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Freeze-dried sublingual tablet containing hydrophobic active substances and preparation method thereof

A technology of active substances and sublingual tablets, which is applied in the field of freeze-dried sublingual tablets and its preparation, can solve the problems of difficulty in administration and absorption, and achieve uniform drug carrying, long residence time, effective and rapid carrying and replenishment Effect

Inactive Publication Date: 2016-06-15
曾岚
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a freeze-dried sublingual tablet containing hydrophobic active substances and its preparation method, aiming to provide a new type of preparation that can effectively and quickly carry and replenish hydrophobic drugs, thereby solving the problem of the presence of hydrophobic drugs. Difficulty in administration and difficulty in absorption

Method used

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  • Freeze-dried sublingual tablet containing hydrophobic active substances and preparation method thereof
  • Freeze-dried sublingual tablet containing hydrophobic active substances and preparation method thereof
  • Freeze-dried sublingual tablet containing hydrophobic active substances and preparation method thereof

Examples

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Effect test

Embodiment 1

[0028] Embodiment 1 A kind of freeze-dried sublingual tablet containing hydrophobic active substance and preparation method thereof

[0029] A freeze-dried sublingual tablet containing a hydrophobic active substance is composed of the active substance and excipients, wherein the components of the excipients are shown in Table 1 below; the active substance is sildenafil citrate.

[0030] The component of auxiliary material in table 1 embodiment 1

[0031]

[0032]

[0033] Process for the preparation of freeze-dried sublingual tablets containing hydrophobic active substances:

[0034] Accurately weigh 0.1 gram of chitosan and 25.0 gram of pullulan into 70 milliliters of water, stir evenly; then add 25 grams of lactose, 14.5 grams of mannitol, 0.5 grams of microcrystalline cellulose, 15 grams of alanine, 15 grams of Polyethylene glycol 6000 and 4.9 grams of γ-cyclodextrin, stir and mix evenly, then add 0.5 grams of citric acid to adjust the pH to 7.0; then add 25 grams of...

Embodiment 2

[0036] Example 2 A freeze-dried sublingual tablet containing a hydrophobic active substance and its preparation method

[0037] A freeze-dried sublingual tablet containing a hydrophobic active substance is composed of the active substance and auxiliary materials, wherein the components of the auxiliary materials are shown in Table 2 below; the active substance is tadalafil.

[0038] The component of auxiliary material in table 2 embodiment 2

[0039]

[0040] Process for the preparation of freeze-dried sublingual tablets containing hydrophobic active substances:

[0041] Accurately weigh 15 grams of methylcellulose and 0.05 grams of amylose and add them to 70 milliliters of water, and stir evenly. Then add 45 grams of lactose, 34.5 grams of mannitol, 0.5 grams of microcrystalline cellulose, 3 grams of phenylalanine, 1.85 grams of polyethylene glycol 2000 and 0.1 grams of γ-cyclodextrin, stir and mix well, and then add 0.5 gram of dipotassium hydrogen phosphate to adjust t...

Embodiment 3

[0043] Example 3 A freeze-dried sublingual tablet containing hydrophobic active substances and its preparation method

[0044] A freeze-dried sublingual tablet containing a hydrophobic active substance is composed of an active substance and an auxiliary material, wherein the components of the auxiliary material are shown in Table 3 below; the active substance is a drug that can be used for acute treatment of angina pectoris and myocardial infarction—nifedipine .

[0045] The composition of auxiliary material in the embodiment 3 of table 3

[0046]

[0047] Process for the preparation of freeze-dried sublingual tablets containing hydrophobic active substances:

[0048] Accurately weigh 15 grams of sodium hydroxymethylcellulose and 25 grams of pullulan into 70 milliliters of water, and stir evenly. Then add 10 grams of lactose, 9.9 grams of mannitol, 0.1 grams of microcrystalline cellulose, 15 grams of alanine, 15 grams of polyethylene glycol 6000 and 10 grams of α-cyclodex...

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Abstract

The invention provides a freeze-dried sublingual tablet containing hydrophobic active substances, which is prepared from active substances and auxiliary materials and is characterized in that the auxiliary materials include medicine carriers and assistants, wherein the medicine carriers are natural polysaccharide high molecular materials which exist in water in nano sizes and have hydrophobic regions, and the active substances are hydrophobic active substances. The freeze-dried sublingual tablet containing hydrophobic active substances, provided by the invention, can effectively and quickly carry and supplement hydrophobic medicines, and the medicines can be carried uniformly, thereby being favorable for playing roles of the medicines; and meanwhile, the hydrophobic medicines are prepared into the freeze-dried sublingual tablets, and then the medicines can quickly pass through the sublingual region to enter the blood for circulation, thereby playing roles.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to a freeze-dried sublingual tablet containing hydrophobic active substances and a preparation method thereof. Background technique [0002] In pharmaceuticals, oral preparations account for a high proportion, among which solid preparations are the most important form of oral preparations. However, the solid preparations currently on the market are mainly aimed at hydrophilic drug molecules, and cannot treat some hydrophobic drugs, vitamins, trace amounts, etc. elements, such as vitamin D3, vitamin B3 and other hydrophobic vitamins; on the other hand, taking these hydrophobic vitamins, drugs or trace elements directly will cause some adverse reactions, such as vitamin B3 and iron supplements will make people The stomach produces severe adverse reactions, therefore, these drugs either cannot be directly made into oral preparations, or the prepared oral preparations have strong side effects. Ho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/19A61K47/36A61K47/38A61K45/00A61K31/519A61K31/4985A61K31/4422A61K31/593A61P9/10A61P37/08
CPCA61K9/205A61K9/006A61K9/19A61K9/2054A61K9/2059A61K31/4422A61K31/4985A61K31/519A61K31/593A61K45/00
Inventor 曾岚
Owner 曾岚
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