| The paper discussed the thinking and the pathway of the manufacture of sustained-release form based on HT as model drug by using the principles of pharmaceutics. The thesis adopted HPMC as the basic matrix material, PVP (8% alcohol solution) as compression aids, magnesium stearate as lubricant. The HT sustained-release tablet was prepared which could release twelve hours continuously in vitro. The basic prescription and preparation technology was initially defined by the study about formulation screening and technology optimizing ,based on the pharmacy rule as indicator and the stability maintaining of HT. Dissolution rate is an important factor of influencing internal quality of tablet. The determination method was initially set up for the dissolution rate of the HT sustained-release tablet. And the various factors were studied, which influence the HT release of HT sustained-release tablet. Orthogonal project was employed to screen the prescriptions which based on the study of mono-factor experiment Verification experiments about the dissolution rate of optimized prescription were done . The results showed that the dissolution rate of HT among the HT sustained-release tablets at 2h,6h,10h was 15~35%,40~60%,>75% respectively. The f2 similar factor analysis explained that the recur capability of HT sustained-release tablets releasing was good and the craft was stable.The quality study of the HT sustained-release tablet was done. The maincomponents included that the identification methods were set up, and the palmetine sustained-release tablet examining method of the correlated material was founded. The studying results according to items of the quality evaluating showed that evaluating method was reasonable and Ihe quality of the HT sustained-release tablet was under the control. The study on the releasing mechanism of HT sustained-release tablet was performed. Higuchi model was selected as the description of the HT sustained-release tablet's releasing mechanism, and the n, the releasing parameter, equaling to 0.72(0.45 *, is 212.0± 62.9nghml"1 and 215.8 ± 62.0 nghml'respectively; W is 2.9± 0.4 h and 0.71± 0.19 h respectively; Cn^ is 81.6 ±40.1 ng-ml'1 and 143.48± 93.2 ngml'respectively. After administering multiple dosage to dogs, AUQ>*risl519.6±761.4nghml'1 and 1523.1 ±737.4nghml1 respectively; T?is4.4±0.2h and 1.7 ± 0.3h respectively; Q? is 320.5 ± 175.6 ngml"1 and 317.3 ± lOSJngml"1 respectively, Cav is 21.3544 ± 10.3448ng/ml and 20.9046± 10.4683ng/ml respectively, DF is 152.7508%±129.5072% and 261.7121%t299.8839% respectively, C*? is 42.53 ± 16.5ng/ml and 8.42 ± 3.16ng/ml respectively, relative bioavailability of singleand multiple dosage regimens is 108.0%±9.1% and 103.2%±3.(^respectively. The evaluation result of bioequivalence showed that AUC is bioequivalent but C^ax and W are beyond the confine. The Cn?x and the DF are smaller by contrast with the ordinary tablet, but the T^x is prolonged. The palmetine sustained-release tablet has the characteristic of sustained-release and the result comes to the purpose of the paper design.In vivo-in vitro correlation evaluation of the palmetine sustained-release tablet was studied by Wanger-Nelson method .The result proved that in vivo-in vitro correlation is significant. The release determination method is scientific and reasonable, which could guarantee the internal quality under the control.It have few reports about palmetine sustained-release form inside and outside China. Little data can be used for reference. So it is a pilot study. The results studied will be a good foundation of comprehensive development for diverse forms.
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