Self-microemulsion composition of insoluble medicine

Abstract

The invention discloses a self-microemulsion composition of an insoluble medicine and without an oil phase. The composition comprises active medicines, a solvent and a surfactant, and can be adsorbed by a solid adsorbent to further obtain a solid self-microemulsion composition. The high in-vitro dissolution rate and the high in-vivo biological utilization degree of the self-microemulsion composition disclosed in the invention are maintained.

Description

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a self-microemulsion composition of poorly soluble drugs. Background technique

[0002] Based on the classification system of biopharmaceuticals, APIs can be divided into four categories according to their differences in solubility and permeability. Drugs with low solubility and high permeability belong to class II of the biopharmaceutical classification, and the rate-limiting step of absorption is the low dissolution rate of the drug. Dosage form plays a decisive role in the absorption of this type of drug in the gastrointestinal tract. Traditional tablets are difficult to improve the bioavailability of this type of drug. Appropriate dosage form is the key to the successful development of this type of drug product. (Lv Yifan et al., Research on the Administration Strategy of Insoluble Drugs, World Clinical Drugs, 2009, 30(1): 41-45)

[0003] Microemulsion (Micro Emul...

Examples

Embodiment 1

[0027] Embodiment 1 The prescription and preparation method of tacrolimus self-microemulsion composition

[0028] Element

[0029] The drug is dissolved in propylene carbonate, then propylene glycol is added, and finally Cremophor RH 40 is added, and magnetic or mechanical stirring is performed to obtain a tacrolimus self-microemulsion composition.

Embodiment 2

[0030] Embodiment 2 The prescription and preparation method of tacrolimus self-microemulsion composition

[0031] Element

[0032] The drug is dissolved in diethylene glycol monoethyl ether, citric acid is added, and finally Labrasol is added, and magnetic or mechanical stirring is performed to obtain the tacrolimus self-microemulsion composition.

Embodiment 3

[0033] The prescription and preparation method of embodiment 3 sirolimus self-microemulsion compositions

[0034] Element

[0035] Dissolving the drug in diethylene glycol monoethyl ether, then adding Cremophor EL 35, stirring magnetically or mechanically to obtain the sirolimus self-microemulsion composition.

technical field

[0001] The invention belongs to the field of pharmaceutical preparations, in particular to a self-microemulsion composition of poorly soluble drugs. Background technique

[0002] Based on the classification system of biopharmaceuticals, APIs can be divided into four categories according to their differences in solubility and permeability. Drugs with low solubility and high permeability belong to class II of the biopharmaceutical classification, and the rate-limiting step of absorption is the low dissolution rate of the drug. Dosage form plays a decisive role in the absorption of this type of drug in the gastrointestinal tract. Traditional tablets are difficult to improve the bioavailability of this type of drug. Appropriate dosage form is the key to the successful development of this type of drug product. (Lv Yifan et al., Research on the Administration Strategy of Insoluble Drugs, World Clinical Drugs, 2009, 30(1): 41-45)

[0003] Microemulsion (Micro Emul...

Examples

Embodiment 1

[0027] Embodiment 1 The prescription and preparation method of tacrolimus self-microemulsion composition

[0028] Element

[0029] The drug is dissolved in propylene carbonate, then propylene glycol is added, and finally Cremophor RH 40 is added, and magnetic or mechanical stirring is performed to obtain a tacrolimus self-microemulsion composition.

Embodiment 2

[0030] Embodiment 2 The prescription and preparation method of tacrolimus self-microemulsion composition

[0031] Element

[0032] The drug is dissolved in diethylene glycol monoethyl ether, citric acid is added, and finally Labrasol is added, and magnetic or mechanical stirring is performed to obtain the tacrolimus self-microemulsion composition.

Embodiment 3

[0033] The prescription and preparation method of embodiment 3 sirolimus self-microemulsion compositions

[0034] Element

[0035] Dissolving the drug in diethylene glycol monoethyl ether, then adding Cremophor EL 35, stirring magnetically or mechanically to obtain the sirolimus self-microemulsion composition.

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