CN1628772A - Botanical originated nim oil contraception formulation - Google Patents
Botanical originated nim oil contraception formulation Download PDFInfo
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- CN1628772A CN1628772A CN 200410040582 CN200410040582A CN1628772A CN 1628772 A CN1628772 A CN 1628772A CN 200410040582 CN200410040582 CN 200410040582 CN 200410040582 A CN200410040582 A CN 200410040582A CN 1628772 A CN1628772 A CN 1628772A
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- neem oil
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Abstract
The invention provides a highly effective, low toxicity nim contraceptive which can be in the dosage forms of microcapsule and granule, the contraceptive is prepared from nim oil or the extracts of different solvents of nim oil as the contraception composition, and a finite proportion of various flavorings, which has strong contraceptive actions to mice.
Description
Technical field
The present invention relates to a kind of natural drug new product, be suitable for the angle control plague of rats, plant source neem oil contraception preparation with good contraceptive efficacy from ecology.
Background technology
Neem oil (Neem oil) is the extract of Azadirachta Indica A. (Azadirachta indica A.Juss) seed.Neem oil is as the antifertility material, and research at home almost is in space state.Studies confirm that in a large number neem oil has good antifertility action.But at present to the dosage form research of neem oil mainly based on cream, even do not make preparation, directly use has caused diversification that can not adapt to its application and the defectives such as palatability that influence animal because of drug flavor.In addition, traditional contraceptive dosage form can not satisfy modern needs, because the dosage form of modern medicines develops to aspects such as water baseization, ultramicronising and slow release and sustained release.Therefore, the present invention makes microcapsule or granular preparation with neem oil or neem oil different solvents extract, not only can improve its stability, extends the expiration date, and can also cover the abnormal flavour of neem oil or neem oil different solvents extract, to increase its agreeable to the taste answering property.
Present China Tibet, Qinghai, Inner Mongol, and the prairie on ground such as Sichuan, Xinjiang, plague of rats harm especially severe, cause animal husbandry, green vegetation and ecological balance, all be subjected to great destruction, give the country and the numerous herdsman masses, bring great economic loss, therefore effectively the control plague of rats is one of key link that ensures the farming and animal husbandry sustainable development.The existing rat-bane of China mainly is the mortality rate that increases Mus, but all there is not lasting effect, and the longest only keeping about 1 year of the low-density time after killing mouse, after this Mus density rises gradually and returns to previous level, and traditional rat-bane also exists drawbacks such as environment and other biological toxic side effect and cost height.These deficiencies in view of traditional rat-bane existence, the present invention explores a kind of new strategy that kills mouse: i.e. angle from keeping ecological balance, seek a kind of vegetalitas apholate of controlling the muroid natality, realize reducing population density by the breeding potential that reduces muroid colony, thereby reach the purpose of fundamentally eliminating the plague of rats, and harmless to human and other animal, Environmental security, effect is lasting.
Summary of the invention
The objective of the invention is to set from Azadirachta Indica A. the neem oil (Neem oil) and the different solvents extract thereof that are squeezed (Azadirachta indica A.juss) seed is mixed with effective, toxic and side effects is little, the microcapsule that technology is grasped easily and the plant source neem oil contraception preparation of two kinds of dosage forms of granular preparation.
For reaching the technical scheme that the foregoing invention purpose adopted be:
Neem oil plant source contraception preparation is a raw material with neem oil or the neem oil different solvents extract that squeezes from neem seed, is mixed with microcapsule and two kinds of dosage forms of granule by certain material proportion again, is used to protect grassland and crops to use.
Each component content (weight %) is in the neem oil plant source contraception microcapsule:
Described microcapsule is to be capsule-core with neem oil or neem oil different solvents extract, accounts for the 30-90% weight ratio, is softgel shell with gelatin and Radix Acaciae senegalis, softgel shell accounts for 5-30%, and allocate emulsifying agent, fixative, dispersant, PH regulator into, by existing complex coacervation, make capsule.Each composition weight proportion is: neem oil or neem oil different solvents extractive content are 30-90%, gelatin and Radix Acaciae senegalis content are 3-30%, emulsifier content is 0-40%, curing agent content is 3-45%, dispersant is 0.1-10%, it is 0.01-0.5% that PH regulates dosage, and each component sum is 100%.
