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Pharmaceutical composition containing orlistat and plant-derived lipase inhibitor

A technology of lipase inhibitor and orlistat, which is applied in the field of medicine, can solve the problems of no lipase inhibitor and lipase, and achieve the effect of alleviating oil spots and reducing gastrointestinal side effects

Active Publication Date: 2018-09-18
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Nakai M et al. (Journal of Agricultural and Food Chemistry, 2005, 53(11): 4593-4598) measured the lipase inhibitory activity of 54 polyphenolic compounds extracted from tea leaves, and found that related compounds inhibit fat IC of enzyme 50 Between 0.048~>20μM, overall lower than other plant-derived lipase inhibitors described by Li Qiang et al. in their review (Natural Product Research and Development. 2015, 27:360~366), however There is no teaching on the specific binding sites of lipase inhibitors extracted from tea leaves and lipase, and there is no teaching on whether the combination of orlistat and lipase inhibitors extracted from tea leaves will produce a synergistic effect

Method used

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  • Pharmaceutical composition containing orlistat and plant-derived lipase inhibitor
  • Pharmaceutical composition containing orlistat and plant-derived lipase inhibitor
  • Pharmaceutical composition containing orlistat and plant-derived lipase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1 capsule preparation

[0064] Example 1 Preparation of capsules containing orlistat and compound 1

[0065] Prescription: (according to 1000 capsules)

[0066]

[0067]

[0068] Preparation Process:

[0069] Separately pass sodium lauryl sulfate, crospovidone, sodium starch glycolate, microcrystalline cellulose, orlistat, and compound 1 powder through an 80-mesh sieve, and set aside. Weigh the prescription amount of sodium lauryl sulfate, crospovidone, sodium starch glycolate, microcrystalline cellulose, orlistat, compound 1 powder, first mix sodium lauryl sulfate, crospovidone The ketone and carboxymethyl starch sodium were mixed evenly, then added microcrystalline cellulose, orlistat, and compound 1, mixed evenly, and passed through an 80-mesh sieve twice. Slowly add 50% ethanol solution containing 10% povidone K30 to the mixed powder to make a soft material, extrude and sieve through a 20-mesh granule, dry the wet granule in a blast drying oven a...

Embodiment 2

[0070] Embodiment 2 tablet preparation

[0071] Embodiment 1 Preparation of tablets containing orlistat and compound 2

[0072] prescription:

[0073]

[0074] Preparation Process:

[0075] Weigh orlistat and compound 2 according to the prescription amount, use microcrystalline cellulose as filler, croscarmellose sodium and polyvinylpyrrolidone as disintegrant, 5% PVP 60% ethanol solution as binder, Micropowder silica gel is used as a flow aid, and it is granulated in one step in a fluidized bed, and then compressed into tablets.

Embodiment 3

[0076] Embodiment 3 granule preparation

[0077] Embodiment 3 Preparation of granules containing orlistat and compound 3

[0078] prescription:

[0079]

[0080]

[0081] Preparation Process:

[0082] Weigh the prescribed amount of orlistat, compound 3, starch, dextrin, and sucrose powder and mix evenly. Add appropriate amount of 80% ethanol to the mixed powder, mix evenly, make soft material, pass through 18-mesh nylon sieve to make wet granules, dry at about 60°C, granulate with 20-mesh sieve, pack separately, and get ready.

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PUM

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Abstract

The invention relates to the technical field of medicine, and in particular, relates to a pharmaceutical composition containing orlistat and a plant-derived lipase inhibitor. The plant-derived lipaseinhibitor is a polyphenol lipase inhibitor extracted from tea leaves. The results of in-vitro experiments show that the interaction index of orlistat and the polyphenol lipase inhibitor in inhibitionof the activity of lipase in the molar ratio range of 1:10 to 10:1 is lower than 1, and suggest that orlistat and the polyphenol lipase inhibitor generate synergistic lipase inhibition effect. The results of animal experiments show that the control effect of the composition containing orlistat and the polyphenol lipase inhibitor on the weight of nutritional obesity rats is better than that of an orlistat group and a polyphenol lipase inhibitor single drug-administration group, and generation of the synergistic effect is further verified. In addition, the polyphenol lipase inhibitor can reducethe unpleasant gastrointestinal side effects of orlistat and alleviate adverse reactions of oil spots, fat / oil stools and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition containing orlistat and a plant-derived lipase inhibitor. Background technique [0002] Orlistat (orlistat) is a lipase inhibitor weight loss drug developed by Roche Pharmaceuticals. The trade name is Xenical. It was first launched in Europe and the United States in the late 1990s. Approved by the Food and Drug Administration to switch to an over-the-counter drug. Its chemical name is N-formyl-L-leucine (s)-1[(2s,3s)3-hexyl-4oxy-2-epoxypropylmethyl]dodecyl ester, also known as tetrahydro Tetrahydrolipstatin (Tetrahydrolipstatin, THL), is a semi-synthetic lipstatin derivative, its chemical structure is shown in the following formula: [0003] [0004] Orlistat forms a covalent bond with the serine residue of gastropancreatic lipase, thereby inactivating the enzyme and unable to hydrolyze triglycerides in food into absorbable fatty acids, thereby ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61K31/353A61P3/04
CPCA61K31/353A61K31/365A61P3/04A61K2300/00
Inventor 向飞杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD
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