdermal permeability of Calamine with different sizesTo compare transdermal permeability properties in vitro of Calamine lotion with defferent mesh sizes. Transdermal permeability in vitro of Calamine lotion with defferent mesh sizes was in accordance with zero-order release kinetics. Compared with other size, transdermal permeability in vitro of Calamine lotion with1000mesh was relatively good. Therefore, decreasing particle size could promote transdermal absorption of drugs.4.3Study on the antimicrobial activity of Calamine with different sizesOn the basis of comparative studies about the physicochemical properties and transdermal penetration in vitro of different particle size of calcined Calamine, studying the antimicrobial activity of Calamine with different sizes by measuring the size of inhibition zone. The results showed:antibacterial activity of calcined Calamine was stronger; different sizes of Calamine had antibacterial activity. The smaller size, the stronger was the antibacterial activity.1000mesh size of Calamine had relatively better inhibitory effect.The above results showed that1000mesh calcined Calamine could be as raw material of calcined Calamine dispersible tablets.5.Study on antibacterial activity of Calamine for saleOn the basis of chemical composition, studying antibacterial activity of Calamine for sale. Results showed the adulterants whose main components were CaCO3were no antibacterial activity. The adulterants could not be as a substitute for Calamine. Therefore, it’s need to establish quality standards to ensure safe, effective and rational use of drugs.6. Study on peparation of calcined Calamine dispersible tabletsPut dispersed homogeneity and disintegration time as indicators, use the single factor to inspect powder raw materials of calcined Calamine with different particle size, the type and usage amout of disintegrating agent and binder. The best prescription ratio of dispersible tablets:1000mesh calcined Calamine:crosslinked methyl cellulose, sodium:3%of sodium carboxymethyl cellulose solution=100:5:34. As Calamine dispersible tablets are mainly used for the preparation of Calamine lotion. It solves the lotion is easy to suspension, precipitation and uneven distribution. Simultaneously, it solves the discomfort in the process of using. So, size and weight of dispersible tablets should be determined on the base of the clinical use. Because this study is still in progress, the details on weight of dispersible tablets and quality standards continue to improve.