Emulsifying agent can be selected any one or more in sucrose ester, spans, Tweens and the castor oil derivatives etc. for use; Firming agent can be selected the formalin of 10-37% for use; Dispersant can be selected any one or more in alkylsulfonate, the diisopropyl phosphate for use; The PH regulator can be selected sodium hydroxide for use, in oxyammonia or the acetic acid any.
The optimal proportion of each component content is in the neem oil plant source contraception microcapsule:
Neem oil or neem oil different solvents extractive content are 35-70%,
Gelatin and Radix Acaciae senegalis content are 10-30%, and emulsifier content is 5-15%,
Curing agent content is 10-20%, and dispersant is 1-5%,
It is 0.05-0.2% that PH regulates dosage, and each component sum is 100%.
Each composition weight % ratio is in the described neem oil plant source contraception granule:
Neem oil or neem oil different solvents extractive content are 20-80%,
Filler content is 10-40%, and binder content is 5-20%,
Disintegrating agent is 2-20%, and lubricant is 0.1-3%,
Flavoring agent is 0.1-2%, and each component sum is 100%.
Filler can be selected a kind of in lactose, starch, dextrin, mannitol, the calcium carbonate etc. for use; Adhesive can select for use in polyvidone, hypromellose, starch slurry, Icing Sugar and the syrup etc. any or several; Disintegrating agent can be selected cross-linking sodium carboxymethyl cellulose for use, polyvinylpolypyrrolidone, carboxymethyl starch sodium, any one or more in low-substituted hydroxypropyl cellulose, the starch etc.; Lubricant can be selected any one or more of Pulvis Talci, magnesium stearate, Polyethylene Glycol, Stepanol MG (sodium) etc. for use.
The optimum weight % ratio of each constituent content is in the neem oil plant source contraception granule:
Neem oil or neem oil different solvents extractive content are 30-60%,
Filler content is 15-35%, and binder content is 6-20%,
Disintegrant content is 5-20%, and lubricant content is 0.5-1.5%,
Flavoring agent content is 0.5-1%, and each component sum is 100%.
In order to understand essence of an invention better, describe the technology contents of invention below in detail with example, but content of the present invention is not limited thereto.
The test effect of product:
Table 1 and 2:50% neem oil plant source contraception microcapsule are to the antifertility power effect and the palatability test of pesticide effectiveness tables of data of male white mouse
Table 3 and 4:40% neem oil plant source contraception granule are to the antifertility power effect and the palatability test of pesticide effectiveness tables of data of male white mouse
From table as can be known: 50% neem oil plant source contraception microcapsule and 40% neem oil plant source contraception granule are to the antifertility action of male white mouse, the 1-6 month after drug withdrawal, contraceptive prevalence rate reaches 100%, the 7-12 month after the drug withdrawal, pregnancy rate gos up to some extent, for about 30-60%.Palatability testing shows, has added 50% neem oil plant source contraception microcapsule and has not compared the feed intake of two treated animals, no significant difference with having the interpolation group with the animal groups of 40% neem oil plant source contraception granule.The contraceptive effect that shows said preparation is certain, and palatability is good.
Table 1 50% neem oil plant source contraception microcapsule formulation is to the antifertility action of male rat
Drug dose (g/kg) pregnancy rate (%) pregnancy rate (%)
(1-6 month) (7-12 month)
1% carboxymethyl cellulose 2 100 100
Neem oil plant source contraceptive 20 30-50
Table 2 does not have 50% neem oil plant source contraception microcapsule formulation bait and contains 50% neem oil plant source contraception microcapsule formulation bait
Average consumption
The 1st day consumption bait (g)
The 2nd day consumption bait (g)
The 3rd day consumption bait (g)
Add up to (g)
Mus body weight g
Poisonous nontoxic poisonous nontoxic poisonous nontoxic poisonous nontoxic
1 25 1.5 1.8 1.9 2.0 2.5 2.0 2.0 1.9
2 26 2.7 2.7 3.2 2.8 3.7 3.3 3.2 2.9
3 27 3.2 2.8 3.4 3.4 3.4 2.8 3.3 3.0
4 28 4.2 4.4 4.7 4.2 4.0 4.5 4.3 4.4
