CN1679530A

CN1679530A - Ibuprofen emulsion

Info

Publication number: CN1679530A
Application number: CN 200510023309
Authority: CN
Inventors: 朱芳海
Original assignee: Individual
Current assignee: Individual
Priority date: 2005-01-13
Filing date: 2005-01-13
Publication date: 2005-10-12

Abstract

An emulsion of ibuprofen is prepared through dissolving ibuprofen in oil solution able to be eaten or injected, and emulsifying. It can be applied exteriorly, or by oral taking or intravenous injection.

Description

Ibuprofen emulsion

Technical field the present invention be with ibuprofen and related substances thereof be dissolved in can oil for oral use or oil for injection in, becoming with suitable method preparation then can be for emulsion preparations oral or injection, to satisfy infant, child, old man and the medication of dysphagia crowd clinical oral administration, the perhaps specific (special) requirements of slow release medication.Its technical field is when belonging to medical production technology class.

The application of background technology ibuprofen in clinical practice had history for many years: aspect the dosage form use, exterior-applied formulations such as existing ointment, cream, gel more are oral formulations such as tablet, capsule, granule, powder, electuary.

Though that ibuprofen has is well analgesic, analgesia, antiphlogistic effects, as nonsteroidal antiinflammatory drug, can produce some clinical side effects also essentially, as the gastrointestinal zest etc.

In the children field, cold, fever occupies the first place, and therefore in department of pediatrics clinical application process, the consumption of ntipyretic analgesic medicine is to stand in the breach.But therefore infant is necessary that this class medicine is carried out suitable dosage form to be improved, so that better service is in the multiformity demand in market because born instinct is all feared and had an injection, takes medicine.

Though Emulsion is as a kind of dosage form existing use in the clinical application practice, as the intra-lipid that is produced by Hua Rui company just being arranged as the total intravenous nutrition preparation, said preparation is exactly with the fat milk of the available refined plant oil of human body preparation becoming particle diameter less than 1 micron, is injected directly among the human body blood circulation; Domestic " KANGLAITE " is the intravenous fat milk of oil preparation becoming with Semen Coicis; Also have domestic among studying at present other medicinal plants of usefulness or " oil " emulsifying of animal become intravenous fat milk or oral breast, as the oral breast of shark oil, the oral breast of safflower oil, the oral breast of Oleum Hippophae etc.

But the active component of these Emulsions itself is exactly an oils.Yet there are no report and the ibuprofen that itself is not oils is also prepared the oral latex emulsion or the injection that become Emulsion, also do not see use in pharmaceutical production or the realm of sale at home.

Summary of the invention the present invention is with ibuprofen preparation becoming Orally taken emulsion, it mainly is advantageous characteristic by O/W (oil-in-water) Emulsion, as: at first be to be dispersed in the water by medicine, form " little oil droplet "---emulsion droplet, and avoided medicine and water directly to contact the chemical instability that is caused; Because " emulsion droplet " can stably be dispersed in the water, form the Emulsion of character similar " milk " in addition, this is that the infant that is in fever and headache is taken medicine, for the head of a family brought greatly convenient.

In addition, also this Emulsion preparation becoming injection for intravenous can be used.So not only can play the clinical effectiveness of rapid antipyretic-antalgic, also alleviate the toxic and side effects of this class medicine simultaneously by the oral gastrointestinal upset that brings.

The specific embodiment is an example with the Orally taken emulsion of ibuprofen here, further introduces its pharmaceutical formulation and production technology, as the concrete implementation example of this patent.

In this embodiment, ibuprofen is dissolved in the refined soybean oil of injection stage with suitable method, to reach dose therapeutically effective, adopts the high pressure homogenize emulsion process then, the soybean oil emulsifying that will contain ibuprofen becomes can stablize the Orally taken emulsion of depositing.This embodiment basic recipe is as follows:

Ibuprofen: 0.10g

Refined soybean oil: 1.00g

Soybean phospholipid: 0.12g

Stabilizing agent: an amount of

Sodium hydroxide: an amount of

Flavoring agent: an amount of

Distilled water adds to: 10.00ml

In this prescription, ibuprofen has good dissolubility in refined soybean oil, can further increase the formula proportion of ibuprofen according to clinical needs.

With the prepared ibuprofen Orally taken emulsion of above prescription, not only ibuprofen preparation can be become can directly oral liquid preparation, and medicine dissolution is in inner phase oil, there are not flavour of a drug, convenient for children and dysphagia crowd's medication demand, the such Orally taken emulsion of what is more important can be avoided to the heating infant notion of " taking medicine " they being taken medicine in the mode of " sucking ", take medicine the psychology of fearing hardships thereby greatly satisfied the child, the social value that has brought into play this technology.

Claims

1, a kind ofly dissolving such as ibuprofen or assistant are enabled stably to be present in oral in oil with other method, become and to reach the dosage form of being correlated with for the Emulsion of oral, injection or external with suitable emulsification method preparation then;

2, right 1 described oil, be meant the oils that to use for safety oils for oral use or safety injection, include but not limited to as vegetable and animals oils such as soybean oil, Oleum Arachidis hypogaeae semen, Oleum sesami, Oleum Camelliae, Oleum Cocois, olive oil, fish oil, also comprise mineral oil such as silicone oil, liquid Paraffin, these oil both can use separately, also can two or more use together;

3, right 1 described " other method of assistant " includes but not limited to that solubilising, hydrotropy, formation ion pair, adjusting acid-base value etc. increase the formulation method of dissolubility;

4, right 1 described " suitable emulsification method " includes but not limited to that wherein one or more such as self-emulsification, colloid mill emulsion process, simple agitation emulsion process, supersound method, high speed shear emulsion process, high pressure homogenize emulsion process are used;

5, right 1 described emulsion preparations mainly is oil-in-water emulsion (O/W), but also includes but not limited to water-in-oil emulsion (W/O), W/O/W type multiple emulsion (W/O/W), Water-In-Oil oil-in multiple emulsion (O/W/O);

Whether 6, right 1 described dissolvings such as " " ibuprofen is meant independent use ibuprofen or unites and uses other related substances, unites other related substanceses of use, no matter be dissolved in the oil still to be dissolved in the water or in the mixed solvent.

7, right 1 described relevant dosage form is meant that some that contain the Emulsion component are for oral administration, other dosage form of injection or external.Include but not limited to as emulsion agent, gel, cream etc.