Orally taken self-microemulsified concentrate of all-trans vitamin A acid

A technology of all-trans retinoic acid and self-microemulsification, which is applied in the field of self-microemulsification concentrates, can solve the problems of increasing process steps and increasing costs, and achieves the effects of simple preparation method, increased absorption degree and speed, and stable properties

Inactive Publication Date: 2006-03-01
TIANJIN PACIFIC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Hard capsule preparations have the problem of sealing between the capsule body and the cap, increasing process steps and increasing costs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Quantity of components (mg / capsule)

[0044] All-trans retinoic acid 10

[0045] Medium Chain Glycerides 140

[0046] Cremphor EL 280

[0047] Propylene Glycol 120

[0048] Poloxamer 50

[0049] Weigh the specified amount of medium-chain glycerides, Cremphor EL, propylene glycol, and poloxamer, stir and dissolve in a water bath at 80°C, mix well, put in the corresponding amount of all-trans retinoic acid, stir for a while and dissolve completely, then cool To 40°C, fill with a capsule liquid filling machine, and cool and solidify at room temperature without sealing.

Embodiment 2

[0051] Quantity of components (mg / capsule)

[0052] All-trans retinoic acid 10

[0053] Masine 140

[0054] Cremphor EL 260

[0055] Transcutol P 100

[0056] PEG 1000 60

[0057] VE (vitamin E) 10

Embodiment 3

[0059] Quantity of components (mg / capsule)

[0060] All-trans retinoic acid 10

[0061] Refined corn oil 140

[0062] Cremphor RH40 200

[0063] Propylene Glycol 120

[0064] Poloxamer 70

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Abstract

The orally taken self-microemulsified concentrate of all-trans vitamin A acid includes all-trans vitamin A acid in treating dosage, as well as oil phase of melting point lower than 70 deg.c, surfactant, co-surfactant and tackifier. The preparation process includes mixing oil phase, surfactant, co-surfactant and tackifier via stirring in water bath at 80 deg.c; adding vitamin A acid via stirring for complete dissolving; cooling to 40 deg.c; and encapsulating. The orally taken self-microemulsified concentrate of all-trans vitamin A acid has greatly increased absorption degree and speed and greatly raised medicine bioavailability.

Description

technical field [0001] The invention relates to an oral self-microemulsifying concentrate of all-trans retinoic acid. More particularly, the present invention relates to room temperature solid or semisolid self-microemulsifying concentrates comprising the active ingredient all-trans retinoic acid (RA), an oil phase, surfactants, co-surfactants and viscosity builders. Background technique [0002] All-trans retinoic acid (RA) is a metabolic intermediate product of vitamin A, which can induce epidermal cell proliferation and differentiation, keratolysis, and has anti-inflammatory activities. It is widely used in the treatment of psoriasis, acne, etc., and RA can induce differentiation Tumor cells are currently the first choice clinical drug for the treatment of acute promyelocytic leukemia and myeloid hyperplasia. The existing oral dosage forms of RA include tablets and capsules. Since RA is almost insoluble in water (solubility<0.2 mg / L), it dissolves slowly and has low o...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/19A61K9/107A61P17/06A61P17/10A61P35/00
Inventor 赵锦花宋德成
Owner TIANJIN PACIFIC PHARMA
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