5 28 3.9 4.2 4.3 3.4 3.7 4.1 4.0 3.9
6 27 3.0 3.0 3.4 2.7 2.7 3.2 3.0 3.0
7 25 2.3 3.0 2.2 1.8 2.7 2.8 2.4 2.5
8 28 4.3 4.3 4.4 4.0 3.9 4.0 4.2 4.1
9 28 4.0 4.3 4.4 4.0 4.5 4.2 4.4 4.2
10 28 5.2 4.7 5.0 5.3 5.6 5.0 5.3 5.0
Average 27 3.4 3.5 3.7 3.4 3.9 3.6 3.8 3.5
Table 3 40% neem oil plant source contraception granular preparation is to the antifertility action of male rat
Drug dose (g/kg) pregnancy rate (%) pregnancy rate (%)
(1-6 month) (7-12 month)
1% carboxymethyl cellulose 2 100 100
Neem oil plant source contraceptive 20 30-60
Table 4 does not have 40% neem oil plant source contraception granular preparation bait and contains 40% neem oil plant source contraception granular preparation bait
Average consumption
The 1st day consumption bait
The 2nd day consumption bait
The 3rd day consumption bait
Add up to
Mus body weight g
Poisonous nontoxic poisonous nontoxic poisonous nontoxic poisonous nontoxic
1 25 1.4 1.9 1.8 2.1 2.4 2.1 1.9 2
2 26 2.6 2.8 3.1 2.9 3.6 3.4 3.1 3
3 27 3.1 2.9 3.3 3.5 3.3 2.9 3.2 3.1
4 28 4.1 4.5 4.6 4.3 3.9 4.6 4.2 4.5
5 28 3.8 4.3 4.2 3.5 3.8 4.2 3.9 4
6 27 2.9 3.1 3.3 2.8 2.6 3.3 2.9 3.1
7 25 2.2 3.1 2.1 1.9 2.6 2.9 2.3 2.6
8 28 4.2 4.4 4.3 4.1 3.8 4.1 4.1 4.2
9 28 3.9 4.4 4.5 4.1 4.4 4.3 4.3 4.3
10 28 5.1 4.8 4.9 5.4 5.5 5.1 5.2 5.1
Average 27 3.3 3.6 3.6 3.5 3.6 3.7 3.6 3.6
Beneficial effect of the present invention is as follows:
1 plant source neem oil contraception microcapsule formulation has 1) good stability, the advantage that the lasting period is long; 2) to Producer, user and Environmental security; 3) covered the bad smell of neem oil and different solvents extract thereof.
2 plant source neem oil contraceptions granular preparation has 1) dustability, tack, aggregation, separation property, hygroscopicity etc. are all less, and it is accurate to be beneficial to divided dose and content; 2) taking convenience suitably adds correctives, has also reached the purpose of covering bad smell.
3 the invention belongs to a kind of plant source Azadirachta Indica A. contraceptive, and the almost non-toxic property of Azadirachta Indica A. product, have solved this difficult problem that almost can't overcome of the caused toxic and side effects of chemical contraceptive, and can make full use of the Azadirachta Indica A. resource.
4 the present invention can control and eliminate the plague of rats effectively from protecting national steppe vegetation and ecological angle, solve the human great difficult problem of this long-term puzzlement.
5 at home, and the present invention has studied the contraceptive efficacy of neem oil and extract thereof first and has been made into different preparations first.And feature with modernized pharmaceutical dosage forms such as ultramicronising and slow release and sustained release.
Though 6 new product effects are remarkable, technology is simple, and production cost is not high, is suitable for applying.
The specific embodiment
The neem oil plant source contraception microcapsule of embodiment 1:30%
In reactor, 30g neem oil or neem oil different solvents extract are added in the aqueous gelatin solution of 25g 10%, add sucrose ester emulsion 6g simultaneously, stir, be heated to 42-45 ℃, add the arabic gum aqueous solution of 25g10% then, the adjustment pH value is 4.5-5.5, stir, be cooled to below 10 ℃, it is 8-9 that reuse 20%NaOH transfers PH, stirs 15min, the formalin that adds 4g diisopropyl phosphate and 10g30% at last stirs 1h under this temperature.Leave standstill, the tipping supernatant washes microsphere with water near neutral, drying for standby.
The neem oil plant source contraception microcapsule of embodiment 2:50%
In reactor, 50g neem oil or neem oil different solvents extract are added in the aqueous gelatin solution of 20g 10%, add sucrose ester emulsion 4g simultaneously, stir, be heated to 42-45 ℃, add the arabic gum aqueous solution of 20g 10% then, the adjustment pH value is 4.5-5.5, stir, be cooled to below 10 ℃, it is 8-9 that reuse 20%NaOH transfers PH, stirs 15min, add formalin and the diisopropyl phosphate 1g of 5g30% at last, under this temperature, stir 1h.Leave standstill, the tipping supernatant washes microsphere with water near neutral, drying for standby.
