| Skullcap(Scutellaria baicalensis Georgi) is a perennial herb belongs to Lamiaceae Scutellaria,is one of the most commonly used traditional medicine of traditional Chinese medicine.Modern scientific research has elucidated that the basic material which play efficacy are flavonoids.Consisting essentially of baicalin(Baicalin, Chinese Pharmacopoeia 2010 edition provides the content of not less than 9.0%), scutellarein(Baicalein), Wogonin(Wogonin), etc.Baicalin is extracted and isolated from the skullcap root,it has much significant pharmacological activity such as antibacterial, diuretic, anti-inflammatory, antiallergic, antispasmodic and anti-cancer and other. Another,baicalin also has the effect of absorbing ultraviolet light, scavenging oxygen free radicals and inhibiting melanin.It can be used in medicine and can also be used in cosmetics, it is a good functional cosmetics raw materials.It has been used in the treatment of such as infectious hepatitis, biliary tract infections and acute lead poisoning in clinical.Baicalin insoluble in ethanol, methanol, acetone, almost insoluble in water,currently its oral bioavailability is not ideal.Baicalin has some absorption in the stomach and upper small intestin,almost no absorption in other bowel.Gastroretentive type controlled release formulations is a new formulation can extend the residence time of the drug in the stomach, increasing the degree of absorption of the drug in the stomach or duodenum, and improve the clinical efficacy,becoming a hot topic in recent years,To make baicalin gastric floating sustained-release formulations, and to study the performance of the floating and release characteristics of the formulation.To study the physical and chemical properties of baicalin and to make baicalin gastroretentive sustained-release preparations,complete the in vitro evaluation of the quality of the resulting formulations and fitting the model to its release characteristics in vitro.Methods:(1) Research the physicochemical properties of baicalin, including such as stability and solubility in different media.(2) To establish an HPLC method for the determination of baicalin and in vitro quality evaluation methods of the preparations.(3) The drug loading, encapsulation efficiency, drug release behavior as the marker,to use single-factor test to examine the preparation process and prescription.The drug loading, encapsulation efficiency, drug release behavior as the marker,the prescription sodium alginate(SA), hydroxypropyl methylcellulose(HPMC), ethyl cellulose(EC), the drug, as the study factors,to design of four factors and three levels orthogonal test, preferably the best prescription.(4) According to the optimized process and formulation,to make three batches of preparation,the drug loading, encapsulation efficiency, drug release behavior as the marker,verification the reproducibility of process and prescription preparations and to fit the preparations in vitro release model.Results:(1) In distilled water, simulated gastric fluid(SGF), pH 2.5 and pH 2.0 phosphate buffered saline(PBS) four kinds of media,baicalin has good stability, low solubility.(2) HPLC method test results show that the determination of baicalin could Meet the requirements of in vitro analysis;Established a scientific and reliable in vitro preparation quality evaluation methods.(3) After screening of prescription preparation process,the optimum formulation is sodium alginate(SA) 70 mg, hydroxypropylmethyl cellulose(HPMC) 20 mg, ethyl cellulose(EC) 20 mg, drug 70 mg, calcium chloride at a concentration of 30 mg / mL crosslinking time 20 min. Objective:(4) The optimal screening and prescription with good reproducibility, in vitro release characteristics to meet the zero-order kinetics equation.Conclusions:The results of Physical and Chemical Properties showed that Baical in adapted into gastric floating formulation.Preparation obtained in this s tudy,process is relatively simple, and easy to get material with good per formance of sustained release characteristics and floating. |
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