CN1589780A - Limonene soft capsule - Google Patents
Limonene soft capsule Download PDFInfo
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- CN1589780A CN1589780A CN 03140378 CN03140378A CN1589780A CN 1589780 A CN1589780 A CN 1589780A CN 03140378 CN03140378 CN 03140378 CN 03140378 A CN03140378 A CN 03140378A CN 1589780 A CN1589780 A CN 1589780A
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- limonene
- soft capsule
- capsule
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Abstract
A limonene soft capsule contains limonene and cirmtim or sterol for increasing the stability and biologic utilization rate of the active medicine in soft capsule.
Description
Technical field
The invention belongs to the chemicals field, more particularly relate to a kind of limonene soft capsule.
Background technology
At present, the medicine of a lot of treatment cholecystitis, cholangitis and cholelithiasis is arranged on the market, have and much have good curative effect, wherein a kind of is the limonene capsule.This types of drugs is a capsule, and main component is that (chemical name is limonene: 1-methyl-4-(1-methyl ethylene) cyclohexene).This product content is orange-yellow moist granule, is applicable to treatments such as cholecystitis, cholangitis, cholelithiasis, biliary postoperative syndrome and dyspepsia.
Yet there is following some main deficiency in these product, directly influence its therapeutic effect:
(1) main pharmacodynamics composition limonene is a volatility oily composition, when being prepared into capsule, need utilize adjuvant with its absorption, curing, often makes the content of capsule be moist graininess; In addition, capsule is nested by two softgel shells and forms, and is not to seal fully between the shell, and the time has been grown, and volatile ingredient oozes out easily, less stable.
(2) uniformity is relatively poor, and every interior content of capsule is difficult to reach consistent.
(3) bioavailability is lower.
Summary of the invention
The objective of the invention is to overcome the shortcoming that existing limonene capsule exists, the soft capsule dosage form of the limonene of a kind of bioavailability height, good stability, good uniformity is provided.
Soft capsule is a kind of novel form that grows up behind sheet, injection, can and be encapsulated in the glued membrane the quantitative pressure injection of oily medicine, drug solution or drug suspension, pastel even drug powder, forms big or small, different seal capsule.Compare with other dosage forms, possess bioavailability height, content accurately, characteristics such as good uniformity, good looking appearance; If the oily medicine also can save technical finesses such as absorption, curing, can effectively avoid the oily medicine from absorb adjuvant, to ooze out, so soft capsule is the optimum dosage form of oiliness medicine.In addition, the medicine of the hydrophobic drug of low melting point substance, bioavailability difference, bad bitterness and stink, trace active medicine and the medicine of meeting light, wet, thermally labile and easy oxidation also are fit to make soft capsule.
Limonene is the oily volatile material, the main dosage form of this medicine is a capsule so far, in the performance therapeutic effect, there is above-mentioned main deficiency, we are at combination stability, bioavailability, when dissolution study carries out modified form, proposed limonene is made the scheme of soft capsule, can also add hesperidin, sterol is made compound recipe limonene soft capsule, this scheme can be brought following beneficial effect:
(1) medicine stability is strengthened greatly;
(2) uniform content of every medicinal soft capsule helps the quality control to medicine;
(3) bioavailability strengthens greatly, and dissolution improves;
(4) can not add adjuvant and directly be prepared into soft capsule, compare with capsule, under the commensurability situation of main effective ingredient, the capsule of the volume ratio of soft capsule significantly reduces, and is beneficial to patient and swallows, and is easy to allow patient accept;
(5) mouthfeel softness, pharynx is obeyed easily, especially for child patient.
The present invention adopts pressing to be prepared into soft capsule, and rubber adopts gelatin, meets " the requirement of Chinese pharmacopoeia version in 2000.When technology was studied, adjuvant was added in combination stability, bioavailability, pharmacologic agent research, as tween, class of department etc., and did not add any adjuvant relatively, and stability, bioavailability, pharmacological effect etc. all do not have notable difference.
The specific embodiment
The invention will be further described below in conjunction with embodiment, but do not limit the present invention in any form.