The neem oil plant source contraception microcapsule of embodiment 3:70%
In reactor, 70g neem oil or neem oil different solvents extract are added in the aqueous gelatin solution of 13g 10%, add sucrose ester emulsion 1g simultaneously, stir, be heated to 42-45 ℃, add the arabic gum aqueous solution of 13g10% then, the adjustment pH value is 4.5-5.5, stir, be cooled to below 10 ℃, it is 8-9 that reuse 20%NaOH transfers PH, stirs 15min, add formalin and the diisopropyl phosphate 1g of 2g30% at last, under this temperature, stir 1h.Leave standstill, the tipping supernatant washes microsphere with water near neutral, drying for standby.
The neem oil plant source contraception microcapsule of embodiment 4:90%
In reactor, 90g neem oil or neem oil different solvents extract are added in the aqueous gelatin solution of 3.5g10%, add sucrose ester emulsion 1g simultaneously, stir, be heated to 42-45 ℃, add the arabic gum aqueous solution of 3.5g10% then, the adjustment pH value is 4.5-5.5, stir, be cooled to below 10 ℃, it is 8-9 that reuse 20%NaOH transfers PH, stirs 15min, add formalin and the diisopropyl phosphate 1g of 1g30% at last, under this temperature, stir 1h.Leave standstill, the tipping supernatant washes microsphere with water near neutral, drying for standby.
The neem oil plant source contraception granule of embodiment 5:20%
In reactor; with the extract of 20g neem oil or neem oil different solvents with after the ethanol of 10g50% mixes; add 35g starch, dextrin and Icing Sugar (7: 1: 1), 15g hydroxypropyl cellulose, 15g starch, 3g Pulvis Talci and 2g Radix Glycyrrhizae respectively and carry out mixed soft material; adopt an extruding pelletization method or a step pelletize machinery granulate; heat drying; granulate is crossed sieve classification, carries out coating at last and becomes product.
The neem oil plant source contraception granule of embodiment 6:40%
In reactor; with the extract of 40g neem oil or neem oil different solvents with after the ethanol of 8g50% mixes; add 30g starch, dextrin and Icing Sugar (7: 1: 1), 9g hydroxypropyl cellulose, 9g starch, 2g Pulvis Talci and 2g Radix Glycyrrhizae respectively and carry out mixed soft material; adopt an extruding pelletization method or a step pelletize machinery granulate; heat drying; granulate is crossed sieve classification, carries out coating at last and becomes product.
The neem oil plant source contraception granule of embodiment 7:60%
In reactor; with the extract of 60g neem oil or neem oil different solvents with after the ethanol of 4g50% mixes; add 20g starch, dextrin and Icing Sugar (7: 1: 1), 7g hydroxypropyl cellulose, 7g starch, 1g Pulvis Talci and 1g Radix Glycyrrhizae respectively and carry out mixed soft material; adopt an extruding pelletization method or a step pelletize machinery granulate; heat drying; granulate is crossed sieve classification, carries out coating at last and becomes product.
The neem oil plant source contraception granule of embodiment 8:80%
In reactor; with the extract of 80g neem oil or neem oil different solvents with after the ethanol of 1g50% mixes; add 14g starch, dextrin and Icing Sugar (7: 1: 1), 2g hydroxypropyl cellulose, 1g starch, 1g Pulvis Talci and 1g Radix Glycyrrhizae respectively and carry out mixed soft material; adopt an extruding pelletization method or a step pelletize machinery granulate; heat drying; granulate is crossed sieve classification, carries out coating at last and becomes product.
Claims (6)
1 one kinds of plant source neem oil contraception preparations is characterized in that neem oil or the seal lemon oil different solvents extract to squeeze is main contraception composition from neem seed, allocate certain material into and be prepared into plant source neem oil contraception microcapsule and granule.
2 plant source neem oil contraception preparations according to claim 1 is characterized in that: described microcapsule is to be capsule-core with neem oil or neem oil different solvents extract, accounts for the 30-90% weight ratio; With gelatin and Radix Acaciae senegalis is softgel shell, and softgel shell accounts for 5-30%, and allocates emulsifying agent, fixative, dispersant, PH regulator into, by complex coacervation, makes capsule.
