Examples	pH value
		Example 1	3.98
Example 2	3.75
		Example 3	3.52
Example 4	3.50
		Example 5	3.30
Comparative example 1	5.95
		Comparative example 2	3.06
Bupropion hydrochloride bulk drug (WR15072702)	5.09
		Reference preparation (13E010P) (core tablet after stripping coating film)	5.36

The reference preparation is bupropion hydrochloride sustained-release tablets (bupropion hydrochloride extended-releasetables), and the manufacturer comprises: valeant Pharmaceuticals North America LLC.

Experimental example 2: stability survey after packaging of coated tablets

After the product was packaged, i.e., coated HDPE bottles (silica gel desiccant), which were placed at 50 ℃ RH 75% for 30 days, the contents of major impurities were measured, and the results are shown in Table 2. The impurities include: Imp-C (1- (3-Chlorophenyl) -2-hydroxypyprop-1-one), 3-cl (3-chlorobenzoic acid), and Imp-F (1- (3-Chlorophenyl) -1-hydroxypyprop-1-one).

Table 2: impurity content detection result (50 ℃ RH 75%/30 days)

From the above results, it is understood that the impurities 3-CL and Imp-F in comparative example 1 increase remarkably after leaving for 30 days, and the impurity content in each of examples and comparative example 2 is below the limit. And the content of related substances is gradually reduced along with the increase of the citric acid proportion in the tablet core.

Experimental example 3: coated tablet dissolution examination

The tablets provided in each example and comparative example were taken separately, and the dissolution effect in water was examined. The results are shown in Table 3.

Table 3: dissolution in Water data (%)

Time(h)	0	1	2	3	4	6	8	12	16
										Comparative example 1	0.0	0.0	0.0	0.1	0.5	9.0	17.4	34.2	47.8
Example 1	0.0	0.1	0.1	0.1	0.4	8.9	18.0	33.9	47.3
										Example 2	0.0	0.0	0.0	0.2	0.7	9.1	18.9	34.3	45.8
Example 3	0.0	0.1	0.6	1.4	3.9	22.3	44.5	77.6	92.8
										Example 4	0.0	0.0	0.4	1.5	6.8	20.4	46.8	76.4	87.3
Example 5	0.0	0.2	0.4	1.8	8.7	30.4	53.9	79.8	90.4
										Comparative example 2	0.0	0.2	0.4	1.8	10.1	36.4	60.7	83.6	93.5
Reference formulation 18H040P	0.0	0.2	2.4	6.2	9.7	16.4	23.2	36.9	50.6

The above results show that citric acid in the core affects the release rate of the coated tablet in an aqueous medium. The release rate in water becomes faster with increasing citric acid dosage, but the release similarity with the reference formulation gradually decreases.

Experimental example 5: human postprandial pre-BE experiment

After eating, the pH value of the stomach and the upper section of the small intestine rises, and the eating is influenced more greatly by the release in the water medium. Thus, human postprandial pre-BE experiments were performed for example 5 and comparative example 2, each using a two-cycle, double-crossover dosing regimen. The test population was 8 healthy male subjects. The results are shown in tables 4 and 5.

Table 4: human body postprandial pre-BE experimental result

Remarking: t represents a self-developing agent, R represents a reference agent

Table 5: human body postprandial pre-BE experimental result

Remarking: t represents a self-developing agent, R represents a reference agent

From the above results, the in vivo pre-BE results obtained in example 5 showed a Cmax T/R value of 109.0% showing a tendency toward higher speed, but the 90% confidence interval was still in the range of 80-125%. The in vivo pre-BE results for comparative example 2 show a Cmax T/R value of 118.8% with a 90% confidence interval exceeding the acceptance criterion of 80-125%.

Although the invention has been described in detail hereinabove by way of general description, specific embodiments and experiments, it will be apparent to those skilled in the art that many modifications and improvements can be made thereto based on the invention. Accordingly, such modifications and improvements are intended to be within the scope of the invention as claimed.

Claims

1. A preparation composition containing bupropion, which is characterized by comprising a tablet core and an outer coating; the tablet core contains bupropion hydrochloride, polyvinyl alcohol, citric acid and glyceryl behenate, wherein the mass ratio of the bupropion hydrochloride to the citric acid is 300: 0.5-6.

2. The preparation composition of claim 1, wherein the mass ratio of bupropion hydrochloride to the citric acid is 300: (0.5-1.5).

3. The preparation composition of claim 1, wherein the mass ratio of bupropion hydrochloride to the citric acid is 300: (0.8-1.2).

4. The preparation composition according to any one of claims 1 to 3, wherein the tablet core contains 92 to 94% by mass of bupropion hydrochloride and 0.15 to 1.8% by mass of citric acid.

5. The preparation composition according to claim 4, wherein the tablet core contains 93.4-93.8% of bupropion hydrochloride and 0.15-0.35% of citric acid in percentage by mass.

6. The preparation composition according to claim 4, wherein the tablet core contains 93.6% of bupropion hydrochloride and 0.28-0.32% of citric acid in percentage by mass.

7. The preparation composition as claimed in any one of claims 1 to 6, wherein the core tablet comprises, by mass, 3.0 to 3.4% of polyvinyl alcohol and 2.8 to 3.2% of glyceryl behenate.

8. The preparation composition according to claim 1, wherein the mass percentages of the components are as follows, based on 100% by mass of the single tablet core: 93.5 percent of bupropion hydrochloride, 3.2 percent of polyvinyl alcohol, 0.3 percent of citric acid and 3.0 percent of glyceryl behenate.

9. The formulation composition according to claim 1, wherein the mass of the single core is 321mg, wherein: 300mg of bupropion hydrochloride, 10.4mg of polyvinyl alcohol, 1.0mg of citric acid and 9.6mg of glyceryl behenate.

10. A process for the preparation of a formulation as claimed in any one of claims 1 to 9, which comprises preparing a core and coating the core;

the preparation of the tablet core comprises the following steps:

(3) drying until the water content meets the requirement, and stopping heating;

(4) mixing the granules dried in the step (3) with glyceryl behenate;

(5) and (6) tabletting.