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Study on the Inclusion Complex of Barnidipine and Buccaladhesive Tablets

Author: GuoJieRu
Tutor: LiGao
School: Huazhong University of Science and Technology
Course: Pharmacy
Keywords: Barnidipine hydrochloride Hydroxypropyl-β- cyclodextrin Inclusion Complex Buccoadhesive Tablets In vitro release Stability
CLC: R283
Type: Master's thesis
Year: 2009
Downloads: 37
Quote: 0
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Abstract

Barnidipine hydrochloride (Barnidipine hydrochloride, BN) is a novel long-acting dihydropyridine calcium antagonists, a single optical isomer, is widely used in the treatment of hypertension. This medicine is specifically acts calcium channels in vascular smooth muscle cell membranes, inhibition of calcium into cells, and selectively enable peripheral vascular smooth muscle relaxation, with persistence, a significant antihypertensive effect. BN's strong fat-soluble, water-soluble, and the first-pass effect is very significant, very low oral bioavailability [1]. This study on the basis of the technology to improve the stability of the drug with water soluble clathrate, the development of new non-oral sustained release dosage forms - oral adhesive sheet in order to improve its bioavailability. In this experiment, hydroxypropyl-β-cyclodextrin (Hydroxypropyl-bata-Cyclodextrin, HP-β-CD) inclusion material, the use of ultrasound - prepared by freeze-drying barnidipine hydrochloride - hydroxypropyl-β-ring dextrin inclusion complexes (BN-HP-β-CD), and a composite score of drug loading and inclusion rate, the use of orthogonal design to optimize the preparation process, to determine the optimal conditions: BN: HP-β-CD The molar ratio of 1:2, ultrasonic time 40min, ultrasonic power of 90%. Simultaneously optimized clathrate. The inclusion ratio determination and phase solubility studies have shown that the inclusion complex of host and guest molecular ratio of 1:1. X-ray diffraction showed that barnidipine hydrochloride in the inclusion in the dispersion in an amorphous state, the The solubilization mechanism may be closely related to the crystal lattice plane spacing, grain size and crystallographic orientation parameter changes; differential scanning calorimetry thermal inclusion compound and the physical mixture of the energy of different changes in temperature. The new phase Fourier transform infrared scanning Spectrum confirmed that in the process of formation of the inclusion compound of cyclodextrin with barnidipine hydrochloride occurred role in the formation of an amorphous state; scanning electron microscope further intuitive verified clathrate form is different from the raw material The new form of the drug and physical mixture. Be prepared by using the optimization process of the clathrate dissolution rate was significantly improved. On this basis, the flow of materials of the adhesive force hydrochloric barnidipine vitro release and tableting as index prescription screening oral adhesive sheet, the first single factor screening, the inner and outer layer sheet were investigated adhesive, the type and amount of the lubricant. Further four factors and three levels of orthogonal experimental design to optimize the adhesive, the amount of lubricant to the final draw hydrochloric barnidipine oral adhesive tablets prescription: the inner tablet containing clathrate 32mg (equivalent of hydrochloric Pakistan Niger besylate 5mg), Carbomer 934P the 16mg (CP934P), hydroxypropyl methyl cellulose (HPMC) 4mg. Outer sheet containing CP934P24mg, HPMC24mg, magnesium stearate 1% (100mg / tablet), hardness 5 ~~ 7kg. In this paper, the in vitro release of of ultraviolet spectrophotometry adhesion piece, this Act is simple, sensitive, highly accurate and economical, convenient; test prepared three batches of samples (batch 090208,090209,090210) were measured adhesion and in vitro release, examine the stability of the preparation process. The evaluation of of hydrochloric acid barnidipine oral adhesive tablets quality, reversed-phase high performance liquid chromatographic method for the determination of the method of the hydrochloric acid barnidipine content, school proved through a series of methods using HPLC as the method for the determination of the product The advantages of high-precision, high recovery, good linearity, reproducibility, simple, rapid. Factors Influencing the Stability tests showed stable preparations under conditions of high temperature of 60 ℃, but in the light conditions hydrochloride barnidipine, decreased significantly; 75% humidity conditions, the first 10 days of Contents and Dissolution. That light and humidity affect the quality of the preparation, suggesting that this product should be protected from light kept under seal. Accelerated stability test: preparations are packaged good stability, the impact of changes in temperature and humidity hydrochloride the barnidipine content, in line with the provisions of the People's Republic of China Pharmacopoeia (2005 edition), and lay the foundation for the new hydrochloric barnidipine preparations.

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