3 plant source neem oil contraception preparations according to claim 1 and 2 is characterized in that each component content for weight % is in the microcapsule:
Neem oil or neem oil different solvents extract 30-90%,
Gelatin and Radix Acaciae senegalis 3-30%, emulsifying agent 2-40%,
Curing agent content is 3-45%, dispersant 0.1-10%,
It is 0.01-0.5% that PH regulates dosage, and each component sum is 100%.
Emulsifying agent can be selected any one or more in sucrose ester, spans, Tweens and the castor oil derivatives etc. for use; Firming agent can be selected the formalin of 10-37% for use; Dispersant can be selected any one or more in alkylsulfonate, the diisopropyl phosphate for use; The PH regulator can be selected sodium hydroxide for use, in oxyammonia or the acetic acid any.
4 plant source neem oil contraception preparations according to claim 1 is characterized in that each composition weight % ratio is in the described granule:
Neem oil or neem oil different solvents extractive content are 20-80%,
Filler content is 10-40%, and binder content is 5-20%,
Disintegrating agent is 2-20%, and lubricant is 0.1-3%,
Flavoring agent is 0.1-2%, and each component sum is 100%;
Filler can be selected a kind of in lactose, starch, paste sugar, mannitol, the calcium carbonate etc. for use; Adhesive can select for use in polyvidone, hypromellose, starch slurry, Icing Sugar and the syrup etc. any or several: disintegrating agent can be selected cross-linking sodium carboxymethyl cellulose for use, polyvinylpolypyrrolidone, carboxymethyl starch sodium, any one or more in low-substituted hydroxypropyl cellulose, the starch etc.; Lubricant can be selected any one or more of Pulvis Talci, magnesium stearate, Polyethylene Glycol, Stepanol MG etc. for use.
5 plant source neem oil contraception preparations according to claim 3, the preparation method that it is characterized in that described microcapsule is in reactor, neem oil or neem oil different solvents extract are added in the aqueous gelatin solution, add the sucrose ester emulsion simultaneously, stir, be heated to 42-45 ℃, add the arabic gum aqueous solution then, the adjustment pH value is 4.5-5.5, stirs, and is cooled to below 10 ℃, it is 8-9 that reuse %NaOH transfers PH, stir 15min, add formalin and diisopropyl phosphate at last, under this temperature, stir 1h.Leave standstill, the tipping supernatant washes microsphere with water near neutral, drying for standby.
6 plant source neem oil contraception preparations according to claim 4; the preparation method that it is characterized in that described granule is in reactor; with the extract of neem oil or neem oil different solvents with after ethanol mixes; add starch, dextrin and Icing Sugar (7: 1: 1), hydroxypropyl cellulose, starch, Pulvis Talci and Radix Glycyrrhizae respectively and carry out mixed soft material; adopt an extruding pelletization method or a step pelletize machinery granulate, heat drying, granulate; cross sieve classification, be packaged into product at last.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100405822A CN1316956C (en) | 2004-08-31 | 2004-08-31 | Botanical originated nim oil contraception formulation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100405822A CN1316956C (en) | 2004-08-31 | 2004-08-31 | Botanical originated nim oil contraception formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1628772A true CN1628772A (en) | 2005-06-22 |
| CN1316956C CN1316956C (en) | 2007-05-23 |
Family
ID=34845836
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2004100405822A Expired - Fee Related CN1316956C (en) | 2004-08-31 | 2004-08-31 | Botanical originated nim oil contraception formulation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1316956C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101091436B (en) * | 2006-06-21 | 2010-12-01 | 王海滨 | Planting method for raising seedling composite seed with capsule |
| CN102696696A (en) * | 2012-06-11 | 2012-10-03 | 四川农业大学 | Grass meal granular formulation for controlling rodent pests in grassland and preparation method as well as application thereof |
| CN107455374A (en) * | 2017-07-17 | 2017-12-12 | 广东省生物资源应用研究所 | A kind of rodents sterilant synergist and its application in muroid bait material is prepared |
-
2004
- 2004-08-31 CN CNB2004100405822A patent/CN1316956C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101091436B (en) * | 2006-06-21 | 2010-12-01 | 王海滨 | Planting method for raising seedling composite seed with capsule |
| CN102696696A (en) * | 2012-06-11 | 2012-10-03 | 四川农业大学 | Grass meal granular formulation for controlling rodent pests in grassland and preparation method as well as application thereof |
| CN107455374A (en) * | 2017-07-17 | 2017-12-12 | 广东省生物资源应用研究所 | A kind of rodents sterilant synergist and its application in muroid bait material is prepared |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1316956C (en) | 2007-05-23 |
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