Biological degradable albumin derivant, pharmacy composition, preparation and application of the same

A technology of albumin and derivatives, applied in the field of pharmaceutical preparations, can solve the problems of drug-induced rash, shortness of breath, bronchospasm, low solubility of paclitaxel, easy dissociation of micelles, etc., and achieve high drug loading and encapsulation efficiency , Good redispersibility, no particle adhesion effect

Inactive Publication Date: 2008-07-16
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solubility of paclitaxel in water is extremely low (_ [US Bristol Myers Squibb (BMS) Company], Anzatax _ (Australian Faulding company) and domestic perilla _ Taxol _ etc. all use polyoxyethylene castor oil (Cremophor EL)-absolute ethanol (50:50, v/v) as paclitaxel composite solvent, and there are following defects in this solubilization method: ①Critical micellar concentration (Critical micellar concentration) of Cremophor EL , CMC) is relatively high, micelles are easy to dissociate during clinical dilution, leading to drug precipitation, so the infusion tube must have an online filter device; ② Cremophor EL in the prescription will cause the release of histamine in the body, and some

Method used

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  • Biological degradable albumin derivant, pharmacy composition, preparation and application of the same
  • Biological degradable albumin derivant, pharmacy composition, preparation and application of the same
  • Biological degradable albumin derivant, pharmacy composition, preparation and application of the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] Preparation of N-octyl human serum albumin

[0098] Dissolve 1g of human serum albumin in water, add 1.02g of n-octanal, react for 1h, add NaBH 4 The aqueous solution was continuously stirred for 12 hours, adjusted to pH 7 with HCl solution, dialyzed in distilled water for 3 days (MWCO=12000-14000), and freeze-dried to obtain the product. Elemental analysis shows that P is 35, that is, there are 35 free amino groups in an albumin molecular chain undergoing chemical reactions.

Embodiment 2

[0100] Preparation of N-octyl human serum albumin

[0101] The reaction conditions were the same as in Example 1, and the octanal reaction time was extended to 8 hours. The elemental analysis of the obtained product showed that P was 67, that is, there were 67 free amino groups in an albumin molecular chain to undergo chemical reactions.

Embodiment 3

[0103] Preparation of N-octanoyl human serum albumin

[0104] Add 3.6 g of n-octanoic acid (0.05 mol) to 4 ml of acetic anhydride, and distill off the acetic acid at 120° C. to obtain n-octanoic anhydride. Disperse 1 g of albumin in water / methanol, add n-octanoic anhydride dropwise under stirring, react at 40°C for 8 hours, dialyze the reaction solution, and freeze-dry to obtain the product. Elemental analysis shows that P is 24, that is, one albumin molecular chain has 24 free amino groups undergoing chemical reactions.

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Abstract

The invention relates to a bio-degradable alb derivative and the related pharmaceutical combinations; wherein, the derivative introduces alkyl, or fatty acyl or deoxycholic acid in the alb skeleton to enable the amphiphilic property and form a nano-micelle by self-organization in water, and can enwrap the drugs through the double effects of the hydrophobic group, the alb molecular chain and the drugs, thereby substantially improving the drug enwrapping ability of the alb and prolonging the stability time. The excipient can be used as the carrier for organic drugs, water-insoluble drugs or dugs with poor water solubility and the carrier of amphipathic drugs, and for the administration inside the vein or muscle injection and oral administration. The preparation method of the bio-degradable alb derivative and the related pharmaceutical combinations is simple and of mature techniques, which is suitable for large scale continuous production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a biodegradable albumin derivative as a drug carrier, and also relates to a preparation method and application of the carrier. Background technique [0002] The biggest obstacle to the administration of poorly soluble drugs (especially injection administration) is low solubility, which makes it difficult to prepare suitable preparations. It is often necessary to adopt various methods to increase solubility, such as preparing the drug into a salt, adding a latent solvent, adding a co-solvent, and adding a surfactant to solubilize. Since salt formation often requires strong acid or strong alkali conditions, it is often not applicable to many drugs, and there are few physiologically safe latent solvents, and the dosage is limited; the safety of co-solvents that increase drug solubility by forming complexes with drugs is not easy Assured, therefore, solubilization by surfact...

Claims

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Application Information

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IPC IPC(8): C07K14/765C07K1/02A61K47/42A61K9/00
Inventor 周建平霍美蓉张勇龚建于迪吕霖
Owner CHINA PHARM UNIV
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