Preparation Of Novel Vitamin A Tablets Using Hydroxyapatite Microspheres As Stabilizer

Among the currently known drugs,many drugs exposed to natural conditions such as room temperature,exposure to air,sunlight,etc,are prone to chemical changes such as degradation,hydrolysis,oxidation,heterogeneous,racemization,decarboxylation,etc,which make their chemical properties change and lose their original biological activity.Therefore,when the main drug is an unstable drug or the main drug contains volatile oil components,the period of validity of the drug is often very short,and the storage conditions are harsh,and disadvantages such as being inconvenient for convenient transportation also occur.In order to ensure that the biological activity of the drug do not lose and the physical and chemical properties do not change.It is very important to adopt a series of protective measures against drugs with poor stability.Commonly used methods include making drugs into coated tablets,microcapsules,and inclusion complexes.It is very important to adopt a series of protection measures for drugs with poor stability.Hydroxyapatite (HA,Ca₁₀?PO₄?₆?OH?₂) is the main component of inorganic minerals that make up teeth and bones.It has excellent biodegradability and biocompatibility,and it is non-toxic and harmless to the human body.At the same time,hydroxyapatite is a porous material.The drug can be adsorbed into the pores to avoid contact with external conditions,thereby effectively retaining the biological activity of the drug,stabilizing the drug properties,prolonging the period of validity of the drug,and having the effect of an absorbent at the same time as stabilizing effect,instead of the original drug excipient.At the same time,spherical materials are widely used in pharmaceutical excipients due to their excellent fluidity.It improves the overall fluidity of the soft material in the preparation,and can directly perform tableting and other operations without the need for complex methods such as granulation,saves the cost of the process,and effectively guarantees that the uniformity of the content of the tablets meets the specifications of the pharmacopoeia.Nowadays,in the area of drug stabilizers,no literature has reported on the application of hydroxyapatite microspheres.In this experiment,vitamin A,an unstable oil drug with high susceptibility to oxidation,easy degradation,and high photosensitivity and heat sensitivity,was used as a model drug.The stabilizing effects of hydroxyapatite on unstable drugs were studied,and vitamin A tablets were prepared using hydroxyapatite as a stabilizer.In this paper,hydroxyapatite was synthesized by spray drying method.It was characterized by IR,XRD,nitrogen adsorption and desorption,SEM,TG,and DTA.The physical and chemical properties of vitamin A were investigated by IR,TG,and DTA.At the same time,the experiment validated the method for determination of the content of vitamin A.Hydroxyapatite-vitamin A complex was prepared by adsorption method and its properties were investigated by IR,XRD,TG,DTA and other characterization methods.The preparation of tablets was carried out using the complex as an effective pharmaceutical ingredient.The experimental results showed that the hydroxyapatite microspheres have been successfully synthesized and the spherical materials have good fluidity.The vitamin A content determination method designed in the experiment could effectively determine the vitamin A content.Hydroxyapatite had a good stabilizing effect on unstable drugs,effectively extending the period of validity of the drug.At the same time,hydroxyapatite also had the effect of an absorbent,which could stabilize the physicochemical properties of the drug while retaining the oily drug and retain its biological activity.In the stability comparison experiment,vitamin A supplemented with hydroxyapatite was more effective than naked drug and other stabilizers in reducing the effects of temperature,humidity,light,and air on the stability of vitamin A.The proportion of vitamin A decreased significantly.When hydroxyapatite was used as a supplementary material for vitamin A tablets,there were no sticking and slivers appeared during the compression process.The tablets that were pressed out had suitable hardness,and the appearance was smooth and uniform without any color difference.The difference in tablet content was very small,which was in accordance with the pharmacopoeia.Uniformity requirements.Based on the above experimental results,it could be concluded that hydroxyapatite microspheres could be used as stabilizer additives to prepare novel vitamin A tablets.