Embodiment 1
Adopt pressing to prepare the limonene soft capsule, rubber adopts gelatin, makes every to contain 0.1 milliliter of limonene volatile oil, does not add any adjuvant.
Using method: oral
Consumption: each 3～5, every day 2～3 times
Embodiment 2
Medicine: every limonene soft capsule and limonene capsule that contains 0.1 milliliter of limonene volatile oil
Limonene soft capsule of the present invention and original limonene capsule all have significant curative effect to cholecystitis, cholangitis, cholelithiasis etc., and aspect stability and bioavailability, soft capsule of the present invention has tangible improvement compared with original capsule preparations, and table 1, table 2 are respectively their comparative results.
(1) Wen Dingxing comparison:
The principal element of influence stability is the volatilization loss of volatile ingredient, adopts weight-loss method, relatively places the weight change of capsule with the limonene of soft capsule dosage form of identical interval, the stability of two kinds of different dosage forms of investigation.
(2) comparison of bioavailability:
With the limonene is to detect index, and two kinds of different dosage forms have been carried out the comparative study of bioavailability, adopts RP-HPLC to measure blood drug level, from kinetic parameter C
Max/ mg
L
-1, T
Max/ h, AUC
0 → 24h/ mghL
-1The result shows that the bioavailability of soft capsule is obviously greater than capsule.
Laboratory animal SD rat, body weight 240～260g, male and female half and half
Medication and blood sampling time fasting overnight (can't help water), next day gastric infusion, dosage is limonene 0.2ml/kg (being equivalent to two limonene capsule and soft capsule respectively).15min before administration and after the administration, 30min, 60min, 80min, 2h, 3h, the blood sampling of 4h and 8h heart, each blood sample point is with 6 rats.
HPLC analysis condition analytical column is μ Bondpaka C
18(0.45mm * 25cm); Mobile phase is methanol: water=7: 3; Flow velocity: 1mL/min; Detect wavelength: λ=268nm.
0.5mL blood plasma is got in the extraction of specimen, adds 5mL CHCl
3, interior mark 50 μ L, 15min is extracted in jolting, and is centrifugal, aqueous phase discarded, the accurate 4mL organic facies of drawing is in a clean tube, at 37 ℃ of water-baths, N
2Dry up under the air-flow, residue dissolves the sample introduction analysis again with 200 μ L mobile phases.
The comparison of table 1 stability (weight-loss method: Δ K (mg))
The comparison of table 2 bioavailability
Claims (2)
1, a kind of limonene soft capsule mainly contains limonene, it is characterized in that said preparation is a soft capsule dosage form.
2, the described limonene soft capsule of claim 1 is characterized in that containing hesperidin, sterol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03140378 CN1589780A (en) | 2003-09-03 | 2003-09-03 | Limonene soft capsule |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03140378 CN1589780A (en) | 2003-09-03 | 2003-09-03 | Limonene soft capsule |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1589780A true CN1589780A (en) | 2005-03-09 |
Family
ID=34597345
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03140378 Pending CN1589780A (en) | 2003-09-03 | 2003-09-03 | Limonene soft capsule |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1589780A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104897837A (en) * | 2015-06-08 | 2015-09-09 | 辽宁华润本溪三药有限公司 | Detection method of pharmaceutical preparation for curing stomach pain caused by qi stagnation |
| CN114624348A (en) * | 2020-12-11 | 2022-06-14 | 北京远大九和药业有限公司 | Method for determining dissolution of eucalyptus, lemon and pinene enteric-coated soft capsules |
-
2003
- 2003-09-03 CN CN 03140378 patent/CN1589780A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104897837A (en) * | 2015-06-08 | 2015-09-09 | 辽宁华润本溪三药有限公司 | Detection method of pharmaceutical preparation for curing stomach pain caused by qi stagnation |
| CN114624348A (en) * | 2020-12-11 | 2022-06-14 | 北京远大九和药业有限公司 | Method for determining dissolution of eucalyptus, lemon and pinene enteric-coated soft capsules |
| CN114624348B (en) * | 2020-12-11 | 2023-06-30 | 北京远大九和药业有限公司 | Method for determining dissolution of eucalyptus and lemon pinane enteric soft capsules |
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| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |